Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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1222 1662 49 None -23 25 Human 6.0 pAC50 = 6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3396 1662 49 None -23 25 Human 6.0 pAC50 = 6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
85 1662 49 None -23 25 Human 6.0 pAC50 = 6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL46516 1662 49 None -23 25 Human 6.0 pAC50 = 6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
DB04842 1662 49 None -23 25 Human 6.0 pAC50 = 6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
2337 3254 77 None -8 29 Human 6.0 pAC50 = 6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 3254 77 None -8 29 Human 6.0 pAC50 = 6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 3254 77 None -8 29 Human 6.0 pAC50 = 6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 3254 77 None -8 29 Human 6.0 pAC50 = 6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 3254 77 None -8 29 Human 6.0 pAC50 = 6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5328940 100214 107 None -1 23 Human 6.0 pAC50 = 6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 100214 107 None -1 23 Human 6.0 pAC50 = 6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
42890 9423 59 None -1 13 Human 5.0 pAC50 = 5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
CHEMBL1117 9423 59 None -1 13 Human 5.0 pAC50 = 5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
2162 41512 100 None -3 22 Human 5.0 pAC50 = 5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 41512 100 None -3 22 Human 5.0 pAC50 = 5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
47979 78208 59 None -3311 9 Human 5.0 pAC50 = 5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 78208 59 None -3311 9 Human 5.0 pAC50 = 5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 8 2 6 0.7 C=CCN1CCCC1CNC(=O)c1cc(S(N)(=O)=O)cc(OC)c1OC 10.1038/s41467-023-40064-9
2105 3052 37 None -251 25 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3052 37 None -251 25 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3052 37 None -251 25 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3052 37 None -251 25 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3052 37 None -251 25 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
4209 3161 75 None -891 17 Human 7.0 pAC50 = 7.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
4893 3161 75 None -891 17 Human 7.0 pAC50 = 7.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
503 3161 75 None -891 17 Human 7.0 pAC50 = 7.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
5385 3161 75 None -891 17 Human 7.0 pAC50 = 7.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
CHEMBL2 3161 75 None -891 17 Human 7.0 pAC50 = 7.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
DB00457 3161 75 None -891 17 Human 7.0 pAC50 = 7.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
5472 205816 75 None -1 16 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL1717 205816 75 None -1 16 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL833 205816 75 None -1 16 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
DB00208 205816 75 None -1 16 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
1028 291 71 None -44 19 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
139148732 291 71 None -44 19 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
479 291 71 None -44 19 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
5816 291 71 None -44 19 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
CHEMBL679 291 71 None -44 19 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
DB00668 291 71 None -44 19 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
5360696 1405 30 None -1737 11 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1405 30 None -1737 11 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1405 30 None -1737 11 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1405 30 None -1737 11 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1405 30 None -1737 11 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
2200 20201 61 None -6 12 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1256819 20201 61 None -6 12 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1305 20201 61 None -6 12 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
DB08799 20201 61 None -6 12 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
6436173 55114 45 None -3 22 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL1617 55114 45 None -3 22 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
108000 56851 39 None -32 5 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 2 1 3 2.9 Cn1cc(C(=O)[C@@H]2CCc3[nH]cnc3C2)c2ccccc21 10.1038/s41467-023-40064-9
135418340 56851 39 None -32 5 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 2 1 3 2.9 Cn1cc(C(=O)[C@@H]2CCc3[nH]cnc3C2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1643895 56851 39 None -32 5 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 2 1 3 2.9 Cn1cc(C(=O)[C@@H]2CCc3[nH]cnc3C2)c2ccccc21 10.1038/s41467-023-40064-9
55645 84368 8 None -3890 11 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 7 2 4 2.1 CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21 10.1038/s41467-023-40064-9
CHEMBL2218861 84368 8 None -3890 11 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 7 2 4 2.1 CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21 10.1038/s41467-023-40064-9
nan 84368 8 None -3890 11 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 7 2 4 2.1 CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21 10.1038/s41467-023-40064-9
135398735 136966 32 None -4 27 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
136262914 136966 32 None -4 27 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL374478 136966 32 None -4 27 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
4976 203577 29 None -1230 15 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL668 203577 29 None -1230 15 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
242 470 124 None -32 33 Human 7.0 pAC50 = 7.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 470 124 None -32 33 Human 7.0 pAC50 = 7.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 470 124 None -32 33 Human 7.0 pAC50 = 7.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 470 124 None -32 33 Human 7.0 pAC50 = 7.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 470 124 None -32 33 Human 7.0 pAC50 = 7.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
213046 2383 59 None -69 17 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2383 59 None -69 17 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2383 59 None -69 17 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2383 59 None -69 17 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2383 59 None -69 17 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
443955 204368 92 None 2 8 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 204368 92 None 2 8 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
1613 2346 53 None -144 34 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 2346 53 None -144 34 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 2346 53 None -144 34 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 2346 53 None -144 34 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 2346 53 None -144 34 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
11626560 200935 94 None -1 14 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 200935 94 None -1 14 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
55483 205095 40 None -7 11 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 356 13 4 4 3.6 Oc1ccc(CCNCCCCCCNCCc2ccccc2)cc1O 10.1038/s41467-023-40064-9
CHEMBL77622 205095 40 None -7 11 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 356 13 4 4 3.6 Oc1ccc(CCNCCCCCCNCCc2ccccc2)cc1O 10.1038/s41467-023-40064-9
2540 4399 111 None -1737 28 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 4399 111 None -1737 28 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
8550 14422 57 None -1 7 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 578 7 1 9 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5ccccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC 10.1038/s41467-023-40064-9
CHEMBL1200515 14422 57 None -1 7 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 578 7 1 9 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5ccccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC 10.1038/s41467-023-40064-9
131411 15390 70 None -4 10 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 476 7 1 6 5.2 CCOC(=O)c1c(CSc2ccccc2)n(C)c2cc(Br)c(O)c(CN(C)C)c12 10.1038/s41467-023-40064-9
28446253 15390 70 None -4 10 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 476 7 1 6 5.2 CCOC(=O)c1c(CSc2ccccc2)n(C)c2cc(Br)c(O)c(CN(C)C)c12 10.1038/s41467-023-40064-9
CHEMBL1214598 15390 70 None -4 10 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 476 7 1 6 5.2 CCOC(=O)c1c(CSc2ccccc2)n(C)c2cc(Br)c(O)c(CN(C)C)c12 10.1038/s41467-023-40064-9
11291 98794 25 None -331 3 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 261 1 0 1 3.9 CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 10.1038/s41467-023-40064-9
CHEMBL278398 98794 25 None -331 3 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 261 1 0 1 3.9 CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 10.1038/s41467-023-40064-9
DB01619 98794 25 None -331 3 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 261 1 0 1 3.9 CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 10.1038/s41467-023-40064-9
2583 3774 118 None -7079 16 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3774 118 None -7079 16 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3774 118 None -7079 16 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3774 118 None -7079 16 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3774 118 None -7079 16 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
71496458 115562 87 None -33 16 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
CHEMBL3353410 115562 87 None -33 16 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
104850 3328 96 None -1122 28 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
4150 3328 96 None -1122 28 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
743 3328 96 None -1122 28 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL111 3328 96 None -1122 28 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
DB06155 3328 96 None -1122 28 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
5282175 14430 36 None -14 4 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 424 16 2 5 5.1 CCCCCCCC(=O)CC[C@@H]1[C@@H](C/C=C\CCCC(=O)OC(C)C)[C@@H](O)C[C@H]1O 10.1038/s41467-023-40064-9
CHEMBL1200661 14430 36 None -14 4 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 424 16 2 5 5.1 CCCCCCCC(=O)CC[C@@H]1[C@@H](C/C=C\CCCC(=O)OC(C)C)[C@@H](O)C[C@H]1O 10.1038/s41467-023-40064-9
65948 18554 109 None -5 6 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 582 9 2 9 4.7 CC1=C(C(=O)OC(C)C)C(c2cccc([N+](=O)[O-])c2)C(C(=O)OC2CN(C(c3ccccc3)c3ccccc3)C2)=C(N)N1 10.1038/s41467-023-40064-9
CHEMBL1275868 18554 109 None -5 6 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 582 9 2 9 4.7 CC1=C(C(=O)OC(C)C)C(c2cccc([N+](=O)[O-])c2)C(C(=O)OC2CN(C(c3ccccc3)c3ccccc3)C2)=C(N)N1 10.1038/s41467-023-40064-9
2794 19378 85 None -14 7 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 472 4 1 4 7.5 CC(C)/N=c1\cc2n(-c3ccc(Cl)cc3)c3ccccc3nc-2cc1Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1292 19378 85 None -14 7 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 472 4 1 4 7.5 CC(C)/N=c1\cc2n(-c3ccc(Cl)cc3)c3ccccc3nc-2cc1Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
7028 52378 22 None -102 3 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 165 3 2 2 1.3 CN[C@@H](C)[C@@H](O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1590 52378 22 None -102 3 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 165 3 2 2 1.3 CN[C@@H](C)[C@@H](O)c1ccccc1 10.1038/s41467-023-40064-9
DB00852 52378 22 None -102 3 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 165 3 2 2 1.3 CN[C@@H](C)[C@@H](O)c1ccccc1 10.1038/s41467-023-40064-9
2467 67423 51 None -3 5 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 307 8 0 5 2.8 COc1cc(OC)c(C(=O)CCCN2CCCC2)c(OC)c1 10.1038/s41467-023-40064-9
CHEMBL188921 67423 51 None -3 5 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 307 8 0 5 2.8 COc1cc(OC)c(C(=O)CCCN2CCCC2)c(OC)c1 10.1038/s41467-023-40064-9
2375 158392 106 None -5 2 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 430 5 2 5 2.9 CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc1ccc(C#N)c(C(F)(F)F)c1 10.1038/s41467-023-40064-9
CHEMBL409 158392 106 None -5 2 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 430 5 2 5 2.9 CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc1ccc(C#N)c(C(F)(F)F)c1 10.1038/s41467-023-40064-9
37264 189420 24 None -8 3 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 435 6 2 10 1.3 COc1cc2c(N)nc(N3CCN(C(=O)OCC(C)(C)O)CC3)nc2c(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL513301 189420 24 None -8 3 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 435 6 2 10 1.3 COc1cc2c(N)nc(N3CCN(C(=O)OCC(C)(C)O)CC3)nc2c(OC)c1OC 10.1038/s41467-023-40064-9
68867 78171 38 None -61 13 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL2104523 78171 38 None -61 13 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
DB08810 78171 38 None -61 13 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
68602 205124 80 None -11 4 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C 10.1038/s41467-023-40064-9
CHEMBL77921 205124 80 None -11 4 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C 10.1038/s41467-023-40064-9
2683 3832 60 None -5 6 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
5487 3832 60 None -5 6 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
7308 3832 60 None -5 6 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
CHEMBL1079 3832 60 None -5 6 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
DB00697 3832 60 None -5 6 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
4066 204624 78 None -870 16 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL73451 204624 78 None -870 16 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
DB01071 204624 78 None -870 16 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
1043 1580 14 None -208 23 Human 6.9 pAC50 = 6.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1580 14 None -208 23 Human 6.9 pAC50 = 6.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
3251 1580 14 None -208 23 Human 6.9 pAC50 = 6.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1580 14 None -208 23 Human 6.9 pAC50 = 6.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
CHEMBL1982133 1580 14 None -208 23 Human 6.9 pAC50 = 6.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1580 14 None -208 23 Human 6.9 pAC50 = 6.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1580 14 None -208 23 Human 6.9 pAC50 = 6.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
202 1507 77 None 1 17 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
60835 1507 77 None 1 17 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
972 1507 77 None 1 17 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1175 1507 77 None 1 17 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
DB00476 1507 77 None 1 17 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
124 2979 47 None -144 25 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2979 47 None -144 25 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2979 47 None -144 25 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2979 47 None -144 25 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2979 47 None -144 25 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
2274 3171 58 None -22 37 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4917 3171 58 None -22 37 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
7279 3171 58 None -22 37 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL728 3171 58 None -22 37 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00433 3171 58 None -22 37 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
212 3804 47 None -524 22 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3804 47 None -524 22 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3804 47 None -524 22 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3804 47 None -524 22 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3804 47 None -524 22 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
56959 31554 103 None 3 9 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 427 9 2 6 2.3 COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1 10.1038/s41467-023-40064-9
CHEMBL1404 31554 103 None 3 9 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 427 9 2 6 2.3 COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1 10.1038/s41467-023-40064-9
CHEMBL1526084 31554 103 None 3 9 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 427 9 2 6 2.3 COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1 10.1038/s41467-023-40064-9
70691408 78210 0 None 3 4 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 1 2 4 1.6 CCC1C2CC3C4N(C)c5ccccc5C45CC(C2[C@H]5O)N3C1O 10.1038/s41467-023-40064-9
CHEMBL2105617 78210 0 None 3 4 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 1 2 4 1.6 CCC1C2CC3C4N(C)c5ccccc5C45CC(C2[C@H]5O)N3C1O 10.1038/s41467-023-40064-9
4640 78264 30 None -11 11 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 379 6 1 4 3.9 COc1cc2[nH]c(C)c(CCN3CCN(c4ccccc4)CC3)c2cc1OC 10.1038/s41467-023-40064-9
CHEMBL2107011 78264 30 None -11 11 Human 5.9 pAC50 = 5.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 379 6 1 4 3.9 COc1cc2[nH]c(C)c(CCN3CCN(c4ccccc4)CC3)c2cc1OC 10.1038/s41467-023-40064-9
243 3200 91 None -1202 5 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1038/s41467-023-40064-9
3052762 3200 91 None -1202 5 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1038/s41467-023-40064-9
3502 3200 91 None -1202 5 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1038/s41467-023-40064-9
CHEMBL117287 3200 91 None -1202 5 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1038/s41467-023-40064-9
DB06480 3200 91 None -1202 5 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1038/s41467-023-40064-9
67462786 120515 56 None -3 6 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 446 9 1 8 4.2 COc1cc(OC)cc(N(CCNC(C)C)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1 10.1038/s41467-023-40064-9
CHEMBL3545376 120515 56 None -3 6 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 446 9 1 8 4.2 COc1cc(OC)cc(N(CCNC(C)C)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1 10.1038/s41467-023-40064-9
122282 133507 57 None - 1 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 198 0 0 2 -0.4 CN1C(=O)N(C)C2C1N(C)C(=O)N2C 10.1038/s41467-023-40064-9
CHEMBL3707390 133507 57 None - 1 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 198 0 0 2 -0.4 CN1C(=O)N(C)C2C1N(C)C(=O)N2C 10.1038/s41467-023-40064-9
3198 205511 76 None -50 37 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1201049 205511 76 None -50 37 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL808 205511 76 None -50 37 Human 4.9 pAC50 = 4.9 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 10.1038/s41467-023-40064-9
137 370 52 None -6606 8 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
2119 370 52 None -6606 8 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
563 370 52 None -6606 8 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
66368 370 52 None -6606 8 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
CHEMBL266195 370 52 None -6606 8 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
DB00866 370 52 None -6606 8 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
2343 14452 57 None 1 4 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 14452 57 None 1 4 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 431 5 2 6 2.2 NS(=O)(=O)c1cc2c(cc1Cl)N=C(CSCc1ccccc1)NS2(=O)=O 10.1038/s41467-023-40064-9
2303 3185 68 None -10000 20 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
4946 3185 68 None -10000 20 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
564 3185 68 None -10000 20 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
63 3185 68 None -10000 20 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
91536 3185 68 None -10000 20 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL27 3185 68 None -10000 20 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL452861 3185 68 None -10000 20 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
DB00571 3185 68 None -10000 20 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
65859 19047 88 None -1 3 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 236 4 2 4 0.2 OC[C@@H](O)CN1CCN(c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1288810 19047 88 None -1 3 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 236 4 2 4 0.2 OC[C@@H](O)CN1CCN(c2ccccc2)CC1 10.1038/s41467-023-40064-9
5468 127226 85 None -1 3 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 260 4 1 3 3.2 CC(C(=O)O)c1ccc(C(=O)c2ccccc2)s1 10.1038/s41467-023-40064-9
CHEMBL365795 127226 85 None -1 3 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 260 4 1 3 3.2 CC(C(=O)O)c1ccc(C(=O)c2ccccc2)s1 10.1038/s41467-023-40064-9
31101 728 40 None -323 29 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
35 728 40 None -323 29 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
403 728 40 None -323 29 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 728 40 None -323 29 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 728 40 None -323 29 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
5311507 194813 41 None -13 12 Human 6.8 pAC50 = 6.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL53904 194813 41 None -13 12 Human 6.8 pAC50 = 6.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
DB01624 194813 41 None -13 12 Human 6.8 pAC50 = 6.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
216416 111579 48 None -18 23 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 111579 48 None -18 23 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
1547484 939 74 None -38 26 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
654 939 74 None -38 26 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
9072 939 74 None -38 26 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL43064 939 74 None -38 26 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00568 939 74 None -38 26 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
2600 3777 74 None -223 32 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3777 74 None -223 32 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3777 74 None -223 32 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3777 74 None -223 32 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3777 74 None -223 32 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
2812 4777 101 None -165 44 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1038/s41467-023-40064-9
CHEMBL104 4777 101 None -165 44 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1038/s41467-023-40064-9
54454 5256 88 None -6 14 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 418 6 1 5 4.6 CCC(C)(C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
CHEMBL1064 5256 88 None -6 14 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 418 6 1 5 4.6 CCC(C)(C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
4260 52556 31 None -14 9 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 52556 31 None -14 9 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 6 0 4 3.0 CC(=O)Oc1cc(C(C)C)c(OCCN(C)C)cc1C 10.1038/s41467-023-40064-9
DB09205 52556 31 None -14 9 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 6 0 4 3.0 CC(=O)Oc1cc(C(C)C)c(OCCN(C)C)cc1C 10.1038/s41467-023-40064-9
4450 178226 69 None -24 11 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 253 1 0 2 3.2 CN1CCOC(c2ccccc2)c2ccccc2C1 10.1038/s41467-023-40064-9
CHEMBL465026 178226 69 None -24 11 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 253 1 0 2 3.2 CN1CCOC(c2ccccc2)c2ccccc2C1 10.1038/s41467-023-40064-9
4746 204889 31 None -15 19 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL1334033 204889 31 None -15 19 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL75880 204889 31 None -15 19 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
168871 89128 14 None -1 13 Human 7.8 pAC50 = 7.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 89128 14 None -1 13 Human 7.8 pAC50 = 7.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
2342 598 39 None -5 8 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
331 598 39 None -5 8 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 598 39 None -5 8 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 598 39 None -5 8 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 598 39 None -5 8 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
150 2507 21 None -676 17 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2507 21 None -676 17 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2507 21 None -676 17 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2507 21 None -676 17 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2507 21 None -676 17 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
24826799 10796 104 None -53 20 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
CHEMBL1171837 10796 104 None -53 20 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
5039 63181 17 None -74 9 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1038/s41467-023-40064-9
CHEMBL1790041 63181 17 None -74 9 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1038/s41467-023-40064-9
DB00863 63181 17 None -74 9 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1038/s41467-023-40064-9
49846579 106167 102 None -7 2 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 867 13 3 11 8.7 CC1(C)CCC(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(NCC5CCOCC5)c([N+](=O)[O-])c4)c(Oc4cnc5[nH]ccc5c4)c3)CC2)=C(c2ccc(Cl)cc2)C1 10.1038/s41467-023-40064-9
CHEMBL3137309 106167 102 None -7 2 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 867 13 3 11 8.7 CC1(C)CCC(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(NCC5CCOCC5)c([N+](=O)[O-])c4)c(Oc4cnc5[nH]ccc5c4)c3)CC2)=C(c2ccc(Cl)cc2)C1 10.1038/s41467-023-40064-9
3947 206393 53 None -26 16 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL87708 206393 53 None -26 16 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
30323 62483 57 None -8 21 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL1563 62483 57 None -8 21 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL178 62483 57 None -8 21 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
5329102 194724 86 None -16 37 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 194724 86 None -16 37 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
124087 1388 114 None -407 27 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
7157 1388 114 None -407 27 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
814 1388 114 None -407 27 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
CHEMBL1172 1388 114 None -407 27 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
DB00967 1388 114 None -407 27 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
441074 19412 82 None -13 11 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 19412 82 None -13 11 Human 4.8 pAC50 = 4.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
3294 2004 111 None -18 23 Human 7.8 pAC50 = 7.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360 2004 111 None -18 23 Human 7.8 pAC50 = 7.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
87 2004 111 None -18 23 Human 7.8 pAC50 = 7.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
CHEMBL14376 2004 111 None -18 23 Human 7.8 pAC50 = 7.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
DB04946 2004 111 None -18 23 Human 7.8 pAC50 = 7.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
2713 205269 82 None -3 27 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 205269 82 None -3 27 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 205269 82 None -3 27 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 205269 82 None -3 27 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 205269 82 None -3 27 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 205269 82 None -3 27 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 205269 82 None -3 27 Human 5.8 pAC50 = 5.8 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
103 4151 61 None -316 22 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2875 4151 61 None -316 22 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
5736 4151 61 None -316 22 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL285802 4151 61 None -316 22 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB09225 4151 61 None -316 22 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
1201549 596 24 None -426 26 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
333 596 24 None -426 26 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 596 24 None -426 26 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 596 24 None -426 26 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 596 24 None -426 26 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 596 24 None -426 26 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
12574 2603 88 None -26 8 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
4810 2603 88 None -26 8 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
CHEMBL19236 2603 88 None -26 8 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
DB09242 2603 88 None -26 8 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
5318 15574 49 None -5 18 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1200348 15574 49 None -5 18 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1221 15574 49 None -5 18 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 10.1038/s41467-023-40064-9
3062316 33573 121 None -3 10 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 487 7 3 9 3.3 Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1 10.1038/s41467-023-40064-9
CHEMBL1421 33573 121 None -3 10 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 487 7 3 9 3.3 Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1 10.1038/s41467-023-40064-9
16363 595 53 None -363 21 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
312 595 53 None -363 21 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
9215 595 53 None -363 21 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL297302 595 53 None -363 21 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB12867 595 53 None -363 21 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
135398737 957 93 None -6 43 Human 7.7 pAC50 = 7.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 957 93 None -6 43 Human 7.7 pAC50 = 7.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 957 93 None -6 43 Human 7.7 pAC50 = 7.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 957 93 None -6 43 Human 7.7 pAC50 = 7.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 957 93 None -6 43 Human 7.7 pAC50 = 7.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
4418 34220 85 None -3 18 Human 6.7 pAC50 = 6.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
CHEMBL142635 34220 85 None -3 18 Human 6.7 pAC50 = 6.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
DB12092 34220 85 None -3 18 Human 6.7 pAC50 = 6.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
118422671 2755 65 None -660 23 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2755 65 None -660 23 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
189562 2755 65 None -660 23 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2755 65 None -660 23 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2755 65 None -660 23 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
9844194 2755 65 None -660 23 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
CHEMBL2365658 2755 65 None -660 23 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
CHEMBL3526436 2755 65 None -660 23 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2755 65 None -660 23 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2755 65 None -660 23 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
214 3858 58 None -134 28 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 3858 58 None -134 28 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 3858 58 None -134 28 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 3858 58 None -134 28 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 3858 58 None -134 28 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 3858 58 None -134 28 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2335 11846 22 None -14 34 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 11846 22 None -14 34 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 11846 22 None -14 34 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 11846 22 None -14 34 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
CHEMBL2103737 78138 0 None -3 8 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL None None None None 10.1038/s41467-023-40064-9
1830 2588 44 None -58 11 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
207 2588 44 None -58 11 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
23897 2588 44 None -58 11 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
CHEMBL460 2588 44 None -58 11 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
DB01618 2588 44 None -58 11 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
2393 3332 82 None -3981 9 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
5078 3332 82 None -3981 9 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
51 3332 82 None -3981 9 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
CHEMBL905 3332 82 None -3981 9 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
DB00953 3332 82 None -3981 9 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
3236 67607 43 None -1 7 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 5 0 2 3.6 CCc1ccc(C(=O)C(C)CN2CCCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL1902981 67607 43 None -1 7 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 5 0 2 3.6 CCc1ccc(C(=O)C(C)CN2CCCCC2)cc1 10.1038/s41467-023-40064-9
1427 2011 54 None -2691 30 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 2011 54 None -2691 30 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 2011 54 None -2691 30 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 2011 54 None -2691 30 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 2011 54 None -2691 30 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2136 3093 30 None -41 21 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
4768 3093 30 None -41 21 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
7268 3093 30 None -41 21 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL753 3093 30 None -41 21 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
DB00925 3093 30 None -41 21 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
2220 3132 82 None -758 17 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
27400 3132 82 None -758 17 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
93 3132 82 None -758 17 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
CHEMBL294951 3132 82 None -758 17 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
DB06153 3132 82 None -758 17 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
4031 99311 28 None -3 12 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 99311 28 None -3 12 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
16351 102728 47 None -338 17 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL304902 102728 47 None -338 17 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
DB13256 102728 47 None -338 17 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
2780 110527 36 None -218 11 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL325109 110527 36 None -218 11 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
DB13511 110527 36 None -218 11 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
11511120 78392 86 None -2 5 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 7 2 6 5.2 COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)/C=C/CN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL2110732 78392 86 None -2 5 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 7 2 6 5.2 COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)/C=C/CN1CCCCC1 10.1038/s41467-023-40064-9
107771 120246 49 None -1 9 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
CHEMBL35228 120246 49 None -1 9 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
3052776 206554 90 None -2 3 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 171 2 1 1 1.9 C#CCN[C@@H]1CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL887 206554 90 None -2 3 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 171 2 1 1 1.9 C#CCN[C@@H]1CCc2ccccc21 10.1038/s41467-023-40064-9
65709 59879 39 None -8 13 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 365 8 0 5 3.3 CCN(CC)CCn1c(=O)c(Cc2ccc(OC)cc2)nc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1729803 59879 39 None -8 13 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 365 8 0 5 3.3 CCN(CC)CCn1c(=O)c(Cc2ccc(OC)cc2)nc2ccccc21 10.1038/s41467-023-40064-9
25181577 78217 56 None -7 8 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 574 9 2 9 5.0 CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 10.1038/s41467-023-40064-9
CHEMBL2105695 78217 56 None -7 8 Human 4.7 pAC50 = 4.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 574 9 2 9 5.0 CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 10.1038/s41467-023-40064-9
2435 721 100 None -7 10 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
395 721 100 None -7 10 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
520 721 100 None -7 10 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
5386 721 100 None -7 10 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL844 721 100 None -7 10 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
DB00484 721 100 None -7 10 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
5440 28722 37 None -707 16 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1378 28722 37 None -707 16 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
DB00372 28722 37 None -707 16 Human 5.7 pAC50 = 5.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
154257 178617 67 None 4 19 Human 6.7 pAC50 = 6.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 178617 67 None 4 19 Human 6.7 pAC50 = 6.7 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
10219 188794 37 None -1 10 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 188794 37 None -1 10 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 188794 37 None -1 10 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
1400 1955 70 None -17 16 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3658 1955 70 None -17 16 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
7199 1955 70 None -17 16 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
91513 1955 70 None -17 16 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL896 1955 70 None -17 16 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
DB00557 1955 70 None -17 16 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
2169 44845 35 None -38 12 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 380 9 3 6 1.4 COc1ccccc1OCCNCC(O)c1ccc(C)c(S(N)(=O)=O)c1 10.1038/s41467-023-40064-9
CHEMBL152231 44845 35 None -38 12 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 380 9 3 6 1.4 COc1ccccc1OCCNCC(O)c1ccc(C)c(S(N)(=O)=O)c1 10.1038/s41467-023-40064-9
9801 91583 35 None -6 16 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 8 1 1 5.4 CC(Cc1ccccc1)NCCC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL24072 91583 35 None -6 16 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 8 1 1 5.4 CC(Cc1ccccc1)NCCC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
1164 1628 26 None -3235 13 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
1626 1628 26 None -3235 13 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
3345 1628 26 None -3235 13 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL596 1628 26 None -3235 13 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
DB00813 1628 26 None -3235 13 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
3658 4105 53 None -12 18 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
517 4105 53 None -12 18 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
5709 4105 53 None -12 18 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL312448 4105 53 None -12 18 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
DB06694 4105 53 None -12 18 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
5591 157529 90 None -14 17 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 157529 90 None -14 17 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
2267 559 71 None -100 14 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
271 559 71 None -100 14 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
7121 559 71 None -100 14 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL639 559 71 None -100 14 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00972 559 71 None -100 14 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
2318 154854 29 None -3 15 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL400599 154854 29 None -3 15 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
2803 954 58 None -15 14 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
516 954 58 None -15 14 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
704 954 58 None -15 14 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
CHEMBL134 954 58 None -15 14 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
DB00575 954 58 None -15 14 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
11434515 261 6 None -13182 11 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 261 6 None -13182 11 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 261 6 None -13182 11 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 261 6 None -13182 11 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 261 6 None -13182 11 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 261 6 None -13182 11 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
2131 57405 25 None -3 7 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 536 14 2 2 4.6 CC[N+](CC)(CCNC(=O)C(=O)NCC[N+](CC)(CC)Cc1ccccc1Cl)Cc1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1652 57405 25 None -3 7 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 536 14 2 2 4.6 CC[N+](CC)(CCNC(=O)C(=O)NCC[N+](CC)(CC)Cc1ccccc1Cl)Cc1ccccc1Cl 10.1038/s41467-023-40064-9
54682461 84684 62 None -5 12 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 84684 62 None -5 12 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
1343 1887 62 None -11 12 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
3519 1887 62 None -11 12 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
522 1887 62 None -11 12 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
CHEMBL862 1887 62 None -11 12 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
DB01018 1887 62 None -11 12 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
25102847 78219 93 None -21 10 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 78219 93 None -21 10 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
65700 78258 28 None -77 8 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 238 1 1 2 3.3 CNC1Cc2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL2106919 78258 28 None -77 8 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 238 1 1 2 3.3 CNC1Cc2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
2333 142333 97 None -22 14 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 10.1038/s41467-023-40064-9
CHEMBL388590 142333 97 None -22 14 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 10.1038/s41467-023-40064-9
10531 1419 21 None -19 26 Human 7.6 pAC50 = 7.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1419 21 None -19 26 Human 7.6 pAC50 = 7.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1419 21 None -19 26 Human 7.6 pAC50 = 7.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1419 21 None -19 26 Human 7.6 pAC50 = 7.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1419 21 None -19 26 Human 7.6 pAC50 = 7.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
1960 2855 67 None -11 19 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
439260 2855 67 None -11 19 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
505 2855 67 None -11 19 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
CHEMBL1437 2855 67 None -11 19 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
DB00368 2855 67 None -11 19 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
5282136 60282 73 None - 1 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 431 11 1 6 2.7 O=C(C[S+]([O-])Cc1ccco1)NC/C=C\COc1cc(CN2CCCCC2)ccn1 10.1038/s41467-023-40064-9
CHEMBL1742461 60282 73 None - 1 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 431 11 1 6 2.7 O=C(C[S+]([O-])Cc1ccco1)NC/C=C\COc1cc(CN2CCCCC2)ccn1 10.1038/s41467-023-40064-9
DB12770 60282 73 None - 1 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 431 11 1 6 2.7 O=C(C[S+]([O-])Cc1ccco1)NC/C=C\COc1cc(CN2CCCCC2)ccn1 10.1038/s41467-023-40064-9
9429 202131 58 None -275 18 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL609109 202131 58 None -275 18 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
DB01622 202131 58 None -275 18 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
260 3867 54 None -26 9 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2775 3867 54 None -26 9 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
656665 3867 54 None -26 9 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL56564 3867 54 None -26 9 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB11699 3867 54 None -26 9 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
60065 84367 6 None -17 11 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 505 7 1 8 4.2 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@@H]2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL2218858 84367 6 None -17 11 Human 4.6 pAC50 = 4.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 505 7 1 8 4.2 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@@H]2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL4743867 214031 14 None -89 15 Human 6.6 pAC50 = 6.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL None None None OCCN1CCN(CCC=C2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1 10.1038/s41467-023-40064-9
1028 291 71 None -44 19 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
139148732 291 71 None -44 19 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
479 291 71 None -44 19 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
5816 291 71 None -44 19 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
CHEMBL679 291 71 None -44 19 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
DB00668 291 71 None -44 19 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
3151 1461 97 None -602 24 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
945 1461 97 None -602 24 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
965 1461 97 None -602 24 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL219916 1461 97 None -602 24 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01184 1461 97 None -602 24 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
47319 26462 35 None 1 6 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 26462 35 None 1 6 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
4846 27985 53 None -1 10 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 308 1 2 6 2.2 O=C(O)c1cc(O)c2c3nc4ccccc4oc-3cc(=O)c2n1 10.1038/s41467-023-40064-9
CHEMBL1372341 27985 53 None -1 10 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 308 1 2 6 2.2 O=C(O)c1cc(O)c2c3nc4ccccc4oc-3cc(=O)c2n1 10.1038/s41467-023-40064-9
5639 98893 75 None -53 13 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 387 7 1 8 0.7 COc1ccccc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1 10.1038/s41467-023-40064-9
CHEMBL279229 98893 75 None -53 13 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 387 7 1 8 0.7 COc1ccccc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1 10.1038/s41467-023-40064-9
2179 167516 76 None -2 15 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL1256655 167516 76 None -2 15 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL43 167516 76 None -2 15 Human 5.6 pAC50 = 5.6 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
180 401 56 None -281 38 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 401 56 None -281 38 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 401 56 None -281 38 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 401 56 None -281 38 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 401 56 None -281 38 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
26757 207976 31 None -7 5 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 187 4 0 1 2.2 C#CCN(C)[C@H](C)Cc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL972 207976 31 None -7 5 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 187 4 0 1 2.2 C#CCN(C)[C@H](C)Cc1ccccc1 10.1038/s41467-023-40064-9
154417 23179 60 None -7079 7 Human 4.5 pAC50 = 4.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 289 4 1 4 1.9 CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
CHEMBL1331216 23179 60 None -7079 7 Human 4.5 pAC50 = 4.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 289 4 1 4 1.9 CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
DB00424 23179 60 None -7079 7 Human 4.5 pAC50 = 4.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 289 4 1 4 1.9 CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
2601 3778 33 None 1 17 Human 8.5 pAC50 = 8.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3778 33 None 1 17 Human 8.5 pAC50 = 8.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3778 33 None 1 17 Human 8.5 pAC50 = 8.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3778 33 None 1 17 Human 8.5 pAC50 = 8.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3778 33 None 1 17 Human 8.5 pAC50 = 8.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
102 4125 48 None -2 20 Human 8.5 pAC50 = 8.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 4125 48 None -2 20 Human 8.5 pAC50 = 8.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 4125 48 None -2 20 Human 8.5 pAC50 = 8.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 4125 48 None -2 20 Human 8.5 pAC50 = 8.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 4125 48 None -2 20 Human 8.5 pAC50 = 8.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
37 777 60 None -63 12 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
460 777 60 None -63 12 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 777 60 None -63 12 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 777 60 None -63 12 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 777 60 None -63 12 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
129211 3747 78 None -660 14 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3747 78 None -660 14 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3747 78 None -660 14 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3747 78 None -660 14 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3747 78 None -660 14 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
3036780 107529 20 None -1513 15 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
46780481 107529 20 None -1513 15 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
9903970 107529 20 None -1513 15 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3187365 107529 20 None -1513 15 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3544974 107529 20 None -1513 15 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL504548 107529 20 None -1513 15 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
DB06216 107529 20 None -1513 15 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
1782 2516 84 None -144 14 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
241 2516 84 None -144 14 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
4168 2516 84 None -144 14 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
CHEMBL86 2516 84 None -144 14 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
DB01233 2516 84 None -144 14 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
2286 3181 51 None -602 28 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927 3181 51 None -602 28 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7282 3181 51 None -602 28 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL643 3181 51 None -602 28 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01069 3181 51 None -602 28 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
44112 121288 48 None -269 12 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 10.1038/s41467-023-40064-9
CHEMBL357995 121288 48 None -269 12 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 10.1038/s41467-023-40064-9
2726 918 68 None -501 42 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 918 68 None -501 42 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 918 68 None -501 42 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 918 68 None -501 42 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 918 68 None -501 42 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
191 403 98 None -524 36 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 403 98 None -524 36 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 403 98 None -524 36 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 403 98 None -524 36 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 403 98 None -524 36 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
228 445 28 None -758 20 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
33 445 28 None -758 20 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
6005 445 28 None -758 20 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
CHEMBL53 445 28 None -758 20 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
DB00714 445 28 None -758 20 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
4413 98071 57 None 1 15 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
CHEMBL273264 98071 57 None 1 15 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
60753 194682 40 None 1 6 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 384 14 2 4 4.2 CCCCCCCN(CC)CCCC(O)c1ccc(NS(C)(=O)=O)cc1 10.1038/s41467-023-40064-9
CHEMBL533 194682 40 None 1 6 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 384 14 2 4 4.2 CCCCCCCN(CC)CCCC(O)c1ccc(NS(C)(=O)=O)cc1 10.1038/s41467-023-40064-9
11079 2731 63 None -13 7 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
3369 2731 63 None -13 7 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
4436 2731 63 None -13 7 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
5509 2731 63 None -13 7 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL761 2731 63 None -13 7 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
DB06711 2731 63 None -13 7 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
2865 4141 73 None -138 20 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 4141 73 None -138 20 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 4141 73 None -138 20 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 4141 73 None -138 20 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 4141 73 None -138 20 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
2351 4298 49 None -1 22 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1008 4298 49 None -1 22 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1257078 4298 49 None -1 22 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
3157 1469 71 None -446 22 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1469 71 None -446 22 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1469 71 None -446 22 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1469 71 None -446 22 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1469 71 None -446 22 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
100 3803 58 None -162 38 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2637 3803 58 None -162 38 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5452 3803 58 None -162 38 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL479 3803 58 None -162 38 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB00679 3803 58 None -162 38 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
3584 3775 64 None -1548 11 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
5401 3775 64 None -1548 11 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
7302 3775 64 None -1548 11 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
CHEMBL611 3775 64 None -1548 11 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
DB01162 3775 64 None -1548 11 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
213 3851 55 None -107 22 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
2717 3851 55 None -107 22 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
5533 3851 55 None -107 22 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL621 3851 55 None -107 22 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00656 3851 55 None -107 22 Human 6.5 pAC50 = 6.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
134 2512 24 None -1819 18 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2512 24 None -1819 18 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2512 24 None -1819 18 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2512 24 None -1819 18 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 2512 24 None -1819 18 Human 5.5 pAC50 = 5.5 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
11658860 2342 51 None -316 11 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
2941 2342 51 None -316 11 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
4374 2342 51 None -316 11 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
CHEMBL360328 2342 51 None -316 11 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
DB04871 2342 51 None -316 11 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
2470 3651 50 None -6165 23 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3300 3651 50 None -6165 23 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
5265 3651 50 None -6165 23 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
99 3651 50 None -6165 23 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL267930 3651 50 None -6165 23 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
19675 51668 43 None -28 15 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 7 1 5 5.0 CC(=O)c1ccc2c(c1)N(CCCN1CCC(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1584 51668 43 None -28 15 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 7 1 5 5.0 CC(=O)c1ccc2c(c1)N(CCCN1CCC(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
4756 16647 50 None -1 16 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
CHEMBL1201022 16647 50 None -1 16 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
CHEMBL1242 16647 50 None -1 16 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
5210 33336 48 None -1 8 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 33336 48 None -1 8 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 33336 48 None -1 8 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 10.1038/s41467-023-40064-9
2895 203590 41 None -186 15 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL669 203590 41 None -186 15 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
DB00924 203590 41 None -186 15 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
68617 205525 62 None -12 30 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 205525 62 None -12 30 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 205525 62 None -12 30 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
2407 3370 76 None -120 17 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
59227 3370 76 None -120 17 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
941 3370 76 None -120 17 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
CHEMBL1303 3370 76 None -120 17 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
DB05271 3370 76 None -120 17 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
6337614 12994 54 None -3 6 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 296 1 0 2 2.7 O=C1c2cccc3c2[C@H](CCC3)CN1[C@@H]1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL1189679 12994 54 None -3 6 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 296 1 0 2 2.7 O=C1c2cccc3c2[C@H](CCC3)CN1[C@@H]1CN2CCC1CC2 10.1038/s41467-023-40064-9
319 1323 44 None -407 18 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1323 44 None -407 18 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1323 44 None -407 18 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
72054 1323 44 None -407 18 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1323 44 None -407 18 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1323 44 None -407 18 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 1323 44 None -407 18 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
1593 2338 66 None -1 6 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
30668 2338 66 None -1 6 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
9868 2338 66 None -1 6 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
CHEMBL17860 2338 66 None -1 6 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
DB04948 2338 66 None -1 6 Human 6.4 pAC50 = 6.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
3149 12612 15 None -11 26 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1187011 12612 15 None -11 26 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
3949 100612 50 None -4 16 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL29188 100612 50 None -4 16 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
2520 204006 70 None -38 20 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 204006 70 None -38 20 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 204006 70 None -38 20 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
5453 203617 102 None -100 14 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 189 3 0 1 0.2 S=P(N1CC1)(N1CC1)N1CC1 10.1038/s41467-023-40064-9
CHEMBL671 203617 102 None -100 14 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 189 3 0 1 0.2 S=P(N1CC1)(N1CC1)N1CC1 10.1038/s41467-023-40064-9
2398 953 62 None -1819 36 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801 953 62 None -1819 36 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
701 953 62 None -1819 36 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL415 953 62 None -1819 36 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB01242 953 62 None -1819 36 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
4940 14468 35 None -151 15 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 340 5 0 4 4.8 CCC(=O)c1ccc2c(c1)N(CC(C)N(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1201210 14468 35 None -151 15 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 340 5 0 4 4.8 CCC(=O)c1ccc2c(c1)N(CC(C)N(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
5357 98734 41 None -407 5 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 7 1 5 1.7 CCN1CCCC1CNC(=O)c1cc(S(=O)(=O)CC)ccc1OC 10.1038/s41467-023-40064-9
CHEMBL277945 98734 41 None -407 5 Human 5.4 pAC50 = 5.4 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 7 1 5 1.7 CCN1CCCC1CNC(=O)c1cc(S(=O)(=O)CC)ccc1OC 10.1038/s41467-023-40064-9
4452 2760 19 None -1513 21 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
983 2760 19 None -1513 21 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
CHEMBL20734 2760 19 None -1513 21 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
209 3055 97 None -199 14 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2113 3055 97 None -199 14 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4748 3055 97 None -199 14 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL567 3055 97 None -199 14 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00850 3055 97 None -199 14 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2351 3284 64 None -93 27 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3284 64 None -93 27 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3284 64 None -93 27 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3284 64 None -93 27 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3284 64 None -93 27 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
16362 3123 71 None -52 35 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3123 71 None -52 35 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3123 71 None -52 35 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3123 71 None -52 35 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3123 71 None -52 35 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
47641 202869 32 None -2 6 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 287 5 0 1 5.0 CN(C/C=C/c1ccccc1)Cc1cccc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL626 202869 32 None -2 6 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 287 5 0 1 5.0 CN(C/C=C/c1ccccc1)Cc1cccc2ccccc12 10.1038/s41467-023-40064-9
2165 203781 71 None -3 8 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 355 6 2 4 5.2 CCN(CC)Cc1cc(Nc2ccnc3cc(Cl)ccc23)ccc1O 10.1038/s41467-023-40064-9
3647519 203781 71 None -3 8 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 355 6 2 4 5.2 CCN(CC)Cc1cc(Nc2ccnc3cc(Cl)ccc23)ccc1O 10.1038/s41467-023-40064-9
CHEMBL682 203781 71 None -3 8 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 355 6 2 4 5.2 CCN(CC)Cc1cc(Nc2ccnc3cc(Cl)ccc23)ccc1O 10.1038/s41467-023-40064-9
1353 1909 93 None -1023 39 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1909 93 None -1023 39 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1909 93 None -1023 39 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1909 93 None -1023 39 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1909 93 None -1023 39 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
1212 1660 50 None -138 35 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
204 1660 50 None -138 35 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3372 1660 50 None -138 35 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL726 1660 50 None -138 35 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00623 1660 50 None -138 35 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
135 2530 43 None -34 33 Human 7.3 pAC50 = 7.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 2530 43 None -34 33 Human 7.3 pAC50 = 7.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 2530 43 None -34 33 Human 7.3 pAC50 = 7.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 2530 43 None -34 33 Human 7.3 pAC50 = 7.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 2530 43 None -34 33 Human 7.3 pAC50 = 7.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
2695 3839 81 None -6 6 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 10.1038/s41467-023-40064-9
5504 3839 81 None -6 6 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 10.1038/s41467-023-40064-9
7310 3839 81 None -6 6 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL770 3839 81 None -6 6 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 10.1038/s41467-023-40064-9
DB00797 3839 81 None -6 6 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 10.1038/s41467-023-40064-9
240 943 43 None -371 23 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
2769 943 43 None -371 23 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
44279790 943 43 None -371 23 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
660 943 43 None -371 23 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
CHEMBL1729 943 43 None -371 23 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
CHEMBL560739 943 43 None -371 23 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
DB00604 943 43 None -371 23 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
2995 204403 53 None -1905 18 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1696 204403 53 None -1905 18 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL72 204403 53 None -1905 18 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
DB01151 204403 53 None -1905 18 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
26987 948 33 None -190 34 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
6063 948 33 None -190 34 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
671 948 33 None -190 34 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
CHEMBL1626 948 33 None -190 34 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
DB00283 948 33 None -190 34 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
20628 96546 28 None -13 13 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 324 6 1 5 3.7 CN(C)CCCNc1c2ccccc2nc2cccc([N+](=O)[O-])c12 10.1038/s41467-023-40064-9
CHEMBL26291 96546 28 None -13 13 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 324 6 1 5 3.7 CN(C)CCCNc1c2ccccc2nc2cccc([N+](=O)[O-])c12 10.1038/s41467-023-40064-9
2389 3329 118 None -23 29 Human 7.3 pAC50 = 7.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 3329 118 None -23 29 Human 7.3 pAC50 = 7.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 3329 118 None -23 29 Human 7.3 pAC50 = 7.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 3329 118 None -23 29 Human 7.3 pAC50 = 7.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 3329 118 None -23 29 Human 7.3 pAC50 = 7.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
2472 67282 48 None 3 4 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 67282 48 None 3 4 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 373 5 1 7 2.1 CCCC(=O)N1CCCN(c2nc(N)c3cc(OC)c(OC)cc3n2)CC1 10.1038/s41467-023-40064-9
4034 55820 55 None -13 18 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1623 55820 55 None -13 18 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
DB00737 55820 55 None -13 18 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
54477 84651 36 None -104 8 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1038/s41467-023-40064-9
CHEMBL22242 84651 36 None -104 8 Human 5.3 pAC50 = 5.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1038/s41467-023-40064-9
1971 2864 38 None -467 32 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2404 2864 38 None -467 32 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543 2864 38 None -467 32 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL445 2864 38 None -467 32 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
DB00540 2864 38 None -467 32 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
1816 2538 102 None -43 12 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
4205 2538 102 None -43 12 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
7241 2538 102 None -43 12 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
CHEMBL654 2538 102 None -43 12 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
DB00370 2538 102 None -43 12 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
135398745 2912 112 None -52 33 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 2912 112 None -52 33 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 2912 112 None -52 33 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 2912 112 None -52 33 Human 6.3 pAC50 = 6.3 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
5048 3131 64 None -3981 5 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1038/s41467-023-40064-9
8924 3131 64 None -3981 5 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1038/s41467-023-40064-9
9948102 3131 64 None -3981 5 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL462605 3131 64 None -3981 5 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1038/s41467-023-40064-9
DB11642 3131 64 None -3981 5 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1038/s41467-023-40064-9
2585 802 103 None -95 34 Human 7.2 pAC50 = 7.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 802 103 None -95 34 Human 7.2 pAC50 = 7.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 802 103 None -95 34 Human 7.2 pAC50 = 7.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 802 103 None -95 34 Human 7.2 pAC50 = 7.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 802 103 None -95 34 Human 7.2 pAC50 = 7.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
3152 188409 103 None -14 10 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
CHEMBL502 188409 103 None -14 10 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
5365247 138427 33 None -4 10 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 316 4 0 2 3.8 CN(C)C/C=C(/c1ccc(Br)cc1)c1cccnc1 10.1038/s41467-023-40064-9
CHEMBL37744 138427 33 None -4 10 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 316 4 0 2 3.8 CN(C)C/C=C(/c1ccc(Br)cc1)c1cccnc1 10.1038/s41467-023-40064-9
1890 2757 49 None -4 24 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
4449 2757 49 None -4 24 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
7247 2757 49 None -4 24 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
CHEMBL623 2757 49 None -4 24 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
DB01149 2757 49 None -4 24 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
2435 3588 83 None -1548 21 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
60149 3588 83 None -1548 21 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
98 3588 83 None -1548 21 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
CHEMBL12713 3588 83 None -1548 21 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
DB06144 3588 83 None -1548 21 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
4567 9946 34 None -11 12 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 3 3 3.4 CC(CCc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL114655 9946 34 None -11 12 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 3 3 3.4 CC(CCc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
1530 2180 50 None -467 25 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
3827 2180 50 None -467 25 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
7206 2180 50 None -467 25 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
CHEMBL534 2180 50 None -467 25 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
DB00920 2180 50 None -467 25 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
5482 14418 80 None -3 13 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 386 6 0 4 5.9 Clc1ccc(C(Cn2ccnc2)OCc2ccsc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1200438 14418 80 None -3 13 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 386 6 0 4 5.9 Clc1ccc(C(Cn2ccnc2)OCc2ccsc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
1524 2179 96 None -1548 18 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
197 2179 96 None -1548 18 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
3822 2179 96 None -1548 18 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
88 2179 96 None -1548 18 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL51 2179 96 None -1548 18 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
DB12465 2179 96 None -1548 18 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
4011 82406 49 None -549 26 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
CHEMBL21731 82406 49 None -549 26 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
9417 133510 54 None -83 15 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL1524185 133510 54 None -83 15 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL370753 133510 54 None -83 15 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
5311017 120602 11 None 2 5 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 239 5 0 1 3.8 C[C@@H](Cc1ccccc1)N(C)Cc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL3545985 120602 11 None 2 5 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 239 5 0 1 3.8 C[C@@H](Cc1ccccc1)N(C)Cc1ccccc1 10.1038/s41467-023-40064-9
DB00865 120602 11 None 2 5 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 239 5 0 1 3.8 C[C@@H](Cc1ccccc1)N(C)Cc1ccccc1 10.1038/s41467-023-40064-9
68712 100336 60 None -1 7 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1038/s41467-023-40064-9
CHEMBL289480 100336 60 None -1 7 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1038/s41467-023-40064-9
3926 207239 40 None -1 18 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 207239 40 None -1 18 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
21772 78397 31 None -457 10 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 293 4 0 1 4.5 CC(CC1c2ccccc2CCc2ccccc21)CN(C)C 10.1038/s41467-023-40064-9
CHEMBL2110816 78397 31 None -457 10 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 293 4 0 1 4.5 CC(CC1c2ccccc2CCc2ccccc21)CN(C)C 10.1038/s41467-023-40064-9
179 400 115 None -104 8 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
2159 400 115 None -104 8 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
963 400 115 None -104 8 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
CHEMBL243712 400 115 None -104 8 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
DB06288 400 115 None -104 8 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
104870 98878 47 None -2 10 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
5374 98878 47 None -2 10 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
CHEMBL279085 98878 47 None -2 10 Human 6.2 pAC50 = 6.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
2291 3182 58 None -134 13 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
2561 3182 58 None -134 13 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
4932 3182 58 None -134 13 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL631 3182 58 None -134 13 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
DB01182 3182 58 None -134 13 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
19910 37406 106 None -1 10 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 190 1 1 4 1.8 O=[N+]([O-])c1ccc(O)c2ncccc12 10.1038/s41467-023-40064-9
CHEMBL1454910 37406 106 None -1 10 Human 5.2 pAC50 = 5.2 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 190 1 1 4 1.8 O=[N+]([O-])c1ccc(O)c2ncccc12 10.1038/s41467-023-40064-9
17676 7070 29 None -165 13 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
5281082 7070 29 None -165 13 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1085 7070 29 None -165 13 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
DB01063 7070 29 None -165 13 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
2477 744 59 None -316 20 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1038/s41467-023-40064-9
36 744 59 None -316 20 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1038/s41467-023-40064-9
437 744 59 None -316 20 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1038/s41467-023-40064-9
CHEMBL49 744 59 None -316 20 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1038/s41467-023-40064-9
DB00490 744 59 None -316 20 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1038/s41467-023-40064-9
162265 202272 22 None 10 2 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 10.1038/s41467-023-40064-9
4786 202272 22 None 10 2 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL61006 202272 22 None 10 2 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 10.1038/s41467-023-40064-9
16722836 18983 99 None -6 13 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 524 10 3 8 4.8 Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1 10.1038/s41467-023-40064-9
CHEMBL1287853 18983 99 None -6 13 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 524 10 3 8 4.8 Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1 10.1038/s41467-023-40064-9
5210 33336 48 None -1 8 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 33336 48 None -1 8 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 33336 48 None -1 8 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 10.1038/s41467-023-40064-9
1234 189219 56 None -28 10 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 189219 56 None -28 10 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 189219 56 None -28 10 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
135409453 3771 41 None -263 36 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3771 41 None -263 36 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 3771 41 None -263 36 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
43815 186918 64 None -77 20 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL1708 186918 64 None -77 20 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL490 186918 64 None -77 20 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
2218 15281 23 None -10 12 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
CHEMBL1213033 15281 23 None -10 12 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
36811 1453 37 None -28 17 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
535 1453 37 None -28 17 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
937 1453 37 None -28 17 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL926 1453 37 None -28 17 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
DB00841 1453 37 None -28 17 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
2146 3098 67 None -181 15 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
485 3098 67 None -181 15 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
6041 3098 67 None -181 15 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL1215 3098 67 None -181 15 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
DB00388 3098 67 None -181 15 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
2448 99321 70 None -363 15 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 99321 70 None -363 15 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
DB12401 99321 70 None -363 15 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
115 343 71 None -14 5 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 343 71 None -14 5 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 343 71 None -14 5 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 343 71 None -14 5 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 343 71 None -14 5 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1038/s41467-023-40064-9
3158 56265 27 None -1202 28 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56265 27 None -1202 28 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
DB01142 56265 27 None -1202 28 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
2142 3094 58 None -31 18 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
4920903 3094 58 None -31 18 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
502 3094 58 None -31 18 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
5775 3094 58 None -31 18 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL597 3094 58 None -31 18 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
DB00692 3094 58 None -31 18 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
72093 35059 9 None -7 28 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 35059 9 None -7 28 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL2103773 35059 9 None -7 28 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
1549120 196484 85 None -5 19 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 319 4 1 4 2.9 CC(/C=C1\SC(=S)N(CC(=O)O)C1=O)=C\c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL56337 196484 85 None -5 19 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 319 4 1 4 2.9 CC(/C=C1\SC(=S)N(CC(=O)O)C1=O)=C\c1ccccc1 10.1038/s41467-023-40064-9
2284 3180 33 None -56 34 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 3180 33 None -56 34 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 3180 33 None -56 34 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 3180 33 None -56 34 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 3180 33 None -56 34 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
156419 937 74 None -13 15 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3308 937 74 None -13 15 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
647 937 74 None -13 15 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL1201284 937 74 None -13 15 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
DB01012 937 74 None -13 15 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3180 14471 41 None -2 10 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 289 8 0 3 3.9 CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL1201217 14471 41 None -2 10 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 289 8 0 3 3.9 CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1 10.1038/s41467-023-40064-9
68555 103110 21 None -190 7 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 103110 21 None -190 7 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
3081361 93932 123 None -1 14 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 93932 123 None -1 14 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
1385580 29274 76 None -104 19 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
4615 29274 76 None -104 19 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL13828 29274 76 None -104 19 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
DB12877 29274 76 None -104 19 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
3689 102769 55 None -128 16 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1372983 102769 55 None -128 16 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL305187 102769 55 None -128 16 Human 6.1 pAC50 = 6.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
22323 15297 32 None -5 11 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 15297 32 None -5 11 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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 15297 32 None -5 11 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 287 2 5 2 2.9 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)c(Cl)c1 10.1038/s41467-023-40064-9
73348210 210947 0 None -169 17 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
CHEMBL3039583 210947 0 None -169 17 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
nan 210947 0 None -169 17 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
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
21722 17990 31 None -22 21 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
CHEMBL126224 17990 31 None -22 21 Human 5.1 pAC50 = 5.1 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
2099 9305 55 None -109 5 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O 10.1038/s41467-023-40064-9
CHEMBL1110 9305 55 None -109 5 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O 10.1038/s41467-023-40064-9
2762 3861 31 None -301 9 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
5587 3861 31 None -301 9 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
7318 3861 31 None -301 9 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL1241 3861 31 None -301 9 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
DB00792 3861 31 None -301 9 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
2372 106466 40 None -354 6 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 345 10 2 5 2.6 COc1ccc(CCNCC(O)COc2cccc(C)c2)cc1OC 10.1038/s41467-023-40064-9
CHEMBL314010 106466 40 None -354 6 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 345 10 2 5 2.6 COc1ccc(CCNCC(O)COc2cccc(C)c2)cc1OC 10.1038/s41467-023-40064-9
3337 206365 27 None -2 6 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
65801 206365 27 None -2 6 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
66264 206365 27 None -2 6 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
91452 206365 27 None -2 6 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
CHEMBL87493 206365 27 None -2 6 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
DB00574 206365 27 None -2 6 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
2202 3130 96 None -16 10 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
4850 3130 96 None -16 10 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
49 3130 96 None -16 10 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
CHEMBL1371770 3130 96 None -16 10 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
DB12478 3130 96 None -16 10 Human 6.0 pAC50 = 6.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
25382 9155 37 None -263 21 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL110094 9155 37 None -263 21 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
135564886 14491 5 None -3 25 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
135673376 14491 5 None -3 25 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
137157436 14491 5 None -3 25 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
145948239 14491 5 None -3 25 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
71587099 14491 5 None -3 25 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
CHEMBL1201304 14491 5 None -3 25 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
3191 102856 97 None -89 33 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
CHEMBL305660 102856 97 None -89 33 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
DB11742 102856 97 None -89 33 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
2247 505 81 None -323 42 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 505 81 None -323 42 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 505 81 None -323 42 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 505 81 None -323 42 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 505 81 None -323 42 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
5284550 41719 15 None -512 16 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL108947 41719 15 None -512 16 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1492500 41719 15 None -512 16 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
DB09167 41719 15 None -512 16 Human 5.0 pAC50 = 5.0 Functional
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtrationCompound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
521 1403 69 None -4 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 1403 69 None -4 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 1403 69 None -4 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 1403 69 None -4 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 1403 69 None -4 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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
1593 2338 66 None -1 6 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C 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 2338 66 None -1 6 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C 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 2338 66 None -1 6 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C 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 2338 66 None -1 6 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C 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 2338 66 None -1 6 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C 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
57345628 71181 0 None 1659 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 244 5 1 3 2.4 CC(Oc1ccccc1CC1CC1)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956195 71181 0 None 1659 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 244 5 1 3 2.4 CC(Oc1ccccc1CC1CC1)C1=NCCN1 10.1016/j.bmc.2012.01.035
57345628 71181 0 None 1659 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysis
ChEMBL 244 5 1 3 2.4 CC(Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml300064v
CHEMBL1956195 71181 0 None 1659 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysis
ChEMBL 244 5 1 3 2.4 CC(Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml300064v
70695474 77670 0 None 794 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysis
ChEMBL 244 5 1 3 2.4 C[C@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml300064v
CHEMBL2089156 77670 0 None 794 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysis
ChEMBL 244 5 1 3 2.4 C[C@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml300064v
44292386 101480 0 None 35 2 Human 8.7 pEC50 = 8.7 Functional
Alpha2c receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha2c 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 101480 0 None 35 2 Human 8.7 pEC50 = 8.7 Functional
Alpha2c receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha2c 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
16757089 92289 1 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 311 5 1 5 3.0 C[C@@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm100977d
CHEMBL242693 92289 1 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 311 5 1 5 3.0 C[C@@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm100977d
57345626 71178 2 None 31 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 268 3 1 3 2.2 CC(Oc1ccccc1Br)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956192 71178 2 None 31 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 268 3 1 3 2.2 CC(Oc1ccccc1Br)C1=NCCN1 10.1016/j.bmc.2012.01.035
24906199 187663 15 None 6 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C 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 187663 15 None 6 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C 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
16757089 92289 1 None - 1 Human 8.0 pEC50 = 8 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 311 5 1 5 3.0 C[C@@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm061487a
CHEMBL242693 92289 1 None - 1 Human 8.0 pEC50 = 8 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 311 5 1 5 3.0 C[C@@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm061487a
49836306 18573 0 None 31 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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 18573 0 None 31 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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
11361608 84743 1 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm100977d
CHEMBL222928 84743 1 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm100977d
11361608 84743 1 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm0408215
CHEMBL222928 84743 1 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm0408215
44269140 33551 0 None 17 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 248 5 1 4 2.2 CC(C)Oc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL14208 33551 0 None 17 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 248 5 1 4 2.2 CC(C)Oc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
44371745 49287 0 None 100 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 218 4 1 3 2.0 CCc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL156336 49287 0 None 100 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 218 4 1 3 2.0 CCc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
57402718 71187 2 None -3 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C 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 71187 2 None -3 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C 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
11097789 102996 1 None -16 5 Human 7.0 pEC50 = 7 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL306792 102996 1 None -16 5 Human 7.0 pEC50 = 7 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
11361608 84743 1 None - 1 Human 7.0 pEC50 = 7 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm061487a
CHEMBL222928 84743 1 None - 1 Human 7.0 pEC50 = 7 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm061487a
24906196 187244 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 261 6 1 5 1.8 CCO/N=C/c1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
CHEMBL492639 187244 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 261 6 1 5 1.8 CCO/N=C/c1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
135453290 133604 33 None -5011 7 Human 5.0 pEC50 = 5 Functional
Activity at adrenergic Alpha-2C receptor expressed in rat-mouse hybrid NH108-15 cell by adenylyl cyclase assayActivity at adrenergic Alpha-2C receptor expressed in rat-mouse hybrid NH108-15 cell by adenylyl cyclase assay
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL371300 133604 33 None -5011 7 Human 5.0 pEC50 = 5 Functional
Activity at adrenergic Alpha-2C receptor expressed in rat-mouse hybrid NH108-15 cell by adenylyl cyclase assayActivity at adrenergic Alpha-2C receptor expressed in rat-mouse hybrid NH108-15 cell by adenylyl cyclase assay
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
57399145 71182 0 None -3 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 234 5 1 4 1.9 CCOc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956196 71182 0 None -3 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 234 5 1 4 1.9 CCOc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
131829 204725 15 None -37 3 Human 7.0 pEC50 = 7.0 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 295 1 4 5 1.7 Brc1c(NC2=NCCN2)ccc2c1NCCN2 10.1016/0960-894X(95)00391-6
CHEMBL74283 204725 15 None -37 3 Human 7.0 pEC50 = 7.0 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 295 1 4 5 1.7 Brc1c(NC2=NCCN2)ccc2c1NCCN2 10.1016/0960-894X(95)00391-6
9859437 168020 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Effective concentration at Alpha-2C adrenergic receptor from CHO-C4 cellsEffective concentration at Alpha-2C adrenergic receptor from CHO-C4 cells
ChEMBL 230 2 3 4 2.3 Cc1c(Nc2ncc[nH]2)ccc2c1NCCO2 10.1021/jm9605142
CHEMBL432155 168020 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Effective concentration at Alpha-2C adrenergic receptor from CHO-C4 cellsEffective concentration at Alpha-2C adrenergic receptor from CHO-C4 cells
ChEMBL 230 2 3 4 2.3 Cc1c(Nc2ncc[nH]2)ccc2c1NCCO2 10.1021/jm9605142
11043720 92170 0 None 257 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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 92170 0 None 257 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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 92170 0 None 257 3 Human 7.0 pEC50 = 7.0 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C 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 92170 0 None 257 3 Human 7.0 pEC50 = 7.0 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C 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
10221005 204320 0 None -575 3 Human 6.0 pEC50 = 6.0 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 267 4 2 5 0.8 Cc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL71479 204320 0 None -575 3 Human 6.0 pEC50 = 6.0 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 267 4 2 5 0.8 Cc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
57345627 71180 0 None 13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 230 4 1 3 2.5 C=C(C)c1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956194 71180 0 None 13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 230 4 1 3 2.5 C=C(C)c1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
2683 3832 60 None -5 6 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 3832 60 None -5 6 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 3832 60 None -5 6 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 3832 60 None -5 6 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 3832 60 None -5 6 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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
49836304 18569 1 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 230 4 1 3 2.3 C[C@@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
CHEMBL1276219 18569 1 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 230 4 1 3 2.3 C[C@@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
24906159 187403 12 None 3 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C 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 187403 12 None 3 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C 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
44292385 101119 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Alpha2c receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha2c receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMP
ChEMBL 270 3 1 3 2.6 c1ccc(C[C@H]2C3CCC(C3)[C@H]2NC2=NCCO2)cc1 10.1021/jm9905256
CHEMBL295186 101119 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Alpha2c receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha2c receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMP
ChEMBL 270 3 1 3 2.6 c1ccc(C[C@H]2C3CCC(C3)[C@H]2NC2=NCCO2)cc1 10.1021/jm9905256
1242 3611 27 None -10 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2015.01.013
935 3611 27 None -10 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2015.01.013
CHEMBL286080 3611 27 None -10 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2015.01.013
185076 187088 5 None -11 3 Human 7.9 pEC50 = 7.9 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL49137 187088 5 None -11 3 Human 7.9 pEC50 = 7.9 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
42669828 121716 2 None - 1 Human 3.8 pEC50 = 3.8 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 243 5 1 3 2.7 Cc1ccccc1Cn1ccnc1CNC(C)C 10.1016/j.bmc.2015.01.013
CHEMBL3588911 121716 2 None - 1 Human 3.8 pEC50 = 3.8 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 243 5 1 3 2.7 Cc1ccccc1Cn1ccnc1CNC(C)C 10.1016/j.bmc.2015.01.013
11140345 204169 0 None -2 5 Human 7.8 pEC50 = 7.8 Functional
Agonist potency at Alpha-2C adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 239 4 2 4 2.0 CSc1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70692 204169 0 None -2 5 Human 7.8 pEC50 = 7.8 Functional
Agonist potency at Alpha-2C adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 239 4 2 4 2.0 CSc1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
45487962 197483 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 218 4 1 3 2.1 CCCc1ccccc1COC1=NCCN1 10.1021/jm901262f
CHEMBL569933 197483 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 218 4 1 3 2.1 CCCc1ccccc1COC1=NCCN1 10.1021/jm901262f
11361608 84743 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm0408215
CHEMBL222928 84743 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm0408215
11277479 84748 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 280 4 1 3 3.4 Cc1cccc(-c2ccccc2OC(C)C2=NCCN2)c1 10.1021/jm0408215
CHEMBL222973 84748 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 280 4 1 3 3.4 Cc1cccc(-c2ccccc2OC(C)C2=NCCN2)c1 10.1021/jm0408215
57345625 71177 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 224 3 1 3 2.1 CC(Oc1ccccc1Cl)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956191 71177 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 224 3 1 3 2.1 CC(Oc1ccccc1Cl)C1=NCCN1 10.1016/j.bmc.2012.01.035
13178306 121707 2 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 187 3 2 2 2.3 Cc1ccccc1NCc1cnc[nH]1 10.1016/j.bmc.2015.01.013
CHEMBL3588902 121707 2 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 187 3 2 2 2.3 Cc1ccccc1NCc1cnc[nH]1 10.1016/j.bmc.2015.01.013
10333157 151236 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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 151236 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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 151236 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C 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 151236 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C 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
49836302 18564 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@H](C)C1=NCCN1 10.1021/jm100977d
CHEMBL1276139 18564 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@H](C)C1=NCCN1 10.1021/jm100977d
49836302 18564 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysis
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@H](C)C1=NCCN1 10.1021/ml300064v
CHEMBL1276139 18564 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysis
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@H](C)C1=NCCN1 10.1021/ml300064v
68712 100336 60 None -1 7 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2C 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 100336 60 None -1 7 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2C 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
57395731 71188 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C 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 71188 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C 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
481 2890 7 None -8 2 Human 5.7 pEC50 = 5.7 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1021/jm000542r
9838763 2890 7 None -8 2 Human 5.7 pEC50 = 5.7 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1021/jm000542r
CHEMBL72958 2890 7 None -8 2 Human 5.7 pEC50 = 5.7 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1021/jm000542r
10199335 204745 0 None -120 2 Human 5.7 pEC50 = 5.7 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74467 204745 0 None -120 2 Human 5.7 pEC50 = 5.7 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
218362 204798 5 None -1 3 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2C 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 204798 5 None -1 3 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2C 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
11109088 204178 0 None -6 5 Human 8.6 pEC50 = 8.6 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 255 4 2 4 2.5 CSc1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70751 204178 0 None -6 5 Human 8.6 pEC50 = 8.6 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 255 4 2 4 2.5 CSc1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
23622576 172770 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C 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 172770 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C 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
44292232 101319 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Alpha2c receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha2c 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 101319 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Alpha2c receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha2c 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
44314200 102950 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2C 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 102950 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2C 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
45487955 198308 0 None 125 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 232 4 1 3 2.7 CCCc1ccccc1C(C)OC1=NCCN1 10.1021/jm901262f
CHEMBL576078 198308 0 None 125 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 232 4 1 3 2.7 CCCc1ccccc1C(C)OC1=NCCN1 10.1021/jm901262f
49836301 18565 1 None 39 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@@H](C)C1=NCCN1 10.1021/jm100977d
CHEMBL1276140 18565 1 None 39 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@@H](C)C1=NCCN1 10.1021/jm100977d
49836308 18782 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 282 4 2 4 2.8 C[C@@H](Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm100977d
CHEMBL1278084 18782 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 282 4 2 4 2.8 C[C@@H](Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm100977d
49836301 18565 1 None 39 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysis
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@@H](C)C1=NCCN1 10.1021/ml300064v
CHEMBL1276140 18565 1 None 39 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysis
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@@H](C)C1=NCCN1 10.1021/ml300064v
49836307 18783 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 282 4 2 4 2.8 C[C@H](Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm100977d
CHEMBL1278085 18783 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 282 4 2 4 2.8 C[C@H](Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm100977d
10266032 188879 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Alpha2c receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha2c receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMP
ChEMBL 286 5 1 3 3.5 c1ccc(CCC[C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
CHEMBL50720 188879 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Alpha2c receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha2c receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMP
ChEMBL 286 5 1 3 3.5 c1ccc(CCC[C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
44421258 84744 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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 84744 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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 84744 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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
44371755 48775 0 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C 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 48775 0 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C 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
44371864 51139 0 None -2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C 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 51139 0 None -2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C 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
11000184 13050 0 None -8 5 Human 7.6 pEC50 = 7.6 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1190038 13050 0 None -8 5 Human 7.6 pEC50 = 7.6 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL540035 13050 0 None -8 5 Human 7.6 pEC50 = 7.6 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
10859076 13680 0 None -5 4 Human 7.6 pEC50 = 7.6 Functional
Agonist potency at Alpha-2C adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1194763 13680 0 None -5 4 Human 7.6 pEC50 = 7.6 Functional
Agonist potency at Alpha-2C adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL553276 13680 0 None -5 4 Human 7.6 pEC50 = 7.6 Functional
Agonist potency at Alpha-2C adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
45487958 198389 0 None -1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 190 2 1 3 1.5 Cc1ccccc1COC1=NCCN1 10.1021/jm901262f
CHEMBL576819 198389 0 None -1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 190 2 1 3 1.5 Cc1ccccc1COC1=NCCN1 10.1021/jm901262f
2435 721 100 None -7 10 Human 8.5 pEC50 = 8.5 Functional
Effective concentration at Alpha-2C adrenergic receptor from CHO-C4 cellsEffective concentration at Alpha-2C adrenergic receptor from CHO-C4 cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
395 721 100 None -7 10 Human 8.5 pEC50 = 8.5 Functional
Effective concentration at Alpha-2C adrenergic receptor from CHO-C4 cellsEffective concentration at Alpha-2C adrenergic receptor from CHO-C4 cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
520 721 100 None -7 10 Human 8.5 pEC50 = 8.5 Functional
Effective concentration at Alpha-2C adrenergic receptor from CHO-C4 cellsEffective concentration at Alpha-2C adrenergic receptor from CHO-C4 cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
5386 721 100 None -7 10 Human 8.5 pEC50 = 8.5 Functional
Effective concentration at Alpha-2C adrenergic receptor from CHO-C4 cellsEffective concentration at Alpha-2C adrenergic receptor from CHO-C4 cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
CHEMBL844 721 100 None -7 10 Human 8.5 pEC50 = 8.5 Functional
Effective concentration at Alpha-2C adrenergic receptor from CHO-C4 cellsEffective concentration at Alpha-2C adrenergic receptor from CHO-C4 cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
DB00484 721 100 None -7 10 Human 8.5 pEC50 = 8.5 Functional
Effective concentration at Alpha-2C adrenergic receptor from CHO-C4 cellsEffective concentration at Alpha-2C adrenergic receptor from CHO-C4 cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
3086326 204529 22 None -13 3 Human 7.5 pEC50 = 7.5 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 247 1 2 5 1.7 Clc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL72753 204529 22 None -13 3 Human 7.5 pEC50 = 7.5 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 247 1 2 5 1.7 Clc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
57400959 71186 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C 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 71186 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C 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
70693375 77669 0 None 12 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysis
ChEMBL 244 5 1 3 2.4 C[C@@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml300064v
CHEMBL2089155 77669 0 None 12 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysis
ChEMBL 244 5 1 3 2.4 C[C@@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml300064v
24906241 192815 0 None 7 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 280 2 1 4 2.5 c1ccc(-c2cccc3c2OC(C2=NCCN2)CO3)cc1 10.1021/jm800250z
CHEMBL522151 192815 0 None 7 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 280 2 1 4 2.5 c1ccc(-c2cccc3c2OC(C2=NCCN2)CO3)cc1 10.1021/jm800250z
434526 77566 28 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 194 3 1 4 1.9 NCCSc1nc2ccccc2o1 10.1016/j.bmc.2015.01.013
CHEMBL2087646 77566 28 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 194 3 1 4 1.9 NCCSc1nc2ccccc2o1 10.1016/j.bmc.2015.01.013
9816461 10717 7 None -60 2 Human 5.5 pEC50 = 5.5 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL117094 10717 7 None -60 2 Human 5.5 pEC50 = 5.5 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL544290 10717 7 None -60 2 Human 5.5 pEC50 = 5.5 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
32238 22653 114 None - 1 Human 3.5 pEC50 = 3.5 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 256 3 1 3 2.9 OC(Cn1ccnc1)c1ccc(Cl)cc1Cl 10.1016/j.bmc.2015.01.013
CHEMBL1327 22653 114 None - 1 Human 3.5 pEC50 = 3.5 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 256 3 1 3 2.9 OC(Cn1ccnc1)c1ccc(Cl)cc1Cl 10.1016/j.bmc.2015.01.013
2146 3098 67 None -181 15 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 3098 67 None -181 15 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 3098 67 None -181 15 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 3098 67 None -181 15 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 3098 67 None -181 15 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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
122180567 121709 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 261 4 1 3 3.8 c1cncc(-c2ccccc2NCc2ccncc2)c1 10.1016/j.bmc.2015.01.013
CHEMBL3588904 121709 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 261 4 1 3 3.8 c1cncc(-c2ccccc2NCc2ccncc2)c1 10.1016/j.bmc.2015.01.013
49836303 18570 1 None 89 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 230 4 1 3 2.3 C[C@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
CHEMBL1276220 18570 1 None 89 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 230 4 1 3 2.3 C[C@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
24906197 187664 0 None 8 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 323 7 1 5 3.0 CC(Oc1ccccc1/C=N/OCc1ccccc1)C1=NCCN1 10.1021/jm800250z
CHEMBL495097 187664 0 None 8 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 323 7 1 5 3.0 CC(Oc1ccccc1/C=N/OCc1ccccc1)C1=NCCN1 10.1021/jm800250z
11300487 85000 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 280 4 1 3 3.4 Cc1ccccc1-c1ccccc1OC(C)C1=NCCN1 10.1021/jm0408215
CHEMBL223830 85000 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 280 4 1 3 3.4 Cc1ccccc1-c1ccccc1OC(C)C1=NCCN1 10.1021/jm0408215
16757089 92289 1 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 311 5 1 5 3.0 C[C@@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm061487a
CHEMBL242693 92289 1 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 311 5 1 5 3.0 C[C@@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm061487a
45487956 198365 0 None 25 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 230 3 1 3 2.6 CC(OC1=NCCN1)c1ccccc1C1CC1 10.1021/jm901262f
CHEMBL576623 198365 0 None 25 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 230 3 1 3 2.6 CC(OC1=NCCN1)c1ccccc1C1CC1 10.1021/jm901262f
44549156 18568 0 None 79 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 230 4 1 3 2.3 CC(Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
CHEMBL1276218 18568 0 None 79 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 230 4 1 3 2.3 CC(Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
11265631 136407 0 None 9 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adrenergic Alpha-2C 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 136407 0 None 9 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adrenergic Alpha-2C 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
2765 942 19 None -38 7 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/jm901262f
515 942 19 None -38 7 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/jm901262f
CHEMBL13852 942 19 None -38 7 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/jm901262f
DB09202 942 19 None -38 7 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/jm901262f
44269089 97003 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 232 4 1 3 2.6 CC(Oc1ccccc1C(C)C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL266613 97003 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 232 4 1 3 2.6 CC(Oc1ccccc1C(C)C)C1=NCCN1 10.1016/j.bmc.2012.01.035
44314198 104410 0 None -2 3 Human 8.4 pEC50 = 8.4 Functional
Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2C 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 104410 0 None -2 3 Human 8.4 pEC50 = 8.4 Functional
Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2C 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 101467 0 None -2 3 Human 8.4 pEC50 = 8.4 Functional
Alpha-2C adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha-2C 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 101467 0 None -2 3 Human 8.4 pEC50 = 8.4 Functional
Alpha-2C adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha-2C 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
11058166 204703 0 None -10 2 Human 6.4 pEC50 = 6.4 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cccc(F)c1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74114 204703 0 None -10 2 Human 6.4 pEC50 = 6.4 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cccc(F)c1NCC1=NCCN1 10.1021/jm000542r
11346584 136982 0 None 112 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm100977d
CHEMBL374584 136982 0 None 112 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm100977d
11346584 136982 0 None 112 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm0408215
CHEMBL374584 136982 0 None 112 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm0408215
11346584 136982 0 None 112 2 Human 7.3 pEC50 = 7.3 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm061487a
CHEMBL374584 136982 0 None 112 2 Human 7.3 pEC50 = 7.3 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm061487a
57345629 71183 0 None 269 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 246 5 1 4 2.0 CC(Oc1ccccc1OC1CC1)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956197 71183 0 None 269 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 246 5 1 4 2.0 CC(Oc1ccccc1OC1CC1)C1=NCCN1 10.1016/j.bmc.2012.01.035
46743607 121710 0 None - 1 Human 3.3 pEC50 = 3.3 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 264 5 2 3 2.8 c1ccc(-c2nc(CNCc3cccnc3)c[nH]2)cc1 10.1016/j.bmc.2015.01.013
CHEMBL3588905 121710 0 None - 1 Human 3.3 pEC50 = 3.3 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 264 5 2 3 2.8 c1ccc(-c2nc(CNCc3cccnc3)c[nH]2)cc1 10.1016/j.bmc.2015.01.013
11140347 204531 1 None -3 5 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72768 204531 1 None -3 5 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
11108001 10870 2 None 1 5 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-2C adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL117248 10870 2 None 1 5 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-2C adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL540542 10870 2 None 1 5 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-2C adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
45487145 197657 0 None 19 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 230 4 1 3 2.5 C=CCc1ccccc1C(C)OC1=NCCN1 10.1021/jm901262f
CHEMBL570973 197657 0 None 19 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 230 4 1 3 2.5 C=CCc1ccccc1C(C)OC1=NCCN1 10.1021/jm901262f
24906198 187662 3 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/jm100977d
CHEMBL495095 187662 3 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/jm100977d
11265631 136407 0 None 9 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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 136407 0 None 9 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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
24906198 187662 3 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysis
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/ml300064v
CHEMBL495095 187662 3 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2C adrenoceptor expressed in CHO cells assessed as extracellular acidification measured after 4 mins by cytosensor microphysiometric analysis
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/ml300064v
24906198 187662 3 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
CHEMBL495095 187662 3 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
11265631 136407 0 None 9 3 Human 7.3 pEC50 = 7.3 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C 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 136407 0 None 9 3 Human 7.3 pEC50 = 7.3 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C 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
11173568 84639 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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 84639 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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
24906160 169454 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 247 5 1 5 1.4 CO/N=C/c1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
CHEMBL442815 169454 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 247 5 1 5 1.4 CO/N=C/c1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
11090351 163389 0 None -20 2 Human 6.3 pEC50 = 6.3 Functional
Agonist potency at Alpha-2C adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL419448 163389 0 None -20 2 Human 6.3 pEC50 = 6.3 Functional
Agonist potency at Alpha-2C adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
10221004 204229 0 None -20 2 Human 5.3 pEC50 = 5.3 Functional
Agonist potency at Alpha-2C adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 267 5 2 5 0.9 CCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70973 204229 0 None -20 2 Human 5.3 pEC50 = 5.3 Functional
Agonist potency at Alpha-2C adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 267 5 2 5 0.9 CCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
11079 2731 63 None -13 7 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/j.bmc.2015.01.013
3369 2731 63 None -13 7 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/j.bmc.2015.01.013
4436 2731 63 None -13 7 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/j.bmc.2015.01.013
5509 2731 63 None -13 7 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/j.bmc.2015.01.013
CHEMBL761 2731 63 None -13 7 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/j.bmc.2015.01.013
DB06711 2731 63 None -13 7 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/j.bmc.2015.01.013
2803 954 58 None -15 14 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2C 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
516 954 58 None -15 14 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2C 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
704 954 58 None -15 14 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2C 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 954 58 None -15 14 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2C 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 954 58 None -15 14 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2C 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
10382537 204164 12 None -4 2 Human 7.3 pEC50 = 7.3 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 339 1 2 5 1.6 Ic1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL70676 204164 12 None -4 2 Human 7.3 pEC50 = 7.3 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 339 1 2 5 1.6 Ic1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
2803 954 58 None -15 14 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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
516 954 58 None -15 14 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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
704 954 58 None -15 14 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 954 58 None -15 14 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 954 58 None -15 14 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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
44371744 50319 0 None 8 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 270 7 1 3 2.9 C=CCc1cccc(CC=C)c1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL157206 50319 0 None 8 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 270 7 1 3 2.9 C=CCc1cccc(CC=C)c1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
135399666 168761 7 None -66 6 Human 5.3 pEC50 = 5.3 Functional
Activity at adrenergic Alpha-2C receptor expressed in rat-mouse hybrid NH108-15 cell by adenylyl cyclase assayActivity at adrenergic Alpha-2C receptor expressed in rat-mouse hybrid NH108-15 cell by adenylyl cyclase assay
ChEMBL 191 2 2 4 1.1 C[C@@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL437314 168761 7 None -66 6 Human 5.3 pEC50 = 5.3 Functional
Activity at adrenergic Alpha-2C receptor expressed in rat-mouse hybrid NH108-15 cell by adenylyl cyclase assayActivity at adrenergic Alpha-2C receptor expressed in rat-mouse hybrid NH108-15 cell by adenylyl cyclase assay
ChEMBL 191 2 2 4 1.1 C[C@@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
2803 954 58 None -15 14 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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
516 954 58 None -15 14 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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
704 954 58 None -15 14 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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 954 58 None -15 14 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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 954 58 None -15 14 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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
44352207 18854 1 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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 18854 1 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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 18854 1 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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 18854 1 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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 18854 1 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C 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 18854 1 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C 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 18854 1 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C 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 18854 1 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C 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
11360447 84999 0 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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 84999 0 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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
49836305 18574 0 None 9 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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 18574 0 None 9 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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
10176999 103552 21 None 1 3 Human 8.2 pEC50 = 8.2 Functional
Effective concentration at Alpha-2C adrenergic receptor from CHO-C4 cellsEffective concentration at Alpha-2C adrenergic receptor from CHO-C4 cells
ChEMBL 231 2 2 4 2.2 Cc1c(Nc2ncc[nH]2)ccc2c1OCCO2 10.1021/jm9605142
CHEMBL308570 103552 21 None 1 3 Human 8.2 pEC50 = 8.2 Functional
Effective concentration at Alpha-2C adrenergic receptor from CHO-C4 cellsEffective concentration at Alpha-2C adrenergic receptor from CHO-C4 cells
ChEMBL 231 2 2 4 2.2 Cc1c(Nc2ncc[nH]2)ccc2c1OCCO2 10.1021/jm9605142
11211035 85001 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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 85001 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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 85001 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C 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 85001 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C 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
9971924 184224 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Alpha2c receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha2c 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 184224 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Alpha2c receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha2c 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
45487089 197638 0 None 79 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 204 2 1 3 2.0 Cc1ccccc1C(C)OC1=NCCN1 10.1021/jm901262f
CHEMBL570863 197638 0 None 79 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 204 2 1 3 2.0 Cc1ccccc1C(C)OC1=NCCN1 10.1021/jm901262f
57393922 71184 0 None 5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 232 5 1 4 2.0 C=COc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956198 71184 0 None 5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 232 5 1 4 2.0 C=COc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
10923927 204176 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 279 3 2 5 0.8 O=S1(=O)CCCc2cccc(NCC3=NCCN3)c21 10.1021/jm000542r
CHEMBL70740 204176 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 279 3 2 5 0.8 O=S1(=O)CCCc2cccc(NCC3=NCCN3)c21 10.1021/jm000542r
770500 121714 3 None - 1 Human 3.2 pEC50 = 3.2 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 242 4 2 3 2.4 NCC(=O)Nc1ccccc1Oc1ccccc1 10.1016/j.bmc.2015.01.013
CHEMBL3588909 121714 3 None - 1 Human 3.2 pEC50 = 3.2 Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysisAgonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
ChEMBL 242 4 2 3 2.4 NCC(=O)Nc1ccccc1Oc1ccccc1 10.1016/j.bmc.2015.01.013
11034737 204526 0 None -1 4 Human 8.1 pEC50 = 8.1 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 289 4 2 4 2.8 CSc1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72724 204526 0 None -1 4 Human 8.1 pEC50 = 8.1 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 289 4 2 4 2.8 CSc1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
16757182 153249 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 311 5 1 5 3.0 C[C@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm100977d
CHEMBL397753 153249 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 311 5 1 5 3.0 C[C@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm100977d
16757182 153249 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 311 5 1 5 3.0 C[C@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm061487a
CHEMBL397753 153249 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 311 5 1 5 3.0 C[C@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm061487a
294234 102891 3 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2C 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 102891 3 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2C 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
24906200 193154 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C 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 193154 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C 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
57395732 71189 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 342 5 1 3 4.8 CC(Oc1c(-c2ccccc2)cccc1-c1ccccc1)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956203 71189 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 342 5 1 3 4.8 CC(Oc1c(-c2ccccc2)cccc1-c1ccccc1)C1=NCCN1 10.1016/j.bmc.2012.01.035
1960 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human Alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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
57395663 71179 0 None -3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 258 3 1 3 2.5 CC(Oc1ccccc1C(F)(F)F)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956193 71179 0 None -3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 258 3 1 3 2.5 CC(Oc1ccccc1C(F)(F)F)C1=NCCN1 10.1016/j.bmc.2012.01.035
1960 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C 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
24906201 187351 0 None 15 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 280 2 1 4 2.5 c1ccc(-c2cccc3c2OCC(C2=NCCN2)O3)cc1 10.1021/jm800250z
CHEMBL493272 187351 0 None 15 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 280 2 1 4 2.5 c1ccc(-c2cccc3c2OCC(C2=NCCN2)O3)cc1 10.1021/jm800250z
9947861 204160 0 None -281 3 Human 6.1 pEC50 = 6.1 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70634 204160 0 None -281 3 Human 6.1 pEC50 = 6.1 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
1960 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C 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 2855 67 None -11 19 Human 6.1 pEC50 = 6.1 Functional
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic Alpha-2C 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
2435 721 100 None -7 10 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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
395 721 100 None -7 10 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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
520 721 100 None -7 10 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 721 100 None -7 10 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 721 100 None -7 10 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 721 100 None -7 10 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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
10934575 204484 0 None -81 5 Human 8.1 pEC50 = 8.1 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 235 4 2 4 2.1 CSc1ccc(C)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72441 204484 0 None -81 5 Human 8.1 pEC50 = 8.1 Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptorAgonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
ChEMBL 235 4 2 4 2.1 CSc1ccc(C)cc1NCC1=NCCN1 10.1021/jm000542r
11173544 166259 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 280 4 1 3 3.4 Cc1ccc(-c2ccccc2OC(C)C2=NCCN2)cc1 10.1021/jm0408215
CHEMBL426900 166259 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 280 4 1 3 3.4 Cc1ccc(-c2ccccc2OC(C)C2=NCCN2)cc1 10.1021/jm0408215
15675860 204427 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 305 1 2 5 2.1 Cc1cnc2c(Br)c(NC3=NCCN3)ccc2n1 10.1016/0960-894X(95)00391-6
CHEMBL72147 204427 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 305 1 2 5 2.1 Cc1cnc2c(Br)c(NC3=NCCN3)ccc2n1 10.1016/0960-894X(95)00391-6
44312036 204563 1 None 19 2 Human 6.1 pEC50 = 6.1 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 305 1 2 5 2.2 CC1CN=C(Nc2ccc3nccnc3c2Br)N1 10.1016/0960-894X(95)00391-6
CHEMBL72995 204563 1 None 19 2 Human 6.1 pEC50 = 6.1 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 305 1 2 5 2.2 CC1CN=C(Nc2ccc3nccnc3c2Br)N1 10.1016/0960-894X(95)00391-6
2435 721 100 None -7 10 Human 8.0 pEC50 = 8.0 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
395 721 100 None -7 10 Human 8.0 pEC50 = 8.0 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
520 721 100 None -7 10 Human 8.0 pEC50 = 8.0 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
5386 721 100 None -7 10 Human 8.0 pEC50 = 8.0 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
CHEMBL844 721 100 None -7 10 Human 8.0 pEC50 = 8.0 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
DB00484 721 100 None -7 10 Human 8.0 pEC50 = 8.0 Functional
Alpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesisAlpha-2C adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
11371902 141636 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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 141636 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human Alpha-2C 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
11140033 20681 0 None 4 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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 20681 0 None 4 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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
11371902 141636 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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 141636 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2C 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
57402717 71185 2 None 10 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 220 4 1 4 1.5 COc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956199 71185 2 None 10 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 220 4 1 4 1.5 COc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
156735109 186603 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
Inhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assayInhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assay
ChEMBL 505 8 1 7 4.0 O=C(NCc1ncc(F)cc1F)c1cnc(N2CCC(N3CCCC(COC4CCC4)C3)CC2)s1 10.1021/acsmedchemlett.1c00423
CHEMBL4878875 186603 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
Inhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assayInhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assay
ChEMBL 505 8 1 7 4.0 O=C(NCc1ncc(F)cc1F)c1cnc(N2CCC(N3CCCC(COC4CCC4)C3)CC2)s1 10.1021/acsmedchemlett.1c00423
156735161 186366 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Inhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assayInhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assay
ChEMBL 465 5 1 6 3.5 O=C(NCc1ncc(F)cc1F)c1cnc(N2CCC(N3CCCC4(CC4)C3)C(F)C2)s1 10.1021/acsmedchemlett.1c00423
CHEMBL4875484 186366 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Inhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assayInhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assay
ChEMBL 465 5 1 6 3.5 O=C(NCc1ncc(F)cc1F)c1cnc(N2CCC(N3CCCC4(CC4)C3)C(F)C2)s1 10.1021/acsmedchemlett.1c00423
164617361 184833 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Inhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assayInhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assay
ChEMBL 499 6 1 7 3.8 COc1cccc2c1CN(C1CCN(c3ncc(C(=O)NCc4ncc(F)cc4F)s3)CC1)CC2 10.1021/acsmedchemlett.1c00423
CHEMBL4852159 184833 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Inhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assayInhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assay
ChEMBL 499 6 1 7 3.8 COc1cccc2c1CN(C1CCN(c3ncc(C(=O)NCc4ncc(F)cc4F)s3)CC1)CC2 10.1021/acsmedchemlett.1c00423
156735115 186423 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Inhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assayInhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assay
ChEMBL 527 8 1 7 3.9 O=C(NCc1ncc(F)cc1F)c1cnc(N2CCC(N3CCCC(OCC4CC4(F)F)C3)CC2)s1 10.1021/acsmedchemlett.1c00423
CHEMBL4876214 186423 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Inhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assayInhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assay
ChEMBL 527 8 1 7 3.9 O=C(NCc1ncc(F)cc1F)c1cnc(N2CCC(N3CCCC(OCC4CC4(F)F)C3)CC2)s1 10.1021/acsmedchemlett.1c00423
156735204 185908 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Inhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assayInhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assay
ChEMBL 483 5 1 6 4.1 Cc1ccc2c(c1)CN(C1CCN(c3ncc(C(=O)NCc4ncc(F)cc4F)s3)CC1)CC2 10.1021/acsmedchemlett.1c00423
CHEMBL4868807 185908 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Inhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assayInhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assay
ChEMBL 483 5 1 6 4.1 Cc1ccc2c(c1)CN(C1CCN(c3ncc(C(=O)NCc4ncc(F)cc4F)s3)CC1)CC2 10.1021/acsmedchemlett.1c00423
156735188 185756 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Inhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assayInhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assay
ChEMBL 505 8 1 7 4.0 O=C(NCc1ncc(F)cc1F)c1cnc(N2CCC(N3CCCC(OCC4CCC4)C3)CC2)s1 10.1021/acsmedchemlett.1c00423
CHEMBL4866383 185756 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Inhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assayInhibition of human alpha 2C adrenergic receptor expressed in CHO-K1 cells coexpressing Gaq and aequorin assessed as suppression of noradrenaline-induced intracellular calcium release by bioluminescence assay
ChEMBL 505 8 1 7 4.0 O=C(NCc1ncc(F)cc1F)c1cnc(N2CCC(N3CCCC(OCC4CCC4)C3)CC2)s1 10.1021/acsmedchemlett.1c00423
136 3290 32 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant alpha2C adrenoceptor assessed as inhibition of epinephrine-induced cAMP accumulationAntagonist activity at human recombinant alpha2C adrenoceptor assessed as inhibition of epinephrine-induced cAMP accumulation
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/jm401895u
223 3290 32 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant alpha2C adrenoceptor assessed as inhibition of epinephrine-induced cAMP accumulationAntagonist activity at human recombinant alpha2C adrenoceptor assessed as inhibition of epinephrine-induced cAMP accumulation
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/jm401895u
643606 3290 32 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant alpha2C adrenoceptor assessed as inhibition of epinephrine-induced cAMP accumulationAntagonist activity at human recombinant alpha2C adrenoceptor assessed as inhibition of epinephrine-induced cAMP accumulation
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/jm401895u
CHEMBL10347 3290 32 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant alpha2C adrenoceptor assessed as inhibition of epinephrine-induced cAMP accumulationAntagonist activity at human recombinant alpha2C adrenoceptor assessed as inhibition of epinephrine-induced cAMP accumulation
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/jm401895u
11306100 168505 0 None - 0 Human 10.5 pKi = 10.5 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 168505 0 None - 0 Human 10.5 pKi = 10.5 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
11271808 60992 0 None - 0 Human 10.0 pKi = 10 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 60992 0 None - 0 Human 10.0 pKi = 10 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
135519400 63892 0 None - 0 Human 10.0 pKi = 10 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 63892 0 None - 0 Human 10.0 pKi = 10 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
135440165 78943 0 None - 0 Human 10.0 pKi = 10 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 78943 0 None - 0 Human 10.0 pKi = 10 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
11214030 60542 0 None - 0 Human 9.7 pKi = 9.7 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 60542 0 None - 0 Human 9.7 pKi = 9.7 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
44387789 60573 0 None - 0 Human 9.7 pKi = 9.7 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 60573 0 None - 0 Human 9.7 pKi = 9.7 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
11259744 60794 0 None - 0 Human 9.7 pKi = 9.7 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 60794 0 None - 0 Human 9.7 pKi = 9.7 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
11785961 63278 0 None - 0 Human 9.7 pKi = 9.7 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 63278 0 None - 0 Human 9.7 pKi = 9.7 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
44324800 206946 0 None - 0 Human 9.7 pKi = 9.7 Functional
Binding affinity for alpha-2C-adrenergic receptorBinding affinity for alpha-2C-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 206946 0 None - 0 Human 9.7 pKi = 9.7 Functional
Binding affinity for alpha-2C-adrenergic receptorBinding affinity for alpha-2C-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
11785068 60554 0 None - 0 Human 9.5 pKi = 9.5 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 60554 0 None - 0 Human 9.5 pKi = 9.5 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 63857 0 None - 0 Human 9.3 pKi = 9.3 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 63857 0 None - 0 Human 9.3 pKi = 9.3 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
11190988 131801 0 None - 0 Human 9.3 pKi = 9.3 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 131801 0 None - 0 Human 9.3 pKi = 9.3 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
11318438 165982 0 None - 0 Human 9.3 pKi = 9.3 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 165982 0 None - 0 Human 9.3 pKi = 9.3 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
44324972 163370 0 None - 0 Human 9.2 pKi = 9.2 Functional
Binding affinity for alpha-2C-adrenergic receptorBinding affinity for alpha-2C-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 163370 0 None - 0 Human 9.2 pKi = 9.2 Functional
Binding affinity for alpha-2C-adrenergic receptorBinding affinity for alpha-2C-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
11191321 62983 0 None - 0 Human 8.8 pKi = 8.8 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 62983 0 None - 0 Human 8.8 pKi = 8.8 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
135405894 78928 0 None - 0 Human 8.8 pKi = 8.8 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 78928 0 None - 0 Human 8.8 pKi = 8.8 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
44579272 187093 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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 187093 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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
71450907 78937 0 None - 0 Human 8.8 pKi = 8.8 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 78937 0 None - 0 Human 8.8 pKi = 8.8 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
44579187 189677 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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 189677 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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
25110718 193307 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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(C[C@H]2COc3ccccc3O2)CC1)c1cccnc1Oc1ccccc1 10.1016/j.bmcl.2008.08.055
CHEMBL524153 193307 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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(C[C@H]2COc3ccccc3O2)CC1)c1cccnc1Oc1ccccc1 10.1016/j.bmcl.2008.08.055
44387798 166271 0 None - 0 Human 8.0 pKi = 8.0 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 166271 0 None - 0 Human 8.0 pKi = 8.0 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
71456239 78938 0 None - 0 Human 7.0 pKi = 7.0 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 78938 0 None - 0 Human 7.0 pKi = 7.0 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
136044137 78935 0 None - 0 Human 7.9 pKi = 7.9 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 78935 0 None - 0 Human 7.9 pKi = 7.9 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C adrenergic receptor
ChEMBL 472 6 1 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc5ccccc5c4)CC3)[C@@H]1CN2 10.1021/jm049619s
135499867 78939 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 78939 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
11224953 78932 0 None - 0 Human 8.6 pKi = 8.6 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 78932 0 None - 0 Human 8.6 pKi = 8.6 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
10758200 63415 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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 63415 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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 190951 4 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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 190951 4 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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
135519421 78933 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C adrenergic receptor
ChEMBL 456 6 1 7 3.3 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H]1CN2 10.1021/jm049619s
CHEMBL2112974 78933 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C adrenergic receptor
ChEMBL 456 6 1 7 3.3 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H]1CN2 10.1021/jm049619s
44579185 181812 1 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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 181812 1 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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
44324737 207236 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity for alpha-2C-adrenergic receptorBinding affinity for alpha-2C-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 207236 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity for alpha-2C-adrenergic receptorBinding affinity for alpha-2C-adrenergic receptor
ChEMBL 473 6 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc5ccccc5c4)CC3)[C@@H]1CO2 10.1021/jm049619s
135477797 78930 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 78930 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
44579230 181542 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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 181542 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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
71456240 78940 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 78940 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
44579228 181652 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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 181652 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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
71456238 78936 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 78936 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
11200476 78929 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 78929 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
44579229 189614 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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 189614 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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
135545454 78941 0 None - 0 Human 8.3 pKi = 8.3 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 78941 0 None - 0 Human 8.3 pKi = 8.3 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
44324765 111566 0 None - 0 Human 8.2 pKi = 8.2 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 111566 0 None - 0 Human 8.2 pKi = 8.2 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
71461647 78931 0 None - 0 Human 8.2 pKi = 8.2 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 78931 0 None - 0 Human 8.2 pKi = 8.2 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
44579271 187092 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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 187092 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic Alpha-2C 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
10073773 161121 16 None - 0 Human 6.2 pKi = 6.2 Functional
Inhibition of recombinant human adrenergic alpha 2C receptor expressed in CHO cells assessed as inhibition of 5-HT stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayInhibition of recombinant human adrenergic alpha 2C receptor expressed in CHO cells assessed as inhibition of 5-HT stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4082473 161121 16 None - 0 Human 6.2 pKi = 6.2 Functional
Inhibition of recombinant human adrenergic alpha 2C receptor expressed in CHO cells assessed as inhibition of 5-HT stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayInhibition of recombinant human adrenergic alpha 2C receptor expressed in CHO cells assessed as inhibition of 5-HT stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4117187 161121 16 None - 0 Human 6.2 pKi = 6.2 Functional
Inhibition of recombinant human adrenergic alpha 2C receptor expressed in CHO cells assessed as inhibition of 5-HT stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayInhibition of recombinant human adrenergic alpha 2C receptor expressed in CHO cells assessed as inhibition of 5-HT stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
DB06140 161121 16 None - 0 Human 6.2 pKi = 6.2 Functional
Inhibition of recombinant human adrenergic alpha 2C receptor expressed in CHO cells assessed as inhibition of 5-HT stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayInhibition of recombinant human adrenergic alpha 2C receptor expressed in CHO cells assessed as inhibition of 5-HT stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
44324765 111566 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity for Alpha-2C adrenergic receptorBinding affinity for Alpha-2C 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 111566 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity for Alpha-2C adrenergic receptorBinding affinity for Alpha-2C 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
136274357 78942 0 None - 0 Human 8.0 pKi = 8.0 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 78942 0 None - 0 Human 8.0 pKi = 8.0 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C adrenergic receptor
ChEMBL 412 4 1 5 3.8 c1ccc2c(c1)NC[C@@H]1C2=NO[C@H]1CN1CCN(Cc2ccc3ccccc3c2)CC1 10.1021/jm049619s
11385652 78934 0 None - 0 Human 8.0 pKi = 8.0 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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 78934 0 None - 0 Human 8.0 pKi = 8.0 Functional
Binding affinity for alpha-2C adrenergic receptorBinding affinity for alpha-2C 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
1343 1887 62 None -11 12 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
3519 1887 62 None -11 12 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
522 1887 62 None -11 12 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
CHEMBL862 1887 62 None -11 12 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
DB01018 1887 62 None -11 12 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
2683 3832 60 None -5 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 3832 60 None -5 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 3832 60 None -5 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 3832 60 None -5 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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 3832 60 None -5 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant alpha-2C 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-2C 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
2803 954 58 None -15 14 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 954 58 None -15 14 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 954 58 None -15 14 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 954 58 None -15 14 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 954 58 None -15 14 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
2435 721 100 None -7 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
395 721 100 None -7 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
520 721 100 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 721 100 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 721 100 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 721 100 None -7 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
124 2979 47 None -144 25 Human 6.9 pEC50 = 6.9 Functional
β-arrestin recruitment and internalizationβ-arrestin recruitment and internalization
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 25080296
2032 2979 47 None -144 25 Human 6.9 pEC50 = 6.9 Functional
β-arrestin recruitment and internalizationβ-arrestin recruitment and internalization
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 25080296
4636 2979 47 None -144 25 Human 6.9 pEC50 = 6.9 Functional
β-arrestin recruitment and internalizationβ-arrestin recruitment and internalization
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 25080296
CHEMBL762 2979 47 None -144 25 Human 6.9 pEC50 = 6.9 Functional
β-arrestin recruitment and internalizationβ-arrestin recruitment and internalization
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 25080296
DB00935 2979 47 None -144 25 Human 6.9 pEC50 = 6.9 Functional
β-arrestin recruitment and internalizationβ-arrestin recruitment and internalization
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 25080296
2803 954 58 None -15 14 Human 5.7 pEC50 = 5.7 Functional
4.64 =value for β-arrestin recruitment and internalization4.64 =value for β-arrestin recruitment and internalization
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 25080296
516 954 58 None -15 14 Human 5.7 pEC50 = 5.7 Functional
4.64 =value for β-arrestin recruitment and internalization4.64 =value for β-arrestin recruitment and internalization
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 25080296
704 954 58 None -15 14 Human 5.7 pEC50 = 5.7 Functional
4.64 =value for β-arrestin recruitment and internalization4.64 =value for β-arrestin recruitment and internalization
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 25080296
CHEMBL134 954 58 None -15 14 Human 5.7 pEC50 = 5.7 Functional
4.64 =value for β-arrestin recruitment and internalization4.64 =value for β-arrestin recruitment and internalization
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 25080296
DB00575 954 58 None -15 14 Human 5.7 pEC50 = 5.7 Functional
4.64 =value for β-arrestin recruitment and internalization4.64 =value for β-arrestin recruitment and internalization
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 25080296
12574 2603 88 None -26 8 Human 5.0 pEC50 = 5.0 Functional
4.73 =value for β-arrestin recruitment and internalization4.73 =value for β-arrestin recruitment and internalization
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 25080296
4810 2603 88 None -26 8 Human 5.0 pEC50 = 5.0 Functional
4.73 =value for β-arrestin recruitment and internalization4.73 =value for β-arrestin recruitment and internalization
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 25080296
CHEMBL19236 2603 88 None -26 8 Human 5.0 pEC50 = 5.0 Functional
4.73 =value for β-arrestin recruitment and internalization4.73 =value for β-arrestin recruitment and internalization
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 25080296
DB09242 2603 88 None -26 8 Human 5.0 pEC50 = 5.0 Functional
4.73 =value for β-arrestin recruitment and internalization4.73 =value for β-arrestin recruitment and internalization
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 25080296
3952 1886 38 None -18 21 Human 5.9 pEC50 = 5.9 Functional
5.14 =value for β-arrestin recruitment and internalization5.14 =value for β-arrestin recruitment and internalization
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 25080296
5353646 1886 38 None -18 21 Human 5.9 pEC50 = 5.9 Functional
5.14 =value for β-arrestin recruitment and internalization5.14 =value for β-arrestin recruitment and internalization
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 25080296
5443 1886 38 None -18 21 Human 5.9 pEC50 = 5.9 Functional
5.14 =value for β-arrestin recruitment and internalization5.14 =value for β-arrestin recruitment and internalization
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 25080296
5702063 1886 38 None -18 21 Human 5.9 pEC50 = 5.9 Functional
5.14 =value for β-arrestin recruitment and internalization5.14 =value for β-arrestin recruitment and internalization
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 25080296
CHEMBL1331786 1886 38 None -18 21 Human 5.9 pEC50 = 5.9 Functional
5.14 =value for β-arrestin recruitment and internalization5.14 =value for β-arrestin recruitment and internalization
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 25080296
CHEMBL420 1886 38 None -18 21 Human 5.9 pEC50 = 5.9 Functional
5.14 =value for β-arrestin recruitment and internalization5.14 =value for β-arrestin recruitment and internalization
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 25080296
DB00629 1886 38 None -18 21 Human 5.9 pEC50 = 5.9 Functional
5.14 =value for β-arrestin recruitment and internalization5.14 =value for β-arrestin recruitment and internalization
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 25080296
2435 721 100 None -7 10 Human 6.4 pEC50 = 6.4 Functional
5.88 = value for β-arrestin recruitment and internalization5.88 = value for β-arrestin recruitment and internalization
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
395 721 100 None -7 10 Human 6.4 pEC50 = 6.4 Functional
5.88 = value for β-arrestin recruitment and internalization5.88 = value for β-arrestin recruitment and internalization
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
520 721 100 None -7 10 Human 6.4 pEC50 = 6.4 Functional
5.88 = value for β-arrestin recruitment and internalization5.88 = value for β-arrestin recruitment and internalization
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
5386 721 100 None -7 10 Human 6.4 pEC50 = 6.4 Functional
5.88 = value for β-arrestin recruitment and internalization5.88 = value for β-arrestin recruitment and internalization
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
CHEMBL844 721 100 None -7 10 Human 6.4 pEC50 = 6.4 Functional
5.88 = value for β-arrestin recruitment and internalization5.88 = value for β-arrestin recruitment and internalization
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
DB00484 721 100 None -7 10 Human 6.4 pEC50 = 6.4 Functional
5.88 = value for β-arrestin recruitment and internalization5.88 = value for β-arrestin recruitment and internalization
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
1960 2855 67 None -11 19 Human 6.3 pEC50 = 6.3 Functional
6.02 = value for β-arrestin recruitment and internalization6.02 = value for β-arrestin recruitment and internalization
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 25080296
439260 2855 67 None -11 19 Human 6.3 pEC50 = 6.3 Functional
6.02 = value for β-arrestin recruitment and internalization6.02 = value for β-arrestin recruitment and internalization
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 25080296
505 2855 67 None -11 19 Human 6.3 pEC50 = 6.3 Functional
6.02 = value for β-arrestin recruitment and internalization6.02 = value for β-arrestin recruitment and internalization
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 25080296
CHEMBL1437 2855 67 None -11 19 Human 6.3 pEC50 = 6.3 Functional
6.02 = value for β-arrestin recruitment and internalization6.02 = value for β-arrestin recruitment and internalization
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 25080296
DB00368 2855 67 None -11 19 Human 6.3 pEC50 = 6.3 Functional
6.02 = value for β-arrestin recruitment and internalization6.02 = value for β-arrestin recruitment and internalization
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 25080296
12574 2603 88 None -26 8 Human 6.9 pEC50 = 6.9 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
4810 2603 88 None -26 8 Human 6.9 pEC50 = 6.9 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
CHEMBL19236 2603 88 None -26 8 Human 6.9 pEC50 = 6.9 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
DB09242 2603 88 None -26 8 Human 6.9 pEC50 = 6.9 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
523 4104 93 None -1 5 Human 7.1 pEC50 = 7.1 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
5707 4104 93 None -1 5 Human 7.1 pEC50 = 7.1 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
CHEMBL297362 4104 93 None -1 5 Human 7.1 pEC50 = 7.1 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
DB11477 4104 93 None -1 5 Human 7.1 pEC50 = 7.1 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
1028 291 71 None -44 19 Human 7.6 pEC50 = 7.6 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
139148732 291 71 None -44 19 Human 7.6 pEC50 = 7.6 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
479 291 71 None -44 19 Human 7.6 pEC50 = 7.6 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
5816 291 71 None -44 19 Human 7.6 pEC50 = 7.6 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
CHEMBL679 291 71 None -44 19 Human 7.6 pEC50 = 7.6 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
DB00668 291 71 None -44 19 Human 7.6 pEC50 = 7.6 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
11079 2731 63 None -13 7 Human 7.7 pEC50 = 7.7 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
3369 2731 63 None -13 7 Human 7.7 pEC50 = 7.7 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
4436 2731 63 None -13 7 Human 7.7 pEC50 = 7.7 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
5509 2731 63 None -13 7 Human 7.7 pEC50 = 7.7 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
CHEMBL761 2731 63 None -13 7 Human 7.7 pEC50 = 7.7 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
DB06711 2731 63 None -13 7 Human 7.7 pEC50 = 7.7 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
1960 2855 67 None -11 19 Human 7.7 pEC50 = 7.7 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
439260 2855 67 None -11 19 Human 7.7 pEC50 = 7.7 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
505 2855 67 None -11 19 Human 7.7 pEC50 = 7.7 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
CHEMBL1437 2855 67 None -11 19 Human 7.7 pEC50 = 7.7 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
DB00368 2855 67 None -11 19 Human 7.7 pEC50 = 7.7 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
2803 954 58 None -15 14 Human 7.8 pEC50 = 7.8 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
516 954 58 None -15 14 Human 7.8 pEC50 = 7.8 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
704 954 58 None -15 14 Human 7.8 pEC50 = 7.8 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
CHEMBL134 954 58 None -15 14 Human 7.8 pEC50 = 7.8 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
DB00575 954 58 None -15 14 Human 7.8 pEC50 = 7.8 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
1343 1887 62 None -11 12 Human 8.0 pEC50 = 8 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
3519 1887 62 None -11 12 Human 8.0 pEC50 = 8 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
522 1887 62 None -11 12 Human 8.0 pEC50 = 8 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
CHEMBL862 1887 62 None -11 12 Human 8.0 pEC50 = 8 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
DB01018 1887 62 None -11 12 Human 8.0 pEC50 = 8 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
2435 721 100 None -7 10 Human 8.2 pEC50 = 8.2 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
395 721 100 None -7 10 Human 8.2 pEC50 = 8.2 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
520 721 100 None -7 10 Human 8.2 pEC50 = 8.2 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
5386 721 100 None -7 10 Human 8.2 pEC50 = 8.2 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
CHEMBL844 721 100 None -7 10 Human 8.2 pEC50 = 8.2 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
DB00484 721 100 None -7 10 Human 8.2 pEC50 = 8.2 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
3952 1886 38 None -18 21 Human 8.4 pEC50 = 8.4 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5353646 1886 38 None -18 21 Human 8.4 pEC50 = 8.4 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5443 1886 38 None -18 21 Human 8.4 pEC50 = 8.4 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5702063 1886 38 None -18 21 Human 8.4 pEC50 = 8.4 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
CHEMBL1331786 1886 38 None -18 21 Human 8.4 pEC50 = 8.4 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
CHEMBL420 1886 38 None -18 21 Human 8.4 pEC50 = 8.4 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
DB00629 1886 38 None -18 21 Human 8.4 pEC50 = 8.4 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
521 1403 69 None -4 5 Human 9.6 pEC50 = 9.6 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
5311068 1403 69 None -4 5 Human 9.6 pEC50 = 9.6 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
835 1403 69 None -4 5 Human 9.6 pEC50 = 9.6 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
CHEMBL778 1403 69 None -4 5 Human 9.6 pEC50 = 9.6 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
DB00633 1403 69 None -4 5 Human 9.6 pEC50 = 9.6 Functional
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
30699 217702 0 None -1 14 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 423 7 2 8 0.5 CC(=O)OCC1=C(N2[C@H](SC1)[C@H](NC(=O)CSC1=CC=NC=C1)C2=O)C(O)=O None
2337 3254 77 None -8 29 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3254 77 None -8 29 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3254 77 None -8 29 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3254 77 None -8 29 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3254 77 None -8 29 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1225 1470 26 None -3 11 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1470 26 None -3 11 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667468 1470 26 None -3 11 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1470 26 None -3 11 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL101740 1470 26 None -3 11 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1470 26 None -3 11 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1470 26 None -3 11 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
1816 2538 102 None -43 12 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10636247
4205 2538 102 None -43 12 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10636247
7241 2538 102 None -43 12 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10636247
CHEMBL654 2538 102 None -43 12 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10636247
DB00370 2538 102 None -43 12 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10636247
102 4125 48 None -2 20 Human 7.4 pIC50 = 7.4 Functional
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 25080296
3659 4125 48 None -2 20 Human 7.4 pIC50 = 7.4 Functional
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 25080296
8969 4125 48 None -2 20 Human 7.4 pIC50 = 7.4 Functional
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 25080296
CHEMBL15245 4125 48 None -2 20 Human 7.4 pIC50 = 7.4 Functional
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 25080296
DB01392 4125 48 None -2 20 Human 7.4 pIC50 = 7.4 Functional
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 25080296
12577 2561 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 25080296
189711 2561 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 25080296
CHEMBL1257057 2561 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 25080296
12574 2603 88 None -26 8 Human 6.5 pIC50 = 6.5 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 25080296
12574 2603 88 None -26 8 Human 6.5 pIC50 = 6.5 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
4810 2603 88 None -26 8 Human 6.5 pIC50 = 6.5 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 25080296
4810 2603 88 None -26 8 Human 6.5 pIC50 = 6.5 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
CHEMBL19236 2603 88 None -26 8 Human 6.5 pIC50 = 6.5 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 25080296
CHEMBL19236 2603 88 None -26 8 Human 6.5 pIC50 = 6.5 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
DB09242 2603 88 None -26 8 Human 6.5 pIC50 = 6.5 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 25080296
DB09242 2603 88 None -26 8 Human 6.5 pIC50 = 6.5 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
1028 291 71 None -44 19 Human 6.7 pIC50 = 6.7 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
139148732 291 71 None -44 19 Human 6.7 pIC50 = 6.7 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
479 291 71 None -44 19 Human 6.7 pIC50 = 6.7 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
5816 291 71 None -44 19 Human 6.7 pIC50 = 6.7 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
CHEMBL679 291 71 None -44 19 Human 6.7 pIC50 = 6.7 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
DB00668 291 71 None -44 19 Human 6.7 pIC50 = 6.7 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
523 4104 93 None -1 5 Human 6.8 pIC50 = 6.8 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
5707 4104 93 None -1 5 Human 6.8 pIC50 = 6.8 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
CHEMBL297362 4104 93 None -1 5 Human 6.8 pIC50 = 6.8 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
DB11477 4104 93 None -1 5 Human 6.8 pIC50 = 6.8 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
3952 1886 38 None -18 21 Human 7.0 pIC50 = 7.0 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 25080296
3952 1886 38 None -18 21 Human 7.0 pIC50 = 7.0 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5353646 1886 38 None -18 21 Human 7.0 pIC50 = 7.0 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 25080296
5353646 1886 38 None -18 21 Human 7.0 pIC50 = 7.0 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5443 1886 38 None -18 21 Human 7.0 pIC50 = 7.0 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 25080296
5443 1886 38 None -18 21 Human 7.0 pIC50 = 7.0 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5702063 1886 38 None -18 21 Human 7.0 pIC50 = 7.0 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 25080296
5702063 1886 38 None -18 21 Human 7.0 pIC50 = 7.0 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
CHEMBL1331786 1886 38 None -18 21 Human 7.0 pIC50 = 7.0 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 25080296
CHEMBL1331786 1886 38 None -18 21 Human 7.0 pIC50 = 7.0 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
CHEMBL420 1886 38 None -18 21 Human 7.0 pIC50 = 7.0 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 25080296
CHEMBL420 1886 38 None -18 21 Human 7.0 pIC50 = 7.0 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
DB00629 1886 38 None -18 21 Human 7.0 pIC50 = 7.0 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 25080296
DB00629 1886 38 None -18 21 Human 7.0 pIC50 = 7.0 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
11079 2731 63 None -13 7 Human 7.1 pIC50 = 7.1 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
3369 2731 63 None -13 7 Human 7.1 pIC50 = 7.1 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
4436 2731 63 None -13 7 Human 7.1 pIC50 = 7.1 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
5509 2731 63 None -13 7 Human 7.1 pIC50 = 7.1 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
CHEMBL761 2731 63 None -13 7 Human 7.1 pIC50 = 7.1 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
DB06711 2731 63 None -13 7 Human 7.1 pIC50 = 7.1 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
1343 1887 62 None -11 12 Human 7.2 pIC50 = 7.2 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
3519 1887 62 None -11 12 Human 7.2 pIC50 = 7.2 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
522 1887 62 None -11 12 Human 7.2 pIC50 = 7.2 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
CHEMBL862 1887 62 None -11 12 Human 7.2 pIC50 = 7.2 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
DB01018 1887 62 None -11 12 Human 7.2 pIC50 = 7.2 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
3658 4105 53 None -12 18 Human 7.2 pIC50 = 7.2 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
517 4105 53 None -12 18 Human 7.2 pIC50 = 7.2 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
5709 4105 53 None -12 18 Human 7.2 pIC50 = 7.2 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
CHEMBL312448 4105 53 None -12 18 Human 7.2 pIC50 = 7.2 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
DB06694 4105 53 None -12 18 Human 7.2 pIC50 = 7.2 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
1960 2855 67 None -11 19 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 25080296
1960 2855 67 None -11 19 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
439260 2855 67 None -11 19 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 25080296
439260 2855 67 None -11 19 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
505 2855 67 None -11 19 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 25080296
505 2855 67 None -11 19 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
CHEMBL1437 2855 67 None -11 19 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 25080296
CHEMBL1437 2855 67 None -11 19 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
DB00368 2855 67 None -11 19 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 25080296
DB00368 2855 67 None -11 19 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
2803 954 58 None -15 14 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 25080296
2803 954 58 None -15 14 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
516 954 58 None -15 14 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 25080296
516 954 58 None -15 14 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
704 954 58 None -15 14 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 25080296
704 954 58 None -15 14 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
CHEMBL134 954 58 None -15 14 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 25080296
CHEMBL134 954 58 None -15 14 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
DB00575 954 58 None -15 14 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 25080296
DB00575 954 58 None -15 14 Human 7.6 pIC50 = 7.6 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
124 2979 47 None -144 25 Human 7.8 pIC50 = 7.8 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 25080296
124 2979 47 None -144 25 Human 7.8 pIC50 = 7.8 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
2032 2979 47 None -144 25 Human 7.8 pIC50 = 7.8 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 25080296
2032 2979 47 None -144 25 Human 7.8 pIC50 = 7.8 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
4636 2979 47 None -144 25 Human 7.8 pIC50 = 7.8 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 25080296
4636 2979 47 None -144 25 Human 7.8 pIC50 = 7.8 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
CHEMBL762 2979 47 None -144 25 Human 7.8 pIC50 = 7.8 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 25080296
CHEMBL762 2979 47 None -144 25 Human 7.8 pIC50 = 7.8 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
DB00935 2979 47 None -144 25 Human 7.8 pIC50 = 7.8 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 25080296
DB00935 2979 47 None -144 25 Human 7.8 pIC50 = 7.8 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
2435 721 100 None -7 10 Human 8.3 pIC50 = 8.3 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
2435 721 100 None -7 10 Human 8.3 pIC50 = 8.3 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
395 721 100 None -7 10 Human 8.3 pIC50 = 8.3 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
395 721 100 None -7 10 Human 8.3 pIC50 = 8.3 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
520 721 100 None -7 10 Human 8.3 pIC50 = 8.3 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
520 721 100 None -7 10 Human 8.3 pIC50 = 8.3 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
5386 721 100 None -7 10 Human 8.3 pIC50 = 8.3 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
5386 721 100 None -7 10 Human 8.3 pIC50 = 8.3 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
CHEMBL844 721 100 None -7 10 Human 8.3 pIC50 = 8.3 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
CHEMBL844 721 100 None -7 10 Human 8.3 pIC50 = 8.3 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
DB00484 721 100 None -7 10 Human 8.3 pIC50 = 8.3 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
DB00484 721 100 None -7 10 Human 8.3 pIC50 = 8.3 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
521 1403 69 None -4 5 Human 9.2 pIC50 = 9.2 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
5311068 1403 69 None -4 5 Human 9.2 pIC50 = 9.2 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
835 1403 69 None -4 5 Human 9.2 pIC50 = 9.2 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
CHEMBL778 1403 69 None -4 5 Human 9.2 pIC50 = 9.2 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
DB00633 1403 69 None -4 5 Human 9.2 pIC50 = 9.2 Functional
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
3930 2149 43 None - 1 Human 7.4 pKB = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 17220913
3930 2149 43 None - 1 Human 7.4 pKB = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 35224877
540335 2149 43 None - 1 Human 7.4 pKB = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 17220913
540335 2149 43 None - 1 Human 7.4 pKB = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 35224877
CHEMBL106525 2149 43 None - 1 Human 7.4 pKB = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 17220913
CHEMBL106525 2149 43 None - 1 Human 7.4 pKB = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 35224877
13130 2963 0 None - 1 Human 9.8 pKB = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 285 2 0 3 3.9 [H][C@@]12N(CCC[C@@]1(C)OCC)CCC3=C2OC4=C3C=CC=C4 23718812
171037438 2963 0 None - 1 Human 9.8 pKB = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 285 2 0 3 3.9 [H][C@@]12N(CCC[C@@]1(C)OCC)CCC3=C2OC4=C3C=CC=C4 23718812




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

57345628 71181 0 None -26 4 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 244 5 1 3 2.4 CC(Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL1956195 71181 0 None -26 4 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 244 5 1 3 2.4 CC(Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
70695474 77670 0 None -47 4 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 244 5 1 3 2.4 C[C@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL2089156 77670 0 None -47 4 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 244 5 1 3 2.4 C[C@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
57345626 71178 2 None -12 4 Human 8.0 pEC50 = 8 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 268 3 1 3 2.2 CC(Oc1ccccc1Br)C1=NCCN1 10.1021/ml400232p
CHEMBL1956192 71178 2 None -12 4 Human 8.0 pEC50 = 8 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 268 3 1 3 2.2 CC(Oc1ccccc1Br)C1=NCCN1 10.1021/ml400232p
72947315 92487 0 None -10 4 Human 6.0 pEC50 = 6 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 232 5 1 4 1.6 c1ccc(OC2CC2)c(OCC2=NCCN2)c1 10.1021/ml400232p
CHEMBL2431280 92487 0 None -10 4 Human 6.0 pEC50 = 6 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 232 5 1 4 1.6 c1ccc(OC2CC2)c(OCC2=NCCN2)c1 10.1021/ml400232p
134137108 142725 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysis
ChEMBL 217 5 2 3 2.1 CCCc1ccccc1NCC1=NCCN1 10.1021/acsmedchemlett.6b00290
CHEMBL3892351 142725 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysis
ChEMBL 217 5 2 3 2.1 CCCc1ccccc1NCC1=NCCN1 10.1021/acsmedchemlett.6b00290
49836304 18569 1 None -2 3 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 230 4 1 3 2.3 C[C@@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL1276219 18569 1 None -2 3 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 230 4 1 3 2.3 C[C@@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
44352155 116806 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysis
ChEMBL 251 4 2 3 2.8 c1ccc(-c2ccccc2NCC2=NCCN2)cc1 10.1021/acsmedchemlett.6b00290
CHEMBL337862 116806 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysis
ChEMBL 251 4 2 3 2.8 c1ccc(-c2ccccc2NCC2=NCCN2)cc1 10.1021/acsmedchemlett.6b00290
44269013 30340 1 None -10 4 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 218 5 1 3 2.0 CCCc1ccccc1OCC1=NCCN1 10.1021/ml400232p
CHEMBL13917 30340 1 None -10 4 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 218 5 1 3 2.0 CCCc1ccccc1OCC1=NCCN1 10.1021/ml400232p
134156190 151363 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysis
ChEMBL 215 5 2 3 1.8 C=CCc1ccccc1NCC1=NCCN1 10.1021/acsmedchemlett.6b00290
CHEMBL3961335 151363 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysis
ChEMBL 215 5 2 3 1.8 C=CCc1ccccc1NCC1=NCCN1 10.1021/acsmedchemlett.6b00290
49836302 18564 1 None -1 3 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@H](C)C1=NCCN1 10.1021/ml400232p
CHEMBL1276139 18564 1 None -1 3 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@H](C)C1=NCCN1 10.1021/ml400232p
129928082 144192 1 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysis
ChEMBL 189 3 2 3 1.4 Cc1ccccc1NCC1=NCCN1 10.1021/acsmedchemlett.6b00290
CHEMBL3904276 144192 1 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysis
ChEMBL 189 3 2 3 1.4 Cc1ccccc1NCC1=NCCN1 10.1021/acsmedchemlett.6b00290
13123534 189451 1 None - 1 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysis
ChEMBL 209 3 2 3 1.8 Clc1ccccc1NCC1=NCCN1 10.1021/acsmedchemlett.6b00290
CHEMBL51358 189451 1 None - 1 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysisAgonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysis
ChEMBL 209 3 2 3 1.8 Clc1ccccc1NCC1=NCCN1 10.1021/acsmedchemlett.6b00290
72947314 92488 0 None -8 4 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 230 5 1 3 2.0 c1ccc(OCC2=NCCN2)c(CC2CC2)c1 10.1021/ml400232p
CHEMBL2431281 92488 0 None -8 4 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 230 5 1 3 2.0 c1ccc(OCC2=NCCN2)c(CC2CC2)c1 10.1021/ml400232p
49836301 18565 1 None -1 4 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@@H](C)C1=NCCN1 10.1021/ml400232p
CHEMBL1276140 18565 1 None -1 4 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@@H](C)C1=NCCN1 10.1021/ml400232p
73291731 92489 0 None -10 4 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 232 5 1 3 2.4 CCCc1ccccc1OC(C)C1=NCCN1 10.1021/ml400232p
CHEMBL2431282 92489 0 None -10 4 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 232 5 1 3 2.4 CCCc1ccccc1OC(C)C1=NCCN1 10.1021/ml400232p
70693375 77669 0 None -5 4 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 244 5 1 3 2.4 C[C@@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL2089155 77669 0 None -5 4 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 244 5 1 3 2.4 C[C@@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
49836303 18570 1 None -10 4 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 230 4 1 3 2.3 C[C@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL1276220 18570 1 None -10 4 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 230 4 1 3 2.3 C[C@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
44549156 18568 0 None -10 4 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 230 4 1 3 2.3 CC(Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL1276218 18568 0 None -10 4 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 230 4 1 3 2.3 CC(Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
2765 942 19 None -15 9 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/ml400232p
515 942 19 None -15 9 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/ml400232p
CHEMBL13852 942 19 None -15 9 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/ml400232p
DB09202 942 19 None -15 9 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/ml400232p
57345629 71183 0 None -45 4 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 246 5 1 4 2.0 CC(Oc1ccccc1OC1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL1956197 71183 0 None -45 4 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 246 5 1 4 2.0 CC(Oc1ccccc1OC1CC1)C1=NCCN1 10.1021/ml400232p
24906198 187662 3 None -3 4 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/ml400232p
CHEMBL495095 187662 3 None -3 4 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/ml400232p
44269006 32351 1 None -1 4 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 216 5 1 3 1.8 C=CCc1ccccc1OCC1=NCCN1 10.1021/ml400232p
CHEMBL14107 32351 1 None -1 4 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 216 5 1 3 1.8 C=CCc1ccccc1OCC1=NCCN1 10.1021/ml400232p
28918670 92485 2 None -4 4 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 254 3 1 3 1.8 Brc1ccccc1OCC1=NCCN1 10.1021/ml400232p
CHEMBL2431279 92485 2 None -4 4 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 254 3 1 3 1.8 Brc1ccccc1OCC1=NCCN1 10.1021/ml400232p
44376984 56221 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 56221 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
44377200 57418 1 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 57418 1 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
22120332 56043 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 56043 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
44377036 120154 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 120154 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
44376954 55738 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 55738 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
44376923 56425 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 56425 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
44376958 57477 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 57477 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
22120322 55919 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 55919 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
44377035 120128 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 120128 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
44376993 56482 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 56482 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
44376900 56266 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 56266 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
3045401 56057 32 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 56057 32 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
10531 1419 21 None -9 24 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1419 21 None -9 24 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1419 21 None -9 24 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1419 21 None -9 24 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1419 21 None -9 24 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
3151 1461 97 None -40 27 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
945 1461 97 None -40 27 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
965 1461 97 None -40 27 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
CHEMBL219916 1461 97 None -40 27 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
DB01184 1461 97 None -40 27 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
3158 56265 27 None -1047 20 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 56265 27 None -1047 20 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
DB01142 56265 27 None -1047 20 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
16220269 189658 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of adrenergic Alpha-2C receptorInhibition of adrenergic Alpha-2C receptor
ChEMBL 361 3 1 2 4.4 CC[C@@H]1O[C@](/C=C/C2CC2)(C(F)(F)F)c2c(ccc(F)c2F)NC1=O 10.1073/pnas.0605125104
CHEMBL515170 189658 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of adrenergic Alpha-2C receptorInhibition of adrenergic Alpha-2C receptor
ChEMBL 361 3 1 2 4.4 CC[C@@H]1O[C@](/C=C/C2CC2)(C(F)(F)F)c2c(ccc(F)c2F)NC1=O 10.1073/pnas.0605125104
2142 3094 58 None -7 37 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
4920903 3094 58 None -7 37 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
502 3094 58 None -7 37 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
5775 3094 58 None -7 37 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
CHEMBL597 3094 58 None -7 37 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
DB00692 3094 58 None -7 37 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
25014630 83537 1 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of alpha2C adrenergic receptorInhibition of alpha2C adrenergic receptor
ChEMBL 326 3 3 4 3.3 N=C(Nc1ccc2c(c1)CCN2C1CCNCC1)c1cccs1 10.1016/j.ejmech.2012.07.006
CHEMBL2203713 83537 1 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of alpha2C adrenergic receptorInhibition of alpha2C adrenergic receptor
ChEMBL 326 3 3 4 3.3 N=C(Nc1ccc2c(c1)CCN2C1CCNCC1)c1cccs1 10.1016/j.ejmech.2012.07.006
3952 1886 38 None -19 12 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5353646 1886 38 None -19 12 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5443 1886 38 None -19 12 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5702063 1886 38 None -19 12 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL1331786 1886 38 None -19 12 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL420 1886 38 None -19 12 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
DB00629 1886 38 None -19 12 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
44318454 206007 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for human cloned Alpha-2C adrenergic receptorBinding affinity for human cloned Alpha-2C adrenergic receptor
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL84931 206007 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for human cloned Alpha-2C adrenergic receptorBinding affinity for human cloned Alpha-2C adrenergic receptor
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
5472 205816 75 None -1 3 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 nan
CHEMBL1717 205816 75 None -1 3 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 nan
CHEMBL833 205816 75 None -1 3 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 nan
DB00208 205816 75 None -1 3 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 nan
1043 1580 14 None -19 29 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1580 14 None -19 29 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
3251 1580 14 None -19 29 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1580 14 None -19 29 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
CHEMBL1982133 1580 14 None -19 29 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1580 14 None -19 29 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1580 14 None -19 29 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
277 1300 62 None -42 50 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1300 62 None -42 50 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1300 62 None -42 50 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1300 62 None -42 50 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1300 62 None -42 50 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL5070958 214247 3 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of alpha 2C adrenergic receptor (unknown origin)Inhibition of alpha 2C adrenergic receptor (unknown origin)
ChEMBL None None None NCCCCN(C[C@H]1Cc2ncccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acs.jmedchem.1c01564
9951544 57374 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 57374 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
123132228 156304 53 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of alpha2c adrenergic receptor (unknown origin)Inhibition of alpha2c 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 156304 53 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of alpha2c adrenergic receptor (unknown origin)Inhibition of alpha2c adrenergic receptor (unknown origin)
ChEMBL 369 5 1 8 2.4 CS(=O)(=O)c1ccc(-c2cnc(NCc3ccco3)n3cnnc23)cc1 10.1021/acs.jmedchem.1c02148
10331436 324 10 None - 6 Human 4.9 pIC50 = 4.9 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
160 324 10 None - 6 Human 4.9 pIC50 = 4.9 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 324 10 None - 6 Human 4.9 pIC50 = 4.9 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
2105 3052 37 None -81 33 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 3052 37 None -81 33 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 3052 37 None -81 33 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 3052 37 None -81 33 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 3052 37 None -81 33 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
2398 953 62 None -4 29 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 953 62 None -4 29 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 953 62 None -4 29 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 953 62 None -4 29 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 953 62 None -4 29 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
15730 71116 80 None 1 10 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1 nan
CHEMBL195437 71116 80 None 1 10 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1 nan
1548953 207677 27 None 1 17 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 207677 27 None 1 17 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
2683 102886 25 None -30 16 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 102886 25 None -30 16 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 102886 25 None -30 16 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
448537 160248 89 None -21 25 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 160248 89 None -21 25 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
1212 1660 50 None -54 66 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1660 50 None -54 66 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1660 50 None -54 66 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1660 50 None -54 66 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1660 50 None -54 66 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
138753276 177175 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of adrenergic receptor alpha2c (unknown origin)Inhibition of adrenergic receptor alpha2c (unknown origin)
ChEMBL 302 4 2 3 2.8 CO[C@H]1CCN(Cc2c(C)cc(C)c3[nH]ccc23)[C@H](CO)C1 10.1021/acs.jmedchem.9b01870
CHEMBL4634827 177175 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of adrenergic receptor alpha2c (unknown origin)Inhibition of adrenergic receptor alpha2c (unknown origin)
ChEMBL 302 4 2 3 2.8 CO[C@H]1CCN(Cc2c(C)cc(C)c3[nH]ccc23)[C@H](CO)C1 10.1021/acs.jmedchem.9b01870
196129 67796 17 None -295 15 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 67796 17 None -295 15 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
8447 188947 84 None -3 13 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 188947 84 None -3 13 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
73453 29614 24 None -3 17 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 29614 24 None -3 17 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
100 3803 58 None -27 55 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3803 58 None -27 55 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3803 58 None -27 55 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3803 58 None -27 55 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3803 58 None -27 55 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
3168 9260 92 None -63 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 9260 92 None -63 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
DB00450 9260 92 None -63 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
135 2530 43 None -6 58 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2530 43 None -6 58 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2530 43 None -6 58 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2530 43 None -6 58 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2530 43 None -6 58 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
138753277 177293 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of adrenergic receptor alpha2c (unknown origin)Inhibition of adrenergic receptor alpha2c (unknown origin)
ChEMBL 303 1 2 3 3.3 Cc1cc(Br)c(NC2=NCCN2)c2ccccc12 10.1021/acs.jmedchem.9b01870
CHEMBL4636550 177293 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of adrenergic receptor alpha2c (unknown origin)Inhibition of adrenergic receptor alpha2c (unknown origin)
ChEMBL 303 1 2 3 3.3 Cc1cc(Br)c(NC2=NCCN2)c2ccccc12 10.1021/acs.jmedchem.9b01870
2162 41512 100 None -1 6 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl nan
CHEMBL1491 41512 100 None -1 6 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl nan
10219 188794 37 None -2 5 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 188794 37 None -2 5 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 188794 37 None -2 5 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
1353 1909 93 None -87 86 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1909 93 None -87 86 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1909 93 None -87 86 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1909 93 None -87 86 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1909 93 None -87 86 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
9904205 205848 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity for human cloned Alpha-2C adrenergic receptorBinding affinity for human cloned Alpha-2C adrenergic receptor
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL83658 205848 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity for human cloned Alpha-2C adrenergic receptorBinding affinity for human cloned Alpha-2C adrenergic receptor
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
11057 176147 23 None -1 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 176147 23 None -1 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 176147 23 None -1 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 176147 23 None -1 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
133 2494 52 None -26 43 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2494 52 None -26 43 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2494 52 None -26 43 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2494 52 None -26 43 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2494 52 None -26 43 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
213 3851 55 None -6 44 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2717 3851 55 None -6 44 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533 3851 55 None -6 44 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
CHEMBL621 3851 55 None -6 44 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
DB00656 3851 55 None -6 44 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2247 505 81 None -25 42 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 505 81 None -25 42 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 505 81 None -25 42 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 505 81 None -25 42 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 505 81 None -25 42 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2335 11846 22 None -2 12 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
8478 11846 22 None -2 12 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL1182210 11846 22 None -2 12 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL221753 11846 22 None -2 12 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
1816 2538 102 None -38 18 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 2538 102 None -38 18 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 2538 102 None -38 18 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 2538 102 None -38 18 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 2538 102 None -38 18 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
44377007 57146 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 57146 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
44376975 55984 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 55984 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
CHEMBL5082142 214785 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of alpha 2C adrenergic receptor (unknown origin)Inhibition of alpha 2C adrenergic receptor (unknown origin)
ChEMBL None None None c1cnc2c(c1)CN[C@@H](CN(CCCCN1CCOCC1)[C@H]1CCCc3cccnc31)C2 10.1021/acs.jmedchem.1c01564
1971 2864 38 None -3 30 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 2864 38 None -3 30 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 2864 38 None -3 30 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 2864 38 None -3 30 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 2864 38 None -3 30 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
45482789 198923 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of adrenergic Alpha-2C receptorInhibition of adrenergic Alpha-2C 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 198923 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of adrenergic Alpha-2C receptorInhibition of adrenergic Alpha-2C 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
CHEMBL5081505 214747 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of alpha 2C adrenergic receptor (unknown origin)Inhibition of alpha 2C adrenergic receptor (unknown origin)
ChEMBL None None None c1cnc2c(c1)CN[C@@H](CN(CCCC1CCNCC1)[C@H]1CCCc3cccnc31)C2 10.1021/acs.jmedchem.1c01564
12488 1655 56 None -2 23 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1655 56 None -2 23 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1655 56 None -2 23 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1655 56 None -2 23 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
57345320 3830 9 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of alpha 2C adrenergic receptor (unknown origin)Inhibition of alpha 2C 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 3830 9 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of alpha 2C adrenergic receptor (unknown origin)Inhibition of alpha 2C 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 3830 9 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of alpha 2C adrenergic receptor (unknown origin)Inhibition of alpha 2C 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
28417 40037 49 None -1 12 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 40037 49 None -1 12 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
DB01406 40037 49 None -1 12 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
2286 3181 51 None -15 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3181 51 None -15 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3181 51 None -15 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3181 51 None -15 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3181 51 None -15 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
1028 291 71 None -67 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
139148732 291 71 None -67 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
479 291 71 None -67 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
5816 291 71 None -67 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
CHEMBL679 291 71 None -67 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
DB00668 291 71 None -67 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
222757 99374 73 None 1 3 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O nan
CHEMBL282575 99374 73 None 1 3 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O nan
2284 3180 33 None -7 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3180 33 None -7 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3180 33 None -7 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3180 33 None -7 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3180 33 None -7 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
124 2979 47 None -60 32 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2979 47 None -60 32 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2979 47 None -60 32 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2979 47 None -60 32 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2979 47 None -60 32 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
102 4125 48 None -2 50 Human 7.6 pIC50 = 7.6 Binding
Displacement of radioligand from human adrenergic Alpha-2C receptor after 60 minsDisplacement of radioligand from human adrenergic Alpha-2C receptor 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 4125 48 None -2 50 Human 7.6 pIC50 = 7.6 Binding
Displacement of radioligand from human adrenergic Alpha-2C receptor after 60 minsDisplacement of radioligand from human adrenergic Alpha-2C receptor 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 4125 48 None -2 50 Human 7.6 pIC50 = 7.6 Binding
Displacement of radioligand from human adrenergic Alpha-2C receptor after 60 minsDisplacement of radioligand from human adrenergic Alpha-2C receptor 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 4125 48 None -2 50 Human 7.6 pIC50 = 7.6 Binding
Displacement of radioligand from human adrenergic Alpha-2C receptor after 60 minsDisplacement of radioligand from human adrenergic Alpha-2C receptor 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 4125 48 None -2 50 Human 7.6 pIC50 = 7.6 Binding
Displacement of radioligand from human adrenergic Alpha-2C receptor after 60 minsDisplacement of radioligand from human adrenergic Alpha-2C receptor 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 57461 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 57461 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
3191 102856 97 None -3 25 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102856 97 None -3 25 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
DB11742 102856 97 None -3 25 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
2353 101110 82 None -1 5 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL12089 101110 82 None -1 5 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL295124 101110 82 None -1 5 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
44376927 55635 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 55635 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
CHEMBL5076569 214447 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of alpha 2C adrenergic receptor (unknown origin)Inhibition of alpha 2C adrenergic receptor (unknown origin)
ChEMBL None None None NCCCCN(C[C@H]1Cc2cccnc2CN1)[C@H]1CCCc2cccnc21 10.1021/acs.jmedchem.1c01564
4011 82406 49 None -28 24 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 82406 49 None -28 24 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
6918276 15609 7 None -47 8 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 15609 7 None -47 8 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
60838 183872 99 None -1 2 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC nan
CHEMBL481 183872 99 None -1 2 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC nan
191 403 98 None -39 29 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 403 98 None -39 29 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 403 98 None -39 29 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 403 98 None -39 29 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 403 98 None -39 29 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
657255 199082 34 None -8 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 199082 34 None -8 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
102 4125 48 None -2 50 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 4125 48 None -2 50 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 4125 48 None -2 50 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 4125 48 None -2 50 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 4125 48 None -2 50 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
2726 918 68 None -31 73 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 918 68 None -31 73 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 918 68 None -31 73 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 918 68 None -31 73 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 918 68 None -31 73 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
2600 3777 74 None -4 13 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 3777 74 None -4 13 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 3777 74 None -4 13 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 3777 74 None -4 13 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 3777 74 None -4 13 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
134551 358 27 None -5 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
271 358 27 None -5 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
885 358 27 None -5 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 358 27 None -5 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
237 204863 48 None -1 13 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL546257 204863 48 None -1 13 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL554190 204863 48 None -1 13 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL7568 204863 48 None -1 13 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
121432827 192244 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of alpha2c adrenergic receptor (unknown origin)Inhibition of alpha2c adrenergic receptor (unknown origin)
ChEMBL 344 4 1 7 2.7 c1cncc(-c2cnc(NCc3cccc4c3CCO4)n3cnnc23)c1 10.1021/acs.jmedchem.1c02148
CHEMBL5205327 192244 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of alpha2c adrenergic receptor (unknown origin)Inhibition of alpha2c adrenergic receptor (unknown origin)
ChEMBL 344 4 1 7 2.7 c1cncc(-c2cnc(NCc3cccc4c3CCO4)n3cnnc23)c1 10.1021/acs.jmedchem.1c02148
CHEMBL1200633 208598 3 None -1 8 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
1201549 596 24 None -18 20 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 596 24 None -18 20 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 596 24 None -18 20 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 596 24 None -18 20 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 596 24 None -18 20 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 596 24 None -18 20 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
1588 2323 27 None -3 44 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2323 27 None -3 44 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2323 27 None -3 44 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2323 27 None -3 44 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2323 27 None -3 44 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
3561 19075 39 None -2 11 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
CHEMBL1289 19075 39 None -2 11 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
5353853 17984 47 None -11 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 17984 47 None -11 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 17984 47 None -11 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
441383 20331 57 None 2 17 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 20331 57 None 2 17 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
135 2530 43 None -6 58 Human 7.4 pIC50 = 7.4 Binding
Binding affinity for human cloned Alpha-2C adrenergic receptorBinding affinity for human cloned Alpha-2C adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
1796 2530 43 None -6 58 Human 7.4 pIC50 = 7.4 Binding
Binding affinity for human cloned Alpha-2C adrenergic receptorBinding affinity for human cloned Alpha-2C adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
4184 2530 43 None -6 58 Human 7.4 pIC50 = 7.4 Binding
Binding affinity for human cloned Alpha-2C adrenergic receptorBinding affinity for human cloned Alpha-2C adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
CHEMBL6437 2530 43 None -6 58 Human 7.4 pIC50 = 7.4 Binding
Binding affinity for human cloned Alpha-2C adrenergic receptorBinding affinity for human cloned Alpha-2C adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
DB06148 2530 43 None -6 58 Human 7.4 pIC50 = 7.4 Binding
Binding affinity for human cloned Alpha-2C adrenergic receptorBinding affinity for human cloned Alpha-2C adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
2337 3254 77 None -10 63 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 3254 77 None -10 63 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 3254 77 None -10 63 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 3254 77 None -10 63 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 3254 77 None -10 63 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
2406 100402 89 None -11 12 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O nan
CHEMBL290106 100402 89 None -11 12 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O nan
68617 205525 62 None -9 26 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL1709 205525 62 None -9 26 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL809 205525 62 None -9 26 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
6761 67797 19 None -3 18 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67797 19 None -3 18 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
5318 15574 49 None -1 13 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1200348 15574 49 None -1 13 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1221 15574 49 None -1 13 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL508338 188964 0 None -25 6 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL None None None None nan
31101 728 40 None -36 36 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
35 728 40 None -36 36 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
403 728 40 None -36 36 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 728 40 None -36 36 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 728 40 None -36 36 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
1836 2590 59 None -31 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2590 59 None -31 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2590 59 None -31 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2590 59 None -31 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2590 59 None -31 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
12575 1986 30 None -8 17 Human 7.3 pIC50 = 7.3 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 1986 30 None -8 17 Human 7.3 pIC50 = 7.3 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 1986 30 None -8 17 Human 7.3 pIC50 = 7.3 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
DB12551 1986 30 None -8 17 Human 7.3 pIC50 = 7.3 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
135398745 2912 112 None -30 66 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2912 112 None -30 66 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2912 112 None -30 66 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2912 112 None -30 66 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
11080 29083 79 None -3 6 Human 4.3 pIC50 = 4.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 29083 79 None -3 6 Human 4.3 pIC50 = 4.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
44376845 55543 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 55543 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
180 401 56 None -16 40 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 401 56 None -16 40 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 401 56 None -16 40 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 401 56 None -16 40 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 401 56 None -16 40 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
44376936 57472 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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 57472 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2C 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
3584 3775 64 None -50 14 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
5401 3775 64 None -50 14 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
7302 3775 64 None -50 14 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
CHEMBL611 3775 64 None -50 14 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
DB01162 3775 64 None -50 14 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
1343 1887 62 None -251 9 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
3519 1887 62 None -251 9 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
522 1887 62 None -251 9 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
CHEMBL862 1887 62 None -251 9 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
DB01018 1887 62 None -251 9 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
4209 3161 75 None -77 33 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
4893 3161 75 None -77 33 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
503 3161 75 None -77 33 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
5385 3161 75 None -77 33 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
CHEMBL2 3161 75 None -77 33 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
DB00457 3161 75 None -77 33 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
1547484 939 74 None -4 20 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 939 74 None -4 20 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 939 74 None -4 20 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 939 74 None -4 20 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 939 74 None -4 20 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
3598 187819 76 None -1 7 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
CHEMBL496 187819 76 None -1 7 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
135398737 957 93 None -3 91 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 957 93 None -3 91 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 957 93 None -3 91 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 957 93 None -3 91 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 957 93 None -3 91 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
42574 15285 90 None -18 3 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 662 4 2 3 7.1 Cc1cc(C(C#N)c2ccc(Cl)cc2)c(Cl)cc1NC(=O)c1cc(I)cc(I)c1O nan
CHEMBL12131 15285 90 None -18 3 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 662 4 2 3 7.1 Cc1cc(C(C#N)c2ccc(Cl)cc2)c(Cl)cc1NC(=O)c1cc(I)cc(I)c1O nan
2351 3284 64 None -4 21 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 3284 64 None -4 21 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 3284 64 None -4 21 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 3284 64 None -4 21 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 3284 64 None -4 21 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
42636941 178947 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]RX821002 form human recombinant Alpha-2C adrenergic receptorDisplacement of [3H]RX821002 form human recombinant Alpha-2C adrenergic receptor
ChEMBL 343 5 0 5 4.4 CCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL470432 178947 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]RX821002 form human recombinant Alpha-2C adrenergic receptorDisplacement of [3H]RX821002 form human recombinant Alpha-2C adrenergic receptor
ChEMBL 343 5 0 5 4.4 CCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
240 943 43 None -5 25 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
2769 943 43 None -5 25 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
44279790 943 43 None -5 25 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
660 943 43 None -5 25 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL1729 943 43 None -5 25 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL560739 943 43 None -5 25 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
DB00604 943 43 None -5 25 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
104903 56342 17 None -1 6 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
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 nan
CHEMBL1630578 56342 17 None -1 6 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
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 nan
107715 200943 22 None -7 20 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 200943 22 None -7 20 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 200943 22 None -7 20 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
2274 3171 58 None -4 32 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3171 58 None -4 32 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3171 58 None -4 32 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3171 58 None -4 32 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3171 58 None -4 32 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL5077132 214482 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of alpha 2C adrenergic receptor (unknown origin)Inhibition of alpha 2C adrenergic receptor (unknown origin)
ChEMBL None None None CN(CCCCN(C[C@H]1Cc2ncccc2CN1)[C@H]1CCCc2cccnc21)C1CCOCC1 10.1021/acs.jmedchem.1c01564
10381889 107067 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for human cloned Alpha-2C adrenergic receptorBinding affinity for human cloned Alpha-2C adrenergic receptor
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL315772 107067 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for human cloned Alpha-2C adrenergic receptorBinding affinity for human cloned Alpha-2C adrenergic receptor
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(01)00721-1
132256889 190445 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of alpha2c adrenergic receptor (unknown origin)Inhibition of alpha2c adrenergic receptor (unknown origin)
ChEMBL 378 5 1 7 3.6 COc1cccc(F)c1CNc1ccc(-c2cnc(C)nc2C)c2nncn12 10.1021/acs.jmedchem.1c02148
CHEMBL5178464 190445 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of alpha2c adrenergic receptor (unknown origin)Inhibition of alpha2c adrenergic receptor (unknown origin)
ChEMBL 378 5 1 7 3.6 COc1cccc(F)c1CNc1ccc(-c2cnc(C)nc2C)c2nncn12 10.1021/acs.jmedchem.1c02148
CHEMBL5083458 214861 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of alpha 2C adrenergic receptor (unknown origin)Inhibition of alpha 2C adrenergic receptor (unknown origin)
ChEMBL None None None c1cnc2c(c1)CN[C@@H](CN(CCCCNC1COC1)[C@H]1CCCc3cccnc31)C2 10.1021/acs.jmedchem.1c01564
2389 3329 118 None -10 67 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3329 118 None -10 67 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3329 118 None -10 67 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3329 118 None -10 67 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3329 118 None -10 67 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
2585 802 103 None -16 22 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 802 103 None -16 22 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 802 103 None -16 22 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 802 103 None -16 22 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 802 103 None -16 22 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
26987 948 33 None -107 21 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 948 33 None -107 21 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 948 33 None -107 21 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 948 33 None -107 21 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 948 33 None -107 21 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
136019934 144528 0 None 7 3 Human 10.0 pKi = 10 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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 144528 0 None 7 3 Human 10.0 pKi = 10 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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
44324800 206946 0 None 5 7 Human 10.0 pKi = 10 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 206946 0 None 5 7 Human 10.0 pKi = 10 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 206946 0 None 5 7 Human 10.0 pKi = 10 Binding
Inhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptorInhibition of [3H]- rauwolscine binding to alpha-2C 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 206946 0 None 5 7 Human 10.0 pKi = 10 Binding
Inhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptorInhibition of [3H]- rauwolscine binding to alpha-2C 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
49781228 17203 1 None -3 4 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17203 1 None -3 4 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
52944548 17150 0 None -1 4 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17150 0 None -1 4 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
49781228 17203 1 None -3 4 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17203 1 None -3 4 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
44330168 4317 0 None 1 2 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 4317 0 None 1 2 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
44330668 4434 0 None 5 2 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 4434 0 None 5 2 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 96618 0 None 5 2 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 96618 0 None 5 2 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
11225779 107730 0 None 1 2 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 107730 0 None 1 2 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 163370 0 None 2 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 163370 0 None 2 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
44324800 206946 0 None 5 7 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 206946 0 None 5 7 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
44330653 208230 0 None 8 2 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 208230 0 None 8 2 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
44324972 163370 0 None 2 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 163370 0 None 2 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
44325050 207279 0 None 3 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 207279 0 None 3 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
44324972 163370 0 None 2 4 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptorInhibition of [3H]- rauwolscine binding to alpha-2C 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 163370 0 None 2 4 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptorInhibition of [3H]- rauwolscine binding to alpha-2C 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
49781228 17203 1 None -3 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17203 1 None -3 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
16655023 107439 2 None 5 7 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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 107439 2 None 5 7 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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
52941512 17196 0 None -1 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17196 0 None -1 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
44330369 111580 0 None 4 2 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 111580 0 None 4 2 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
10480357 208216 0 None 9 2 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 208216 0 None 9 2 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
44330114 108080 0 None 1 2 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 108080 0 None 1 2 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
44330635 208424 0 None 2 2 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 208424 0 None 2 2 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
52948958 17151 0 None -1 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17151 0 None -1 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
44579228 181652 0 None 13 3 Human 9.3 pKi = 9.3 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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 181652 0 None 13 3 Human 9.3 pKi = 9.3 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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
102 4125 48 None -2 50 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO cellsDisplacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO 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.ejmech.2014.12.045
3659 4125 48 None -2 50 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO cellsDisplacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO 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.ejmech.2014.12.045
8969 4125 48 None -2 50 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO cellsDisplacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO 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.ejmech.2014.12.045
CHEMBL15245 4125 48 None -2 50 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO cellsDisplacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO 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.ejmech.2014.12.045
DB01392 4125 48 None -2 50 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO cellsDisplacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO 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.ejmech.2014.12.045
102 4125 48 None -2 50 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO 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/jm401895u
3659 4125 48 None -2 50 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO 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/jm401895u
8969 4125 48 None -2 50 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO 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/jm401895u
CHEMBL15245 4125 48 None -2 50 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO 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/jm401895u
DB01392 4125 48 None -2 50 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO 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/jm401895u
44330645 208432 0 None 3 2 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 208432 0 None 3 2 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
44324765 111566 0 None 2 5 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 111566 0 None 2 5 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
44324765 111566 0 None 2 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptorInhibition of [3H]- rauwolscine binding to alpha-2C 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 111566 0 None 2 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptorInhibition of [3H]- rauwolscine binding to alpha-2C 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
49781222 17249 0 None -2 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17249 0 None -2 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
44579230 181542 0 None 8 3 Human 9.2 pKi = 9.2 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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 181542 0 None 8 3 Human 9.2 pKi = 9.2 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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
44330368 112190 0 None 3 2 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 112190 0 None 3 2 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
44325049 111521 0 None 2 3 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 111521 0 None 2 3 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
1588 2323 27 None -3 44 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2323 27 None -3 44 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2323 27 None -3 44 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2323 27 None -3 44 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2323 27 None -3 44 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
11203101 71681 0 None 44 3 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
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 71681 0 None 44 3 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
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
16655023 107439 2 None 5 7 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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 107439 2 None 5 7 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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 107439 2 None 5 7 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 107439 2 None 5 7 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
44330427 163373 0 None 4 2 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 163373 0 None 4 2 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
44330598 207636 0 None 8 2 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 207636 0 None 8 2 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
108094 3421 27 None -2 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 10.1021/jm800250z
526 3421 27 None -2 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 10.1021/jm800250z
528 3421 27 None -2 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 10.1021/jm800250z
CHEMBL10332 3421 27 None -2 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 10.1021/jm800250z
499 4075 18 None -3 15 Human 9.1 pKi = 9.1 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
5685 4075 18 None -3 15 Human 9.1 pKi = 9.1 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
CHEMBL25554 4075 18 None -3 15 Human 9.1 pKi = 9.1 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
44579229 189614 0 None 6 3 Human 9.1 pKi = 9.1 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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 189614 0 None 6 3 Human 9.1 pKi = 9.1 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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
44579187 189677 0 None 25 3 Human 9.1 pKi = 9.1 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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 189677 0 None 25 3 Human 9.1 pKi = 9.1 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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
44438167 148968 0 None 52 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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 148968 0 None 52 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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
102 4125 48 None -2 50 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C 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 4125 48 None -2 50 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C 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 4125 48 None -2 50 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C 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 4125 48 None -2 50 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C 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 4125 48 None -2 50 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C 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
10028898 111653 0 None 11 2 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 111653 0 None 11 2 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
44324737 207236 0 None 2 5 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 207236 0 None 2 5 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 207236 0 None 2 5 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptorInhibition of [3H]- rauwolscine binding to alpha-2C 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 207236 0 None 2 5 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptorInhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptor
ChEMBL 473 6 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc5ccccc5c4)CC3)[C@@H]1CO2 10.1021/jm049619s
102 4125 48 None -2 50 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
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 4125 48 None -2 50 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
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 4125 48 None -2 50 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
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 4125 48 None -2 50 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
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 4125 48 None -2 50 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
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
25110718 193307 0 None 16 3 Human 9.1 pKi = 9.1 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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 193307 0 None 16 3 Human 9.1 pKi = 9.1 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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
44330857 4392 0 None 5 2 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 4392 0 None 5 2 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
136019934 144528 0 None 7 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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 144528 0 None 7 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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
124 2979 47 None -60 32 Human 9.0 pKi = 9 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C 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 2979 47 None -60 32 Human 9.0 pKi = 9 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C 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 2979 47 None -60 32 Human 9.0 pKi = 9 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C 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 2979 47 None -60 32 Human 9.0 pKi = 9 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C 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 2979 47 None -60 32 Human 9.0 pKi = 9 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C 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
136 3290 32 None 3 16 Human 9.0 pKi = 9 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 3290 32 None 3 16 Human 9.0 pKi = 9 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 3290 32 None 3 16 Human 9.0 pKi = 9 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 3290 32 None 3 16 Human 9.0 pKi = 9 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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
44402346 132737 0 None - 1 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
ChEMBL 530 7 4 5 3.9 O=C(NCCCNC(=O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O)OCc1ccccc1 10.1016/j.bmcl.2005.03.116
CHEMBL369938 132737 0 None - 1 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
ChEMBL 530 7 4 5 3.9 O=C(NCCCNC(=O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O)OCc1ccccc1 10.1016/j.bmcl.2005.03.116
135398737 957 93 None -3 91 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 957 93 None -3 91 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 957 93 None -3 91 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 957 93 None -3 91 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 957 93 None -3 91 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
52950140 17156 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17156 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
107715 200943 22 None -7 20 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 200943 22 None -7 20 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 200943 22 None -7 20 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
49781223 17250 0 None -2 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17250 0 None -2 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
2389 3329 118 None -10 67 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3329 118 None -10 67 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3329 118 None -10 67 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3329 118 None -10 67 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3329 118 None -10 67 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
10824121 120479 1 None - 1 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity against alpha-2C adrenergic receptor of male Wistar ratIn vitro binding affinity against alpha-2C adrenergic receptor of male Wistar rat
ChEMBL 242 2 1 2 2.8 Brc1csc(Cc2c[nH]cn2)c1 10.1021/jm0003891
CHEMBL1203852 120479 1 None - 1 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity against alpha-2C adrenergic receptor of male Wistar ratIn vitro binding affinity against alpha-2C adrenergic receptor of male Wistar rat
ChEMBL 242 2 1 2 2.8 Brc1csc(Cc2c[nH]cn2)c1 10.1021/jm0003891
CHEMBL354272 120479 1 None - 1 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity against alpha-2C adrenergic receptor of male Wistar ratIn vitro binding affinity against alpha-2C adrenergic receptor of male Wistar rat
ChEMBL 242 2 1 2 2.8 Brc1csc(Cc2c[nH]cn2)c1 10.1021/jm0003891
44324800 206946 0 None 5 7 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 206946 0 None 5 7 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
49781224 17141 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17141 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
10531 1419 21 None -9 24 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1419 21 None -9 24 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1419 21 None -9 24 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1419 21 None -9 24 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1419 21 None -9 24 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
49781007 17239 0 None 2 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17239 0 None 2 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
44324937 206911 0 None -1 3 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 206911 0 None -1 3 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
1043 1580 14 None -19 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1580 14 None -19 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
3251 1580 14 None -19 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1580 14 None -19 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
CHEMBL1982133 1580 14 None -19 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1580 14 None -19 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1580 14 None -19 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
44579272 187093 0 None 5 3 Human 8.7 pKi = 8.7 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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 187093 0 None 5 3 Human 8.7 pKi = 8.7 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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
102 4125 48 None -2 50 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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 4125 48 None -2 50 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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 4125 48 None -2 50 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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 4125 48 None -2 50 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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 4125 48 None -2 50 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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
56944383 112117 0 None -3 12 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3290012 112117 0 None -3 12 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
44324906 206785 0 None -3 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 206785 0 None -3 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
44324725 206815 0 None 13 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 206815 0 None 13 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
49781005 17212 0 None -3 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17212 0 None -3 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
2389 3329 118 None -10 67 Human 8.0 pKi = 8 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C 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 3329 118 None -10 67 Human 8.0 pKi = 8 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C 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 3329 118 None -10 67 Human 8.0 pKi = 8 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C 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 3329 118 None -10 67 Human 8.0 pKi = 8 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C 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 3329 118 None -10 67 Human 8.0 pKi = 8 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C 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
16655023 107439 2 None 5 7 Human 8.0 pKi = 8 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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 107439 2 None 5 7 Human 8.0 pKi = 8 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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
44330621 4400 0 None 6 2 Human 8.0 pKi = 8 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 4400 0 None 6 2 Human 8.0 pKi = 8 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
44324972 163370 0 None 2 4 Human 8.0 pKi = 8 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 163370 0 None 2 4 Human 8.0 pKi = 8 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
49781006 17238 0 None -3 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17238 0 None -3 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
441082 1162 48 None -2 8 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C4 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 1162 48 None -2 8 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C4 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 1162 48 None -2 8 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C4 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
441082 1162 48 None -2 8 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C4 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 1162 48 None -2 8 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C4 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 1162 48 None -2 8 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C4 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
10707358 179283 0 None -7 3 Human 8.0 pKi = 8.0 Binding
Inhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 272 4 1 3 3.2 c1ccc(CC[C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
CHEMBL47313 179283 0 None -7 3 Human 8.0 pKi = 8.0 Binding
Inhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 272 4 1 3 3.2 c1ccc(CC[C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
242 470 124 None -23 52 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
34 470 124 None -23 52 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
60795 470 124 None -23 52 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
CHEMBL1112 470 124 None -23 52 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
DB01238 470 124 None -23 52 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
135398737 957 93 None -3 91 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 957 93 None -3 91 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 957 93 None -3 91 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 957 93 None -3 91 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 957 93 None -3 91 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
135398745 2912 112 None -30 66 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C 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 2912 112 None -30 66 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C 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 2912 112 None -30 66 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C 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 2912 112 None -30 66 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C 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
2337 3254 77 None -10 63 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
50 3254 77 None -10 63 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
5002 3254 77 None -10 63 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
CHEMBL716 3254 77 None -10 63 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
DB01224 3254 77 None -10 63 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
16090600 169179 0 None 10 3 Human 7.0 pKi = 7 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 360 6 2 4 5.1 Cc1nc2ccccc2c(Nc2ccc(NCCN3CCCC3)cc2)c1C 10.1016/j.ejmech.2010.12.026
CHEMBL440594 169179 0 None 10 3 Human 7.0 pKi = 7 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 360 6 2 4 5.1 Cc1nc2ccccc2c(Nc2ccc(NCCN3CCCC3)cc2)c1C 10.1016/j.ejmech.2010.12.026
9982218 101762 6 None -12 6 Human 7.0 pKi = 7 Binding
Bnding affinity against cloned human Alpha-2C adrenergic receptor was evaluatedBnding affinity against cloned human Alpha-2C adrenergic receptor was evaluated
ChEMBL 471 9 2 5 4.1 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
CHEMBL1435188 101762 6 None -12 6 Human 7.0 pKi = 7 Binding
Bnding affinity against cloned human Alpha-2C adrenergic receptor was evaluatedBnding affinity against cloned human Alpha-2C adrenergic receptor was evaluated
ChEMBL 471 9 2 5 4.1 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
CHEMBL299879 101762 6 None -12 6 Human 7.0 pKi = 7 Binding
Bnding affinity against cloned human Alpha-2C adrenergic receptor was evaluatedBnding affinity against cloned human Alpha-2C adrenergic receptor was evaluated
ChEMBL 471 9 2 5 4.1 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
16090600 169179 0 None 10 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 360 6 2 4 5.1 Cc1nc2ccccc2c(Nc2ccc(NCCN3CCCC3)cc2)c1C 10.1021/jm060262x
CHEMBL440594 169179 0 None 10 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 360 6 2 4 5.1 Cc1nc2ccccc2c(Nc2ccc(NCCN3CCCC3)cc2)c1C 10.1021/jm060262x
10793665 106950 0 None -562 6 Human 6.0 pKi = 6 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 106950 0 None -562 6 Human 6.0 pKi = 6 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
42574 15285 90 None -18 3 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 662 4 2 3 7.1 Cc1cc(C(C#N)c2ccc(Cl)cc2)c(Cl)cc1NC(=O)c1cc(I)cc(I)c1O nan
CHEMBL12131 15285 90 None -18 3 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 662 4 2 3 7.1 Cc1cc(C(C#N)c2ccc(Cl)cc2)c(Cl)cc1NC(=O)c1cc(I)cc(I)c1O nan
153287553 171102 0 None -158 6 Human 6.0 pKi = 6 Binding
Displacement of [3H]-Rauwolscine from human recombinant adrenergic Alpha2C receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human recombinant adrenergic Alpha2C receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 264 1 1 2 3.7 C[C@@]12CN(c3ccccc3)c3ccccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
CHEMBL4457754 171102 0 None -158 6 Human 6.0 pKi = 6 Binding
Displacement of [3H]-Rauwolscine from human recombinant adrenergic Alpha2C receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human recombinant adrenergic Alpha2C receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 264 1 1 2 3.7 C[C@@]12CN(c3ccccc3)c3ccccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
2719 916 74 None -6 11 Human 5.0 pKi = 5 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) 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 916 74 None -6 11 Human 5.0 pKi = 5 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) 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
607 916 74 None -6 11 Human 5.0 pKi = 5 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) 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 916 74 None -6 11 Human 5.0 pKi = 5 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) 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 916 74 None -6 11 Human 5.0 pKi = 5 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) 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
9817231 158234 22 None -1 7 Human 5.0 pKi = 5 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) 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 158234 22 None -1 7 Human 5.0 pKi = 5 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) 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
3598 187819 76 None -1 7 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
CHEMBL496 187819 76 None -1 7 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
11801828 206542 0 None -63 6 Human 6.0 pKi = 6.0 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 206542 0 None -63 6 Human 6.0 pKi = 6.0 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
132584404 143347 0 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]Rauwolscine from human Alpha2C receptor expressed in MDCK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]Rauwolscine from human Alpha2C 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 143347 0 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]Rauwolscine from human Alpha2C receptor expressed in MDCK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]Rauwolscine from human Alpha2C 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
11333552 121713 5 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 223 4 1 4 1.1 COc1ccccc1OCC1CNCCO1 10.1016/j.bmc.2015.01.013
CHEMBL3588908 121713 5 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 223 4 1 4 1.1 COc1ccccc1OCC1CNCCO1 10.1016/j.bmc.2015.01.013
2351 3284 64 None -4 21 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 3284 64 None -4 21 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 3284 64 None -4 21 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 3284 64 None -4 21 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 3284 64 None -4 21 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
122180567 121709 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 261 4 1 3 3.8 c1cncc(-c2ccccc2NCc2ccncc2)c1 10.1016/j.bmc.2015.01.013
CHEMBL3588904 121709 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 261 4 1 3 3.8 c1cncc(-c2ccccc2NCc2ccncc2)c1 10.1016/j.bmc.2015.01.013
11948707 166165 0 None -269 13 Human 7.0 pKi = 7.0 Binding
Binding affinity to alpha 2C adrenergic receptor by radioligand binding assayBinding affinity to alpha 2C 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 166165 0 None -269 13 Human 7.0 pKi = 7.0 Binding
Binding affinity to alpha 2C adrenergic receptor by radioligand binding assayBinding affinity to alpha 2C 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
16090635 82513 0 None 5 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 378 4 1 4 4.7 CCc1c(C)nc2c(c1Nc1ccc(N3CCN(C)C(C)C3)cc1)CCCC2 10.1016/j.ejmech.2010.12.026
CHEMBL217768 82513 0 None 5 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 378 4 1 4 4.7 CCc1c(C)nc2c(c1Nc1ccc(N3CCN(C)C(C)C3)cc1)CCCC2 10.1016/j.ejmech.2010.12.026
44289035 100512 0 None -575 7 Human 6.0 pKi = 6.0 Binding
In vivo inhibitory effect against Alpha-2C adrenergic receptorIn vivo inhibitory effect against Alpha-2C 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 100512 0 None -575 7 Human 6.0 pKi = 6.0 Binding
In vivo inhibitory effect against Alpha-2C adrenergic receptorIn vivo inhibitory effect against Alpha-2C 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
127036186 137412 0 None -34 19 Human 6.0 pKi = 6.0 Binding
Binding affinity to alpha-2C adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2C 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 137412 0 None -34 19 Human 6.0 pKi = 6.0 Binding
Binding affinity to alpha-2C adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2C 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
44210114 192714 19 None -6 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to alpha2C AR (unknown origin) assessed as inhibition constantBinding affinity to alpha2C AR (unknown origin) assessed as inhibition constant
ChEMBL 492 5 0 6 4.3 O=C1C2C3CCC(C3)C2C(=O)N1CC1CCCCC1CN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmcl.2021.128275
CHEMBL5219924 192714 19 None -6 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to alpha2C AR (unknown origin) assessed as inhibition constantBinding affinity to alpha2C AR (unknown origin) assessed as inhibition constant
ChEMBL 492 5 0 6 4.3 O=C1C2C3CCC(C3)C2C(=O)N1CC1CCCCC1CN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmcl.2021.128275
11293787 148211 0 None 27 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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 148211 0 None 27 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cells
ChEMBL 447 6 0 5 5.8 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4F)cc13)CC2 10.1016/j.bmcl.2006.12.094
1393724 121901 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 222 3 1 2 2.7 N#Cc1cccc(-c2ccccc2CCN)c1 10.1016/j.bmc.2015.01.013
CHEMBL3590203 121901 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 222 3 1 2 2.7 N#Cc1cccc(-c2ccccc2CCN)c1 10.1016/j.bmc.2015.01.013
16090635 82513 0 None 5 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 82513 0 None 5 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
46869265 16255 0 None -5 7 Human 6.0 pKi = 6.0 Binding
Binding affinity to adrenergic Alpha-2C receptorBinding affinity to adrenergic Alpha-2C 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 16255 0 None -5 7 Human 6.0 pKi = 6.0 Binding
Binding affinity to adrenergic Alpha-2C receptorBinding affinity to adrenergic Alpha-2C 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
CHEMBL5274312 193807 0 None 1 5 Human 6.0 pKi = 6.0 Binding
Binding affinity to adrenergic alpha 2c receptor (unknown origin)Binding affinity to adrenergic alpha 2c receptor (unknown origin)
ChEMBL 383 4 0 3 5.0 CC[Si](C#Cc1cccc2c1OC(C(F)(F)F)C([N+](=O)[O-])=C2)(CC)CC 10.1016/j.bmcl.2022.128981
10489502 4516 2 None -11 3 Human 6.0 pKi = 6.0 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 227 2 2 2 3.5 Clc1cccc(Cl)c1Nc1ncc[nH]1 10.1021/jm9605142
CHEMBL1022 4516 2 None -11 3 Human 6.0 pKi = 6.0 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 227 2 2 2 3.5 Clc1cccc(Cl)c1Nc1ncc[nH]1 10.1021/jm9605142
49836307 18783 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C 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 18783 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 C[C@H](Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm100977d
240 943 43 None -5 25 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
2769 943 43 None -5 25 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
44279790 943 43 None -5 25 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
660 943 43 None -5 25 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL1729 943 43 None -5 25 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL560739 943 43 None -5 25 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
DB00604 943 43 None -5 25 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
11386747 75489 9 None -1 2 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (Radioligand binding assay (MDS Pharma Service)) EUB0000296b ADRA2CSelectivity interaction (Radioligand binding assay (MDS Pharma Service)) EUB0000296b ADRA2C
ChEMBL 513 4 1 5 6.4 CC(=O)Nc1c(C(C)=O)c(=O)n(C)c2nc(-c3ccc(Cl)cc3Cl)c(-c3ccc(Cl)cc3)cc12 10.6019/CHEMBL5212743
CHEMBL204232 75489 9 None -1 2 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (Radioligand binding assay (MDS Pharma Service)) EUB0000296b ADRA2CSelectivity interaction (Radioligand binding assay (MDS Pharma Service)) EUB0000296b ADRA2C
ChEMBL 513 4 1 5 6.4 CC(=O)Nc1c(C(C)=O)c(=O)n(C)c2nc(-c3ccc(Cl)cc3Cl)c(-c3ccc(Cl)cc3)cc12 10.6019/CHEMBL5212743
11140347 204531 1 None -18 6 Human 6.9 pKi = 6.9 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 204531 1 None -18 6 Human 6.9 pKi = 6.9 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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
71455894 83800 0 None 1 12 Human 5.9 pKi = 5.9 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmcl.2012.08.046
CHEMBL2205827 83800 0 None 1 12 Human 5.9 pKi = 5.9 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmcl.2012.08.046
71455894 83800 0 None 1 12 Human 5.9 pKi = 5.9 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmc.2013.07.045
CHEMBL2205827 83800 0 None 1 12 Human 5.9 pKi = 5.9 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmc.2013.07.045
104903 56342 17 None -1 6 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
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 nan
CHEMBL1630578 56342 17 None -1 6 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
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 nan
10841190 107040 0 None -162 6 Human 5.9 pKi = 5.9 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 107040 0 None -162 6 Human 5.9 pKi = 5.9 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
44311789 204733 0 None 1 5 Human 4.9 pKi = 4.9 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
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 204733 0 None 1 5 Human 4.9 pKi = 4.9 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 345 1 2 5 3.1 Brc1c(NC2=N[C@@H]3CCCC[C@@H]3N2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
10220337 200449 53 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 236 2 0 2 2.7 Brc1cccc(Cn2ccnc2)c1 10.1016/j.bmc.2015.01.013
CHEMBL598391 200449 53 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 236 2 0 2 2.7 Brc1cccc(Cn2ccnc2)c1 10.1016/j.bmc.2015.01.013
2274 3171 58 None -4 32 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3171 58 None -4 32 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3171 58 None -4 32 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3171 58 None -4 32 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3171 58 None -4 32 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
218362 204798 5 None -5 4 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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 204798 5 None -5 4 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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
68712 100336 60 None -1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2C 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 100336 60 None -1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2C 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
9883506 70562 0 None 1 6 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human alpha-2C adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2C 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 70562 0 None 1 6 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human alpha-2C adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2C 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
9816048 187276 0 None -12 3 Human 6.9 pKi = 6.9 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 231 1 4 5 1.2 Cc1c(NC2=NCCN2)ccc2c1NCCN2 10.1021/jm960359r
CHEMBL49284 187276 0 None -12 3 Human 6.9 pKi = 6.9 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 231 1 4 5 1.2 Cc1c(NC2=NCCN2)ccc2c1NCCN2 10.1021/jm960359r
118717249 115123 0 None -18 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RS-79948-197 from human alpha2C adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation countingDisplacement of [3H]RS-79948-197 from human alpha2C 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 115123 0 None -18 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RS-79948-197 from human alpha2C adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation countingDisplacement of [3H]RS-79948-197 from human alpha2C 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
50985821 176216 31 None 2 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to alpha2C receptor (unknown origin) by radioligand displacement assayBinding affinity to alpha2C receptor (unknown origin) by radioligand displacement assay
ChEMBL 474 5 2 5 6.2 N=c1c2c(-c3ccccc3)c(-c3ccccc3)n(Cc3ccccc3)c2ncn1[C@H]1CC[C@H](O)CC1 10.1021/acs.jmedchem.2c00204
CHEMBL4594433 176216 31 None 2 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to alpha2C receptor (unknown origin) by radioligand displacement assayBinding affinity to alpha2C receptor (unknown origin) by radioligand displacement assay
ChEMBL 474 5 2 5 6.2 N=c1c2c(-c3ccccc3)c(-c3ccccc3)n(Cc3ccccc3)c2ncn1[C@H]1CC[C@H](O)CC1 10.1021/acs.jmedchem.2c00204
44292232 101319 0 None -4 3 Human 6.9 pKi = 6.9 Binding
Inhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 222 3 1 3 2.2 CCC[C@H]1C2CCC(C2)[C@H]1NC1=NCCO1 10.1021/jm9905256
CHEMBL296660 101319 0 None -4 3 Human 6.9 pKi = 6.9 Binding
Inhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 222 3 1 3 2.2 CCC[C@H]1C2CCC(C2)[C@H]1NC1=NCCO1 10.1021/jm9905256
9971924 184224 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Inhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 298 5 1 3 3.4 c1ccc(CCC[C@H]2C3CCC(C3)[C@H]2NC2=NCCO2)cc1 10.1021/jm9905256
CHEMBL48341 184224 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Inhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 298 5 1 3 3.4 c1ccc(CCC[C@H]2C3CCC(C3)[C@H]2NC2=NCCO2)cc1 10.1021/jm9905256
11221758 84615 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1ccccc1[N+](=O)[O-])C1=NCCN1 10.1021/jm0408215
CHEMBL222138 84615 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1ccccc1[N+](=O)[O-])C1=NCCN1 10.1021/jm0408215
49836304 18569 1 None -2 3 Human 6.9 pKi = 6.9 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 230 4 1 3 2.3 C[C@@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL1276219 18569 1 None -2 3 Human 6.9 pKi = 6.9 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 230 4 1 3 2.3 C[C@@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
49836304 18569 1 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 230 4 1 3 2.3 C[C@@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
CHEMBL1276219 18569 1 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 230 4 1 3 2.3 C[C@@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
49836305 18574 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 C[C@H](Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
CHEMBL1276248 18574 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 C[C@H](Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
56852956 112041 1 None -32 9 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]clonidine from human adrenergic-alpha2C receptor by PDSP assayDisplacement of [3H]clonidine from human adrenergic-alpha2C receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 112041 1 None -32 9 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]clonidine from human adrenergic-alpha2C receptor by PDSP assayDisplacement of [3H]clonidine from human adrenergic-alpha2C receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
24906203 187216 0 None -3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 280 2 1 4 2.5 c1ccc(-c2ccc3c(c2)OC(C2=NCCN2)CO3)cc1 10.1021/jm800250z
CHEMBL492445 187216 0 None -3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 280 2 1 4 2.5 c1ccc(-c2ccc3c(c2)OC(C2=NCCN2)CO3)cc1 10.1021/jm800250z
11380132 84417 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1ccccn1)C1=NCCN1 10.1021/jm0408215
CHEMBL221989 84417 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1ccccn1)C1=NCCN1 10.1021/jm0408215
56852956 112041 1 None -32 9 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]clonidine from human adrenergic-alpha2C receptor by PDSP assayDisplacement of [3H]clonidine from human adrenergic-alpha2C receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 112041 1 None -32 9 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]clonidine from human adrenergic-alpha2C receptor by PDSP assayDisplacement of [3H]clonidine from human adrenergic-alpha2C receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
44371744 50319 0 None -7 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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 50319 0 None -7 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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
2585 802 103 None -16 22 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 802 103 None -16 22 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 802 103 None -16 22 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 802 103 None -16 22 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 802 103 None -16 22 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
44325044 207381 0 None 5 3 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 207381 0 None 5 3 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
213041 17131 28 None -2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17131 28 None -2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
CHEMBL4535474 213986 39 None -1 6 Human 6.9 pKi = 6.9 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000320b ADRA2CSelectivity interaction (GPCR panel (PDSP screen)) EUB0000320b ADRA2C
ChEMBL None None None CNCc1ccccc1-c1csc([C@@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL5212743
489 145 28 None -380 12 Human 6.9 pKi = 6.9 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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 145 28 None -380 12 Human 6.9 pKi = 6.9 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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 145 28 None -380 12 Human 6.9 pKi = 6.9 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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
11371902 141636 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
CHEMBL385310 141636 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
11371902 141636 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm0408215
CHEMBL385310 141636 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm0408215
11741010 83249 0 None 4 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 83249 0 None 4 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
11741010 83249 0 None 4 3 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 388 3 1 4 5.4 Cc1cc(C)c2c(Nc3ccc(N4CCN(C)C(C)C4)cc3)c(C)c(C)nc2c1 10.1016/j.ejmech.2010.12.026
CHEMBL218730 83249 0 None 4 3 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 388 3 1 4 5.4 Cc1cc(C)c2c(Nc3ccc(N4CCN(C)C(C)C4)cc3)c(C)c(C)nc2c1 10.1016/j.ejmech.2010.12.026
135356876 174072 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human alpha2C receptor expressed in MDCK cells by PDSP assayBinding affinity to human alpha2C 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 174072 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human alpha2C receptor expressed in MDCK cells by PDSP assayBinding affinity to human alpha2C 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
9809007 172562 8 None -724 6 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 172562 8 None -724 6 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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
16090598 82453 0 None 5 3 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 394 3 1 4 5.4 Cc1nc2cccc(Cl)c2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1016/j.ejmech.2010.12.026
CHEMBL217568 82453 0 None 5 3 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 394 3 1 4 5.4 Cc1nc2cccc(Cl)c2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1016/j.ejmech.2010.12.026
16090598 82453 0 None 5 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 82453 0 None 5 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
71450548 83798 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 295 3 1 3 2.0 COc1cccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL2205824 83798 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 295 3 1 3 2.0 COc1cccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
42656257 121717 0 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 242 2 1 3 2.6 COc1ccc(C2NCCCn3cccc32)cc1 10.1016/j.bmc.2015.01.013
CHEMBL3588912 121717 0 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 242 2 1 3 2.6 COc1ccc(C2NCCCn3cccc32)cc1 10.1016/j.bmc.2015.01.013
26987 948 33 None -107 21 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 948 33 None -107 21 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 948 33 None -107 21 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 948 33 None -107 21 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 948 33 None -107 21 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
10198248 187447 40 None -6 6 Human 5.9 pKi = 5.9 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 213 1 2 5 1.0 c1cnc2cc(NC3=NCCN3)ccc2n1 10.1016/0960-894X(95)00391-6
CHEMBL49395 187447 40 None -6 6 Human 5.9 pKi = 5.9 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 213 1 2 5 1.0 c1cnc2cc(NC3=NCCN3)ccc2n1 10.1016/0960-894X(95)00391-6
13091268 78222 0 None -158 14 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned adrenergic alpha-2C receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-2C 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 78222 0 None -158 14 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned adrenergic alpha-2C receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-2C 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
44582678 181572 0 None 3 10 Human 6.8 pKi = 6.8 Binding
Inhibition of human cloned Alpha-2C adrenergic receptor by competitive binding experimentInhibition of human cloned Alpha-2C adrenergic receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL476839 181572 0 None 3 10 Human 6.8 pKi = 6.8 Binding
Inhibition of human cloned Alpha-2C adrenergic receptor by competitive binding experimentInhibition of human cloned Alpha-2C adrenergic receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
11108001 10870 2 None -12 6 Human 6.8 pKi = 6.8 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 10870 2 None -12 6 Human 6.8 pKi = 6.8 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 10870 2 None -12 6 Human 6.8 pKi = 6.8 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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
11380133 169365 0 None -5 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1ccncc1)C1=NCCN1 10.1021/jm0408215
CHEMBL442045 169365 0 None -5 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1ccncc1)C1=NCCN1 10.1021/jm0408215
3151 1461 97 None -40 27 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
945 1461 97 None -40 27 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
965 1461 97 None -40 27 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
CHEMBL219916 1461 97 None -40 27 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
DB01184 1461 97 None -40 27 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
73291731 92489 0 None -10 4 Human 6.8 pKi = 6.8 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 232 5 1 3 2.4 CCCc1ccccc1OC(C)C1=NCCN1 10.1021/ml400232p
CHEMBL2431282 92489 0 None -10 4 Human 6.8 pKi = 6.8 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 232 5 1 3 2.4 CCCc1ccccc1OC(C)C1=NCCN1 10.1021/ml400232p
45487955 198308 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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 198308 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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
9827677 168420 0 None -7413 7 Human 5.8 pKi = 5.8 Binding
In vivo inhibitory effect against Alpha-2C adrenergic receptorIn vivo inhibitory effect against Alpha-2C 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 168420 0 None -7413 7 Human 5.8 pKi = 5.8 Binding
In vivo inhibitory effect against Alpha-2C adrenergic receptorIn vivo inhibitory effect against Alpha-2C 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
50878551 90743 61 None -22 18 Human 5.8 pKi = 5.8 Binding
Binding affinity to alpha-2C adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2C 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 90743 61 None -22 18 Human 5.8 pKi = 5.8 Binding
Binding affinity to alpha-2C adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2C 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
44455426 155147 0 None -2 12 Human 6.8 pKi = 6.8 Binding
Inhibition of human cloned Alpha-2C adrenergic receptor by competitive binding experimentInhibition of human cloned Alpha-2C adrenergic receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL402143 155147 0 None -2 12 Human 6.8 pKi = 6.8 Binding
Inhibition of human cloned Alpha-2C adrenergic receptor by competitive binding experimentInhibition of human cloned Alpha-2C adrenergic receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
144852560 170934 0 None -85 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expressed in MDCK cells by radioligand binding assayDisplacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expressed in MDCK cells by radioligand binding assay
ChEMBL 343 2 2 5 3.8 Clc1ccc(C#Cc2nc(NC3CCCC3)c3nc[nH]c3n2)s1 10.1039/C8MD00317C
CHEMBL4455344 170934 0 None -85 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expressed in MDCK cells by radioligand binding assayDisplacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expressed in MDCK cells by radioligand binding assay
ChEMBL 343 2 2 5 3.8 Clc1ccc(C#Cc2nc(NC3CCCC3)c3nc[nH]c3n2)s1 10.1039/C8MD00317C
71463063 83799 0 None -2 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 295 3 1 3 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205825 83799 0 None -2 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 295 3 1 3 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
21830793 91833 10 None -100 45 Human 7.8 pKi = 7.8 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin)Binding affinity to adrenergic alpha2C 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 91833 10 None -100 45 Human 7.8 pKi = 7.8 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin)Binding affinity to adrenergic alpha2C 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
10044968 96543 0 None 54 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 374 3 1 4 5.0 Cc1ccc2c(Nc3ccc(N4CCN(C)C(C)C4)cc3)c(C)c(C)nc2c1 10.1016/j.ejmech.2010.12.026
CHEMBL262901 96543 0 None 54 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 374 3 1 4 5.0 Cc1ccc2c(Nc3ccc(N4CCN(C)C(C)C4)cc3)c(C)c(C)nc2c1 10.1016/j.ejmech.2010.12.026
10044968 96543 0 None 54 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 96543 0 None 54 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
44579231 181565 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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 181565 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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
3158 56265 27 None -1047 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 56265 27 None -1047 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
DB01142 56265 27 None -1047 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
10609673 103774 0 None -11 3 Human 5.8 pKi = 5.8 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 233 4 2 4 2.5 COc1ccc(Nc2ncc[nH]2)c(C)c1OC 10.1021/jm9605142
CHEMBL308863 103774 0 None -11 3 Human 5.8 pKi = 5.8 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 233 4 2 4 2.5 COc1ccc(Nc2ncc[nH]2)c(C)c1OC 10.1021/jm9605142
118734875 118735 0 None -489 3 Human 5.8 pKi = 5.8 Binding
Inhibition of alpha-2C adrenergic receptor (unknown origin)Inhibition of alpha-2C adrenergic receptor (unknown origin)
ChEMBL 327 6 1 4 2.4 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)[C@@H]3C[C@H]23)cc1 10.1016/j.ejmech.2015.03.054
CHEMBL3417585 118735 0 None -489 3 Human 5.8 pKi = 5.8 Binding
Inhibition of alpha-2C adrenergic receptor (unknown origin)Inhibition of alpha-2C adrenergic receptor (unknown origin)
ChEMBL 327 6 1 4 2.4 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)[C@@H]3C[C@H]23)cc1 10.1016/j.ejmech.2015.03.054
73352414 92530 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 257 3 1 1 3.3 C1CCC(CN[C@H]2C3C4CC5C6C4CC3C6C52)CC1 10.1016/j.bmc.2013.07.045
CHEMBL2432038 92530 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 257 3 1 1 3.3 C1CCC(CN[C@H]2C3C4CC5C6C4CC3C6C52)CC1 10.1016/j.bmc.2013.07.045
737253 118501 139 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 191 1 1 3 1.0 CN1CCN(c2ccc(N)cc2)CC1 10.1016/j.bmc.2015.01.013
CHEMBL341473 118501 139 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 191 1 1 3 1.0 CN1CCN(c2ccc(N)cc2)CC1 10.1016/j.bmc.2015.01.013
32238 22653 114 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 256 3 1 3 2.9 OC(Cn1ccnc1)c1ccc(Cl)cc1Cl 10.1016/j.bmc.2015.01.013
CHEMBL1327 22653 114 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 256 3 1 3 2.9 OC(Cn1ccnc1)c1ccc(Cl)cc1Cl 10.1016/j.bmc.2015.01.013
44582705 186994 0 None 3 13 Human 6.8 pKi = 6.8 Binding
Inhibition of human cloned Alpha-2C adrenergic receptor by competitive binding experimentInhibition of human cloned Alpha-2C adrenergic receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL490632 186994 0 None 3 13 Human 6.8 pKi = 6.8 Binding
Inhibition of human cloned Alpha-2C adrenergic receptor by competitive binding experimentInhibition of human cloned Alpha-2C adrenergic receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
71463022 83696 7 None -1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]clonidine from alpha2C adrenergic receptor after 40 mins by scintillation counting analysisDisplacement of [3H]clonidine from alpha2C 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 83696 7 None -1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]clonidine from alpha2C adrenergic receptor after 40 mins by scintillation counting analysisDisplacement of [3H]clonidine from alpha2C 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
770500 121714 3 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 242 4 2 3 2.4 NCC(=O)Nc1ccccc1Oc1ccccc1 10.1016/j.bmc.2015.01.013
CHEMBL3588909 121714 3 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 242 4 2 3 2.4 NCC(=O)Nc1ccccc1Oc1ccccc1 10.1016/j.bmc.2015.01.013
4306793 121715 1 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 282 3 1 3 2.6 O=C(CCC1CCCC1)N1CCSC12CCNCC2 10.1016/j.bmc.2015.01.013
CHEMBL3588910 121715 1 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 282 3 1 3 2.6 O=C(CCC1CCCC1)N1CCSC12CCNCC2 10.1016/j.bmc.2015.01.013
10651654 111481 0 None -85 6 Human 6.8 pKi = 6.8 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 111481 0 None -85 6 Human 6.8 pKi = 6.8 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
24906202 187215 0 None -5 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 280 2 1 4 2.5 c1ccc(-c2ccc3c(c2)OCC(C2=NCCN2)O3)cc1 10.1021/jm800250z
CHEMBL492444 187215 0 None -5 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 280 2 1 4 2.5 c1ccc(-c2ccc3c(c2)OCC(C2=NCCN2)O3)cc1 10.1021/jm800250z
3652 46242 70 None -2 9 Human 4.8 pKi = 4.8 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) 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 46242 70 None -2 9 Human 4.8 pKi = 4.8 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) 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
16090626 82133 0 None 77 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 378 3 1 4 4.9 Cc1nc2ccc(F)cc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1016/j.ejmech.2010.12.026
CHEMBL216727 82133 0 None 77 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 378 3 1 4 4.9 Cc1nc2ccc(F)cc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1016/j.ejmech.2010.12.026
2142 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
4920903 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
502 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
5775 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
CHEMBL597 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
DB00692 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
16090626 82133 0 None 77 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 82133 0 None 77 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
9906978 42709 2 None -1 12 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned adrenergic alpha-2C receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-2C 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 42709 2 None -1 12 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned adrenergic alpha-2C receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-2C 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
10527469 156263 3 None -35 16 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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 156263 3 None -35 16 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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
11211035 85001 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 284 4 1 3 3.3 CC(Oc1ccccc1-c1cccc(F)c1)C1=NCCN1 10.1021/jm061487a
CHEMBL223836 85001 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 284 4 1 3 3.3 CC(Oc1ccccc1-c1cccc(F)c1)C1=NCCN1 10.1021/jm061487a
11211035 85001 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 284 4 1 3 3.3 CC(Oc1ccccc1-c1cccc(F)c1)C1=NCCN1 10.1021/jm0408215
CHEMBL223836 85001 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 284 4 1 3 3.3 CC(Oc1ccccc1-c1cccc(F)c1)C1=NCCN1 10.1021/jm0408215
2803 954 58 None -4 19 Human 6.8 pKi = 6.8 Binding
Binding affinity towards alpha-2C adrenergic receptorBinding affinity towards alpha-2C adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm990569e
516 954 58 None -4 19 Human 6.8 pKi = 6.8 Binding
Binding affinity towards alpha-2C adrenergic receptorBinding affinity towards alpha-2C adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm990569e
704 954 58 None -4 19 Human 6.8 pKi = 6.8 Binding
Binding affinity towards alpha-2C adrenergic receptorBinding affinity towards alpha-2C adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm990569e
CHEMBL134 954 58 None -4 19 Human 6.8 pKi = 6.8 Binding
Binding affinity towards alpha-2C adrenergic receptorBinding affinity towards alpha-2C adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm990569e
DB00575 954 58 None -4 19 Human 6.8 pKi = 6.8 Binding
Binding affinity towards alpha-2C adrenergic receptorBinding affinity towards alpha-2C adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm990569e
11393666 192984 0 None -407 19 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX 821002 from recombinant human alpha2C receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]RX 821002 from recombinant human alpha2C 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 192984 0 None -407 19 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX 821002 from recombinant human alpha2C receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]RX 821002 from recombinant human alpha2C 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 192984 0 None -407 19 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX 821002 from recombinant human alpha2C receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]RX 821002 from recombinant human alpha2C 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
3952 1886 38 None -19 12 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5353646 1886 38 None -19 12 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5443 1886 38 None -19 12 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5702063 1886 38 None -19 12 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL1331786 1886 38 None -19 12 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL420 1886 38 None -19 12 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
DB00629 1886 38 None -19 12 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
92766 106540 35 None -1 6 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 106540 35 None -1 6 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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
44275807 98968 0 None -1479 10 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human Alpha-2C adrenergic receptorBinding affinity towards human Alpha-2C adrenergic receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
CHEMBL27979 98968 0 None -1479 10 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human Alpha-2C adrenergic receptorBinding affinity towards human Alpha-2C adrenergic receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
11199581 136557 0 None -5 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1ccccc1O)C1=NCCN1 10.1021/jm0408215
CHEMBL373830 136557 0 None -5 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1ccccc1O)C1=NCCN1 10.1021/jm0408215
132060746 163068 0 None -9 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2C receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2C receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 405 4 0 4 4.4 O=C(OCc1ccccc1)N1Cc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
CHEMBL4176474 163068 0 None -9 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2C receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2C receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 405 4 0 4 4.4 O=C(OCc1ccccc1)N1Cc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
9894818 98923 0 None -93 7 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 98923 0 None -93 7 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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
10859076 13680 0 None -2 6 Human 6.8 pKi = 6.8 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 13680 0 None -2 6 Human 6.8 pKi = 6.8 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 13680 0 None -2 6 Human 6.8 pKi = 6.8 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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
9894818 98923 0 None -93 7 Human 6.8 pKi = 6.8 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 98923 0 None -93 7 Human 6.8 pKi = 6.8 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
21392988 204815 4 None -1 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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 204815 4 None -1 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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
11109088 204178 0 None -36 6 Human 6.8 pKi = 6.8 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 204178 0 None -36 6 Human 6.8 pKi = 6.8 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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
4567175 82474 5 None -2 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 318 3 1 4 3.7 CN1CCN(c2ccc(Nc3ccnc4ccccc34)cc2)CC1 10.1016/j.ejmech.2010.12.026
CHEMBL217665 82474 5 None -2 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 318 3 1 4 3.7 CN1CCN(c2ccc(Nc3ccnc4ccccc34)cc2)CC1 10.1016/j.ejmech.2010.12.026
12575 1986 30 None -8 17 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1021/jm800250z
54459 1986 30 None -8 17 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1021/jm800250z
CHEMBL10316 1986 30 None -8 17 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1021/jm800250z
DB12551 1986 30 None -8 17 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1021/jm800250z
11346584 136982 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm061487a
CHEMBL374584 136982 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm061487a
12575 1986 30 None -8 17 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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 1986 30 None -8 17 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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 1986 30 None -8 17 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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
DB12551 1986 30 None -8 17 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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
11346584 136982 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm100977d
CHEMBL374584 136982 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm100977d
11346584 136982 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm0408215
CHEMBL374584 136982 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm0408215
3584 3775 64 None -50 14 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00010a001
5401 3775 64 None -50 14 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00010a001
7302 3775 64 None -50 14 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00010a001
CHEMBL611 3775 64 None -50 14 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00010a001
DB01162 3775 64 None -50 14 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00010a001
4567175 82474 5 None -2 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 318 3 1 4 3.7 CN1CCN(c2ccc(Nc3ccnc4ccccc34)cc2)CC1 10.1021/jm060262x
CHEMBL217665 82474 5 None -2 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 318 3 1 4 3.7 CN1CCN(c2ccc(Nc3ccnc4ccccc34)cc2)CC1 10.1021/jm060262x
9960497 117073 0 None -512 6 Human 5.8 pKi = 5.8 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 117073 0 None -512 6 Human 5.8 pKi = 5.8 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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
CHEMBL5273955 193786 0 None -1 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]RX821002 from human alpha2C receptor stably expressed in HEK293T cells by Cheng-Prusoff equation analysisDisplacement of [3H]RX821002 from human alpha2C receptor stably expressed in HEK293T cells by Cheng-Prusoff equation analysis
ChEMBL 305 3 2 2 4.1 C#Cc1cc(Nc2ccccc2C(=O)O)cc(C(F)(F)F)c1 10.1021/acs.jmedchem.2c01997
71452382 83792 0 None -53 10 Human 5.8 pKi = 5.8 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 309 4 1 3 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205812 83792 0 None -53 10 Human 5.8 pKi = 5.8 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 309 4 1 3 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
5472 205816 75 None -1 3 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 nan
CHEMBL1717 205816 75 None -1 3 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 nan
CHEMBL833 205816 75 None -1 3 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 nan
DB00208 205816 75 None -1 3 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 nan
9815633 99633 3 None -44 6 Human 6.8 pKi = 6.8 Binding
Binding affinity towards alpha-2C adrenergic receptorBinding affinity towards alpha-2C adrenergic receptor
ChEMBL 204 1 1 2 2.9 c1nc(C2CCCc3sccc32)c[nH]1 10.1021/jm990569e
CHEMBL284213 99633 3 None -44 6 Human 6.8 pKi = 6.8 Binding
Binding affinity towards alpha-2C adrenergic receptorBinding affinity towards alpha-2C adrenergic receptor
ChEMBL 204 1 1 2 2.9 c1nc(C2CCCc3sccc32)c[nH]1 10.1021/jm990569e
9815633 99633 3 None -44 6 Rat 6.8 pKi = 6.8 Binding
in vitro alpha-2C adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2C 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 99633 3 None -44 6 Rat 6.8 pKi = 6.8 Binding
in vitro alpha-2C adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2C 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
21509921 104456 0 None -16 24 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 104456 0 None -16 24 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
73346042 91832 5 None -1737 17 Human 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin)Binding affinity to adrenergic alpha2C 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 91832 5 None -1737 17 Human 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin)Binding affinity to adrenergic alpha2C 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
21509921 104456 0 None -16 24 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 104456 0 None -16 24 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
599482 202982 9 None -12 5 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Alpha-2C adrenergic receptorBinding affinity towards Alpha-2C adrenergic receptor
ChEMBL 202 1 2 2 1.8 COc1ccc2c3c([nH]c2c1)CNCC3 10.1016/j.bmcl.2003.09.027
CHEMBL6310 202982 9 None -12 5 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Alpha-2C adrenergic receptorBinding affinity towards Alpha-2C adrenergic receptor
ChEMBL 202 1 2 2 1.8 COc1ccc2c3c([nH]c2c1)CNCC3 10.1016/j.bmcl.2003.09.027
49836302 18564 1 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@H](C)C1=NCCN1 10.1021/ml400232p
CHEMBL1276139 18564 1 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@H](C)C1=NCCN1 10.1021/ml400232p
49836302 18564 1 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@H](C)C1=NCCN1 10.1021/jm100977d
CHEMBL1276139 18564 1 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@H](C)C1=NCCN1 10.1021/jm100977d
49836302 18564 1 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX821002 from human alpha2C adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2C 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 18564 1 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX821002 from human alpha2C adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2C 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
71452387 83801 0 None -1 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2012.08.046
CHEMBL2205829 83801 0 None -1 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2012.08.046
71452387 83801 0 None -1 7 Human 5.8 pKi = 5.8 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmc.2013.07.045
CHEMBL2205829 83801 0 None -1 7 Human 5.8 pKi = 5.8 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmc.2013.07.045
11225732 93655 0 None 16 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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 93655 0 None 16 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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
1816 2538 102 None -38 18 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
4205 2538 102 None -38 18 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
7241 2538 102 None -38 18 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
CHEMBL654 2538 102 None -38 18 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
DB00370 2538 102 None -38 18 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
118734876 118736 0 None -398 3 Human 5.8 pKi = 5.8 Binding
Inhibition of alpha-2C adrenergic receptor (unknown origin)Inhibition of alpha-2C adrenergic receptor (unknown origin)
ChEMBL 327 6 1 4 2.4 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)[C@H]3C[C@@H]23)cc1 10.1016/j.ejmech.2015.03.054
CHEMBL3417586 118736 0 None -398 3 Human 5.8 pKi = 5.8 Binding
Inhibition of alpha-2C adrenergic receptor (unknown origin)Inhibition of alpha-2C adrenergic receptor (unknown origin)
ChEMBL 327 6 1 4 2.4 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)[C@H]3C[C@@H]23)cc1 10.1016/j.ejmech.2015.03.054
181743 178570 5 None -91 22 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Clonidine from human adrenergic Alpha-2C receptorDisplacement of [3H]Clonidine from human adrenergic Alpha-2C receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL467094 178570 5 None -91 22 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Clonidine from human adrenergic Alpha-2C receptorDisplacement of [3H]Clonidine from human adrenergic Alpha-2C receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
71452384 83795 0 None -8 5 Human 5.7 pKi = 5.7 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmcl.2012.08.046
CHEMBL2205816 83795 0 None -8 5 Human 5.7 pKi = 5.7 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmcl.2012.08.046
71452384 83795 0 None -8 5 Human 5.7 pKi = 5.7 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmc.2013.07.045
CHEMBL2205816 83795 0 None -8 5 Human 5.7 pKi = 5.7 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmc.2013.07.045
277 1300 62 None -42 50 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1300 62 None -42 50 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1300 62 None -42 50 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1300 62 None -42 50 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1300 62 None -42 50 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
71452383 83794 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 339 5 1 4 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmcl.2012.08.046
CHEMBL2205814 83794 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 339 5 1 4 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmcl.2012.08.046
12575 1986 30 None -8 17 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cells
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1016/j.bmcl.2006.12.094
54459 1986 30 None -8 17 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cells
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1016/j.bmcl.2006.12.094
CHEMBL10316 1986 30 None -8 17 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cells
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1016/j.bmcl.2006.12.094
DB12551 1986 30 None -8 17 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cells
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1016/j.bmcl.2006.12.094
44438147 93487 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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 93487 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cells
ChEMBL 406 5 1 9 2.5 COc1cc2c(cc1OC)CN(Cc1cnc(N)n3nc(-c4ccco4)nc13)CC2 10.1016/j.bmcl.2006.12.094
44438152 93606 0 None 42 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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 93606 0 None 42 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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
10176999 103552 21 None -11 3 Human 7.7 pKi = 7.7 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 231 2 2 4 2.2 Cc1c(Nc2ncc[nH]2)ccc2c1OCCO2 10.1021/jm9605142
CHEMBL308570 103552 21 None -11 3 Human 7.7 pKi = 7.7 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 231 2 2 4 2.2 Cc1c(Nc2ncc[nH]2)ccc2c1OCCO2 10.1021/jm9605142
44402344 140957 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
ChEMBL 340 1 3 3 2.6 O=C(O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O 10.1016/j.bmcl.2005.03.116
CHEMBL382310 140957 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
ChEMBL 340 1 3 3 2.6 O=C(O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O 10.1016/j.bmcl.2005.03.116
10220053 206918 0 None -3 3 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 206918 0 None -3 3 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 206918 0 None -3 3 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptorInhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptor
ChEMBL 218 2 1 2 1.9 Fc1ccc2c(c1)CC(CC1CN=CN1)C2 10.1021/jm049619s
CHEMBL90997 206918 0 None -3 3 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptorInhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptor
ChEMBL 218 2 1 2 1.9 Fc1ccc2c(c1)CC(CC1CN=CN1)C2 10.1021/jm049619s
10758200 63415 0 None -5 5 Human 7.7 pKi = 7.7 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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 63415 0 None -5 5 Human 7.7 pKi = 7.7 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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
71151588 118256 0 None -1905 10 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO cellsDisplacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO cells
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409256 118256 0 None -1905 10 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO cellsDisplacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO cells
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
9895326 207025 0 None -177 6 Human 6.7 pKi = 6.7 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 207025 0 None -177 6 Human 6.7 pKi = 6.7 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
44288769 101146 0 None -1737 7 Human 5.7 pKi = 5.7 Binding
In vivo inhibitory effect against Alpha-2C adrenergic receptorIn vivo inhibitory effect against Alpha-2C 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 101146 0 None -1737 7 Human 5.7 pKi = 5.7 Binding
In vivo inhibitory effect against Alpha-2C adrenergic receptorIn vivo inhibitory effect against Alpha-2C 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
11301655 200 37 None -1258 4 Human 5.7 pKi = 5.7 Binding
Inhibition of alpha2C adrenergic receptor (unknown origin)Inhibition of alpha2C adrenergic receptor (unknown origin)
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.7b00151
8441 200 37 None -1258 4 Human 5.7 pKi = 5.7 Binding
Inhibition of alpha2C adrenergic receptor (unknown origin)Inhibition of alpha2C adrenergic receptor (unknown origin)
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.7b00151
CHEMBL127257 200 37 None -1258 4 Human 5.7 pKi = 5.7 Binding
Inhibition of alpha2C adrenergic receptor (unknown origin)Inhibition of alpha2C adrenergic receptor (unknown origin)
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.7b00151
44209472 70170 2 None -107 11 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation countingDisplacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation counting
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940420 70170 2 None -107 11 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation countingDisplacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation counting
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
3086326 204529 22 None -5 6 Human 6.7 pKi = 6.7 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 247 1 2 5 1.7 Clc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL72753 204529 22 None -5 6 Human 6.7 pKi = 6.7 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 247 1 2 5 1.7 Clc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
49781005 17212 0 None -3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17212 0 None -3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
10934575 204484 0 None -11 6 Human 6.7 pKi = 6.7 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 204484 0 None -11 6 Human 6.7 pKi = 6.7 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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
44352207 18854 1 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm800250z
CHEMBL128168 18854 1 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm800250z
44352207 18854 1 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
CHEMBL128168 18854 1 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
44352207 18854 1 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
CHEMBL128168 18854 1 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
44352207 18854 1 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm0408215
CHEMBL128168 18854 1 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm0408215
44288874 101093 0 None -1995 7 Human 5.7 pKi = 5.7 Binding
In vivo inhibitory effect against Alpha-2C adrenergic receptorIn vivo inhibitory effect against Alpha-2C 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 101093 0 None -1995 7 Human 5.7 pKi = 5.7 Binding
In vivo inhibitory effect against Alpha-2C adrenergic receptorIn vivo inhibitory effect against Alpha-2C 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
25142456 82404 2 None 3 9 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned adrenergic alpha 2C receptor receptorBinding affinity to human cloned adrenergic alpha 2C receptor receptor
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
CHEMBL217299 82404 2 None 3 9 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned adrenergic alpha 2C receptor receptorBinding affinity to human cloned adrenergic alpha 2C receptor receptor
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
44330679 208272 0 None 10 2 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 208272 0 None 10 2 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
9928332 97178 5 None -1 9 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 97178 5 None -1 9 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 97178 5 None -1 9 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptorInhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptor
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1021/jm049619s
CHEMBL268258 97178 5 None -1 9 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptorInhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptor
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1021/jm049619s
49781887 17142 0 None -5 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17142 0 None -5 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
11079 2731 63 None -2 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/j.bmc.2015.01.013
3369 2731 63 None -2 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/j.bmc.2015.01.013
4436 2731 63 None -2 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/j.bmc.2015.01.013
5509 2731 63 None -2 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/j.bmc.2015.01.013
CHEMBL761 2731 63 None -2 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/j.bmc.2015.01.013
DB06711 2731 63 None -2 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/j.bmc.2015.01.013
10045713 166103 0 None 309 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 386 3 1 4 5.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN4CCCCC4C3)cc2)c1C 10.1021/jm060262x
CHEMBL425983 166103 0 None 309 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 386 3 1 4 5.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN4CCCCC4C3)cc2)c1C 10.1021/jm060262x
44324887 165013 0 None -2 3 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 165013 0 None -2 3 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
102 4125 48 None -2 50 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 4125 48 None -2 50 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 4125 48 None -2 50 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 4125 48 None -2 50 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 4125 48 None -2 50 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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
10045713 166103 0 None 309 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 386 3 1 4 5.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN4CCCCC4C3)cc2)c1C 10.1016/j.ejmech.2010.12.026
CHEMBL425983 166103 0 None 309 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 386 3 1 4 5.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN4CCCCC4C3)cc2)c1C 10.1016/j.ejmech.2010.12.026
9805944 56225 37 None -3 9 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]HEAT from adrenergic Alpha-2C receptorDisplacement of [125I]HEAT from adrenergic Alpha-2C receptor
ChEMBL 462 7 2 3 4.7 CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm800510m
CHEMBL1627 56225 37 None -3 9 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]HEAT from adrenergic Alpha-2C receptorDisplacement of [125I]HEAT from adrenergic Alpha-2C receptor
ChEMBL 462 7 2 3 4.7 CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm800510m
73453 29614 24 None -3 17 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 29614 24 None -3 17 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
44579271 187092 0 None 22 3 Human 8.6 pKi = 8.6 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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 187092 0 None 22 3 Human 8.6 pKi = 8.6 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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
49781887 17142 0 None -5 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17142 0 None -5 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
44402345 71429 0 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
ChEMBL 496 5 4 5 3.5 CC(C)(C)OC(=O)NCCCNC(=O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O 10.1016/j.bmcl.2005.03.116
CHEMBL196064 71429 0 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
ChEMBL 496 5 4 5 3.5 CC(C)(C)OC(=O)NCCCNC(=O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O 10.1016/j.bmcl.2005.03.116
44330584 108117 0 None 1 2 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 108117 0 None 1 2 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
52943739 17157 0 None -6 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17157 0 None -6 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
135398737 957 93 None -3 91 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
38 957 93 None -3 91 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
722 957 93 None -3 91 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
CHEMBL42 957 93 None -3 91 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
DB00363 957 93 None -3 91 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
46225029 199331 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to Alpha2C adrenoceptor receptorBinding affinity to Alpha2C adrenoceptor receptor
ChEMBL 297 4 1 2 2.4 Fc1cccc(CCNC23OC4C5C6CC(C7C6C4C72)C53)c1 10.1016/j.bmcl.2009.11.019
CHEMBL590615 199331 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to Alpha2C adrenoceptor receptorBinding affinity to Alpha2C adrenoceptor receptor
ChEMBL 297 4 1 2 2.4 Fc1cccc(CCNC23OC4C5C6CC(C7C6C4C72)C53)c1 10.1016/j.bmcl.2009.11.019
16725934 147421 0 None 38 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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 147421 0 None 38 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cells
ChEMBL 429 6 0 5 5.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4)cc13)CC2 10.1016/j.bmcl.2006.12.094
123981 16457 22 None -4 8 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor
ChEMBL 195 0 0 1 2.4 CN1CCc2cccc(Cl)c2CC1 10.1021/jm00019a001
CHEMBL123349 16457 22 None -4 8 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor
ChEMBL 195 0 0 1 2.4 CN1CCc2cccc(Cl)c2CC1 10.1021/jm00019a001
CHEMBL536803 16457 22 None -4 8 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor
ChEMBL 195 0 0 1 2.4 CN1CCc2cccc(Cl)c2CC1 10.1021/jm00019a001
49781887 17142 0 None -5 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17142 0 None -5 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
118656529 120688 0 None 2 4 Human 6.7 pKi = 6.7 Binding
Binding affinity to human adrenergic alpha-2C receptor after 90 mins by radioligand displacement assayBinding affinity to human adrenergic alpha-2C receptor after 90 mins by radioligand displacement assay
ChEMBL 325 8 1 5 2.6 Fc1cccc(CCCNCCc2ccnc(-n3ccnc3)n2)c1 10.1021/jm501719e
CHEMBL3407810 120688 0 None 2 4 Human 6.7 pKi = 6.7 Binding
Binding affinity to human adrenergic alpha-2C receptor after 90 mins by radioligand displacement assayBinding affinity to human adrenergic alpha-2C receptor after 90 mins by radioligand displacement assay
ChEMBL 325 8 1 5 2.6 Fc1cccc(CCCNCCc2ccnc(-n3ccnc3)n2)c1 10.1021/jm501719e
CHEMBL3547107 120688 0 None 2 4 Human 6.7 pKi = 6.7 Binding
Binding affinity to human adrenergic alpha-2C receptor after 90 mins by radioligand displacement assayBinding affinity to human adrenergic alpha-2C receptor after 90 mins by radioligand displacement assay
ChEMBL 325 8 1 5 2.6 Fc1cccc(CCCNCCc2ccnc(-n3ccnc3)n2)c1 10.1021/jm501719e
44401041 70485 0 None -46 7 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 313 2 0 3 4.1 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL194659 70485 0 None -46 7 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 313 2 0 3 4.1 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
12574 2603 88 None -87 6 Human 5.7 pKi = 5.7 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1021/jm960012o
4810 2603 88 None -87 6 Human 5.7 pKi = 5.7 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1021/jm960012o
CHEMBL19236 2603 88 None -87 6 Human 5.7 pKi = 5.7 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1021/jm960012o
DB09242 2603 88 None -87 6 Human 5.7 pKi = 5.7 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1021/jm960012o
10032383 110108 0 None -194 6 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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 110108 0 None -194 6 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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 110108 0 None -194 6 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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
24906200 193154 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 328 5 1 3 4.5 c1ccc(-c2ccccc2OC(C2=NCCN2)c2ccccc2)cc1 10.1021/jm800250z
CHEMBL523048 193154 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 328 5 1 3 4.5 c1ccc(-c2ccccc2OC(C2=NCCN2)c2ccccc2)cc1 10.1021/jm800250z
9816063 103072 0 None -14 6 Human 6.7 pKi = 6.7 Binding
Binding affinity towards alpha-2C adrenergic receptorBinding affinity towards alpha-2C adrenergic receptor
ChEMBL 232 1 1 2 3.6 Cc1sc(C)c2c1CCCC2c1c[nH]cn1 10.1021/jm990569e
CHEMBL30739 103072 0 None -14 6 Human 6.7 pKi = 6.7 Binding
Binding affinity towards alpha-2C adrenergic receptorBinding affinity towards alpha-2C adrenergic receptor
ChEMBL 232 1 1 2 3.6 Cc1sc(C)c2c1CCCC2c1c[nH]cn1 10.1021/jm990569e
2398 953 62 None -4 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 953 62 None -4 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 953 62 None -4 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 953 62 None -4 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 953 62 None -4 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2105 3052 37 None -81 33 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 3052 37 None -81 33 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 3052 37 None -81 33 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 3052 37 None -81 33 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 3052 37 None -81 33 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
16090632 141714 0 None 46 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 141714 0 None 46 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 348 4 3 5 3.3 C[C@@H]1CN(c2ccc(Nc3c(CO)cnc4ccccc34)cc2)CCN1 10.1021/jm060262x
9816063 103072 0 None -14 6 Rat 6.7 pKi = 6.7 Binding
in vitro alpha-2C adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2C 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 103072 0 None -14 6 Rat 6.7 pKi = 6.7 Binding
in vitro alpha-2C adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2C 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
16090632 141714 0 None 46 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 348 4 3 5 3.3 C[C@@H]1CN(c2ccc(Nc3c(CO)cnc4ccccc34)cc2)CCN1 10.1016/j.ejmech.2010.12.026
CHEMBL385722 141714 0 None 46 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 348 4 3 5 3.3 C[C@@H]1CN(c2ccc(Nc3c(CO)cnc4ccccc34)cc2)CCN1 10.1016/j.ejmech.2010.12.026
15730 71116 80 None 1 10 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1 nan
CHEMBL195437 71116 80 None 1 10 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1 nan
53325861 56854 0 None 2 3 Human 5.7 pKi = 5.7 Binding
Inhibition of Alpha-2C adrenergic receptorInhibition of Alpha-2C adrenergic receptor
ChEMBL 297 4 0 1 3.4 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmcl.2010.11.075
CHEMBL1643902 56854 0 None 2 3 Human 5.7 pKi = 5.7 Binding
Inhibition of Alpha-2C adrenergic receptorInhibition of Alpha-2C adrenergic receptor
ChEMBL 297 4 0 1 3.4 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmcl.2010.11.075
53325861 56854 0 None 2 3 Human 5.7 pKi = 5.7 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 297 4 0 1 3.4 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
CHEMBL1643902 56854 0 None 2 3 Human 5.7 pKi = 5.7 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 297 4 0 1 3.4 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
126225 94974 5 None -9 7 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor
ChEMBL 263 1 0 2 4.2 C=Cc1sc2ccc(Cl)c3c2c1CN(C)CC3 10.1021/jm00019a001
CHEMBL25467 94974 5 None -9 7 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor
ChEMBL 263 1 0 2 4.2 C=Cc1sc2ccc(Cl)c3c2c1CN(C)CC3 10.1021/jm00019a001
3584 3775 64 None -50 14 Human 6.7 pKi = 6.7 Binding
The compound was tested for binding affinity against alpha-2C-adrenoceptor, from human clones.The compound was tested for binding affinity against alpha-2C-adrenoceptor, from human clones.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
5401 3775 64 None -50 14 Human 6.7 pKi = 6.7 Binding
The compound was tested for binding affinity against alpha-2C-adrenoceptor, from human clones.The compound was tested for binding affinity against alpha-2C-adrenoceptor, from human clones.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
7302 3775 64 None -50 14 Human 6.7 pKi = 6.7 Binding
The compound was tested for binding affinity against alpha-2C-adrenoceptor, from human clones.The compound was tested for binding affinity against alpha-2C-adrenoceptor, from human clones.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
CHEMBL611 3775 64 None -50 14 Human 6.7 pKi = 6.7 Binding
The compound was tested for binding affinity against alpha-2C-adrenoceptor, from human clones.The compound was tested for binding affinity against alpha-2C-adrenoceptor, from human clones.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
DB01162 3775 64 None -50 14 Human 6.7 pKi = 6.7 Binding
The compound was tested for binding affinity against alpha-2C-adrenoceptor, from human clones.The compound was tested for binding affinity against alpha-2C-adrenoceptor, from human clones.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
131829 204725 15 None -33 6 Human 6.7 pKi = 6.7 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 295 1 4 5 1.7 Brc1c(NC2=NCCN2)ccc2c1NCCN2 10.1016/0960-894X(95)00391-6
CHEMBL74283 204725 15 None -33 6 Human 6.7 pKi = 6.7 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 295 1 4 5 1.7 Brc1c(NC2=NCCN2)ccc2c1NCCN2 10.1016/0960-894X(95)00391-6
1548953 207677 27 None 1 17 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 207677 27 None 1 17 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
2683 102886 25 None -30 16 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 102886 25 None -30 16 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 102886 25 None -30 16 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
11097789 102996 1 None -43 6 Human 6.7 pKi = 6.7 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 102996 1 None -43 6 Human 6.7 pKi = 6.7 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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
11140345 204169 0 None -1 6 Human 6.7 pKi = 6.7 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 204169 0 None -1 6 Human 6.7 pKi = 6.7 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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
44401194 71293 0 None -28 7 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 313 2 0 3 4.1 CN(C)C[C@@H]1CC2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL195706 71293 0 None -28 7 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 313 2 0 3 4.1 CN(C)C[C@@H]1CC2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
1212 1660 50 None -54 66 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1660 50 None -54 66 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1660 50 None -54 66 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1660 50 None -54 66 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1660 50 None -54 66 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
448537 160248 89 None -21 25 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 160248 89 None -21 25 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
26987 948 33 None -107 21 Human 6.7 pKi = 6.7 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) 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 948 33 None -107 21 Human 6.7 pKi = 6.7 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) 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
671 948 33 None -107 21 Human 6.7 pKi = 6.7 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) 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 948 33 None -107 21 Human 6.7 pKi = 6.7 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) 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 948 33 None -107 21 Human 6.7 pKi = 6.7 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) 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
3584 3775 64 None -50 14 Human 6.7 pKi = 6.7 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980077m
5401 3775 64 None -50 14 Human 6.7 pKi = 6.7 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980077m
7302 3775 64 None -50 14 Human 6.7 pKi = 6.7 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980077m
CHEMBL611 3775 64 None -50 14 Human 6.7 pKi = 6.7 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980077m
DB01162 3775 64 None -50 14 Human 6.7 pKi = 6.7 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980077m
42669828 121716 2 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 243 5 1 3 2.7 Cc1ccccc1Cn1ccnc1CNC(C)C 10.1016/j.bmc.2015.01.013
CHEMBL3588911 121716 2 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 243 5 1 3 2.7 Cc1ccccc1Cn1ccnc1CNC(C)C 10.1016/j.bmc.2015.01.013
15853467 208132 0 None -67 6 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Alpha-2C adrenergic receptorBinding affinity against human Alpha-2C 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 208132 0 None -67 6 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Alpha-2C adrenergic receptorBinding affinity against human Alpha-2C 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
10326069 39294 1 None -125 9 Human 5.7 pKi = 5.7 Binding
Binding affinity for recombinant human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligand.Binding affinity for recombinant human Alpha-2C 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 39294 1 None -125 9 Human 5.7 pKi = 5.7 Binding
Binding affinity for recombinant human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligand.Binding affinity for recombinant human Alpha-2C 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
73349359 92541 0 None -3 8 Human 5.6 pKi = 5.6 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 341 6 1 4 2.9 COc1cc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432051 92541 0 None -3 8 Human 5.6 pKi = 5.6 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 341 6 1 4 2.9 COc1cc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC 10.1016/j.bmc.2013.07.045
44424855 85452 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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 85452 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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 163450 0 None -2 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 163450 0 None -2 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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
10324985 76779 8 None -17 17 Human 7.6 pKi = 7.6 Binding
Binding affinity to adrenergic alpha-2C receptorBinding affinity to adrenergic alpha-2C receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 76779 8 None -17 17 Human 7.6 pKi = 7.6 Binding
Binding affinity to adrenergic alpha-2C receptorBinding affinity to adrenergic alpha-2C receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 76779 8 None -17 17 Human 7.6 pKi = 7.6 Binding
Binding affinity to adrenergic alpha-2C receptorBinding affinity to adrenergic alpha-2C receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
9859437 168020 0 None -38 3 Human 6.6 pKi = 6.6 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 230 2 3 4 2.3 Cc1c(Nc2ncc[nH]2)ccc2c1NCCO2 10.1021/jm9605142
CHEMBL432155 168020 0 None -38 3 Human 6.6 pKi = 6.6 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 230 2 3 4 2.3 Cc1c(Nc2ncc[nH]2)ccc2c1NCCO2 10.1021/jm9605142
3303 2242 46 None -338 15 Human 6.6 pKi = 6.6 Binding
Inhibition of alpha2C adrenergic receptor (unknown origin)Inhibition of alpha2C adrenergic receptor (unknown origin)
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
5311200 2242 46 None -338 15 Human 6.6 pKi = 6.6 Binding
Inhibition of alpha2C adrenergic receptor (unknown origin)Inhibition of alpha2C adrenergic receptor (unknown origin)
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
CHEMBL267014 2242 46 None -338 15 Human 6.6 pKi = 6.6 Binding
Inhibition of alpha2C adrenergic receptor (unknown origin)Inhibition of alpha2C adrenergic receptor (unknown origin)
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
13149 2543 36 None -38 17 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C 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 2543 36 None -38 17 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C 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 2543 36 None -38 17 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C 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
196129 67796 17 None -295 15 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 67796 17 None -295 15 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
70693375 77669 0 None -5 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 244 5 1 3 2.4 C[C@@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL2089155 77669 0 None -5 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 244 5 1 3 2.4 C[C@@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
11361608 84743 1 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C 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 84743 1 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C 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 84743 1 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C 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 84743 1 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm100977d
11361608 84743 1 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C 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 84743 1 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm0408215
11300487 85000 0 None -5 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 280 4 1 3 3.4 Cc1ccccc1-c1ccccc1OC(C)C1=NCCN1 10.1021/jm0408215
CHEMBL223830 85000 0 None -5 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 280 4 1 3 3.4 Cc1ccccc1-c1ccccc1OC(C)C1=NCCN1 10.1021/jm0408215
70693375 77669 0 None -5 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human alpha2C adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2C 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 77669 0 None -5 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human alpha2C adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2C 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
286547 67239 112 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 191 1 1 3 1.0 CN1CCN(c2ccccc2N)CC1 10.1016/j.bmc.2015.01.013
CHEMBL1879790 67239 112 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 191 1 1 3 1.0 CN1CCN(c2ccccc2N)CC1 10.1016/j.bmc.2015.01.013
4209 3161 75 None -77 33 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
4893 3161 75 None -77 33 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
503 3161 75 None -77 33 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
5385 3161 75 None -77 33 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
CHEMBL2 3161 75 None -77 33 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
DB00457 3161 75 None -77 33 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
44314198 104410 0 None -8 4 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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 104410 0 None -8 4 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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 101467 0 None -8 3 Human 7.6 pKi = 7.6 Binding
Inhibitory constant determined using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant determined using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 210 3 1 3 2.3 CCC[C@H]1CCCC[C@@H]1NC1=NCCO1 10.1021/jm9905256
CHEMBL297752 101467 0 None -8 3 Human 7.6 pKi = 7.6 Binding
Inhibitory constant determined using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant determined using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 210 3 1 3 2.3 CCC[C@H]1CCCC[C@@H]1NC1=NCCO1 10.1021/jm9905256
10490084 204956 1 None -11 3 Human 5.6 pKi = 5.6 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 237 2 2 2 2.9 Brc1ccccc1Nc1ncc[nH]1 10.1021/jm9605142
CHEMBL76457 204956 1 None -11 3 Human 5.6 pKi = 5.6 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 237 2 2 2 2.9 Brc1ccccc1Nc1ncc[nH]1 10.1021/jm9605142
8447 188947 84 None -3 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 188947 84 None -3 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
10603951 206514 0 None -12 6 Human 6.6 pKi = 6.6 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 206514 0 None -12 6 Human 6.6 pKi = 6.6 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
10531532 207092 0 None -28 6 Human 6.6 pKi = 6.6 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 207092 0 None -28 6 Human 6.6 pKi = 6.6 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
24906243 187246 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 310 3 1 5 2.5 COC1(C2=NCCN2)COc2cccc(-c3ccccc3)c2O1 10.1021/jm800250z
CHEMBL492648 187246 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 310 3 1 5 2.5 COC1(C2=NCCN2)COc2cccc(-c3ccccc3)c2O1 10.1021/jm800250z
11277479 84748 0 None -4 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 280 4 1 3 3.4 Cc1cccc(-c2ccccc2OC(C)C2=NCCN2)c1 10.1021/jm0408215
CHEMBL222973 84748 0 None -4 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 280 4 1 3 3.4 Cc1cccc(-c2ccccc2OC(C)C2=NCCN2)c1 10.1021/jm0408215
132060733 162122 0 None -1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2C receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2C 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 162122 0 None -1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2C receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2C 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
71452341 83695 7 None 3 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]clonidine from alpha2C adrenergic receptor after 40 mins by scintillation counting analysisDisplacement of [3H]clonidine from alpha2C 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 83695 7 None 3 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]clonidine from alpha2C adrenergic receptor after 40 mins by scintillation counting analysisDisplacement of [3H]clonidine from alpha2C 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
10109188 166073 0 None 43 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 360 4 1 4 4.6 CCc1c(C)nc2ccccc2c1Nc1ccc(N2CCN(C)CC2)cc1 10.1016/j.ejmech.2010.12.026
CHEMBL425803 166073 0 None 43 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 360 4 1 4 4.6 CCc1c(C)nc2ccccc2c1Nc1ccc(N2CCN(C)CC2)cc1 10.1016/j.ejmech.2010.12.026
100 3803 58 None -27 55 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3803 58 None -27 55 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3803 58 None -27 55 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3803 58 None -27 55 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3803 58 None -27 55 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
10109188 166073 0 None 43 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 360 4 1 4 4.6 CCc1c(C)nc2ccccc2c1Nc1ccc(N2CCN(C)CC2)cc1 10.1021/jm060262x
CHEMBL425803 166073 0 None 43 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 360 4 1 4 4.6 CCc1c(C)nc2ccccc2c1Nc1ccc(N2CCN(C)CC2)cc1 10.1021/jm060262x
44371755 48775 0 None -21 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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 48775 0 None -21 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 218 3 1 3 2.1 Cc1cccc(C)c1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
11173544 166259 0 None -6 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 280 4 1 3 3.4 Cc1ccc(-c2ccccc2OC(C)C2=NCCN2)cc1 10.1021/jm0408215
CHEMBL426900 166259 0 None -6 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 280 4 1 3 3.4 Cc1ccc(-c2ccccc2OC(C)C2=NCCN2)cc1 10.1021/jm0408215
10221004 204229 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 204229 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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
73355420 92549 0 None 2 2 Human 5.6 pKi = 5.6 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 355 6 0 4 3.3 COc1cc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432061 92549 0 None 2 2 Human 5.6 pKi = 5.6 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 355 6 0 4 3.3 COc1cc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC 10.1016/j.bmc.2013.07.045
132060743 162234 0 None 1 13 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2C receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2C 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 162234 0 None 1 13 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2C receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2C 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
3168 9260 92 None -63 22 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 9260 92 None -63 22 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
DB00450 9260 92 None -63 22 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
11090351 163389 0 None 2 4 Human 6.6 pKi = 6.6 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL419448 163389 0 None 2 4 Human 6.6 pKi = 6.6 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
16757089 92289 1 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C 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 92289 1 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C 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 92289 1 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C 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 92289 1 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C 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
10220232 99719 6 None -1 6 Human 7.6 pKi = 7.6 Binding
Binding affinity towards alpha-2C adrenergic receptorBinding affinity towards alpha-2C adrenergic receptor
ChEMBL 230 1 1 2 3.5 Cc1sc(C)c2c1CCC=C2c1c[nH]cn1 10.1021/jm990569e
CHEMBL284795 99719 6 None -1 6 Human 7.6 pKi = 7.6 Binding
Binding affinity towards alpha-2C adrenergic receptorBinding affinity towards alpha-2C adrenergic receptor
ChEMBL 230 1 1 2 3.5 Cc1sc(C)c2c1CCC=C2c1c[nH]cn1 10.1021/jm990569e
135 2530 43 None -6 58 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2530 43 None -6 58 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2530 43 None -6 58 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2530 43 None -6 58 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2530 43 None -6 58 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
10219 188794 37 None -2 5 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 188794 37 None -2 5 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 188794 37 None -2 5 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
44401243 168492 0 None -10 9 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 329 2 0 3 4.6 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL435301 168492 0 None -10 9 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 329 2 0 3 4.6 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
10220232 99719 6 None -1 6 Rat 7.6 pKi = 7.6 Binding
in vitro alpha-2C adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2C 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 99719 6 None -1 6 Rat 7.6 pKi = 7.6 Binding
in vitro alpha-2C adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2C 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
24906199 187663 15 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 258 4 1 3 3.1 CC(Oc1ccccc1C1CCCC1)C1=NCCN1 10.1021/jm800250z
CHEMBL495096 187663 15 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 258 4 1 3 3.1 CC(Oc1ccccc1C1CCCC1)C1=NCCN1 10.1021/jm800250z
164615845 185188 0 None -2 6 Human 5.6 pKi = 5.6 Binding
Inhibition of alpha2c adrenergic receptor (unknown origin)Inhibition of alpha2c 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 185188 0 None -2 6 Human 5.6 pKi = 5.6 Binding
Inhibition of alpha2c adrenergic receptor (unknown origin)Inhibition of alpha2c 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
2162 41512 100 None -1 6 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl nan
CHEMBL1491 41512 100 None -1 6 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl nan
44269122 98107 2 None -9 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 190 3 1 3 1.5 CC(Oc1ccccc1)C1=NCCN1 10.1021/jm800250z
CHEMBL273485 98107 2 None -9 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 190 3 1 3 1.5 CC(Oc1ccccc1)C1=NCCN1 10.1021/jm800250z
45487144 197699 0 None -9 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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 197699 0 None -9 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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 98107 2 None -9 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 190 3 1 3 1.5 CC(Oc1ccccc1)C1=NCCN1 10.1021/jm100977d
CHEMBL273485 98107 2 None -9 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 190 3 1 3 1.5 CC(Oc1ccccc1)C1=NCCN1 10.1021/jm100977d
10903226 13768 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 281 6 2 5 1.3 CCCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1195368 13768 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 281 6 2 5 1.3 CCCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL554416 13768 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 281 6 2 5 1.3 CCCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
1353 1909 93 None -87 86 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1909 93 None -87 86 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1909 93 None -87 86 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1909 93 None -87 86 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1909 93 None -87 86 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
11000184 13050 0 None -6 6 Human 6.6 pKi = 6.6 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 13050 0 None -6 6 Human 6.6 pKi = 6.6 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 13050 0 None -6 6 Human 6.6 pKi = 6.6 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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
45487089 197638 0 None -10 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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 197638 0 None -10 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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
10923927 204176 0 None -4 4 Human 5.6 pKi = 5.6 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 204176 0 None -4 4 Human 5.6 pKi = 5.6 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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
3080926 155593 21 None -10 3 Human 4.6 pKi = 4.6 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 186 1 1 3 1.8 c1ccc2oc(C3=NCCN3)cc2c1 10.1021/ml400232p
CHEMBL404505 155593 21 None -10 3 Human 4.6 pKi = 4.6 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 186 1 1 3 1.8 c1ccc2oc(C3=NCCN3)cc2c1 10.1021/ml400232p
185076 187088 5 None -7 7 Human 7.6 pKi = 7.6 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1021/jm960359r
CHEMBL49137 187088 5 None -7 7 Human 7.6 pKi = 7.6 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1021/jm960359r
133 2494 52 None -26 43 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2494 52 None -26 43 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2494 52 None -26 43 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2494 52 None -26 43 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2494 52 None -26 43 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
185076 187088 5 None -7 7 Human 7.6 pKi = 7.6 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1021/jm9605142
CHEMBL49137 187088 5 None -7 7 Human 7.6 pKi = 7.6 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1021/jm9605142
3930 2149 43 None 53 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 10.1016/j.ejmech.2010.12.026
540335 2149 43 None 53 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 10.1016/j.ejmech.2010.12.026
CHEMBL106525 2149 43 None 53 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 10.1016/j.ejmech.2010.12.026
139406787 177143 0 None -2 4 Human 5.6 pKi = 5.6 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin)Binding affinity to adrenergic alpha2C 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 177143 0 None -2 4 Human 5.6 pKi = 5.6 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin)Binding affinity to adrenergic alpha2C 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
11057 176147 23 None -1 20 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 176147 23 None -1 20 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 176147 23 None -1 20 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 176147 23 None -1 20 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
57345628 71181 0 None -26 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 244 5 1 3 2.4 CC(Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL1956195 71181 0 None -26 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 244 5 1 3 2.4 CC(Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
70695474 77670 0 None -47 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 244 5 1 3 2.4 C[C@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL2089156 77670 0 None -47 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 244 5 1 3 2.4 C[C@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
122442272 138346 0 None -9 15 Human 6.6 pKi = 6.6 Binding
Binding affinity to human alpha-2C adrenergic receptor by radioligand binding assayBinding affinity to human alpha-2C 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 138346 0 None -9 15 Human 6.6 pKi = 6.6 Binding
Binding affinity to human alpha-2C adrenergic receptor by radioligand binding assayBinding affinity to human alpha-2C 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 138346 0 None -9 15 Human 6.6 pKi = 6.6 Binding
Binding affinity to human alpha-2C adrenergic receptor by radioligand binding assayBinding affinity to human alpha-2C adrenergic receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
44371864 51139 0 None -8 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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 51139 0 None -8 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 246 5 1 3 2.6 CCc1cccc(CC)c1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
57345628 71181 0 None -26 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 244 5 1 3 2.4 CC(Oc1ccccc1CC1CC1)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956195 71181 0 None -26 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 244 5 1 3 2.4 CC(Oc1ccccc1CC1CC1)C1=NCCN1 10.1016/j.bmc.2012.01.035
57345628 71181 0 None -26 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human alpha2C adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2C 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 71181 0 None -26 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human alpha2C adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2C 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
70695474 77670 0 None -47 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human alpha2C adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2C 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 77670 0 None -47 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human alpha2C adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2C 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
122442272 138346 0 None -9 15 Human 6.6 pKi = 6.6 Binding
Binding affinity to human alpha-2C adrenergic receptor by radioligand binding assayBinding affinity to human alpha-2C 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 138346 0 None -9 15 Human 6.6 pKi = 6.6 Binding
Binding affinity to human alpha-2C adrenergic receptor by radioligand binding assayBinding affinity to human alpha-2C 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 138346 0 None -9 15 Human 6.6 pKi = 6.6 Binding
Binding affinity to human alpha-2C adrenergic receptor by radioligand binding assayBinding affinity to human alpha-2C adrenergic receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
73346336 92543 0 None -5 6 Human 5.6 pKi = 5.6 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 325 5 0 2 3.0 CN(CCCc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432054 92543 0 None -5 6 Human 5.6 pKi = 5.6 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 325 5 0 2 3.0 CN(CCCc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
3930 2149 43 None 53 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 10.1021/jm060262x
540335 2149 43 None 53 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 10.1021/jm060262x
CHEMBL106525 2149 43 None 53 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 10.1021/jm060262x
518 3610 1 None -1 6 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor
ChEMBL 299 0 0 2 3.8 CN1CCc2c3c(C1)c(Br)oc3ccc2Cl 10.1021/jm00019a001
9839317 3610 1 None -1 6 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor
ChEMBL 299 0 0 2 3.8 CN1CCc2c3c(C1)c(Br)oc3ccc2Cl 10.1021/jm00019a001
CHEMBL123138 3610 1 None -1 6 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor
ChEMBL 299 0 0 2 3.8 CN1CCc2c3c(C1)c(Br)oc3ccc2Cl 10.1021/jm00019a001
1268096 16163 26 None 3 4 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 16163 26 None 3 4 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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
185076 187088 5 None -7 7 Human 7.6 pKi = 7.6 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL49137 187088 5 None -7 7 Human 7.6 pKi = 7.6 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
3157 1469 71 None -39 12 Human 6.6 pKi = 6.6 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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 1469 71 None -39 12 Human 6.6 pKi = 6.6 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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 1469 71 None -39 12 Human 6.6 pKi = 6.6 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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 1469 71 None -39 12 Human 6.6 pKi = 6.6 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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 1469 71 None -39 12 Human 6.6 pKi = 6.6 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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
10793963 99670 0 None -30 6 Human 6.6 pKi = 6.6 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 99670 0 None -30 6 Human 6.6 pKi = 6.6 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
57345626 71178 2 None -12 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 268 3 1 3 2.2 CC(Oc1ccccc1Br)C1=NCCN1 10.1021/ml400232p
CHEMBL1956192 71178 2 None -12 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 268 3 1 3 2.2 CC(Oc1ccccc1Br)C1=NCCN1 10.1021/ml400232p
57345626 71178 2 None -12 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 268 3 1 3 2.2 CC(Oc1ccccc1Br)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956192 71178 2 None -12 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 268 3 1 3 2.2 CC(Oc1ccccc1Br)C1=NCCN1 10.1016/j.bmc.2012.01.035
44312037 204617 1 None -2 6 Human 4.6 pKi = 4.6 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 308 1 1 5 2.9 Brc1c(NC2=NCCS2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL73392 204617 1 None -2 6 Human 4.6 pKi = 4.6 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 308 1 1 5 2.9 Brc1c(NC2=NCCS2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
213 3851 55 None -6 44 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2717 3851 55 None -6 44 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533 3851 55 None -6 44 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
CHEMBL621 3851 55 None -6 44 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
DB00656 3851 55 None -6 44 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2247 505 81 None -25 42 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 505 81 None -25 42 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 505 81 None -25 42 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 505 81 None -25 42 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 505 81 None -25 42 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2335 11846 22 None -2 12 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
8478 11846 22 None -2 12 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL1182210 11846 22 None -2 12 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL221753 11846 22 None -2 12 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
136680386 207701 0 None -60 6 Human 6.5 pKi = 6.5 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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 207701 0 None -60 6 Human 6.5 pKi = 6.5 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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 207701 0 None -60 6 Human 6.5 pKi = 6.5 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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
132060720 162487 0 None -7 9 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2C receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2C 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 162487 0 None -7 9 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2C receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2C 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
68712 100336 60 None -1 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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 100336 60 None -1 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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
44371745 49287 0 None -12 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 218 4 1 3 2.0 CCc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL156336 49287 0 None -12 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 218 4 1 3 2.0 CCc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
25130235 187585 1 None -8 11 Human 6.5 pKi = 6.5 Binding
Binding affinity to adrenergic Alpha-2C receptorBinding affinity to adrenergic Alpha-2C receptor
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494678 187585 1 None -8 11 Human 6.5 pKi = 6.5 Binding
Binding affinity to adrenergic Alpha-2C receptorBinding affinity to adrenergic Alpha-2C receptor
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
10682720 205160 0 None -7 3 Human 6.5 pKi = 6.5 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C 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 205160 0 None -7 3 Human 6.5 pKi = 6.5 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C 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
44579186 181974 0 None 2 3 Human 8.5 pKi = 8.5 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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 181974 0 None 2 3 Human 8.5 pKi = 8.5 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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
44402583 71412 0 None - 1 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
ChEMBL 425 5 4 4 2.5 O=C(O)CCCNC(=O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O 10.1016/j.bmcl.2005.03.116
CHEMBL195925 71412 0 None - 1 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
ChEMBL 425 5 4 4 2.5 O=C(O)CCCNC(=O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O 10.1016/j.bmcl.2005.03.116
44215744 207440 0 None 1 3 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 207440 0 None 1 3 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
2389 3329 118 None -10 67 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
5073 3329 118 None -10 67 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
96 3329 118 None -10 67 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
CHEMBL85 3329 118 None -10 67 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
DB00734 3329 118 None -10 67 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
44438168 93816 0 None 53 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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 93816 0 None 53 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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
11653915 124010 0 None 1 6 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human alpha-2C adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2C 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 124010 0 None 1 6 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human alpha-2C adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2C 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
16090630 83235 0 None 309 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 83235 0 None 309 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 390 4 2 5 4.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)(C)C3)cc2)c1CO 10.1021/jm060262x
135 2530 43 None -6 58 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
1796 2530 43 None -6 58 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
4184 2530 43 None -6 58 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
CHEMBL6437 2530 43 None -6 58 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
DB06148 2530 43 None -6 58 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
16090630 83235 0 None 309 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 390 4 2 5 4.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)(C)C3)cc2)c1CO 10.1016/j.ejmech.2010.12.026
CHEMBL218675 83235 0 None 309 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 390 4 2 5 4.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)(C)C3)cc2)c1CO 10.1016/j.ejmech.2010.12.026
2803 954 58 None -4 19 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960012o
516 954 58 None -4 19 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960012o
704 954 58 None -4 19 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960012o
CHEMBL134 954 58 None -4 19 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960012o
DB00575 954 58 None -4 19 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960012o
2216 446 50 None -3 6 Human 7.5 pKi = 7.5 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 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
229 446 50 None -3 6 Human 7.5 pKi = 7.5 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 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 446 50 None -3 6 Human 7.5 pKi = 7.5 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 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 446 50 None -3 6 Human 7.5 pKi = 7.5 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 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 446 50 None -3 6 Human 7.5 pKi = 7.5 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 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
2803 954 58 None -4 19 Human 7.5 pKi = 7.5 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960359r
516 954 58 None -4 19 Human 7.5 pKi = 7.5 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960359r
704 954 58 None -4 19 Human 7.5 pKi = 7.5 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960359r
CHEMBL134 954 58 None -4 19 Human 7.5 pKi = 7.5 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960359r
DB00575 954 58 None -4 19 Human 7.5 pKi = 7.5 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960359r
1971 2864 38 None -3 30 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 2864 38 None -3 30 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 2864 38 None -3 30 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 2864 38 None -3 30 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 2864 38 None -3 30 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
44325027 207072 0 None 1 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 207072 0 None 1 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
521 1403 69 None -30 7 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha-2c receptor expressed in CHO cells in presence of GppNHp/NaDisplacement of [3H]RX 821002 from human adrenergic alpha-2c receptor expressed in CHO cells in presence of GppNHp/Na
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm061487a
5311068 1403 69 None -30 7 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha-2c receptor expressed in CHO cells in presence of GppNHp/NaDisplacement of [3H]RX 821002 from human adrenergic alpha-2c receptor expressed in CHO cells in presence of GppNHp/Na
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm061487a
835 1403 69 None -30 7 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha-2c receptor expressed in CHO cells in presence of GppNHp/NaDisplacement of [3H]RX 821002 from human adrenergic alpha-2c receptor expressed in CHO cells in presence of GppNHp/Na
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm061487a
CHEMBL778 1403 69 None -30 7 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha-2c receptor expressed in CHO cells in presence of GppNHp/NaDisplacement of [3H]RX 821002 from human adrenergic alpha-2c receptor expressed in CHO cells in presence of GppNHp/Na
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm061487a
DB00633 1403 69 None -30 7 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha-2c receptor expressed in CHO cells in presence of GppNHp/NaDisplacement of [3H]RX 821002 from human adrenergic alpha-2c receptor expressed in CHO cells in presence of GppNHp/Na
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm061487a
9960497 100474 0 None -933 6 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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 100474 0 None -933 6 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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
9894818 98923 0 None -93 7 Human 6.5 pKi = 6.5 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 98923 0 None -93 7 Human 6.5 pKi = 6.5 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
10333157 151236 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 C[C@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
CHEMBL396013 151236 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 C[C@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
10333157 151236 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 C[C@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
CHEMBL396013 151236 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 C[C@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
11246610 84310 0 None -2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C 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 84310 0 None -2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1ccc([N+](=O)[O-])cc1)C1=NCCN1 10.1021/jm0408215
44209480 70168 0 None -281 11 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation countingDisplacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940418 70168 0 None -281 11 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation countingDisplacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
73353884 92320 0 None -2 8 Human 5.5 pKi = 5.5 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2 10.1016/j.bmc.2013.07.045
CHEMBL2429890 92320 0 None -2 8 Human 5.5 pKi = 5.5 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2 10.1016/j.bmc.2013.07.045
11173568 84639 0 None -8 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 281 4 2 4 2.7 CC(Oc1ccccc1-c1cccc(N)c1)C1=NCCN1 10.1021/jm0408215
CHEMBL222371 84639 0 None -8 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 281 4 2 4 2.7 CC(Oc1ccccc1-c1cccc(N)c1)C1=NCCN1 10.1021/jm0408215
24906160 169454 0 None -4 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 247 5 1 5 1.4 CO/N=C/c1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
CHEMBL442815 169454 0 None -4 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 247 5 1 5 1.4 CO/N=C/c1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
75306277 109252 0 None -15 23 Human 7.5 pKi = 7.5 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 109252 0 None -15 23 Human 7.5 pKi = 7.5 Binding
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
49836308 18782 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C 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 18782 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 C[C@@H](Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm100977d
44288945 168913 0 None -794 7 Human 6.5 pKi = 6.5 Binding
In vivo inhibitory effect against Alpha-2C adrenergic receptorIn vivo inhibitory effect against Alpha-2C 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 168913 0 None -794 7 Human 6.5 pKi = 6.5 Binding
In vivo inhibitory effect against Alpha-2C adrenergic receptorIn vivo inhibitory effect against Alpha-2C 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
49836306 18573 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 C[C@@H](Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
CHEMBL1276247 18573 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 C[C@@H](Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
12488 1655 56 None -2 23 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1655 56 None -2 23 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1655 56 None -2 23 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1655 56 None -2 23 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
44402352 71624 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
ChEMBL 396 4 4 4 1.9 NCCCNC(=O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O 10.1016/j.bmcl.2005.03.116
CHEMBL196344 71624 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
ChEMBL 396 4 4 4 1.9 NCCCNC(=O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O 10.1016/j.bmcl.2005.03.116
10266032 188879 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Inhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 286 5 1 3 3.5 c1ccc(CCC[C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
CHEMBL50720 188879 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Inhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 286 5 1 3 3.5 c1ccc(CCC[C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
10841387 99616 0 None -91 6 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 99616 0 None -91 6 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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
9894818 98923 0 None -93 7 Human 6.5 pKi = 6.5 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 98923 0 None -93 7 Human 6.5 pKi = 6.5 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
10841387 99616 0 None -91 6 Human 6.5 pKi = 6.5 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 99616 0 None -91 6 Human 6.5 pKi = 6.5 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
44390749 63908 0 None -173 6 Human 6.5 pKi = 6.5 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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 63908 0 None -173 6 Human 6.5 pKi = 6.5 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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
44579184 190951 4 None 2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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 190951 4 None 2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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
294234 102891 3 None -6 4 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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 102891 3 None -6 4 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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
487 3632 21 None -912 12 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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 3632 21 None -912 12 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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 3632 21 None -912 12 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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 3632 21 None -912 12 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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
11186227 84720 0 None -9 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1ccc(O)cc1)C1=NCCN1 10.1021/jm0408215
CHEMBL222798 84720 0 None -9 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1ccc(O)cc1)C1=NCCN1 10.1021/jm0408215
44582676 189777 0 None -2 17 Human 6.5 pKi = 6.5 Binding
Inhibition of human cloned Alpha-2C adrenergic receptor by competitive binding experimentInhibition of human cloned Alpha-2C 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 189777 0 None -2 17 Human 6.5 pKi = 6.5 Binding
Inhibition of human cloned Alpha-2C adrenergic receptor by competitive binding experimentInhibition of human cloned Alpha-2C 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
9884781 38672 1 None -1 5 Human 6.5 pKi = 6.5 Binding
Inhibition of alpha2C adrenergic receptor (unknown origin)Inhibition of alpha2C 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 38672 1 None -1 5 Human 6.5 pKi = 6.5 Binding
Inhibition of alpha2C adrenergic receptor (unknown origin)Inhibition of alpha2C 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
24906196 187244 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 261 6 1 5 1.8 CCO/N=C/c1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
CHEMBL492639 187244 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 261 6 1 5 1.8 CCO/N=C/c1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
CHEMBL4778870 214045 8 None -9 5 Human 5.5 pKi = 5.5 Binding
GPCRScan assay: inhibition of Alpha2CGPCRScan assay: inhibition of Alpha2C
ChEMBL None None None CC1CCN(c2ccnc(NCc3cn(C)cn3)n2)CC1 10.6019/CHEMBL4800732
10319299 81585 0 None 48 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 408 4 1 4 5.7 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1-c1ccccc1 10.1016/j.ejmech.2010.12.026
CHEMBL216290 81585 0 None 48 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 408 4 1 4 5.7 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1-c1ccccc1 10.1016/j.ejmech.2010.12.026
10132386 97096 2 None 63 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 346 3 1 4 4.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1C 10.1016/j.ejmech.2010.12.026
CHEMBL267464 97096 2 None 63 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 346 3 1 4 4.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1C 10.1016/j.ejmech.2010.12.026
16090621 141573 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 422 5 1 4 5.6 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1Cc1ccccc1 10.1016/j.ejmech.2010.12.026
CHEMBL384925 141573 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 422 5 1 4 5.6 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1Cc1ccccc1 10.1016/j.ejmech.2010.12.026
9794524 204841 2 None -10 3 Human 6.5 pKi = 6.5 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 225 2 2 4 2.4 Cc1c(Nc2ncc[nH]2)ccc2nccnc12 10.1021/jm9605142
CHEMBL75491 204841 2 None -10 3 Human 6.5 pKi = 6.5 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 225 2 2 4 2.4 Cc1c(Nc2ncc[nH]2)ccc2nccnc12 10.1021/jm9605142
CHEMBL4778870 214045 8 None -9 5 Human 5.5 pKi = 5.5 Binding
GPCRScan assay: inhibition of Alpha2CGPCRScan assay: inhibition of Alpha2C
ChEMBL None None None CC1CCN(c2ccnc(NCc3cn(C)cn3)n2)CC1 10.6019/CHEMBL4800732
28417 40037 49 None -1 12 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 40037 49 None -1 12 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
DB01406 40037 49 None -1 12 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
1267 3802 49 None -144 28 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C4 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 3802 49 None -144 28 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C4 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 3802 49 None -144 28 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm8003625
CHEMBL4798829 214051 7 None -6 2 Human 5.5 pKi = 5.5 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000752a ADRA2CSelectivity interaction (GPCR panel (PDSP screen)) EUB0000752a ADRA2C
ChEMBL None None None c1ccc2oc(-c3csc(C4CCN(Cc5nc6ncccc6[nH]5)CC4)n3)cc2c1 10.6019/CHEMBL5212743
10319299 81585 0 None 48 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 408 4 1 4 5.7 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1-c1ccccc1 10.1021/jm060262x
CHEMBL216290 81585 0 None 48 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 408 4 1 4 5.7 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1-c1ccccc1 10.1021/jm060262x
10132386 97096 2 None 63 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 346 3 1 4 4.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1C 10.1021/jm060262x
CHEMBL267464 97096 2 None 63 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 346 3 1 4 4.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1C 10.1021/jm060262x
16090621 141573 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 422 5 1 4 5.6 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1Cc1ccccc1 10.1021/jm060262x
CHEMBL384925 141573 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 422 5 1 4 5.6 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1Cc1ccccc1 10.1021/jm060262x
10946567 16467 0 None -28 6 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor
ChEMBL 265 1 0 2 4.1 CCc1sc2ccc(Cl)c3c2c1CN(C)CC3 10.1021/jm00019a001
CHEMBL123448 16467 0 None -28 6 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor
ChEMBL 265 1 0 2 4.1 CCc1sc2ccc(Cl)c3c2c1CN(C)CC3 10.1021/jm00019a001
155561439 175664 0 None -2 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expressed in MDCK cells by radioligand binding assayDisplacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expressed in MDCK cells by radioligand binding assay
ChEMBL 411 4 4 7 3.5 Oc1ccc(CCNc2nc(C#Cc3ccc(Cl)s3)nc3[nH]cnc23)cc1O 10.1039/C8MD00317C
CHEMBL4581568 175664 0 None -2 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expressed in MDCK cells by radioligand binding assayDisplacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expressed in MDCK cells by radioligand binding assay
ChEMBL 411 4 4 7 3.5 Oc1ccc(CCNc2nc(C#Cc3ccc(Cl)s3)nc3[nH]cnc23)cc1O 10.1039/C8MD00317C
2286 3181 51 None -15 30 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3181 51 None -15 30 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3181 51 None -15 30 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3181 51 None -15 30 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3181 51 None -15 30 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
44329026 208423 0 None -69 6 Human 6.5 pKi = 6.5 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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 208423 0 None -69 6 Human 6.5 pKi = 6.5 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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
1028 291 71 None -67 30 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
139148732 291 71 None -67 30 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
479 291 71 None -67 30 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
5816 291 71 None -67 30 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
CHEMBL679 291 71 None -67 30 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
DB00668 291 71 None -67 30 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
222757 99374 73 None 1 3 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O nan
CHEMBL282575 99374 73 None 1 3 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O nan
44325038 206914 0 None 3 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 206914 0 None 3 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
3072540 82413 13 None 32 3 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 382 4 1 4 5.3 CCN1CCN(c2ccc(Nc3c4ccccc4nc4ccccc34)cc2)CC1 10.1016/j.ejmech.2010.12.026
CHEMBL217366 82413 13 None 32 3 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 382 4 1 4 5.3 CCN1CCN(c2ccc(Nc3c4ccccc4nc4ccccc34)cc2)CC1 10.1016/j.ejmech.2010.12.026
16757089 92289 1 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha-2c receptor expressed in CHO cells in presence of GppNHp/NaDisplacement of [3H]RX 821002 from human adrenergic alpha-2c receptor expressed in CHO cells in presence of GppNHp/Na
ChEMBL 311 5 1 5 3.0 C[C@@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm061487a
CHEMBL242693 92289 1 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha-2c receptor expressed in CHO cells in presence of GppNHp/NaDisplacement of [3H]RX 821002 from human adrenergic alpha-2c receptor expressed in CHO cells in presence of GppNHp/Na
ChEMBL 311 5 1 5 3.0 C[C@@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm061487a
2284 3180 33 None -7 29 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3180 33 None -7 29 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3180 33 None -7 29 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3180 33 None -7 29 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3180 33 None -7 29 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
3072540 82413 13 None 32 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 382 4 1 4 5.3 CCN1CCN(c2ccc(Nc3c4ccccc4nc4ccccc34)cc2)CC1 10.1021/jm060262x
CHEMBL217366 82413 13 None 32 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 382 4 1 4 5.3 CCN1CCN(c2ccc(Nc3c4ccccc4nc4ccccc34)cc2)CC1 10.1021/jm060262x
242 470 124 None -23 52 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-clonidine from human alpha 2C receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-clonidine from human alpha 2C receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
34 470 124 None -23 52 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-clonidine from human alpha 2C receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-clonidine from human alpha 2C receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
60795 470 124 None -23 52 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-clonidine from human alpha 2C receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-clonidine from human alpha 2C receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
CHEMBL1112 470 124 None -23 52 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-clonidine from human alpha 2C receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-clonidine from human alpha 2C receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
DB01238 470 124 None -23 52 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-clonidine from human alpha 2C receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-clonidine from human alpha 2C receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
9809007 172562 8 None -724 6 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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 172562 8 None -724 6 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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
487 3632 21 None -912 12 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 3632 21 None -912 12 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 3632 21 None -912 12 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 3632 21 None -912 12 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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
4150 787 39 None -95 12 Human 5.4 pKi = 5.4 Binding
Inhibition of alpha2C receptor (unknown origin)Inhibition of alpha2C receptor (unknown origin)
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1021/acs.jmedchem.0c00724
5288 787 39 None -95 12 Human 5.4 pKi = 5.4 Binding
Inhibition of alpha2C receptor (unknown origin)Inhibition of alpha2C receptor (unknown origin)
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1021/acs.jmedchem.0c00724
644019 787 39 None -95 12 Human 5.4 pKi = 5.4 Binding
Inhibition of alpha2C receptor (unknown origin)Inhibition of alpha2C receptor (unknown origin)
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1021/acs.jmedchem.0c00724
CHEMBL190461 787 39 None -95 12 Human 5.4 pKi = 5.4 Binding
Inhibition of alpha2C receptor (unknown origin)Inhibition of alpha2C receptor (unknown origin)
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1021/acs.jmedchem.0c00724
DB09061 787 39 None -95 12 Human 5.4 pKi = 5.4 Binding
Inhibition of alpha2C receptor (unknown origin)Inhibition of alpha2C receptor (unknown origin)
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1021/acs.jmedchem.0c00724
9809007 172562 8 None -724 6 Human 6.4 pKi = 6.4 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 172562 8 None -724 6 Human 6.4 pKi = 6.4 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
9851486 206697 0 None -316 6 Human 6.4 pKi = 6.4 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 206697 0 None -316 6 Human 6.4 pKi = 6.4 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
73349362 92548 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 311 5 0 1 3.8 CN(CCCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
CHEMBL2432060 92548 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 311 5 0 1 3.8 CN(CCCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
16090633 80459 0 None 25 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 80459 0 None 25 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
16090633 80459 0 None 25 3 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 380 4 2 5 3.8 C[C@@H]1CN(c2ccc(Nc3c(CO)cnc4ccc(F)cc34)cc2)CCN1C 10.1016/j.ejmech.2010.12.026
CHEMBL214661 80459 0 None 25 3 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 380 4 2 5 3.8 C[C@@H]1CN(c2ccc(Nc3c(CO)cnc4ccc(F)cc34)cc2)CCN1C 10.1016/j.ejmech.2010.12.026
57400959 71186 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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 71186 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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
124 2979 47 None -60 32 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2979 47 None -60 32 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2979 47 None -60 32 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2979 47 None -60 32 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2979 47 None -60 32 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
10436842 100254 0 None -4786 7 Human 5.4 pKi = 5.4 Binding
In vivo inhibitory effect against Alpha-2C adrenergic receptorIn vivo inhibitory effect against Alpha-2C 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 100254 0 None -4786 7 Human 5.4 pKi = 5.4 Binding
In vivo inhibitory effect against Alpha-2C adrenergic receptorIn vivo inhibitory effect against Alpha-2C 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
16090597 141468 0 None 5 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 388 3 1 4 5.4 Cc1nc2c(C)ccc(C)c2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1016/j.ejmech.2010.12.026
CHEMBL384318 141468 0 None 5 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 388 3 1 4 5.4 Cc1nc2c(C)ccc(C)c2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1016/j.ejmech.2010.12.026
16090597 141468 0 None 5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 141468 0 None 5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
10508332 105989 0 None -269 6 Human 6.4 pKi = 6.4 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 105989 0 None -269 6 Human 6.4 pKi = 6.4 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
28918670 92485 2 None -4 4 Human 6.4 pKi = 6.4 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 254 3 1 3 1.8 Brc1ccccc1OCC1=NCCN1 10.1021/ml400232p
CHEMBL2431279 92485 2 None -4 4 Human 6.4 pKi = 6.4 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 254 3 1 3 1.8 Brc1ccccc1OCC1=NCCN1 10.1021/ml400232p
127036953 137513 0 None -39 22 Human 6.4 pKi = 6.4 Binding
Binding affinity to alpha-2C adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2C 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 137513 0 None -39 22 Human 6.4 pKi = 6.4 Binding
Binding affinity to alpha-2C adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2C 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 33551 0 None -4 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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 33551 0 None -4 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 248 5 1 4 2.2 CC(C)Oc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
73352415 92536 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 293 4 0 2 2.5 CN(CCc1ccccc1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432044 92536 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 293 4 0 2 2.5 CN(CCc1ccccc1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
10916464 204151 0 None -8 5 Human 5.4 pKi = 5.4 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 204151 0 None -8 5 Human 5.4 pKi = 5.4 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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
12576 514 94 None -2 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 514 94 None -2 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 514 94 None -2 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 514 94 None -2 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
44438166 93815 0 None 33 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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 93815 0 None 33 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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
46891598 7174 0 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]rauwolscine from adrenergic Alpha-2C receptorDisplacement of [3H]rauwolscine from adrenergic Alpha-2C 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 7174 0 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]rauwolscine from adrenergic Alpha-2C receptorDisplacement of [3H]rauwolscine from adrenergic Alpha-2C 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
44424855 85452 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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 85452 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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
44324859 111610 0 None 4 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 111610 0 None 4 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
44324765 111566 0 None 2 5 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 111566 0 None 2 5 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
16090631 82389 0 None 630 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 390 4 2 5 4.5 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C(C)O 10.1016/j.ejmech.2010.12.026
CHEMBL217253 82389 0 None 630 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 390 4 2 5 4.5 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C(C)O 10.1016/j.ejmech.2010.12.026
16090631 82389 0 None 630 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 82389 0 None 630 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
3191 102856 97 None -3 25 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102856 97 None -3 25 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
DB11742 102856 97 None -3 25 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
10655607 204753 5 None -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 199 2 3 3 2.0 c1c[nH]c(Nc2ccc3[nH]cnc3c2)n1 10.1021/jm9605142
CHEMBL74544 204753 5 None -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 199 2 3 3 2.0 c1c[nH]c(Nc2ccc3[nH]cnc3c2)n1 10.1021/jm9605142
12304323 9046 5 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to adrenergic alpha2c receptorBinding affinity to adrenergic alpha2c receptor
ChEMBL 464 4 8 12 -0.5 O=c1c(O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/np1000329
CHEMBL1098724 9046 5 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to adrenergic alpha2c receptorBinding affinity to adrenergic alpha2c receptor
ChEMBL 464 4 8 12 -0.5 O=c1c(O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/np1000329
10507651 206505 0 None -45 6 Human 6.4 pKi = 6.4 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 206505 0 None -45 6 Human 6.4 pKi = 6.4 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
10382537 204164 12 None -60 6 Human 6.4 pKi = 6.4 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 339 1 2 5 1.6 Ic1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL70676 204164 12 None -60 6 Human 6.4 pKi = 6.4 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 339 1 2 5 1.6 Ic1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL4748908 214033 1 None -4 12 Human 6.4 pKi = 6.4 Binding
GPCRScan assay: inhibition of Alpha2CGPCRScan assay: inhibition of Alpha2C
ChEMBL None None None CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1 10.6019/CHEMBL4800732
2353 101110 82 None -1 5 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL12089 101110 82 None -1 5 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL295124 101110 82 None -1 5 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL4748908 214033 1 None -4 12 Human 6.4 pKi = 6.4 Binding
GPCRScan assay: inhibition of Alpha2CGPCRScan assay: inhibition of Alpha2C
ChEMBL None None None CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1 10.6019/CHEMBL4800732
10627021 107093 0 None -301 6 Human 6.4 pKi = 6.4 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 107093 0 None -301 6 Human 6.4 pKi = 6.4 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
10317643 98538 0 None 32 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 380 4 2 5 3.8 CC1CN(c2ccc(Nc3c(CO)cnc4ccc(F)cc34)cc2)CCN1C 10.1016/j.ejmech.2010.12.026
CHEMBL276417 98538 0 None 32 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 380 4 2 5 3.8 CC1CN(c2ccc(Nc3c(CO)cnc4ccc(F)cc34)cc2)CCN1C 10.1016/j.ejmech.2010.12.026
10818003 106419 0 None -7 6 Human 6.4 pKi = 6.4 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 106419 0 None -7 6 Human 6.4 pKi = 6.4 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
66561967 74702 0 None -6 7 Human 5.4 pKi = 5.4 Binding
Inhibition of alpha2C adrenergic receptorInhibition of alpha2C adrenergic receptor
ChEMBL 213 2 0 1 2.0 C1CC2CCC1N2CC12C3C4C5C3C1C5C42 10.1016/j.bmcl.2012.04.077
CHEMBL2030626 74702 0 None -6 7 Human 5.4 pKi = 5.4 Binding
Inhibition of alpha2C adrenergic receptorInhibition of alpha2C adrenergic receptor
ChEMBL 213 2 0 1 2.0 C1CC2CCC1N2CC12C3C4C5C3C1C5C42 10.1016/j.bmcl.2012.04.077
44421258 84744 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 264 3 1 3 2.8 c1ccc(-c2ccccc2C2OC2C2=NCCN2)cc1 10.1021/jm0408215
CHEMBL1204386 84744 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 264 3 1 3 2.8 c1ccc(-c2ccccc2C2OC2C2=NCCN2)cc1 10.1021/jm0408215
CHEMBL222933 84744 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 264 3 1 3 2.8 c1ccc(-c2ccccc2C2OC2C2=NCCN2)cc1 10.1021/jm0408215
127035062 136449 0 None -14 19 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha 2C receptor stably expressed in MDCK cells after 90 mins by scintillation counting methodDisplacement of [3H]Rauwolscine from human recombinant alpha 2C 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 136449 0 None -14 19 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha 2C receptor stably expressed in MDCK cells after 90 mins by scintillation counting methodDisplacement of [3H]Rauwolscine from human recombinant alpha 2C 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
10317643 98538 0 None 32 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 380 4 2 5 3.8 CC1CN(c2ccc(Nc3c(CO)cnc4ccc(F)cc34)cc2)CCN1C 10.1021/jm060262x
CHEMBL276417 98538 0 None 32 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 380 4 2 5 3.8 CC1CN(c2ccc(Nc3c(CO)cnc4ccc(F)cc34)cc2)CCN1C 10.1021/jm060262x
155770281 177745 0 None -5 9 Human 5.4 pKi = 5.4 Binding
Binding affinity to alpha2c (unknown origin)Binding affinity to alpha2c (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4642592 177745 0 None -5 9 Human 5.4 pKi = 5.4 Binding
Binding affinity to alpha2c (unknown origin)Binding affinity to alpha2c (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
122186880 122978 0 None -4 5 Human 6.4 pKi = 6.4 Binding
Binding affinity to alpha2C adrenoceptor (unknown origin)Binding affinity to alpha2C 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 122978 0 None -4 5 Human 6.4 pKi = 6.4 Binding
Binding affinity to alpha2C adrenoceptor (unknown origin)Binding affinity to alpha2C adrenoceptor (unknown origin)
ChEMBL 415 3 0 5 4.8 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
71463061 83793 0 None -5 9 Human 5.4 pKi = 5.4 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 339 5 1 4 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1OC 10.1016/j.bmcl.2012.08.046
CHEMBL2205813 83793 0 None -5 9 Human 5.4 pKi = 5.4 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 339 5 1 4 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1OC 10.1016/j.bmcl.2012.08.046
2435 721 100 None -33 12 Human 7.4 pKi = 7.4 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
395 721 100 None -33 12 Human 7.4 pKi = 7.4 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
520 721 100 None -33 12 Human 7.4 pKi = 7.4 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
5386 721 100 None -33 12 Human 7.4 pKi = 7.4 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
CHEMBL844 721 100 None -33 12 Human 7.4 pKi = 7.4 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
DB00484 721 100 None -33 12 Human 7.4 pKi = 7.4 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
44328654 107183 0 None -114 6 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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 107183 0 None -114 6 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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
4011 82406 49 None -28 24 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 82406 49 None -28 24 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
33630 178955 99 None -9 28 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expressed in MDCK cells by radioligand binding assayDisplacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expressed in MDCK cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL47050 178955 99 None -9 28 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expressed in MDCK cells by radioligand binding assayDisplacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expressed in MDCK cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
73213196 104458 4 None -4 13 Human 6.4 pKi = 6.4 Binding
Binding affinity to adrenergic alpha 2C receptor (unknown origin)Binding affinity to adrenergic alpha 2C receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2014.05.016
CHEMBL3104093 104458 4 None -4 13 Human 6.4 pKi = 6.4 Binding
Binding affinity to adrenergic alpha 2C receptor (unknown origin)Binding affinity to adrenergic alpha 2C receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2014.05.016
73213196 104458 4 None -4 13 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 104458 4 None -4 13 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
73213196 104458 4 None -4 13 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 104458 4 None -4 13 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
57401706 70169 0 None -7 11 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation countingDisplacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation counting
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940419 70169 0 None -7 11 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation countingDisplacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation counting
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
463 1404 22 None -48 13 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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 1404 22 None -48 13 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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 1404 22 None -48 13 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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 1404 22 None -48 13 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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 1404 22 None -48 13 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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
6918276 15609 7 None -47 8 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 15609 7 None -47 8 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
44269089 97003 0 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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 97003 0 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 232 4 1 3 2.6 CC(Oc1ccccc1C(C)C)C1=NCCN1 10.1016/j.bmc.2012.01.035
9809007 172562 8 None -724 6 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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 172562 8 None -724 6 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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
191 403 98 None -39 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 403 98 None -39 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 403 98 None -39 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 403 98 None -39 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 403 98 None -39 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
60838 183872 99 None -1 2 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC nan
CHEMBL481 183872 99 None -1 2 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC nan
44288847 165307 0 None -3311 5 Human 5.3 pKi = 5.3 Binding
In vivo inhibitory effect against Alpha-2C adrenergic receptorIn vivo inhibitory effect against Alpha-2C 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 165307 0 None -3311 5 Human 5.3 pKi = 5.3 Binding
In vivo inhibitory effect against Alpha-2C adrenergic receptorIn vivo inhibitory effect against Alpha-2C 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
10769331 111531 0 None -91 6 Human 7.3 pKi = 7.3 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 111531 0 None -91 6 Human 7.3 pKi = 7.3 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
135453290 133604 33 None -1548 8 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]clonidine from cloned human adrenergic Alpha-2C receptor expressed in Sf9 cellsDisplacement of [3H]clonidine from cloned human adrenergic Alpha-2C receptor expressed in Sf9 cells
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL371300 133604 33 None -1548 8 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]clonidine from cloned human adrenergic Alpha-2C receptor expressed in Sf9 cellsDisplacement of [3H]clonidine from cloned human adrenergic Alpha-2C receptor expressed in Sf9 cells
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
136680384 207653 0 None -104 6 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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 207653 0 None -104 6 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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 207653 0 None -104 6 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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
71461344 83804 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 266 2 1 3 1.3 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1cccnc1 10.1016/j.bmc.2013.07.045
CHEMBL2205833 83804 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 266 2 1 3 1.3 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1cccnc1 10.1016/j.bmc.2013.07.045
73347827 92542 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 311 4 0 2 2.6 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432052 92542 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 311 4 0 2 2.6 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
1443 2026 34 None -11 11 Human 6.3 pKi = 6.3 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
33625 2026 34 None -11 11 Human 6.3 pKi = 6.3 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
501 2026 34 None -11 11 Human 6.3 pKi = 6.3 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
CHEMBL279516 2026 34 None -11 11 Human 6.3 pKi = 6.3 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
DB08950 2026 34 None -11 11 Human 6.3 pKi = 6.3 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
10474335 194690 23 None -16 10 Human 6.3 pKi = 6.3 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 370 6 0 3 4.8 COc1cccc2c1CCCC2CCCN1CCN(C2CCCCC2)CC1 10.1038/s41586-020-2286-9
CHEMBL53325 194690 23 None -16 10 Human 6.3 pKi = 6.3 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 370 6 0 3 4.8 COc1cccc2c1CCCC2CCCN1CCN(C2CCCCC2)CC1 10.1038/s41586-020-2286-9
10626982 111493 0 None -8 6 Human 6.3 pKi = 6.3 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 111493 0 None -8 6 Human 6.3 pKi = 6.3 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
9947861 204160 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70634 204160 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
44269013 30340 1 None -10 4 Human 6.3 pKi = 6.3 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 218 5 1 3 2.0 CCCc1ccccc1OCC1=NCCN1 10.1021/ml400232p
CHEMBL13917 30340 1 None -10 4 Human 6.3 pKi = 6.3 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 218 5 1 3 2.0 CCCc1ccccc1OCC1=NCCN1 10.1021/ml400232p
57345625 71177 0 None -16 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 224 3 1 3 2.1 CC(Oc1ccccc1Cl)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956191 71177 0 None -16 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 224 3 1 3 2.1 CC(Oc1ccccc1Cl)C1=NCCN1 10.1016/j.bmc.2012.01.035
45487962 197483 0 None -10 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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 197483 0 None -10 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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
44312198 204587 0 None -1 4 Human 4.3 pKi = 4.3 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 292 1 1 5 2.2 Brc1c(NC2=NCCO2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL73164 204587 0 None -1 4 Human 4.3 pKi = 4.3 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 292 1 1 5 2.2 Brc1c(NC2=NCCO2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
44579185 181812 1 None 7 3 Human 8.3 pKi = 8.3 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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 181812 1 None 7 3 Human 8.3 pKi = 8.3 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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
10362866 82297 0 None 114 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 388 3 1 4 5.4 Cc1ccc2c(Nc3ccc(N4CCN(C)C(C)C4)cc3)c(C)c(C)nc2c1C 10.1016/j.ejmech.2010.12.026
CHEMBL217203 82297 0 None 114 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 388 3 1 4 5.4 Cc1ccc2c(Nc3ccc(N4CCN(C)C(C)C4)cc3)c(C)c(C)nc2c1C 10.1016/j.ejmech.2010.12.026
10070896 83194 0 None 281 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 422 4 1 4 6.1 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1-c1ccccc1 10.1016/j.ejmech.2010.12.026
CHEMBL218457 83194 0 None 281 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 422 4 1 4 6.1 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1-c1ccccc1 10.1016/j.ejmech.2010.12.026
10362866 82297 0 None 114 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 82297 0 None 114 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
10070896 83194 0 None 281 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 83194 0 None 281 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 422 4 1 4 6.1 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1-c1ccccc1 10.1021/jm060262x
441975 16449 56 None 1 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 16449 56 None 1 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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
124 2979 47 None -60 32 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C 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 2979 47 None -60 32 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C 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 2979 47 None -60 32 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C 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 2979 47 None -60 32 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C 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 2979 47 None -60 32 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C 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 4125 48 None -2 50 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 4125 48 None -2 50 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 4125 48 None -2 50 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 4125 48 None -2 50 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 4125 48 None -2 50 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
44402531 69610 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
ChEMBL 468 5 4 6 0.9 COC(=O)CNC(=O)CNC(=O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O 10.1016/j.bmcl.2005.03.116
CHEMBL193458 69610 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
ChEMBL 468 5 4 6 0.9 COC(=O)CNC(=O)CNC(=O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O 10.1016/j.bmcl.2005.03.116
44325075 111763 0 None 2 2 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 111763 0 None 2 2 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
10473701 83236 0 None 165 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 360 3 1 4 4.8 Cc1cnc2ccccc2c1Nc1ccc(N2CCN(C)C(C)(C)C2)cc1 10.1016/j.ejmech.2010.12.026
CHEMBL218679 83236 0 None 165 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 360 3 1 4 4.8 Cc1cnc2ccccc2c1Nc1ccc(N2CCN(C)C(C)(C)C2)cc1 10.1016/j.ejmech.2010.12.026
10473701 83236 0 None 165 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 360 3 1 4 4.8 Cc1cnc2ccccc2c1Nc1ccc(N2CCN(C)C(C)(C)C2)cc1 10.1021/jm060262x
CHEMBL218679 83236 0 None 165 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 360 3 1 4 4.8 Cc1cnc2ccccc2c1Nc1ccc(N2CCN(C)C(C)(C)C2)cc1 10.1021/jm060262x
134551 358 27 None -5 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
271 358 27 None -5 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
885 358 27 None -5 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 358 27 None -5 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
49781005 17212 0 None -3 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17212 0 None -3 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
10251036 81883 0 None 70 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 81883 0 None 70 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
10251036 81883 0 None 70 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 410 4 2 5 4.7 CN1CCN(c2ccc(Nc3c(CO)cnc4cc(Cl)ccc34)cc2)CC1(C)C 10.1016/j.ejmech.2010.12.026
CHEMBL216464 81883 0 None 70 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 410 4 2 5 4.7 CN1CCN(c2ccc(Nc3c(CO)cnc4cc(Cl)ccc34)cc2)CC1(C)C 10.1016/j.ejmech.2010.12.026
10475736 165861 0 None 26 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 394 4 2 5 4.1 CN1CCN(c2ccc(Nc3c(CO)cnc4ccc(F)cc34)cc2)CC1(C)C 10.1016/j.ejmech.2010.12.026
CHEMBL424917 165861 0 None 26 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 394 4 2 5 4.1 CN1CCN(c2ccc(Nc3c(CO)cnc4ccc(F)cc34)cc2)CC1(C)C 10.1016/j.ejmech.2010.12.026
10475736 165861 0 None 26 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 165861 0 None 26 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
657255 199082 34 None -8 15 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 199082 34 None -8 15 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
16090599 81543 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 360 3 1 4 5.0 Cc1nc2c(C)cccc2c(Nc2ccc(N3CCCN(C)C3)cc2)c1C 10.1016/j.ejmech.2010.12.026
CHEMBL216072 81543 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 360 3 1 4 5.0 Cc1nc2c(C)cccc2c(Nc2ccc(N3CCCN(C)C3)cc2)c1C 10.1016/j.ejmech.2010.12.026
50878551 90743 61 None -22 18 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Clonidine from human recombinant adrenergic alpha2C receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Clonidine from human recombinant adrenergic alpha2C receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90743 61 None -22 18 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Clonidine from human recombinant adrenergic alpha2C receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Clonidine from human recombinant adrenergic alpha2C receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
45487958 198389 0 None -14 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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 198389 0 None -14 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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
7059292 76298 7 None -5 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2C 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 76298 7 None -5 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2C 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
73346332 92533 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 297 3 0 2 2.6 CN(Cc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432041 92533 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 297 3 0 2 2.6 CN(Cc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
50878551 90743 61 None -22 18 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Clonidine from human recombinant adrenergic alpha2C receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Clonidine from human recombinant adrenergic alpha2C receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90743 61 None -22 18 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Clonidine from human recombinant adrenergic alpha2C receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Clonidine from human recombinant adrenergic alpha2C receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
10198135 205123 3 None -51 3 Human 6.3 pKi = 6.3 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 203 3 2 3 2.5 COc1ccc(Nc2ncc[nH]2)c(C)c1 10.1021/jm9605142
CHEMBL77913 205123 3 None -51 3 Human 6.3 pKi = 6.3 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 203 3 2 3 2.5 COc1ccc(Nc2ncc[nH]2)c(C)c1 10.1021/jm9605142
44329027 4166 0 None -26 6 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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 4166 0 None -26 6 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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
10177445 166040 0 None 32 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 374 4 1 4 5.2 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1C(C)C 10.1016/j.ejmech.2010.12.026
CHEMBL425622 166040 0 None 32 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 374 4 1 4 5.2 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1C(C)C 10.1016/j.ejmech.2010.12.026
10177445 166040 0 None 32 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 374 4 1 4 5.2 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1C(C)C 10.1021/jm060262x
CHEMBL425622 166040 0 None 32 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 374 4 1 4 5.2 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1C(C)C 10.1021/jm060262x
44292381 101392 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Inhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 244 2 1 3 2.7 c1ccc([C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
CHEMBL297228 101392 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Inhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 244 2 1 3 2.7 c1ccc([C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
46743607 121710 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 264 5 2 3 2.8 c1ccc(-c2nc(CNCc3cccnc3)c[nH]2)cc1 10.1016/j.bmc.2015.01.013
CHEMBL3588905 121710 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 264 5 2 3 2.8 c1ccc(-c2nc(CNCc3cccnc3)c[nH]2)cc1 10.1016/j.bmc.2015.01.013
71450550 83805 0 None -1 16 Human 6.3 pKi = 6.3 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205836 83805 0 None -1 16 Human 6.3 pKi = 6.3 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
8032110 121708 14 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 198 3 1 2 3.0 Cc1ccccc1NCc1ccncc1 10.1016/j.bmc.2015.01.013
CHEMBL3588903 121708 14 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 198 3 1 2 3.0 Cc1ccccc1NCc1ccncc1 10.1016/j.bmc.2015.01.013
16757182 153249 0 None -7 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C 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 153249 0 None -7 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C 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 153249 0 None -7 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C 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 153249 0 None -7 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C 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
2726 918 68 None -31 73 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 918 68 None -31 73 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 918 68 None -31 73 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 918 68 None -31 73 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 918 68 None -31 73 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
2600 3777 74 None -4 13 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 3777 74 None -4 13 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 3777 74 None -4 13 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 3777 74 None -4 13 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 3777 74 None -4 13 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2765 942 19 None -15 9 Human 6.3 pKi = 6.3 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/ml400232p
515 942 19 None -15 9 Human 6.3 pKi = 6.3 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/ml400232p
CHEMBL13852 942 19 None -15 9 Human 6.3 pKi = 6.3 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/ml400232p
DB09202 942 19 None -15 9 Human 6.3 pKi = 6.3 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/ml400232p
2765 942 19 None -15 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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
515 942 19 None -15 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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 942 19 None -15 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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 942 19 None -15 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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
49783209 17607 0 None -977 27 Human 6.3 pKi = 6.3 Binding
Binding affinity to human adrenergic Alpha-2C receptorBinding affinity to human adrenergic Alpha-2C receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 17607 0 None -977 27 Human 6.3 pKi = 6.3 Binding
Binding affinity to human adrenergic Alpha-2C receptorBinding affinity to human adrenergic Alpha-2C receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
71459604 83791 0 None 1 14 Human 6.3 pKi = 6.3 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL2205811 83791 0 None 1 14 Human 6.3 pKi = 6.3 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
2803 954 58 None -4 19 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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
516 954 58 None -4 19 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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
704 954 58 None -4 19 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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 954 58 None -4 19 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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 954 58 None -4 19 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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
237 204863 48 None -1 13 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL546257 204863 48 None -1 13 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL554190 204863 48 None -1 13 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL7568 204863 48 None -1 13 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
101333429 117074 0 None -1412 6 Human 6.3 pKi = 6.3 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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 117074 0 None -1412 6 Human 6.3 pKi = 6.3 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C 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
11564613 19411 108 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 191 1 1 3 1.0 CN1CCN(c2cccc(N)c2)CC1 10.1016/j.bmc.2015.01.013
CHEMBL129399 19411 108 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 191 1 1 3 1.0 CN1CCN(c2cccc(N)c2)CC1 10.1016/j.bmc.2015.01.013
CHEMBL1200633 208598 3 None -1 8 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
1201549 596 24 None -18 20 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 596 24 None -18 20 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 596 24 None -18 20 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 596 24 None -18 20 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 596 24 None -18 20 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 596 24 None -18 20 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
10531766 206995 0 None -512 6 Human 6.2 pKi = 6.2 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 206995 0 None -512 6 Human 6.2 pKi = 6.2 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
12699315 76296 0 None -4 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2C 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 76296 0 None -4 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2C 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
CHEMBL4513786 213965 7 None -1047 8 Human 5.2 pKi = 5.2 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl ADRA2CSelectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl ADRA2C
ChEMBL None None None CCCCN(CCCC)C(=O)CN1C[C@@H](c2cc(OC)c3c(c2)OCO3)[C@H](C(=O)O)[C@H]1CC(C)(C)CCC 10.6019/CHEMBL5212743
CHEMBL4796803 213965 7 None -1047 8 Human 5.2 pKi = 5.2 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl ADRA2CSelectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl ADRA2C
ChEMBL None None None CCCCN(CCCC)C(=O)CN1C[C@@H](c2cc(OC)c3c(c2)OCO3)[C@H](C(=O)O)[C@H]1CC(C)(C)CCC 10.6019/CHEMBL5212743
124 2979 47 None -60 32 Human 7.2 pKi = 7.2 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 2979 47 None -60 32 Human 7.2 pKi = 7.2 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 2979 47 None -60 32 Human 7.2 pKi = 7.2 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 2979 47 None -60 32 Human 7.2 pKi = 7.2 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 2979 47 None -60 32 Human 7.2 pKi = 7.2 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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
3561 19075 39 None -2 11 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
CHEMBL1289 19075 39 None -2 11 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
11448533 84689 0 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 267 4 0 3 3.6 CC(Oc1ccccc1-c1ccccc1)C1=NCCO1 10.1021/jm0408215
CHEMBL222591 84689 0 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 267 4 0 3 3.6 CC(Oc1ccccc1-c1ccccc1)C1=NCCO1 10.1021/jm0408215
11473729 84690 0 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 265 4 0 2 4.4 CC(Oc1ccccc1-c1ccccc1)C1=NCCC1 10.1021/jm0408215
CHEMBL222593 84690 0 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 265 4 0 2 4.4 CC(Oc1ccccc1-c1ccccc1)C1=NCCC1 10.1021/jm0408215
44401164 69814 0 None -309 9 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL193639 69814 0 None -309 9 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
49783419 17747 0 None -1778 13 Human 6.2 pKi = 6.2 Binding
Binding affinity to human adrenergic Alpha-2C receptorBinding affinity to human adrenergic Alpha-2C receptor
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258671 17747 0 None -1778 13 Human 6.2 pKi = 6.2 Binding
Binding affinity to human adrenergic Alpha-2C receptorBinding affinity to human adrenergic Alpha-2C receptor
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
24771824 57341 57 None 1 2 Human 6.2 pKi = 6.2 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000306b ADRA2CSelectivity interaction (GPCR panel (PDSP screen)) EUB0000306b ADRA2C
ChEMBL 455 4 1 5 5.4 O=C(Nc1cccnn1)N1CCC(=Cc2cccc(Oc3ccc(C(F)(F)F)cn3)c2)CC1 10.6019/CHEMBL5212743
CHEMBL1651534 57341 57 None 1 2 Human 6.2 pKi = 6.2 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000306b ADRA2CSelectivity interaction (GPCR panel (PDSP screen)) EUB0000306b ADRA2C
ChEMBL 455 4 1 5 5.4 O=C(Nc1cccnn1)N1CCC(=Cc2cccc(Oc3ccc(C(F)(F)F)cn3)c2)CC1 10.6019/CHEMBL5212743
CHEMBL4780458 214046 0 None -2 4 Human 6.2 pKi = 6.2 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000540a ADRA2CSelectivity interaction (GPCR panel (PDSP screen)) EUB0000540a ADRA2C
ChEMBL None None None O=C(Nc1cccnn1)N1CC(C/C=C/c2cncc(Oc3ccc(C(F)(F)F)cn3)n2)C1 10.6019/CHEMBL5212743
44324765 111566 0 None 2 5 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 111566 0 None 2 5 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 207323 0 None 1 3 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 207323 0 None 1 3 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
10474679 97175 0 None 288 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 376 4 2 5 4.0 CN1CCN(c2ccc(Nc3c(CO)cnc4ccccc34)cc2)CC1(C)C 10.1016/j.ejmech.2010.12.026
CHEMBL268217 97175 0 None 288 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 376 4 2 5 4.0 CN1CCN(c2ccc(Nc3c(CO)cnc4ccccc34)cc2)CC1(C)C 10.1016/j.ejmech.2010.12.026
10474679 97175 0 None 288 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 376 4 2 5 4.0 CN1CCN(c2ccc(Nc3c(CO)cnc4ccccc34)cc2)CC1(C)C 10.1021/jm060262x
CHEMBL268217 97175 0 None 288 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 376 4 2 5 4.0 CN1CCN(c2ccc(Nc3c(CO)cnc4ccccc34)cc2)CC1(C)C 10.1021/jm060262x
6761 67797 19 None -3 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67797 19 None -3 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
16090596 82289 0 None 158 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 82289 0 None 158 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
16090596 82289 0 None 158 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 374 3 1 4 5.0 Cc1nc2c(C)cccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1016/j.ejmech.2010.12.026
CHEMBL217177 82289 0 None 158 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 374 3 1 4 5.0 Cc1nc2c(C)cccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1016/j.ejmech.2010.12.026
44568347 191649 0 None -28 15 Human 6.2 pKi = 6.2 Binding
Antagonist activity at adrenergic alpha2C receptor (unknown origin) by PDSP assayAntagonist activity at adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 356 6 0 4 5.2 CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL519609 191649 0 None -28 15 Human 6.2 pKi = 6.2 Binding
Antagonist activity at adrenergic alpha2C receptor (unknown origin) by PDSP assayAntagonist activity at adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 356 6 0 4 5.2 CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
118717248 115122 0 None -18 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RS-79948-197 from human alpha2C adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation countingDisplacement of [3H]RS-79948-197 from human alpha2C 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 115122 0 None -18 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RS-79948-197 from human alpha2C adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation countingDisplacement of [3H]RS-79948-197 from human alpha2C 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
11098175 204168 0 None -5 5 Human 6.2 pKi = 6.2 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 204168 0 None -5 5 Human 6.2 pKi = 6.2 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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
11034737 204526 0 None -3 6 Human 6.2 pKi = 6.2 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 204526 0 None -3 6 Human 6.2 pKi = 6.2 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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
57345627 71180 0 None -8 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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 71180 0 None -8 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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
5353853 17984 47 None -11 15 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 17984 47 None -11 15 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 17984 47 None -11 15 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
441383 20331 57 None 2 17 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 20331 57 None 2 17 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
2337 3254 77 None -10 63 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 3254 77 None -10 63 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 3254 77 None -10 63 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 3254 77 None -10 63 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 3254 77 None -10 63 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
57401787 71251 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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 71251 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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
56645363 121488 12 None 2 4 Human 6.2 pKi = 6.2 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000313b ADRA2CSelectivity interaction (GPCR panel (PDSP screen)) EUB0000313b ADRA2C
ChEMBL 311 3 1 4 3.8 CC(C)(O)c1cncc(-c2nc3ccc(F)cc3n2C2CC2)c1 10.6019/CHEMBL5212743
CHEMBL3582478 121488 12 None 2 4 Human 6.2 pKi = 6.2 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000313b ADRA2CSelectivity interaction (GPCR panel (PDSP screen)) EUB0000313b ADRA2C
ChEMBL 311 3 1 4 3.8 CC(C)(O)c1cncc(-c2nc3ccc(F)cc3n2C2CC2)c1 10.6019/CHEMBL5212743
1960 2855 67 None -20 26 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960012o
439260 2855 67 None -20 26 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960012o
505 2855 67 None -20 26 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960012o
CHEMBL1437 2855 67 None -20 26 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960012o
DB00368 2855 67 None -20 26 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960012o
49836303 18570 1 None -10 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 230 4 1 3 2.3 C[C@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL1276220 18570 1 None -10 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 230 4 1 3 2.3 C[C@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
49836303 18570 1 None -10 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 230 4 1 3 2.3 C[C@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
CHEMBL1276220 18570 1 None -10 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 230 4 1 3 2.3 C[C@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
1265 941 60 None -112 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C4 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 941 60 None -112 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C4 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 941 60 None -112 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cells
ChEMBL 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1021/jm8003625
10508016 207154 0 None -17 6 Human 6.2 pKi = 6.2 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 207154 0 None -17 6 Human 6.2 pKi = 6.2 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
72947314 92488 0 None -8 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 230 5 1 3 2.0 c1ccc(OCC2=NCCN2)c(CC2CC2)c1 10.1021/ml400232p
CHEMBL2431281 92488 0 None -8 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 230 5 1 3 2.0 c1ccc(OCC2=NCCN2)c(CC2CC2)c1 10.1021/ml400232p
127036932 137346 0 None -20 22 Human 6.2 pKi = 6.2 Binding
Binding affinity to alpha-2C adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2C 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 137346 0 None -20 22 Human 6.2 pKi = 6.2 Binding
Binding affinity to alpha-2C adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2C 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
57395732 71189 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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 71189 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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
2406 100402 89 None -11 12 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O nan
CHEMBL290106 100402 89 None -11 12 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O nan
122295 9866 7 None -1 9 Human 7.2 pKi = 7.2 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 10.1021/jm00018a001
CHEMBL114166 9866 7 None -1 9 Human 7.2 pKi = 7.2 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 10.1021/jm00018a001
122295 9866 7 None -1 9 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor
ChEMBL 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 10.1021/jm00019a001
CHEMBL114166 9866 7 None -1 9 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor
ChEMBL 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 10.1021/jm00019a001
44568614 187621 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 252 4 1 3 2.8 c1ccc(OC(C2=NCCN2)c2ccccc2)cc1 10.1021/jm800250z
CHEMBL494885 187621 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 252 4 1 3 2.8 c1ccc(OC(C2=NCCN2)c2ccccc2)cc1 10.1021/jm800250z
11265631 136407 0 None 2 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1cccnc1)C1=NCCN1 10.1021/jm061487a
CHEMBL373535 136407 0 None 2 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1cccnc1)C1=NCCN1 10.1021/jm061487a
11265631 136407 0 None 2 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1cccnc1)C1=NCCN1 10.1021/jm0408215
CHEMBL373535 136407 0 None 2 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1cccnc1)C1=NCCN1 10.1021/jm0408215
24882007 12471 1 None -12 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RS-79948-197 from human alpha2C adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation countingDisplacement of [3H]RS-79948-197 from human alpha2C 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 12471 1 None -12 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RS-79948-197 from human alpha2C adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation countingDisplacement of [3H]RS-79948-197 from human alpha2C 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
15675860 204427 0 None -8 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 305 1 2 5 2.1 Cc1cnc2c(Br)c(NC3=NCCN3)ccc2n1 10.1016/0960-894X(95)00391-6
CHEMBL72147 204427 0 None -8 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 305 1 2 5 2.1 Cc1cnc2c(Br)c(NC3=NCCN3)ccc2n1 10.1016/0960-894X(95)00391-6
44312036 204563 1 None 5 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 305 1 2 5 2.2 CC1CN=C(Nc2ccc3nccnc3c2Br)N1 10.1016/0960-894X(95)00391-6
CHEMBL72995 204563 1 None 5 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 305 1 2 5 2.2 CC1CN=C(Nc2ccc3nccnc3c2Br)N1 10.1016/0960-894X(95)00391-6
434526 77566 28 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 194 3 1 4 1.9 NCCSc1nc2ccccc2o1 10.1016/j.bmc.2015.01.013
CHEMBL2087646 77566 28 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 194 3 1 4 1.9 NCCSc1nc2ccccc2o1 10.1016/j.bmc.2015.01.013
44421258 84744 0 None -3 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 264 3 1 3 2.8 c1ccc(-c2ccccc2C2OC2C2=NCCN2)cc1 10.1021/jm0408215
CHEMBL1204386 84744 0 None -3 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 264 3 1 3 2.8 c1ccc(-c2ccccc2C2OC2C2=NCCN2)cc1 10.1021/jm0408215
CHEMBL222933 84744 0 None -3 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 264 3 1 3 2.8 c1ccc(-c2ccccc2C2OC2C2=NCCN2)cc1 10.1021/jm0408215
1960 2855 67 None -12 26 Mouse 6.2 pKi = 6.2 Binding
Binding affinity to mouse alpha-2C receptor expressed in COS7 cellsBinding affinity to mouse alpha-2C receptor expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O nan
439260 2855 67 None -12 26 Mouse 6.2 pKi = 6.2 Binding
Binding affinity to mouse alpha-2C receptor expressed in COS7 cellsBinding affinity to mouse alpha-2C receptor expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O nan
505 2855 67 None -12 26 Mouse 6.2 pKi = 6.2 Binding
Binding affinity to mouse alpha-2C receptor expressed in COS7 cellsBinding affinity to mouse alpha-2C receptor expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O nan
CHEMBL1437 2855 67 None -12 26 Mouse 6.2 pKi = 6.2 Binding
Binding affinity to mouse alpha-2C receptor expressed in COS7 cellsBinding affinity to mouse alpha-2C receptor expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O nan
DB00368 2855 67 None -12 26 Mouse 6.2 pKi = 6.2 Binding
Binding affinity to mouse alpha-2C receptor expressed in COS7 cellsBinding affinity to mouse alpha-2C receptor expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O nan
68617 205525 62 None -9 26 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL1709 205525 62 None -9 26 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL809 205525 62 None -9 26 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL4777443 214044 0 None -31 14 Human 6.2 pKi = 6.2 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000741a ADRA2CSelectivity interaction (GPCR panel (PDSP screen)) EUB0000741a ADRA2C
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
44288877 168597 0 None -933 5 Human 5.2 pKi = 5.2 Binding
In vivo inhibitory effect against Alpha-2C adrenergic receptorIn vivo inhibitory effect against Alpha-2C 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 168597 0 None -933 5 Human 5.2 pKi = 5.2 Binding
In vivo inhibitory effect against Alpha-2C adrenergic receptorIn vivo inhibitory effect against Alpha-2C 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
CHEMBL4516843 213968 0 None - 1 Human 6.2 pKi = 6.2 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000548a ADRA2CSelectivity interaction (GPCR panel (PDSP screen)) EUB0000548a ADRA2C
ChEMBL None None None NS(=O)(=O)c1cc(NC(=O)C2(c3ccccc3Cl)CC2)ccc1Oc1cccc(Cl)c1 10.6019/CHEMBL5212743
49781004 17211 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17211 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
10848826 188878 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Inhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 258 3 1 3 2.8 c1ccc(C[C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
CHEMBL50719 188878 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Inhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 258 3 1 3 2.8 c1ccc(C[C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
57345629 71183 0 None -45 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 246 5 1 4 2.0 CC(Oc1ccccc1OC1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL1956197 71183 0 None -45 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 246 5 1 4 2.0 CC(Oc1ccccc1OC1CC1)C1=NCCN1 10.1021/ml400232p
57345629 71183 0 None -45 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 246 5 1 4 2.0 CC(Oc1ccccc1OC1CC1)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956197 71183 0 None -45 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 246 5 1 4 2.0 CC(Oc1ccccc1OC1CC1)C1=NCCN1 10.1016/j.bmc.2012.01.035
24906197 187664 0 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 323 7 1 5 3.0 CC(Oc1ccccc1/C=N/OCc1ccccc1)C1=NCCN1 10.1021/jm800250z
CHEMBL495097 187664 0 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 323 7 1 5 3.0 CC(Oc1ccccc1/C=N/OCc1ccccc1)C1=NCCN1 10.1021/jm800250z
44401042 124827 0 None -181 9 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 329 2 0 3 4.6 CN(C)C[C@@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL364270 124827 0 None -181 9 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 329 2 0 3 4.6 CN(C)C[C@@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL179334 63301 0 None -3715 6 Human 6.2 pKi = 6.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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
36381 12940 5 None -1 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmcl.2012.08.046
CHEMBL1189234 12940 5 None -1 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmcl.2012.08.046
36381 12940 5 None -1 6 Human 6.2 pKi = 6.2 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmc.2013.07.045
CHEMBL1189234 12940 5 None -1 6 Human 6.2 pKi = 6.2 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmc.2013.07.045
73355415 92531 0 None -3 13 Human 6.2 pKi = 6.2 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
CHEMBL2432039 92531 0 None -3 13 Human 6.2 pKi = 6.2 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
9839050 112377 0 None -144 9 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C 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 112377 0 None -144 9 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 293 2 0 2 3.8 CN(C)C[C@H]1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1021/jm049632c
1593 2338 66 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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 2338 66 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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 2338 66 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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 2338 66 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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 2338 66 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1016/j.bmc.2012.01.035
9923679 81760 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 332 3 1 4 4.0 Cc1cc(Nc2ccc(N3CCN(C)CC3)cc2)c2ccccc2n1 10.1021/jm060262x
CHEMBL216399 81760 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 332 3 1 4 4.0 Cc1cc(Nc2ccc(N3CCN(C)CC3)cc2)c2ccccc2n1 10.1021/jm060262x
9923679 81760 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 332 3 1 4 4.0 Cc1cc(Nc2ccc(N3CCN(C)CC3)cc2)c2ccccc2n1 10.1016/j.ejmech.2010.12.026
CHEMBL216399 81760 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 332 3 1 4 4.0 Cc1cc(Nc2ccc(N3CCN(C)CC3)cc2)c2ccccc2n1 10.1016/j.ejmech.2010.12.026
11058166 204703 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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 204703 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2C 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
24906241 192815 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 280 2 1 4 2.5 c1ccc(-c2cccc3c2OC(C2=NCCN2)CO3)cc1 10.1021/jm800250z
CHEMBL522151 192815 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 280 2 1 4 2.5 c1ccc(-c2cccc3c2OC(C2=NCCN2)CO3)cc1 10.1021/jm800250z
71457691 83797 0 None -2 10 Human 6.2 pKi = 6.2 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 295 3 1 3 2.0 COc1ccccc1CN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205823 83797 0 None -2 10 Human 6.2 pKi = 6.2 Binding
Binding affinity to alpha2C adrenergic receptorBinding affinity to alpha2C adrenergic receptor
ChEMBL 295 3 1 3 2.0 COc1ccccc1CN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
10045088 80586 0 None 407 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 376 4 2 5 3.9 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1CO 10.1016/j.ejmech.2010.12.026
CHEMBL214996 80586 0 None 407 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 376 4 2 5 3.9 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1CO 10.1016/j.ejmech.2010.12.026
10045088 80586 0 None 407 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 376 4 2 5 3.9 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1CO 10.1021/jm060262x
CHEMBL214996 80586 0 None 407 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 376 4 2 5 3.9 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1CO 10.1021/jm060262x
16090623 82452 0 None 77 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 388 3 1 4 5.4 Cc1ccc2c(Nc3ccc(N4CCN(C)[C@H](C)C4)cc3)c(C)c(C)nc2c1C 10.1016/j.ejmech.2010.12.026
CHEMBL217567 82452 0 None 77 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 388 3 1 4 5.4 Cc1ccc2c(Nc3ccc(N4CCN(C)[C@H](C)C4)cc3)c(C)c(C)nc2c1C 10.1016/j.ejmech.2010.12.026
16090623 82452 0 None 77 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 82452 0 None 77 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
129211 3747 78 None -51 16 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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 3747 78 None -51 16 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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 3747 78 None -51 16 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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 3747 78 None -51 16 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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 3747 78 None -51 16 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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
49836301 18565 1 None -1 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@@H](C)C1=NCCN1 10.1021/ml400232p
CHEMBL1276140 18565 1 None -1 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@@H](C)C1=NCCN1 10.1021/ml400232p
44269006 32351 1 None -1 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 216 5 1 3 1.8 C=CCc1ccccc1OCC1=NCCN1 10.1021/ml400232p
CHEMBL14107 32351 1 None -1 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 216 5 1 3 1.8 C=CCc1ccccc1OCC1=NCCN1 10.1021/ml400232p
49836301 18565 1 None -1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@@H](C)C1=NCCN1 10.1021/jm100977d
CHEMBL1276140 18565 1 None -1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@@H](C)C1=NCCN1 10.1021/jm100977d
49836301 18565 1 None -1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human alpha2C adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2C 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 18565 1 None -1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human alpha2C adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2C 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
11140033 20681 0 None -7 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 265 4 2 3 3.2 CC(Nc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm0408215
CHEMBL130884 20681 0 None -7 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 265 4 2 3 3.2 CC(Nc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm0408215
11199593 137197 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 282 4 1 3 3.8 CC(Sc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm0408215
CHEMBL374954 137197 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 282 4 1 3 3.8 CC(Sc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm0408215
5318 15574 49 None -1 13 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1200348 15574 49 None -1 13 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1221 15574 49 None -1 13 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
44424855 85452 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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 85452 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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
13178306 121707 2 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 187 3 2 2 2.3 Cc1ccccc1NCc1cnc[nH]1 10.1016/j.bmc.2015.01.013
CHEMBL3588902 121707 2 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 187 3 2 2 2.3 Cc1ccccc1NCc1cnc[nH]1 10.1016/j.bmc.2015.01.013
11360447 84999 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1cccs1)C1=NCCN1 10.1021/jm0408215
CHEMBL223829 84999 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1cccs1)C1=NCCN1 10.1021/jm0408215
10651080 105940 0 None -83 6 Human 6.1 pKi = 6.1 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 105940 0 None -83 6 Human 6.1 pKi = 6.1 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
46743614 121711 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 317 4 1 3 2.7 CCNCC(=O)N1CCn2cccc2C1c1cccc(Cl)c1 10.1016/j.bmc.2015.01.013
CHEMBL3588906 121711 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 317 4 1 3 2.7 CCNCC(=O)N1CCn2cccc2C1c1cccc(Cl)c1 10.1016/j.bmc.2015.01.013
44401164 69814 0 None -309 9 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL193639 69814 0 None -309 9 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL508338 188964 0 None -25 6 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL None None None None nan
490 191 8 None -724 12 Human 7.1 pKi = 7.1 Binding
Ancillary Binding affinity to cloned human Alpha-2C adrenergic receptorAncillary Binding affinity to cloned human Alpha-2C 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 191 8 None -724 12 Human 7.1 pKi = 7.1 Binding
Ancillary Binding affinity to cloned human Alpha-2C adrenergic receptorAncillary Binding affinity to cloned human Alpha-2C 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 191 8 None -724 12 Human 7.1 pKi = 7.1 Binding
Ancillary Binding affinity to cloned human Alpha-2C adrenergic receptorAncillary Binding affinity to cloned human Alpha-2C 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
57395731 71188 0 None -7 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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 71188 0 None -7 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 232 4 1 4 1.7 CC(=O)c1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
57403508 71250 0 None -2 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 308 3 1 4 2.3 c1ccc(C2(c3ccccc3)COC(C3=NCCN3)CO2)cc1 10.1016/j.bmc.2012.02.016
CHEMBL1956905 71250 0 None -2 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 308 3 1 4 2.3 c1ccc(C2(c3ccccc3)COC(C3=NCCN3)CO2)cc1 10.1016/j.bmc.2012.02.016
44401105 69574 0 None -83 9 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 373 2 0 3 4.7 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL193435 69574 0 None -83 9 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 373 2 0 3 4.7 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1021/jm049632c
57399145 71182 0 None -7 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 234 5 1 4 1.9 CCOc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956196 71182 0 None -7 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 234 5 1 4 1.9 CCOc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
31101 728 40 None -36 36 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
35 728 40 None -36 36 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
403 728 40 None -36 36 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 728 40 None -36 36 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 728 40 None -36 36 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
16090624 82399 0 None 13 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 82399 0 None 13 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
16090624 82399 0 None 13 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 374 3 1 4 5.0 Cc1ccc2c(Nc3ccc(N4CCN(C)[C@@H](C)C4)cc3)c(C)c(C)nc2c1 10.1016/j.ejmech.2010.12.026
CHEMBL217278 82399 0 None 13 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 374 3 1 4 5.0 Cc1ccc2c(Nc3ccc(N4CCN(C)[C@@H](C)C4)cc3)c(C)c(C)nc2c1 10.1016/j.ejmech.2010.12.026
1836 2590 59 None -31 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2590 59 None -31 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2590 59 None -31 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2590 59 None -31 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2590 59 None -31 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
16090634 82292 0 None 4 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 296 3 1 4 3.2 Cc1cncc(C)c1Nc1ccc(N2CCN(C)CC2)cc1 10.1016/j.ejmech.2010.12.026
CHEMBL217180 82292 0 None 4 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 296 3 1 4 3.2 Cc1cncc(C)c1Nc1ccc(N2CCN(C)CC2)cc1 10.1016/j.ejmech.2010.12.026
135398745 2912 112 None -30 66 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2912 112 None -30 66 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2912 112 None -30 66 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2912 112 None -30 66 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
25053351 173003 0 None -371 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cells
ChEMBL 455 4 1 3 5.0 CN[C@@H](C(=O)N(C)[C@H]1CC[C@@]2(C)C(=CC[C@@H]3[C@@H]2CC[C@]24CN(C)[C@@H](C)[C@H]2CC[C@@H]34)C1)C(C)C 10.1021/jm8003625
CHEMBL451821 173003 0 None -371 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cells
ChEMBL 455 4 1 3 5.0 CN[C@@H](C(=O)N(C)[C@H]1CC[C@@]2(C)C(=CC[C@@H]3[C@@H]2CC[C@]24CN(C)[C@@H](C)[C@H]2CC[C@@H]34)C1)C(C)C 10.1021/jm8003625
23622576 172770 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 272 4 1 3 3.5 CC(Oc1ccccc1C1CCCCC1)C1=NCCN1 10.1021/jm800250z
CHEMBL451229 172770 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 272 4 1 3 3.5 CC(Oc1ccccc1C1CCCCC1)C1=NCCN1 10.1021/jm800250z
73213195 104457 0 None -26 12 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 104457 0 None -26 12 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
16090599 81543 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 360 3 1 4 5.0 Cc1nc2c(C)cccc2c(Nc2ccc(N3CCCN(C)C3)cc2)c1C 10.1021/jm060262x
CHEMBL216072 81543 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 360 3 1 4 5.0 Cc1nc2c(C)cccc2c(Nc2ccc(N3CCCN(C)C3)cc2)c1C 10.1021/jm060262x
10579368 106002 0 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 106002 0 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
73213195 104457 0 None -26 12 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 104457 0 None -26 12 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
3584 3775 64 None -50 14 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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 3775 64 None -50 14 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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 3775 64 None -50 14 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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 3775 64 None -50 14 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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 3775 64 None -50 14 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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
44401106 124325 0 None -120 9 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL363581 124325 0 None -120 9 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
44549156 18568 0 None -10 4 Human 7.1 pKi = 7.1 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 230 4 1 3 2.3 CC(Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL1276218 18568 0 None -10 4 Human 7.1 pKi = 7.1 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 230 4 1 3 2.3 CC(Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
45487956 198365 0 None -3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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 198365 0 None -3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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 18568 0 None -10 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 230 4 1 3 2.3 CC(Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
CHEMBL1276218 18568 0 None -10 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 230 4 1 3 2.3 CC(Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
44292385 101119 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Inhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 270 3 1 3 2.6 c1ccc(C[C@H]2C3CCC(C3)[C@H]2NC2=NCCO2)cc1 10.1021/jm9905256
CHEMBL295186 101119 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Inhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 270 3 1 3 2.6 c1ccc(C[C@H]2C3CCC(C3)[C@H]2NC2=NCCO2)cc1 10.1021/jm9905256
11080 29083 79 None -3 6 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 29083 79 None -3 6 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
72947315 92487 0 None -10 4 Human 6.1 pKi = 6.1 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 232 5 1 4 1.6 c1ccc(OC2CC2)c(OCC2=NCCN2)c1 10.1021/ml400232p
CHEMBL2431280 92487 0 None -10 4 Human 6.1 pKi = 6.1 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 232 5 1 4 1.6 c1ccc(OC2CC2)c(OCC2=NCCN2)c1 10.1021/ml400232p
127026052 137551 0 None -47 19 Human 6.1 pKi = 6.1 Binding
Binding affinity to alpha-2C adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2C 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 137551 0 None -47 19 Human 6.1 pKi = 6.1 Binding
Binding affinity to alpha-2C adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2C 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
44456400 12832 0 None -3 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha2C-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysisDisplacement of [3H]Rauwolscine from human recombinant alpha2C-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 12832 0 None -3 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha2C-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysisDisplacement of [3H]Rauwolscine from human recombinant alpha2C-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 12832 0 None -3 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha2C-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysisDisplacement of [3H]Rauwolscine from human recombinant alpha2C-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 12832 0 None -3 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha2C-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysisDisplacement of [3H]Rauwolscine from human recombinant alpha2C-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
11750482 147419 0 None 19 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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 147419 0 None 19 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cells
ChEMBL 419 6 0 6 5.3 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccco4)cc13)CC2 10.1016/j.bmcl.2006.12.094
44402579 132752 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
ChEMBL 411 3 3 5 1.8 COC(=O)CNC(=O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O 10.1016/j.bmcl.2005.03.116
CHEMBL370005 132752 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
ChEMBL 411 3 3 5 1.8 COC(=O)CNC(=O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O 10.1016/j.bmcl.2005.03.116
10318507 58951 0 None 104 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 394 3 1 4 5.4 Cc1nc2cc(Cl)ccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1016/j.ejmech.2010.12.026
CHEMBL1689423 58951 0 None 104 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 394 3 1 4 5.4 Cc1nc2cc(Cl)ccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1016/j.ejmech.2010.12.026
16090595 141399 0 None 109 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 374 3 1 4 5.0 Cc1ccc2c(Nc3ccc(N4CCN(C)[C@H](C)C4)cc3)c(C)c(C)nc2c1 10.1016/j.ejmech.2010.12.026
CHEMBL383978 141399 0 None 109 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 374 3 1 4 5.0 Cc1ccc2c(Nc3ccc(N4CCN(C)[C@H](C)C4)cc3)c(C)c(C)nc2c1 10.1016/j.ejmech.2010.12.026
10318507 58951 0 None 104 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 58951 0 None 104 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
16090595 141399 0 None 109 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 141399 0 None 109 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
136019934 144528 0 None 7 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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 144528 0 None 7 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic Alpha-2C 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
2142 3094 58 None -7 37 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
4920903 3094 58 None -7 37 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
502 3094 58 None -7 37 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
5775 3094 58 None -7 37 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
CHEMBL597 3094 58 None -7 37 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
DB00692 3094 58 None -7 37 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
16090622 82296 0 None 165 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 346 3 1 4 4.4 Cc1cnc2ccccc2c1Nc1ccc(N2CCN(C)C(C)C2)cc1 10.1016/j.ejmech.2010.12.026
CHEMBL217202 82296 0 None 165 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 346 3 1 4 4.4 Cc1cnc2ccccc2c1Nc1ccc(N2CCN(C)C(C)C2)cc1 10.1016/j.ejmech.2010.12.026
16090628 141785 0 None 309 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 388 4 1 4 5.3 CCc1c(C)nc2c(C)cccc2c1Nc1ccc(N2CCCN(C)CC2)cc1 10.1016/j.ejmech.2010.12.026
CHEMBL386169 141785 0 None 309 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 388 4 1 4 5.3 CCc1c(C)nc2c(C)cccc2c1Nc1ccc(N2CCCN(C)CC2)cc1 10.1016/j.ejmech.2010.12.026
16090622 82296 0 None 165 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 346 3 1 4 4.4 Cc1cnc2ccccc2c1Nc1ccc(N2CCN(C)C(C)C2)cc1 10.1021/jm060262x
CHEMBL217202 82296 0 None 165 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 346 3 1 4 4.4 Cc1cnc2ccccc2c1Nc1ccc(N2CCN(C)C(C)C2)cc1 10.1021/jm060262x
16090628 141785 0 None 309 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 388 4 1 4 5.3 CCc1c(C)nc2c(C)cccc2c1Nc1ccc(N2CCCN(C)CC2)cc1 10.1021/jm060262x
CHEMBL386169 141785 0 None 309 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 388 4 1 4 5.3 CCc1c(C)nc2c(C)cccc2c1Nc1ccc(N2CCCN(C)CC2)cc1 10.1021/jm060262x
44402477 133747 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
ChEMBL 718 6 6 6 4.6 O=C(NCCCNC(=O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O)[C@@H]1[C@H](O)CC[C@@H]2CN3CCc4c([nH]c5ccccc45)[C@H]3C[C@H]21 10.1016/j.bmcl.2005.03.116
CHEMBL371516 133747 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamineIn vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
ChEMBL 718 6 6 6 4.6 O=C(NCCCNC(=O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O)[C@@H]1[C@H](O)CC[C@@H]2CN3CCc4c([nH]c5ccccc45)[C@H]3C[C@H]21 10.1016/j.bmcl.2005.03.116
180 401 56 None -16 40 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 401 56 None -16 40 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 401 56 None -16 40 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 401 56 None -16 40 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 401 56 None -16 40 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
9837551 101622 0 None -7 3 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 232 1 3 5 1.2 Cc1c(NC2=NCCN2)ccc2c1NCCO2 10.1021/jm960359r
CHEMBL298936 101622 0 None -7 3 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 232 1 3 5 1.2 Cc1c(NC2=NCCN2)ccc2c1NCCO2 10.1021/jm960359r
16090601 82390 0 None 199 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 376 4 2 5 3.9 Cc1c(CO)nc2ccccc2c1Nc1ccc(N2CCN(C)[C@H](C)C2)cc1 10.1016/j.ejmech.2010.12.026
CHEMBL217254 82390 0 None 199 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 376 4 2 5 3.9 Cc1c(CO)nc2ccccc2c1Nc1ccc(N2CCN(C)[C@H](C)C2)cc1 10.1016/j.ejmech.2010.12.026
10065083 32101 1 None -12 10 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation countingDisplacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation counting
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2011.12.019
CHEMBL140872 32101 1 None -12 10 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation countingDisplacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation counting
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2011.12.019
2142 3094 58 None -7 37 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human alpha-2C adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2C 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 3094 58 None -7 37 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human alpha-2C adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2C 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 3094 58 None -7 37 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human alpha-2C adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2C 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 3094 58 None -7 37 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human alpha-2C adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2C 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 3094 58 None -7 37 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human alpha-2C adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2C 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 3094 58 None -7 37 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human alpha-2C adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2C 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
9828476 206922 0 None -354 6 Human 7.1 pKi = 7.1 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 206922 0 None -354 6 Human 7.1 pKi = 7.1 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
5280953 97360 109 None 1 8 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Alpha-2C adrenergic receptorBinding affinity towards Alpha-2C adrenergic receptor
ChEMBL 212 1 1 2 3.0 COc1ccc2c(c1)[nH]c1c(C)nccc12 10.1016/j.bmcl.2003.09.027
CHEMBL269538 97360 109 None 1 8 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Alpha-2C adrenergic receptorBinding affinity towards Alpha-2C adrenergic receptor
ChEMBL 212 1 1 2 3.0 COc1ccc2c(c1)[nH]c1c(C)nccc12 10.1016/j.bmcl.2003.09.027
10508132 107015 0 None -13 6 Human 6.1 pKi = 6.1 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 107015 0 None -13 6 Human 6.1 pKi = 6.1 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
491 192 9 None -1000 12 Human 7.1 pKi = 7.1 Binding
Ancillary Binding affinity to cloned human Alpha-2C adrenergic receptorAncillary Binding affinity to cloned human Alpha-2C 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 192 9 None -1000 12 Human 7.1 pKi = 7.1 Binding
Ancillary Binding affinity to cloned human Alpha-2C adrenergic receptorAncillary Binding affinity to cloned human Alpha-2C 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 192 9 None -1000 12 Human 7.1 pKi = 7.1 Binding
Ancillary Binding affinity to cloned human Alpha-2C adrenergic receptorAncillary Binding affinity to cloned human Alpha-2C 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
16090627 81565 0 None 10 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 390 9 2 4 5.9 CCc1c(C)nc2c(C)cccc2c1Nc1ccc(NCCN(CC)CC)cc1 10.1021/jm060262x
CHEMBL216197 81565 0 None 10 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 390 9 2 4 5.9 CCc1c(C)nc2c(C)cccc2c1Nc1ccc(NCCN(CC)CC)cc1 10.1021/jm060262x
135398745 2912 112 None -30 66 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
47 2912 112 None -30 66 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
CHEMBL715 2912 112 None -30 66 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
DB00334 2912 112 None -30 66 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
16090627 81565 0 None 10 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 390 9 2 4 5.9 CCc1c(C)nc2c(C)cccc2c1Nc1ccc(NCCN(CC)CC)cc1 10.1016/j.ejmech.2010.12.026
CHEMBL216197 81565 0 None 10 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 390 9 2 4 5.9 CCc1c(C)nc2c(C)cccc2c1Nc1ccc(NCCN(CC)CC)cc1 10.1016/j.ejmech.2010.12.026
2435 721 100 None -33 12 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
395 721 100 None -33 12 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
520 721 100 None -33 12 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
5386 721 100 None -33 12 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
CHEMBL844 721 100 None -33 12 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
DB00484 721 100 None -33 12 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosinBinding affinity for human Alpha-2C adrenergic receptor from cultured LM(tk-) cells using [3H]- prazosin
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
1242 3611 27 None -4 18 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2015.01.013
935 3611 27 None -4 18 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2015.01.013
CHEMBL286080 3611 27 None -4 18 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2015.01.013
16090594 82123 0 None 10 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 388 3 1 4 5.4 Cc1ccc2c(Nc3ccc(N4CCN(C)[C@@H](C)C4)cc3)c(C)c(C)nc2c1C 10.1016/j.ejmech.2010.12.026
CHEMBL216674 82123 0 None 10 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 388 3 1 4 5.4 Cc1ccc2c(Nc3ccc(N4CCN(C)[C@@H](C)C4)cc3)c(C)c(C)nc2c1C 10.1016/j.ejmech.2010.12.026
24841480 183897 0 None -416 20 Human 6.1 pKi = 6.1 Binding
Antagonist activity at adrenergic alpha2C receptor (unknown origin) by PDSP assayAntagonist activity at adrenergic alpha2C 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 183897 0 None -416 20 Human 6.1 pKi = 6.1 Binding
Antagonist activity at adrenergic alpha2C receptor (unknown origin) by PDSP assayAntagonist activity at adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
57402717 71185 2 None -14 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 220 4 1 4 1.5 COc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956199 71185 2 None -14 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 220 4 1 4 1.5 COc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
24906201 187351 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 280 2 1 4 2.5 c1ccc(-c2cccc3c2OCC(C2=NCCN2)O3)cc1 10.1021/jm800250z
CHEMBL493272 187351 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 280 2 1 4 2.5 c1ccc(-c2cccc3c2OCC(C2=NCCN2)O3)cc1 10.1021/jm800250z
4657799 121712 3 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 254 5 1 2 2.7 NCCCN(C(=O)c1ccccc1)c1ccccc1 10.1016/j.bmc.2015.01.013
CHEMBL3588907 121712 3 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysisDisplacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis
ChEMBL 254 5 1 2 2.7 NCCCN(C(=O)c1ccccc1)c1ccccc1 10.1016/j.bmc.2015.01.013
16090594 82123 0 None 10 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 82123 0 None 10 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
44456400 12832 0 None -3 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha2C-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysisDisplacement of [3H]Rauwolscine from human recombinant alpha2C-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 12832 0 None -3 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha2C-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysisDisplacement of [3H]Rauwolscine from human recombinant alpha2C-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 12832 0 None -3 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha2C-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysisDisplacement of [3H]Rauwolscine from human recombinant alpha2C-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 12832 0 None -3 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha2C-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysisDisplacement of [3H]Rauwolscine from human recombinant alpha2C-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
24906198 187662 3 None -3 4 Human 7.1 pKi = 7.1 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/ml400232p
CHEMBL495095 187662 3 None -3 4 Human 7.1 pKi = 7.1 Binding
Binding affinity at human alpha2C ARBinding affinity at human alpha2C AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/ml400232p
44314200 102950 0 None -3 4 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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 102950 0 None -3 4 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2C 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
24906198 187662 3 None -3 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
CHEMBL495095 187662 3 None -3 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
45487145 197657 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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 197657 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human Alpha-2C 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 187662 3 None -3 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/jm100977d
CHEMBL495095 187662 3 None -3 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/jm100977d
24906198 187662 3 None -3 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from human alpha2C adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2C 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 187662 3 None -3 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from human alpha2C adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2C 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
44292386 101480 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Inhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 296 4 1 3 3.5 C(=C/c1ccccc1)\C[C@H]1C2CCC(C2)[C@H]1NC1=NCCO1 10.1021/jm9905256
CHEMBL297827 101480 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Inhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptorInhibitory constant, using [3H]rauwolscine in LM(tk-) cells stably transfected with cloned human Alpha-2C adrenergic receptor
ChEMBL 296 4 1 3 3.5 C(=C/c1ccccc1)\C[C@H]1C2CCC(C2)[C@H]1NC1=NCCO1 10.1021/jm9905256
57339144 92236 78 None -11 6 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b ADRA2CSelectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b ADRA2C
ChEMBL 529 6 1 5 4.8 O=C(c1ccc(C(=O)N2CCC(N3CCCC3)CC2)c(Nc2ccccc2)c1)N1CCC(N2CCCC2)CC1 10.6019/CHEMBL5212743
CHEMBL2426364 92236 78 None -11 6 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b ADRA2CSelectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b ADRA2C
ChEMBL 529 6 1 5 4.8 O=C(c1ccc(C(=O)N2CCC(N3CCCC3)CC2)c(Nc2ccccc2)c1)N1CCC(N2CCCC2)CC1 10.6019/CHEMBL5212743
199798 74704 9 None 3 2 Human 6.1 pKi = 6.1 Binding
Inhibition of alpha2C adrenergic receptorInhibition of alpha2C adrenergic receptor
ChEMBL 167 2 0 1 2.7 C1CCC(CN2CCCC2)CC1 10.1016/j.bmcl.2012.04.077
CHEMBL2030634 74704 9 None 3 2 Human 6.1 pKi = 6.1 Binding
Inhibition of alpha2C adrenergic receptorInhibition of alpha2C adrenergic receptor
ChEMBL 167 2 0 1 2.7 C1CCC(CN2CCCC2)CC1 10.1016/j.bmcl.2012.04.077
73349361 92546 0 None 1 7 Human 6.1 pKi = 6.1 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 279 4 0 1 3.3 CN(CCc1ccccc1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
CHEMBL2432058 92546 0 None 1 7 Human 6.1 pKi = 6.1 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 279 4 0 1 3.3 CN(CCc1ccccc1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
16090625 82428 0 None 7 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 82428 0 None 7 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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
16090625 82428 0 None 7 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 374 3 1 4 5.0 Cc1nc2cccc(C)c2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1016/j.ejmech.2010.12.026
CHEMBL217452 82428 0 None 7 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 374 3 1 4 5.0 Cc1nc2cccc(C)c2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1016/j.ejmech.2010.12.026
10674896 206642 0 None -478 6 Human 6.1 pKi = 6.1 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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 206642 0 None -478 6 Human 6.1 pKi = 6.1 Binding
Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptorBinding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C 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
57402718 71187 2 None -8 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 218 4 1 4 1.3 CC(Oc1ccccc1C=O)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956201 71187 2 None -8 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
ChEMBL 218 4 1 4 1.3 CC(Oc1ccccc1C=O)C1=NCCN1 10.1016/j.bmc.2012.01.035
3584 3775 64 None -50 14 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
5401 3775 64 None -50 14 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
7302 3775 64 None -50 14 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
CHEMBL611 3775 64 None -50 14 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
DB01162 3775 64 None -50 14 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
9795515 204818 0 None -17 3 Human 7.1 pKi = 7.1 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C 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 204818 0 None -17 3 Human 7.1 pKi = 7.1 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C 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
10632290 204744 5 None -2 3 Human 5.1 pKi = 5.1 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 211 2 2 4 2.1 c1c[nH]c(Nc2ccc3nccnc3c2)n1 10.1021/jm9605142
CHEMBL74449 204744 5 None -2 3 Human 5.1 pKi = 5.1 Binding
Displacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2C adrenergic receptor expressed in CHO cells
ChEMBL 211 2 2 4 2.1 c1c[nH]c(Nc2ccc3nccnc3c2)n1 10.1021/jm9605142
44328920 108639 0 None -77 6 Human 6.1 pKi = 6.1 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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 108639 0 None -77 6 Human 6.1 pKi = 6.1 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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
44324900 206896 0 None 2 3 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 206896 0 None 2 3 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
44325028 206969 0 None 2 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 206969 0 None 2 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 207183 0 None 2 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 207183 0 None 2 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
44324860 207496 0 None 1 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 207496 0 None 1 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
49781008 17248 0 None -7 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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 17248 0 None -7 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic Alpha-2C 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
24839550 137313 14 None -14 15 Human 6.1 pKi = 6.1 Binding
Binding affinity to alpha-2C adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2C 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 137313 14 None -14 15 Human 6.1 pKi = 6.1 Binding
Binding affinity to alpha-2C adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2C 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
16090601 82390 0 None 199 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 82390 0 None 199 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 376 4 2 5 3.9 Cc1c(CO)nc2ccccc2c1Nc1ccc(N2CCN(C)[C@H](C)C2)cc1 10.1021/jm060262x
44579303 186770 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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
CHEMBL488974 186770 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic Alpha-2C 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
16090602 82446 0 None 239 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C 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 82446 0 None 239 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]rauwolscine from human ADRA2C expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2C expressed in S115 cells
ChEMBL 362 4 2 5 3.6 C[C@@H]1CN(c2ccc(Nc3c(CO)cnc4ccccc34)cc2)CCN1C 10.1021/jm060262x
16090602 82446 0 None 239 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 362 4 2 5 3.6 C[C@@H]1CN(c2ccc(Nc3c(CO)cnc4ccccc34)cc2)CCN1C 10.1016/j.ejmech.2010.12.026
CHEMBL217542 82446 0 None 239 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned Alpha-2C adrenergic receptorBinding affinity to human cloned Alpha-2C adrenergic receptor
ChEMBL 362 4 2 5 3.6 C[C@@H]1CN(c2ccc(Nc3c(CO)cnc4ccccc34)cc2)CCN1C 10.1016/j.ejmech.2010.12.026
2803 954 58 None -4 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2C 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
516 954 58 None -4 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2C 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
704 954 58 None -4 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2C 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 954 58 None -4 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2C 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 954 58 None -4 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2C 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
44438161 147139 0 None 22 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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 147139 0 None 22 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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
44438165 166782 0 None 48 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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 166782 0 None 48 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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
44330571 163997 0 None 2 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 163997 0 None 2 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity to human alpha-2C adrenergic receptorIn vitro binding affinity to human alpha-2C 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 163997 0 None 2 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 163997 0 None 2 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
44324737 207236 0 None 2 5 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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 207236 0 None 2 5 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards human adrenergic alpha-2C adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human adrenergic alpha-2C 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
44438148 93488 0 None 14 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 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 93488 0 None 14 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cellsDisplacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cells
ChEMBL 430 6 0 6 5.1 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccn4)cc13)CC2 10.1016/j.bmcl.2006.12.094
11465618 102396 23 None -36 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]RX 821002 from recombinant human alpha2C receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]RX 821002 from recombinant human alpha2C 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 102396 23 None -36 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]RX 821002 from recombinant human alpha2C receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]RX 821002 from recombinant human alpha2C 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 102396 23 None -36 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]RX 821002 from recombinant human alpha2C receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]RX 821002 from recombinant human alpha2C 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
9809007 172562 8 None -724 6 Human 6.0 pKi = 6.0 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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 172562 8 None -724 6 Human 6.0 pKi = 6.0 Binding
Binding affinity against human Alpha-2c adrenergic receptorBinding affinity against human Alpha-2c 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
24906159 187403 12 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 233 4 2 5 1.3 CC(Oc1ccccc1/C=N/O)C1=NCCN1 10.1021/jm800250z
CHEMBL493675 187403 12 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 233 4 2 5 1.3 CC(Oc1ccccc1/C=N/O)C1=NCCN1 10.1021/jm800250z
11186523 127509 0 None -66 9 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C 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 127509 0 None -66 9 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C 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
1343 1887 62 None -251 9 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
3519 1887 62 None -251 9 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
522 1887 62 None -251 9 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
CHEMBL862 1887 62 None -251 9 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
DB01018 1887 62 None -251 9 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
4209 3161 75 None -77 33 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
4893 3161 75 None -77 33 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
503 3161 75 None -77 33 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
5385 3161 75 None -77 33 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
CHEMBL2 3161 75 None -77 33 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
DB00457 3161 75 None -77 33 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
9906978 42709 2 None -1 12 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned adrenergic alpha-2C receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-2C 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 42709 2 None -1 12 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned adrenergic alpha-2C receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-2C 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
4209 3161 75 None -77 33 Human 7.0 pKi = 7.0 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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 3161 75 None -77 33 Human 7.0 pKi = 7.0 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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 3161 75 None -77 33 Human 7.0 pKi = 7.0 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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 3161 75 None -77 33 Human 7.0 pKi = 7.0 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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 3161 75 None -77 33 Human 7.0 pKi = 7.0 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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 3161 75 None -77 33 Human 7.0 pKi = 7.0 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
1547484 939 74 None -4 20 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 939 74 None -4 20 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 939 74 None -4 20 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 939 74 None -4 20 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 939 74 None -4 20 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL4520788 213973 10 None -4 25 Human 7.0 pKi = 7.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a ADRA2CSelectivity interaction (GPCR panel (PDSP screen)) EUB0000743a ADRA2C
ChEMBL None None None CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL5212743
5280805 85403 81 None -29 3 Human 5.0 pKi = 5.0 Binding
Binding affinity to adrenergic alpha2c receptorBinding affinity to adrenergic alpha2c 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 85403 81 None -29 3 Human 5.0 pKi = 5.0 Binding
Binding affinity to adrenergic alpha2c receptorBinding affinity to adrenergic alpha2c 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
4407909 192864 1 None -16 10 Human 6.0 pKi = 6.0 Binding
Binding affinity to alpha2c (unknown origin) assessed as inhibition constantBinding affinity to alpha2c (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5182943 192864 1 None -16 10 Human 6.0 pKi = 6.0 Binding
Binding affinity to alpha2c (unknown origin) assessed as inhibition constantBinding affinity to alpha2c (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221893 192864 1 None -16 10 Human 6.0 pKi = 6.0 Binding
Binding affinity to alpha2c (unknown origin) assessed as inhibition constantBinding affinity to alpha2c (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
57395663 71179 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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 71179 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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
11043720 92170 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 C[C@@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
CHEMBL242265 92170 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 C[C@@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
11043720 92170 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 C[C@@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
CHEMBL242265 92170 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 C[C@@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
49783415 17676 0 None -1348 13 Human 6.0 pKi = 6 Binding
Binding affinity to human adrenergic Alpha-2C receptorBinding affinity to human adrenergic Alpha-2C receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258452 17676 0 None -1348 13 Human 6.0 pKi = 6 Binding
Binding affinity to human adrenergic Alpha-2C receptorBinding affinity to human adrenergic Alpha-2C receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
73355418 92544 0 None 1 3 Human 6.0 pKi = 6 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 325 5 0 3 3.3 COc1ccc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432056 92544 0 None 1 3 Human 6.0 pKi = 6 Binding
Inhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2C receptor (unknown origin) by PDSP assay
ChEMBL 325 5 0 3 3.3 COc1ccc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC 10.1016/j.bmc.2013.07.045
3952 1886 38 None -19 12 Human 6.4 pKd = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5353646 1886 38 None -19 12 Human 6.4 pKd = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5443 1886 38 None -19 12 Human 6.4 pKd = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5702063 1886 38 None -19 12 Human 6.4 pKd = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
CHEMBL1331786 1886 38 None -19 12 Human 6.4 pKd = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
CHEMBL420 1886 38 None -19 12 Human 6.4 pKd = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
DB00629 1886 38 None -19 12 Human 6.4 pKd = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
108094 3421 27 None -2 4 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 35224877
108094 3421 27 None -2 4 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 7908642
108094 3421 27 None -2 4 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 8819505
526 3421 27 None -2 4 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 35224877
526 3421 27 None -2 4 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 7908642
526 3421 27 None -2 4 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 8819505
528 3421 27 None -2 4 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 35224877
528 3421 27 None -2 4 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 7908642
528 3421 27 None -2 4 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 8819505
CHEMBL10332 3421 27 None -2 4 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 35224877
CHEMBL10332 3421 27 None -2 4 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 7908642
CHEMBL10332 3421 27 None -2 4 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 8819505
136 3290 32 None 3 16 Human 9.5 pKd = 9.5 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 3290 32 None 3 16 Human 9.5 pKd = 9.5 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 3290 32 None 3 16 Human 9.5 pKd = 9.5 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 3290 32 None 3 16 Human 9.5 pKd = 9.5 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 3290 32 None 3 16 Human 9.5 pKd = 9.5 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 3290 32 None 3 16 Human 9.5 pKd = 9.5 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 3290 32 None 3 16 Human 9.5 pKd = 9.5 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 3290 32 None 3 16 Human 9.5 pKd = 9.5 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 3290 32 None 3 16 Human 9.5 pKd = 9.5 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 3290 32 None 3 16 Human 9.5 pKd = 9.5 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 3290 32 None 3 16 Human 9.5 pKd = 9.5 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 3290 32 None 3 16 Human 9.5 pKd = 9.5 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
None 216026 0 3H-RAUWOLSCINE 8 3 Human 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 339 0 0 3 3.3 CN1CCC2(CCN3CCC4=C(C3C2)OC5=CC=CC=C45)N(C1=O)C None
138107169 215950 0 3H-RAUWOLSCINE -1 23 Human 10.4 pKi = 10.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215950 0 3H-RAUWOLSCINE -1 23 Human 10.4 pKi = 10.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
138107169 215950 0 3H-RAUWOLSCINE -3 23 North American opossum 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215950 0 3H-RAUWOLSCINE -3 23 North American opossum 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
138107169 215950 0 3H-RAUWOLSCINE -1 23 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215950 0 3H-RAUWOLSCINE -1 23 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
5268 3654 40 3H-RAUWOLSCINE -1 18 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 3654 40 3H-RAUWOLSCINE -1 18 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 3654 40 3H-RAUWOLSCINE -1 18 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
138107169 215950 0 3H-RAUWOLSCINE -1 23 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215950 0 3H-RAUWOLSCINE -1 23 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
None 216027 0 3H-RAUWOLSCINE 2 3 Human 9.9 pKi = 9.9 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
102 4125 48 3H-RAUWOLSCINE -2 50 Human 9.7 pKi = 9.7 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 4125 48 3H-RAUWOLSCINE -2 50 Human 9.7 pKi = 9.7 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 4125 48 3H-RAUWOLSCINE -2 50 Human 9.7 pKi = 9.7 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 4125 48 3H-RAUWOLSCINE -2 50 Human 9.7 pKi = 9.7 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 4125 48 3H-RAUWOLSCINE -2 50 Human 9.7 pKi = 9.7 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
102 4125 48 3H-RAUWOLSCINE -2 50 Human 9.7 pKi = 9.7 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 4125 48 3H-RAUWOLSCINE -2 50 Human 9.7 pKi = 9.7 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 4125 48 3H-RAUWOLSCINE -2 50 Human 9.7 pKi = 9.7 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 4125 48 3H-RAUWOLSCINE -2 50 Human 9.7 pKi = 9.7 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 4125 48 3H-RAUWOLSCINE -2 50 Human 9.7 pKi = 9.7 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
CHEMBL1196898 216028 0 3H-RAUWOLSCINE -1 3 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 248 3 1 5 1.2 CCOC1(COC2=CC=CC=C2O1)C3=NCCN3 None
102 4125 48 3H-RX821002 -2 50 Human 9.6 pKi = 9.6 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 4125 48 3H-RX821002 -2 50 Human 9.6 pKi = 9.6 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 4125 48 3H-RX821002 -2 50 Human 9.6 pKi = 9.6 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 4125 48 3H-RX821002 -2 50 Human 9.6 pKi = 9.6 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 4125 48 3H-RX821002 -2 50 Human 9.6 pKi = 9.6 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
5268 3654 40 3H-RAUWOLSCINE -1 18 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 3654 40 3H-RAUWOLSCINE -1 18 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 3654 40 3H-RAUWOLSCINE -1 18 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
None 215956 0 3H-RAUWOLSCINE -4 19 Human 9.6 pKi = 9.6 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 4125 48 3H-RAUWOLSCINE -2 50 Human 9.5 pKi = 9.5 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 4125 48 3H-RAUWOLSCINE -2 50 Human 9.5 pKi = 9.5 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 4125 48 3H-RAUWOLSCINE -2 50 Human 9.5 pKi = 9.5 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 4125 48 3H-RAUWOLSCINE -2 50 Human 9.5 pKi = 9.5 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 4125 48 3H-RAUWOLSCINE -2 50 Human 9.5 pKi = 9.5 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
164512323 216029 0 3H-RAUWOLSCINE 5 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
6419959 216029 0 3H-RAUWOLSCINE 5 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
5268 3654 40 3H-RAUWOLSCINE -1 18 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 3654 40 3H-RAUWOLSCINE -1 18 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 3654 40 3H-RAUWOLSCINE -1 18 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
102 4125 48 3H-RAUWOLSCINE 2 50 North American opossum 9.4 pKi = 9.4 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 4125 48 3H-RAUWOLSCINE 2 50 North American opossum 9.4 pKi = 9.4 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 4125 48 3H-RAUWOLSCINE 2 50 North American opossum 9.4 pKi = 9.4 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 4125 48 3H-RAUWOLSCINE 2 50 North American opossum 9.4 pKi = 9.4 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 4125 48 3H-RAUWOLSCINE 2 50 North American opossum 9.4 pKi = 9.4 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
None 215956 0 3H-RAUWOLSCINE -4 19 Human 9.4 pKi = 9.4 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
12576 514 94 3H-RAUWOLSCINE -2 6 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 None
71310 514 94 3H-RAUWOLSCINE -2 6 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 None
CHEMBL353972 514 94 3H-RAUWOLSCINE -2 6 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 None
DB11481 514 94 3H-RAUWOLSCINE -2 6 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 None
None 215959 0 3H-RAUWOLSCINE 1 5 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 295 5 2 3 3.0 C1CC2=CC=CC=C2C(=O)C1CNCCC3=CC=C(C=C3)O None
138107169 215950 0 35S-GTPGammaS -1 23 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215950 0 35S-GTPGammaS -1 23 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
12575 1986 30 3H-RAUWOLSCINE -8 17 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
54459 1986 30 3H-RAUWOLSCINE -8 17 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
CHEMBL10316 1986 30 3H-RAUWOLSCINE -8 17 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
DB12551 1986 30 3H-RAUWOLSCINE -8 17 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
None 216030 0 3H-RAUWOLSCINE 9 3 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 401 6 1 5 0.6 CS(=O)(=O)NCCN(C1CCN2CCC3=CC=CC=C3C2C1)S(=O)(=O)C None
5268 3654 40 3H-RAUWOLSCINE -1 18 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 3654 40 3H-RAUWOLSCINE -1 18 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 3654 40 3H-RAUWOLSCINE -1 18 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
5268 3654 40 3H-RAUWOLSCINE -2 18 North American opossum 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 3654 40 3H-RAUWOLSCINE -2 18 North American opossum 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 3654 40 3H-RAUWOLSCINE -2 18 North American opossum 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
None 215956 0 3H-RAUWOLSCINE -4 19 Human 9.1 pKi = 9.1 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
2601 3778 33 3H-RX821002 -2 21 Human 9.1 pKi = 9.1 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 3778 33 3H-RX821002 -2 21 Human 9.1 pKi = 9.1 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 3778 33 3H-RX821002 -2 21 Human 9.1 pKi = 9.1 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 3778 33 3H-RX821002 -2 21 Human 9.1 pKi = 9.1 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 3778 33 3H-RX821002 -2 21 Human 9.1 pKi = 9.1 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 215950 0 3H-MK912 -1 23 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215950 0 3H-MK912 -1 23 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
108094 3421 27 35S-GTPGammaS -2 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
526 3421 27 35S-GTPGammaS -2 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
528 3421 27 35S-GTPGammaS -2 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
CHEMBL10332 3421 27 35S-GTPGammaS -2 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
44438167 148968 0 UNDEFINED 52 3 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 505 7 1 7 3.8 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)NC4CN5CCC4CC5)cc13)CC2 None
CHEMBL394218 148968 0 UNDEFINED 52 3 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 505 7 1 7 3.8 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)NC4CN5CCC4CC5)cc13)CC2 None
None 215957 0 3H-RAUWOLSCINE 2 6 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 358 4 0 3 2.8 CCCS(=O)(=O)N(C)C1CCN2CCC3=CC=CC=C3C2C1.Cl None
5268 3654 40 3H-MK912 -1 18 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 3654 40 3H-MK912 -1 18 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 3654 40 3H-MK912 -1 18 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
164512323 216029 0 3H-RAUWOLSCINE 5 5 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
6419959 216029 0 3H-RAUWOLSCINE 5 5 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
2389 3329 118 3H-CLONIDINE -10 67 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3329 118 3H-CLONIDINE -10 67 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3329 118 3H-CLONIDINE -10 67 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3329 118 3H-CLONIDINE -10 67 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3329 118 3H-CLONIDINE -10 67 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
6040 216031 0 3H-RAUWOLSCINE 1 3 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 233 2 0 3 2.3 C1CCN(CC1)CC2COC3=CC=CC=C3O2 None
41 1657 0 3H-RX821002 -1 17 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
72036 1657 0 3H-RX821002 -1 17 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
CHEMBL1765294 1657 0 3H-RX821002 -1 17 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
None 215956 0 3H-RAUWOLSCINE -10 19 North American opossum 8.8 pKi = 8.8 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 216029 0 3H-RAUWOLSCINE 5 5 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
6419959 216029 0 3H-RAUWOLSCINE 5 5 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
219050 3371 25 3H-RX821002 -10 21 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
52 3371 25 3H-RX821002 -10 21 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
CHEMBL431367 3371 25 3H-RX821002 -10 21 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
108094 3421 27 3H-MK912 -2 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
526 3421 27 3H-MK912 -2 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
528 3421 27 3H-MK912 -2 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
CHEMBL10332 3421 27 3H-MK912 -2 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
None 216705 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
102 4125 48 3H-RX821002 -26 50 Rat 8.0 pKi = 8.0 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 4125 48 3H-RX821002 -26 50 Rat 8.0 pKi = 8.0 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 4125 48 3H-RX821002 -26 50 Rat 8.0 pKi = 8.0 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 4125 48 3H-RX821002 -26 50 Rat 8.0 pKi = 8.0 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 4125 48 3H-RX821002 -26 50 Rat 8.0 pKi = 8.0 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
4209 3161 75 3H-RAUWOLSCINE -77 33 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3161 75 3H-RAUWOLSCINE -77 33 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3161 75 3H-RAUWOLSCINE -77 33 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3161 75 3H-RAUWOLSCINE -77 33 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3161 75 3H-RAUWOLSCINE -77 33 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3161 75 3H-RAUWOLSCINE -77 33 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
165193 215943 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
4946 215943 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 215943 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 215943 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
CHEMBL27 215943 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
DB00571 215943 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
119570 3157 96 3H-RX821002 -89 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3157 96 3H-RX821002 -89 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3157 96 3H-RX821002 -89 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3157 96 3H-RX821002 -89 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3157 96 3H-RX821002 -89 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
243 3200 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 3200 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 3200 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 3200 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 3200 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 3259 23 3H-RX821002 -2089 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3259 23 3H-RX821002 -2089 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3259 23 3H-RX821002 -2089 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
523 4104 93 35S-GTPGammaS -2 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C None
5707 4104 93 35S-GTPGammaS -2 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C None
CHEMBL297362 4104 93 35S-GTPGammaS -2 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C None
DB11477 4104 93 35S-GTPGammaS -2 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C None
2662 11382 131 3H-CLONIDINE -41 31 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 11382 131 3H-CLONIDINE -41 31 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 15559 106 3H-CLONIDINE -1348 31 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 15559 106 3H-CLONIDINE -1348 31 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
156391 46798 99 3H-CLONIDINE -1 30 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 46798 99 3H-CLONIDINE -1 30 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 46798 99 3H-CLONIDINE -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
44603087 67790 0 UNDEFINED -2951 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 527 5 1 6 4.2 COc1ccc(-c2c(C#N)c(C(=O)NN3CCCCC3)nn2-c2ccccc2I)cc1 None
CHEMBL1079079 67790 0 UNDEFINED -2951 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 527 5 1 6 4.2 COc1ccc(-c2c(C#N)c(C(=O)NN3CCCCC3)nn2-c2ccccc2I)cc1 None
CHEMBL1908985 67790 0 UNDEFINED -2951 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 527 5 1 6 4.2 COc1ccc(-c2c(C#N)c(C(=O)NN3CCCCC3)nn2-c2ccccc2I)cc1 None
10624 70298 19 125I-Clonidine -776 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 70298 19 125I-Clonidine -776 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 70298 19 125I-Clonidine -776 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
DB11664 70298 19 125I-Clonidine -776 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
2244 94231 100 3H-CLONIDINE -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
CHEMBL25 94231 100 3H-CLONIDINE -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
3663 99965 83 3H-CLONIDINE -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
CHEMBL286494 99965 83 3H-CLONIDINE -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
446220 133519 14 3H-CLONIDINE -1778 46 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 133519 14 3H-CLONIDINE -1778 46 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 188273 124 3H-CLONIDINE -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 188273 124 3H-CLONIDINE -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 188273 124 3H-CLONIDINE -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
3672 192531 136 3H-CLONIDINE -1 28 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 192531 136 3H-CLONIDINE -1 28 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 193613 112 3H-CLONIDINE -1 28 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 193613 112 3H-CLONIDINE -1 28 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
4495 196533 92 3H-CLONIDINE -1 30 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 196533 92 3H-CLONIDINE -1 30 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 200549 115 3H-CLONIDINE -1 30 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 200549 115 3H-CLONIDINE -1 30 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 200549 115 3H-CLONIDINE -1 30 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 203023 92 3H-CLONIDINE -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 203023 92 3H-CLONIDINE -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
4054 205499 72 125I-Clonidine -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 205499 72 125I-Clonidine -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 205499 72 125I-Clonidine -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
119607 206201 113 3H-CLONIDINE -97 28 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 206201 113 3H-CLONIDINE -97 28 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
11954224 215951 0 3H-CLONIDINE -4168 60 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
3251 215951 0 3H-CLONIDINE -4168 60 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
CHEMBL1982133 215951 0 3H-CLONIDINE -4168 60 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
DB00696 215951 0 3H-CLONIDINE -4168 60 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
None 215991 0 3H-RAUWOLSCINE -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
25137849 216177 0 3H-CLONIDINE 1 41 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 216177 0 3H-CLONIDINE 1 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 216309 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 216310 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 216311 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 216312 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 216313 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 216314 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 216315 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 216316 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 216325 0 3H-CLONIDINE -16 28 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 216326 0 3H-CLONIDINE -16 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 520 1 7 9 4.3 CC1=CC(=C2C3=C1C4=C5C(=C(C=C4CO)O)C(=O)C6=C(C=C(C7=C6C5=C3C8=C7C(=CC(=C8C2=O)O)O)O)O)O None
None 216327 0 3H-CLONIDINE -2 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.6 C1=CC(=C(C=C1C2=C(C(=C3C(=CC(=O)C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
None 216329 0 3H-CLONIDINE -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 448 3 7 11 0.4 CC1C(C(C(C(O1)OC2=C(OC3=CC(=O)C=C(C3=C2O)O)C4=CC(=C(C=C4)O)O)O)O)O None
None 216340 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 216387 0 3H-CLONIDINE -1 30 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 216388 0 3H-CLONIDINE -1 29 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 216389 0 3H-CLONIDINE -1 29 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 216390 0 3H-CLONIDINE -1 28 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 216391 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 216392 0 3H-CLONIDINE -1 30 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 216393 0 3H-CLONIDINE -7 29 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 216487 0 3H-CLONIDINE -4570 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 6 0 3 5.0 CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3 None
115237 55583 119 3H-RAUWOLSCINE -29 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55583 119 3H-RAUWOLSCINE -29 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 55583 119 3H-RAUWOLSCINE -29 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
11293787 148211 0 UNDEFINED 27 3 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 447 6 0 5 5.8 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4F)cc13)CC2 None
CHEMBL393597 148211 0 UNDEFINED 27 3 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 447 6 0 5 5.8 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4F)cc13)CC2 None
1343 1887 62 3H-MK912 -251 9 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
3519 1887 62 3H-MK912 -251 9 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
522 1887 62 3H-MK912 -251 9 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
CHEMBL862 1887 62 3H-MK912 -251 9 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
DB01018 1887 62 3H-MK912 -251 9 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
1615 167789 24 3H-CLONIDINE -3 45 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167789 24 3H-CLONIDINE -3 45 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
2726 918 68 3H-RAUWOLSCINE -67 73 North American opossum 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 918 68 3H-RAUWOLSCINE -67 73 North American opossum 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 918 68 3H-RAUWOLSCINE -67 73 North American opossum 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 918 68 3H-RAUWOLSCINE -67 73 North American opossum 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 918 68 3H-RAUWOLSCINE -67 73 North American opossum 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1220 187 55 3H-RAUWOLSCINE -93 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 55 3H-RAUWOLSCINE -93 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 55 3H-RAUWOLSCINE -93 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 55 3H-RAUWOLSCINE -93 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
135409468 2033 69 3H-CLONIDINE -41 40 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 2033 69 3H-CLONIDINE -41 40 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 2033 69 3H-CLONIDINE -41 40 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
186 1805 52 3H-CLONIDINE -194 17 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 1805 52 3H-CLONIDINE -194 17 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 1805 52 3H-CLONIDINE -194 17 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
164512323 216029 0 3H-RAUWOLSCINE 5 5 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
6419959 216029 0 3H-RAUWOLSCINE 5 5 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
2142 3094 58 3H-RAUWOLSCINE -7 37 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3094 58 3H-RAUWOLSCINE -7 37 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3094 58 3H-RAUWOLSCINE -7 37 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3094 58 3H-RAUWOLSCINE -7 37 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3094 58 3H-RAUWOLSCINE -7 37 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3094 58 3H-RAUWOLSCINE -7 37 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
2402 3368 62 3H-RX821002 -5 25 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3368 62 3H-RX821002 -5 25 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3368 62 3H-RX821002 -5 25 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3368 62 3H-RX821002 -5 25 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3368 62 3H-RX821002 -5 25 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
1212 1660 50 3H-RAUWOLSCINE -54 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1660 50 3H-RAUWOLSCINE -54 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1660 50 3H-RAUWOLSCINE -54 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1660 50 3H-RAUWOLSCINE -54 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1660 50 3H-RAUWOLSCINE -54 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
25137849 216177 0 3H-CLONIDINE 1 41 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 216177 0 3H-CLONIDINE 1 41 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
7153 98018 77 3H-CLONIDINE -6 34 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98018 77 3H-CLONIDINE -6 34 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
3658 4105 53 35S-GTPGammaS -17 8 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
517 4105 53 35S-GTPGammaS -17 8 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
5709 4105 53 35S-GTPGammaS -17 8 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
CHEMBL312448 4105 53 35S-GTPGammaS -17 8 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
DB06694 4105 53 35S-GTPGammaS -17 8 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
122211 462 0 3H-RAUWOLSCINE -9 6 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
524 462 0 3H-RAUWOLSCINE -9 6 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
3036780 107529 20 3H-RAUWOLSCINE -72 54 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
46780481 107529 20 3H-RAUWOLSCINE -72 54 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107529 20 3H-RAUWOLSCINE -72 54 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107529 20 3H-RAUWOLSCINE -72 54 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107529 20 3H-RAUWOLSCINE -72 54 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL504548 107529 20 3H-RAUWOLSCINE -72 54 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
DB06216 107529 20 3H-RAUWOLSCINE -72 54 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
None 216238 0 3H-RX821002 47 2 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 457 7 1 3 4.9 CCC(=O)NC1=C(C=C(C=C1C)C(=O)N2CCC(CC2)N(C)CCC3=CC=CC=C3)C.Cl None
2803 954 58 35S-GTPGammaS -4 19 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 954 58 35S-GTPGammaS -4 19 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 954 58 35S-GTPGammaS -4 19 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 954 58 35S-GTPGammaS -4 19 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 954 58 35S-GTPGammaS -4 19 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
484 2856 51 35S-GTPGammaS -8 35 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2856 51 35S-GTPGammaS -8 35 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2856 51 35S-GTPGammaS -8 35 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
67409 216032 0 3H-RAUWOLSCINE -2 3 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 235 2 0 1 3.9 C=CCN1CC2=CC=CC=C2C3=CC=CC=C3C1 None
8966 216032 0 3H-RAUWOLSCINE -2 3 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 235 2 0 1 3.9 C=CCN1CC2=CC=CC=C2C3=CC=CC=C3C1 None
None 216033 0 3H-RAUWOLSCINE -1 3 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 200 3 1 1 2.8 CC1=C(C(=CC=C1)C)CCC2=CN=CN2 None
4209 3161 75 3H-CLONIDINE -77 33 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3161 75 3H-CLONIDINE -77 33 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3161 75 3H-CLONIDINE -77 33 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3161 75 3H-CLONIDINE -77 33 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3161 75 3H-CLONIDINE -77 33 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3161 75 3H-CLONIDINE -77 33 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
185 4004 60 3H-CLONIDINE -4466 38 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 4004 60 3H-CLONIDINE -4466 38 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 4004 60 3H-CLONIDINE -4466 38 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 4004 60 3H-CLONIDINE -4466 38 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
4209 3161 75 3H-RAUWOLSCINE -77 33 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3161 75 3H-RAUWOLSCINE -77 33 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3161 75 3H-RAUWOLSCINE -77 33 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3161 75 3H-RAUWOLSCINE -77 33 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3161 75 3H-RAUWOLSCINE -77 33 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3161 75 3H-RAUWOLSCINE -77 33 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
68602 205124 80 35S-GTPGammaS -4 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 205124 80 35S-GTPGammaS -4 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
21830793 91833 10 3H-8-OH-DPAT -102 45 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 91833 10 3H-8-OH-DPAT -102 45 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
1223 952 41 3H-RAUWOLSCINE -85 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 952 41 3H-RAUWOLSCINE -85 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 952 41 3H-RAUWOLSCINE -85 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
103 4151 61 3H-RAUWOLSCINE -33 54 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4151 61 3H-RAUWOLSCINE -33 54 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4151 61 3H-RAUWOLSCINE -33 54 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4151 61 3H-RAUWOLSCINE -33 54 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4151 61 3H-RAUWOLSCINE -33 54 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
133621 2010 0 35S-GTPGammaS -3 5 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 244 3 0 4 2.3 CCn1ccnc1CC1COc2c(O1)cccc2 None
3470 2010 0 35S-GTPGammaS -3 5 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 244 3 0 4 2.3 CCn1ccnc1CC1COc2c(O1)cccc2 None
CHEMBL347695 2010 0 35S-GTPGammaS -3 5 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 244 3 0 4 2.3 CCn1ccnc1CC1COc2c(O1)cccc2 None
179 400 115 125I-Clonidine -40 51 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 400 115 125I-Clonidine -40 51 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 400 115 125I-Clonidine -40 51 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 400 115 125I-Clonidine -40 51 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 400 115 125I-Clonidine -40 51 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
162265 202272 22 3H-CLONIDINE -8 45 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 202272 22 3H-CLONIDINE -8 45 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 202272 22 3H-CLONIDINE -8 45 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
213 3851 55 125I-Clonidine -6 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3851 55 125I-Clonidine -6 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3851 55 125I-Clonidine -6 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3851 55 125I-Clonidine -6 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3851 55 125I-Clonidine -6 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
1524 2179 96 3H-RAUWOLSCINE -120 52 Human 6.8 pKi = 6.8 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 2179 96 3H-RAUWOLSCINE -120 52 Human 6.8 pKi = 6.8 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 2179 96 3H-RAUWOLSCINE -120 52 Human 6.8 pKi = 6.8 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 2179 96 3H-RAUWOLSCINE -120 52 Human 6.8 pKi = 6.8 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 2179 96 3H-RAUWOLSCINE -120 52 Human 6.8 pKi = 6.8 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 2179 96 3H-RAUWOLSCINE -120 52 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3294 2004 111 3H-RX821002 -16 45 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2004 111 3H-RX821002 -16 45 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2004 111 3H-RX821002 -16 45 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2004 111 3H-RX821002 -16 45 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2004 111 3H-RX821002 -16 45 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
3294 2004 111 3H-RX821002 -16 45 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2004 111 3H-RX821002 -16 45 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2004 111 3H-RX821002 -16 45 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2004 111 3H-RX821002 -16 45 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2004 111 3H-RX821002 -16 45 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1028 291 71 35S-GTPGammaS -67 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 291 71 35S-GTPGammaS -67 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
479 291 71 35S-GTPGammaS -67 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 291 71 35S-GTPGammaS -67 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 291 71 35S-GTPGammaS -67 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 291 71 35S-GTPGammaS -67 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
3036780 107529 20 3H-CLONIDINE -72 54 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
46780481 107529 20 3H-CLONIDINE -72 54 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107529 20 3H-CLONIDINE -72 54 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107529 20 3H-CLONIDINE -72 54 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107529 20 3H-CLONIDINE -72 54 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL504548 107529 20 3H-CLONIDINE -72 54 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
DB06216 107529 20 3H-CLONIDINE -72 54 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
1830 2588 44 3H-CLONIDINE -6 28 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2588 44 3H-CLONIDINE -6 28 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2588 44 3H-CLONIDINE -6 28 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2588 44 3H-CLONIDINE -6 28 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2588 44 3H-CLONIDINE -6 28 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1816 2538 102 3H-RAUWOLSCINE -38 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 2538 102 3H-RAUWOLSCINE -38 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 2538 102 3H-RAUWOLSCINE -38 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 2538 102 3H-RAUWOLSCINE -38 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 2538 102 3H-RAUWOLSCINE -38 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
11225732 93655 0 UNDEFINED 16 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 497 6 0 5 6.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4C(F)(F)F)cc13)CC2 None
CHEMBL246852 93655 0 UNDEFINED 16 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 497 6 0 5 6.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4C(F)(F)F)cc13)CC2 None
3337 206365 27 3H-CLONIDINE -13 41 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206365 27 3H-CLONIDINE -13 41 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206365 27 3H-CLONIDINE -13 41 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206365 27 3H-CLONIDINE -13 41 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206365 27 3H-CLONIDINE -13 41 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 206365 27 3H-CLONIDINE -13 41 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
124 2979 47 3H-MK912 -60 32 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2979 47 3H-MK912 -60 32 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2979 47 3H-MK912 -60 32 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2979 47 3H-MK912 -60 32 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2979 47 3H-MK912 -60 32 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
None 216237 0 3H-CLONIDINE -27542 30 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
12575 1986 30 UNDEFINED -8 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
54459 1986 30 UNDEFINED -8 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
CHEMBL10316 1986 30 UNDEFINED -8 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
DB12551 1986 30 UNDEFINED -8 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
44438147 93487 0 UNDEFINED 19 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 406 5 1 9 2.5 COc1cc2c(cc1OC)CN(Cc1cnc(N)n3nc(-c4ccco4)nc13)CC2 None
CHEMBL246228 93487 0 UNDEFINED 19 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 406 5 1 9 2.5 COc1cc2c(cc1OC)CN(Cc1cnc(N)n3nc(-c4ccco4)nc13)CC2 None
44438152 93606 0 UNDEFINED 42 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 459 7 0 6 5.7 COc1cccc(-c2cc3c(CN4CCc5cc(OC)c(OC)cc5C4)ccc(OC)c3o2)c1 None
CHEMBL246639 93606 0 UNDEFINED 42 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 459 7 0 6 5.7 COc1cccc(-c2cc3c(CN4CCc5cc(OC)c(OC)cc5C4)ccc(OC)c3o2)c1 None
12575 1986 30 35S-GTPGammaS -8 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
54459 1986 30 35S-GTPGammaS -8 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
CHEMBL10316 1986 30 35S-GTPGammaS -8 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
DB12551 1986 30 35S-GTPGammaS -8 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
135 2530 43 3H-RAUWOLSCINE -14 58 North American opossum 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2530 43 3H-RAUWOLSCINE -14 58 North American opossum 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2530 43 3H-RAUWOLSCINE -14 58 North American opossum 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2530 43 3H-RAUWOLSCINE -14 58 North American opossum 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2530 43 3H-RAUWOLSCINE -14 58 North American opossum 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2435 721 100 35S-GTPGammaS -33 12 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
395 721 100 35S-GTPGammaS -33 12 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
520 721 100 35S-GTPGammaS -33 12 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
5386 721 100 35S-GTPGammaS -33 12 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
CHEMBL844 721 100 35S-GTPGammaS -33 12 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
DB00484 721 100 35S-GTPGammaS -33 12 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
3337 206365 27 3H-CLONIDINE -13 41 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206365 27 3H-CLONIDINE -13 41 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206365 27 3H-CLONIDINE -13 41 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206365 27 3H-CLONIDINE -13 41 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206365 27 3H-CLONIDINE -13 41 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 206365 27 3H-CLONIDINE -13 41 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
12575 1986 30 3H-RAUWOLSCINE -1 17 North American opossum 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
54459 1986 30 3H-RAUWOLSCINE -1 17 North American opossum 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
CHEMBL10316 1986 30 3H-RAUWOLSCINE -1 17 North American opossum 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
DB12551 1986 30 3H-RAUWOLSCINE -1 17 North American opossum 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
68602 205124 80 3H-RX821002 -4 8 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C None
CHEMBL77921 205124 80 3H-RX821002 -4 8 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C None
123981 16457 22 3H-RAUWOLSCINE -4 8 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 195 0 0 1 2.4 CN1CCc2cccc(Cl)c2CC1 None
CHEMBL123349 16457 22 3H-RAUWOLSCINE -4 8 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 195 0 0 1 2.4 CN1CCc2cccc(Cl)c2CC1 None
CHEMBL536803 16457 22 3H-RAUWOLSCINE -4 8 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 195 0 0 1 2.4 CN1CCc2cccc(Cl)c2CC1 None
12576 514 94 3H-RAUWOLSCINE -4 6 North American opossum 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 None
71310 514 94 3H-RAUWOLSCINE -4 6 North American opossum 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 None
CHEMBL353972 514 94 3H-RAUWOLSCINE -4 6 North American opossum 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 None
DB11481 514 94 3H-RAUWOLSCINE -4 6 North American opossum 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 None
135398737 957 93 3H-RAUWOLSCINE -3 91 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 957 93 3H-RAUWOLSCINE -3 91 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 957 93 3H-RAUWOLSCINE -3 91 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 957 93 3H-RAUWOLSCINE -3 91 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 957 93 3H-RAUWOLSCINE -3 91 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
16725934 147421 0 UNDEFINED 38 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 429 6 0 5 5.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4)cc13)CC2 None
CHEMBL392992 147421 0 UNDEFINED 38 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 429 6 0 5 5.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4)cc13)CC2 None
138107169 215950 0 3H-RAUWOLSCINE -3 23 North American opossum 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215950 0 3H-RAUWOLSCINE -3 23 North American opossum 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
2216 446 50 35S-GTPGammaS -3 6 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
229 446 50 35S-GTPGammaS -3 6 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
7117 446 50 35S-GTPGammaS -3 6 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
CHEMBL647 446 50 35S-GTPGammaS -3 6 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
DB00964 446 50 35S-GTPGammaS -3 6 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
135398745 2912 112 3H-RAUWOLSCINE -30 66 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 2912 112 3H-RAUWOLSCINE -30 66 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 2912 112 3H-RAUWOLSCINE -30 66 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 2912 112 3H-RAUWOLSCINE -30 66 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
None 216133 0 3H-CLONIDINE -2238 24 Human 5.7 pKi = 5.7 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
6917970 3689 61 3H-CLONIDINE -48 34 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
8370 3689 61 3H-CLONIDINE -48 34 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
CHEMBL487387 3689 61 3H-CLONIDINE -48 34 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
None 216339 0 3H-RX821002 -29 19 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 451 8 2 4 3.2 CCNC(=O)N(CCCN(C)C)C(=O)C1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)CC=C None
2695 3839 81 3H-RAUWOLSCINE -30 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
5504 3839 81 3H-RAUWOLSCINE -30 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
7310 3839 81 3H-RAUWOLSCINE -30 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
CHEMBL770 3839 81 3H-RAUWOLSCINE -30 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
DB00797 3839 81 3H-RAUWOLSCINE -30 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
2726 918 68 3H-RAUWOLSCINE -31 73 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 918 68 3H-RAUWOLSCINE -31 73 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 918 68 3H-RAUWOLSCINE -31 73 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 918 68 3H-RAUWOLSCINE -31 73 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 918 68 3H-RAUWOLSCINE -31 73 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
124 2979 47 35S-GTPGammaS -60 32 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2979 47 35S-GTPGammaS -60 32 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2979 47 35S-GTPGammaS -60 32 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2979 47 35S-GTPGammaS -60 32 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2979 47 35S-GTPGammaS -60 32 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
3337 206365 27 3H-CLONIDINE -13 41 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206365 27 3H-CLONIDINE -13 41 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206365 27 3H-CLONIDINE -13 41 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206365 27 3H-CLONIDINE -13 41 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206365 27 3H-CLONIDINE -13 41 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 206365 27 3H-CLONIDINE -13 41 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
1353 1909 93 3H-RAUWOLSCINE -87 86 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1909 93 3H-RAUWOLSCINE -87 86 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1909 93 3H-RAUWOLSCINE -87 86 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1909 93 3H-RAUWOLSCINE -87 86 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1909 93 3H-RAUWOLSCINE -87 86 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2142 3094 58 35S-GTPGammaS -7 37 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3094 58 35S-GTPGammaS -7 37 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3094 58 35S-GTPGammaS -7 37 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3094 58 35S-GTPGammaS -7 37 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3094 58 35S-GTPGammaS -7 37 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3094 58 35S-GTPGammaS -7 37 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
104911 216017 0 3H-CLONIDINE -10715 38 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
135 2530 43 3H-RAUWOLSCINE -6 58 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2530 43 3H-RAUWOLSCINE -6 58 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2530 43 3H-RAUWOLSCINE -6 58 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2530 43 3H-RAUWOLSCINE -6 58 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2530 43 3H-RAUWOLSCINE -6 58 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
10297 27110 30 3H-CLONIDINE 1 44 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 27110 30 3H-CLONIDINE 1 44 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
5524 216462 0 35S-GTPGammaS -2 4 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 215 1 2 3 1.9 C1CCC2=C(C1)C=CC=C2NC3=NCCN3 None
138107169 215950 0 3H-RAUWOLSCINE -1 23 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215950 0 3H-RAUWOLSCINE -1 23 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
31101 728 40 3H-RX821002 -36 36 Human 7.6 pKi = 7.6 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
35 728 40 3H-RX821002 -36 36 Human 7.6 pKi = 7.6 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
403 728 40 3H-RX821002 -36 36 Human 7.6 pKi = 7.6 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 728 40 3H-RX821002 -36 36 Human 7.6 pKi = 7.6 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 728 40 3H-RX821002 -36 36 Human 7.6 pKi = 7.6 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
2337 3254 77 125I-Clonidine -10 63 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 3254 77 3H-CLONIDINE -10 63 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3254 77 125I-Clonidine -10 63 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3254 77 3H-CLONIDINE -10 63 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3254 77 125I-Clonidine -10 63 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3254 77 3H-CLONIDINE -10 63 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3254 77 125I-Clonidine -10 63 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3254 77 3H-CLONIDINE -10 63 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3254 77 125I-Clonidine -10 63 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3254 77 3H-CLONIDINE -10 63 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1212 1660 50 3H-CLONIDINE -54 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1660 50 3H-CLONIDINE -54 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1660 50 3H-CLONIDINE -54 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1660 50 3H-CLONIDINE -54 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1660 50 3H-CLONIDINE -54 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398745 2912 112 3H-CLONIDINE -30 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2912 112 3H-CLONIDINE -30 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2912 112 3H-CLONIDINE -30 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2912 112 3H-CLONIDINE -30 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
162265 202272 22 3H-CLONIDINE -8 45 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 202272 22 3H-CLONIDINE -8 45 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 202272 22 3H-CLONIDINE -8 45 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
1212 1660 50 3H-CLONIDINE -54 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1660 50 3H-CLONIDINE -54 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1660 50 3H-CLONIDINE -54 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1660 50 3H-CLONIDINE -54 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1660 50 3H-CLONIDINE -54 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398745 2912 112 3H-CLONIDINE -30 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2912 112 3H-CLONIDINE -30 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2912 112 3H-CLONIDINE -30 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2912 112 3H-CLONIDINE -30 66 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2142 3094 58 3H-RAUWOLSCINE -7 37 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3094 58 3H-RAUWOLSCINE -7 37 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3094 58 3H-RAUWOLSCINE -7 37 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3094 58 3H-RAUWOLSCINE -7 37 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3094 58 3H-RAUWOLSCINE -7 37 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3094 58 3H-RAUWOLSCINE -7 37 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
2337 3254 77 3H-CLONIDINE -10 63 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3254 77 3H-CLONIDINE -10 63 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3254 77 3H-CLONIDINE -10 63 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3254 77 3H-CLONIDINE -10 63 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3254 77 3H-CLONIDINE -10 63 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2181 3126 46 3H-RAUWOLSCINE -36 35 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 3126 46 3H-RAUWOLSCINE -36 35 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 3126 46 3H-RAUWOLSCINE -36 35 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 3126 46 3H-RAUWOLSCINE -36 35 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 3126 46 3H-RAUWOLSCINE -36 35 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
102 4125 48 3H-MK912 -2 50 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 4125 48 3H-MK912 -2 50 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 4125 48 3H-MK912 -2 50 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 4125 48 3H-MK912 -2 50 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 4125 48 3H-MK912 -2 50 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
None 215956 0 3H-MK912 -4 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
2389 3329 118 3H-RAUWOLSCINE -10 67 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3329 118 3H-RAUWOLSCINE -10 67 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3329 118 3H-RAUWOLSCINE -10 67 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3329 118 3H-RAUWOLSCINE -10 67 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3329 118 3H-RAUWOLSCINE -10 67 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
931 216461 0 35S-GTPGammaS 1 4 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 128 0 0 0 2.8 C1=CC=C2C=CC=CC2=C1 None
44438168 93816 0 UNDEFINED 53 3 Human 8.5 pKi = 8.5 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 93816 0 UNDEFINED 53 3 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 533 7 0 7 4.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)N4CCC(N5CCCC5)CC4)cc13)CC2 None
115237 55583 119 3H-CLONIDINE -29 55 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55583 119 3H-CLONIDINE -29 55 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 55583 119 3H-CLONIDINE -29 55 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
135 2530 43 3H-RAUWOLSCINE -6 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2530 43 3H-RAUWOLSCINE -6 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2530 43 3H-RAUWOLSCINE -6 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2530 43 3H-RAUWOLSCINE -6 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2530 43 3H-RAUWOLSCINE -6 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
122211 462 0 3H-RAUWOLSCINE -9 6 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
524 462 0 3H-RAUWOLSCINE -9 6 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
4209 3161 75 35S-GTPGammaS -77 33 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3161 75 35S-GTPGammaS -77 33 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3161 75 35S-GTPGammaS -77 33 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3161 75 35S-GTPGammaS -77 33 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3161 75 35S-GTPGammaS -77 33 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3161 75 35S-GTPGammaS -77 33 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
124 2979 47 3H-RAUWOLSCINE -60 32 Human 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 2979 47 3H-RAUWOLSCINE -60 32 Human 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 2979 47 3H-RAUWOLSCINE -60 32 Human 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 2979 47 3H-RAUWOLSCINE -60 32 Human 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 2979 47 3H-RAUWOLSCINE -60 32 Human 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
122211 462 0 3H-MK912 -9 6 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
524 462 0 3H-MK912 -9 6 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
None 216034 0 3H-RAUWOLSCINE -5 3 Human 6.5 pKi = 6.5 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
2142 3094 58 3H-RAUWOLSCINE -12 37 North American opossum 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3094 58 3H-RAUWOLSCINE -12 37 North American opossum 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3094 58 3H-RAUWOLSCINE -12 37 North American opossum 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3094 58 3H-RAUWOLSCINE -12 37 North American opossum 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3094 58 3H-RAUWOLSCINE -12 37 North American opossum 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3094 58 3H-RAUWOLSCINE -12 37 North American opossum 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
135398737 957 93 3H-CLONIDINE -3 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 957 93 3H-RAUWOLSCINE -3 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 957 93 3H-CLONIDINE -3 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 957 93 3H-RAUWOLSCINE -3 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 957 93 3H-CLONIDINE -3 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 957 93 3H-RAUWOLSCINE -3 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 957 93 3H-CLONIDINE -3 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 957 93 3H-RAUWOLSCINE -3 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 957 93 3H-CLONIDINE -3 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 957 93 3H-RAUWOLSCINE -3 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
3075702 217330 0 3H-RAUWOLSCINE 1 37 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 198 3 1 3 1.5 C1CNC1COC2=CN=C(C=C2)Cl None
1267 3802 49 3H-RAUWOLSCINE -144 28 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3802 49 3H-RAUWOLSCINE -144 28 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3802 49 3H-RAUWOLSCINE -144 28 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
2337 3254 77 3H-RAUWOLSCINE -10 63 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3254 77 3H-RAUWOLSCINE -10 63 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3254 77 3H-RAUWOLSCINE -10 63 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3254 77 3H-RAUWOLSCINE -10 63 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3254 77 3H-RAUWOLSCINE -10 63 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
4209 3161 75 3H-RAUWOLSCINE -97 33 North American opossum 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3161 75 3H-RAUWOLSCINE -97 33 North American opossum 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3161 75 3H-RAUWOLSCINE -97 33 North American opossum 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3161 75 3H-RAUWOLSCINE -97 33 North American opossum 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3161 75 3H-RAUWOLSCINE -97 33 North American opossum 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3161 75 3H-RAUWOLSCINE -97 33 North American opossum 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
25058166 215958 0 3H-RX821002 -18 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 215958 0 3H-RX821002 -18 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
242 470 124 3H-CLONIDINE -23 52 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-CLONIDINE -23 52 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-CLONIDINE -23 52 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-CLONIDINE -23 52 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-CLONIDINE -23 52 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
2726 918 68 3H-RAUWOLSCINE -31 73 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 918 68 3H-RAUWOLSCINE -31 73 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 918 68 3H-RAUWOLSCINE -31 73 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 918 68 3H-RAUWOLSCINE -31 73 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 918 68 3H-RAUWOLSCINE -31 73 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
242 470 124 3H-CLONIDINE -23 52 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-CLONIDINE -23 52 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-CLONIDINE -23 52 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-CLONIDINE -23 52 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-CLONIDINE -23 52 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
2695 3839 81 35S-GTPGammaS -30 6 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
5504 3839 81 35S-GTPGammaS -30 6 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
7310 3839 81 35S-GTPGammaS -30 6 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
CHEMBL770 3839 81 35S-GTPGammaS -30 6 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
DB00797 3839 81 35S-GTPGammaS -30 6 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
16362 3123 71 3H-CLONIDINE -263 30 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3123 71 3H-CLONIDINE -263 30 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3123 71 3H-CLONIDINE -263 30 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3123 71 3H-CLONIDINE -263 30 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3123 71 3H-CLONIDINE -263 30 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
242 470 124 3H-CLONIDINE -23 52 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-CLONIDINE -23 52 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-CLONIDINE -23 52 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-CLONIDINE -23 52 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-CLONIDINE -23 52 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
1343 1887 62 35S-GTPGammaS -251 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
3519 1887 62 35S-GTPGammaS -251 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
522 1887 62 35S-GTPGammaS -251 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
CHEMBL862 1887 62 35S-GTPGammaS -251 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
DB01018 1887 62 35S-GTPGammaS -251 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
214 3858 58 3H-CLONIDINE -60 30 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3858 58 3H-CLONIDINE -60 30 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3858 58 3H-CLONIDINE -60 30 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3858 58 3H-CLONIDINE -60 30 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3858 58 3H-CLONIDINE -60 30 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3858 58 3H-CLONIDINE -60 30 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
None 217651 0 UNDEFINED - 1 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.5 C1=CC(=C(C=C1C2=C(C(=O)C3=C(C=C(C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
135398737 957 93 3H-RAUWOLSCINE -3 91 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 957 93 3H-RAUWOLSCINE -3 91 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 957 93 3H-RAUWOLSCINE -3 91 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 957 93 3H-RAUWOLSCINE -3 91 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 957 93 3H-RAUWOLSCINE -3 91 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
44438166 93815 0 UNDEFINED 33 3 Human 8.4 pKi = 8.4 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 93815 0 UNDEFINED 33 3 Human 8.4 pKi = 8.4 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
135 2530 43 3H-RAUWOLSCINE -14 58 North American opossum 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2530 43 3H-RAUWOLSCINE -14 58 North American opossum 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2530 43 3H-RAUWOLSCINE -14 58 North American opossum 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2530 43 3H-RAUWOLSCINE -14 58 North American opossum 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2530 43 3H-RAUWOLSCINE -14 58 North American opossum 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
3652 46242 70 None -2 9 Human 8.3 pKi = 8.3 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscine
Drug Central 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 None
CHEMBL1535 46242 70 None -2 9 Human 8.3 pKi = 8.3 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscine
Drug Central 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 None
None 216327 0 3H-CLONIDINE -2 28 Human 5.4 pKi = 5.4 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
11079 2731 63 35S-GTPGammaS -2 5 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
3369 2731 63 35S-GTPGammaS -2 5 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
4436 2731 63 35S-GTPGammaS -2 5 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
5509 2731 63 35S-GTPGammaS -2 5 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
CHEMBL761 2731 63 35S-GTPGammaS -2 5 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
DB06711 2731 63 35S-GTPGammaS -2 5 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
2726 918 68 3H-RAUWOLSCINE -31 73 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 918 68 3H-RAUWOLSCINE -31 73 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 918 68 3H-RAUWOLSCINE -31 73 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 918 68 3H-RAUWOLSCINE -31 73 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 918 68 3H-RAUWOLSCINE -31 73 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
6852400 215935 0 3H-RAUWOLSCINE -104 22 Human 7.4 pKi = 7.4 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 215935 0 3H-RAUWOLSCINE -104 22 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
104870 98878 47 3H-RX821002 -3 21 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 98878 47 3H-RX821002 -3 21 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 98878 47 3H-RX821002 -3 21 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
122295 9866 7 3H-RAUWOLSCINE -1 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 None
CHEMBL114166 9866 7 3H-RAUWOLSCINE -1 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 None
None 216237 0 3H-CLONIDINE -27542 30 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
3952 1886 38 35S-GTPGammaS -19 12 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5353646 1886 38 35S-GTPGammaS -19 12 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5443 1886 38 35S-GTPGammaS -19 12 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5702063 1886 38 35S-GTPGammaS -19 12 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
CHEMBL1331786 1886 38 35S-GTPGammaS -19 12 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
CHEMBL420 1886 38 35S-GTPGammaS -19 12 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
DB00629 1886 38 35S-GTPGammaS -19 12 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
45266826 217689 0 3H-RAUWOLSCINE -6 8 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 177 3 1 2 1.8 CC1=CC=C(C=C1)C(=O)C(C)NC None
2435 3588 83 3H-CLONIDINE -104 49 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2435 3588 83 3H-RAUWOLSCINE -104 49 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3588 83 3H-CLONIDINE -104 49 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3588 83 3H-RAUWOLSCINE -104 49 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3588 83 3H-CLONIDINE -104 49 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3588 83 3H-RAUWOLSCINE -104 49 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3588 83 3H-CLONIDINE -104 49 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3588 83 3H-RAUWOLSCINE -104 49 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3588 83 3H-CLONIDINE -104 49 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3588 83 3H-RAUWOLSCINE -104 49 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2726 918 68 3H-CLONIDINE -31 73 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 918 68 3H-CLONIDINE -31 73 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 918 68 3H-CLONIDINE -31 73 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 918 68 3H-CLONIDINE -31 73 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 918 68 3H-CLONIDINE -31 73 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
68712 100336 60 35S-GTPGammaS -1 5 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 None
CHEMBL289480 100336 60 35S-GTPGammaS -1 5 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 None
122211 462 0 3H-RAUWOLSCINE -30 6 North American opossum 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
524 462 0 3H-RAUWOLSCINE -30 6 North American opossum 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
2719 916 74 None -6 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscine
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
5535 916 74 None -6 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscine
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
607 916 74 None -6 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscine
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
CHEMBL76 916 74 None -6 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscine
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
DB00608 916 74 None -6 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscine
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
164512323 216029 0 3H-RAUWOLSCINE 5 5 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
6419959 216029 0 3H-RAUWOLSCINE 5 5 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
2142 3094 58 3H-RX821002 -7 37 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3094 58 3H-RX821002 -7 37 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3094 58 3H-RX821002 -7 37 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3094 58 3H-RX821002 -7 37 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3094 58 3H-RX821002 -7 37 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3094 58 3H-RX821002 -7 37 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5280805 85403 81 None -29 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to adrenergic alpha2c receptorBinding affinity to adrenergic alpha2c 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 85403 81 None -29 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to adrenergic alpha2c receptorBinding affinity to adrenergic alpha2c 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
135 2530 43 3H-RAUWOLSCINE -6 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2530 43 3H-RAUWOLSCINE -6 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2530 43 3H-RAUWOLSCINE -6 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2530 43 3H-RAUWOLSCINE -6 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2530 43 3H-RAUWOLSCINE -6 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2695 3839 81 None -30 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
5504 3839 81 None -30 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
7310 3839 81 None -30 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
CHEMBL770 3839 81 None -30 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
DB00797 3839 81 None -30 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
222757 99374 73 None 1 3 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O None
CHEMBL282575 99374 73 None 1 3 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O None
28417 40037 49 None -1 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 40037 49 None -1 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
DB01406 40037 49 None -1 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
448537 160248 89 None -21 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
CHEMBL411 160248 89 None -21 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
12574 2603 88 None -87 6 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
Drug Central 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC None
4810 2603 88 None -87 6 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
Drug Central 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC None
CHEMBL19236 2603 88 None -87 6 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
Drug Central 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC None
DB09242 2603 88 None -87 6 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
Drug Central 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC None
6018 11063 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 11063 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
2402 3368 62 None -5 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3368 62 None -5 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3368 62 None -5 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3368 62 None -5 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3368 62 None -5 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
104903 56342 17 None -1 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 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 None
CHEMBL1630578 56342 17 None -1 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 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 None
3598 187819 76 None -1 7 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 187819 76 None -1 7 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl None
2803 954 58 35S-GTPGammaS -4 19 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 954 58 35S-GTPGammaS -4 19 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 954 58 35S-GTPGammaS -4 19 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 954 58 35S-GTPGammaS -4 19 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 954 58 35S-GTPGammaS -4 19 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
11954259 215977 0 3H-CLONIDINE -173 44 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
11954259 215977 0 3H-CLONIDINE -173 44 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
119570 3157 96 3H-CLONIDINE -89 40 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3157 96 3H-CLONIDINE -89 40 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3157 96 3H-CLONIDINE -89 40 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3157 96 3H-CLONIDINE -89 40 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3157 96 3H-CLONIDINE -89 40 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
100 3803 58 3H-RAUWOLSCINE -27 55 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 3803 58 3H-RAUWOLSCINE -27 55 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 3803 58 3H-RAUWOLSCINE -27 55 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 3803 58 3H-RAUWOLSCINE -27 55 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 3803 58 3H-RAUWOLSCINE -27 55 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
1353 1909 93 3H-CLONIDINE -87 86 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
1353 1909 93 3H-RAUWOLSCINE -87 86 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 1909 93 3H-CLONIDINE -87 86 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 1909 93 3H-RAUWOLSCINE -87 86 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 1909 93 3H-CLONIDINE -87 86 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 1909 93 3H-RAUWOLSCINE -87 86 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 1909 93 3H-CLONIDINE -87 86 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 1909 93 3H-RAUWOLSCINE -87 86 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 1909 93 3H-CLONIDINE -87 86 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 1909 93 3H-RAUWOLSCINE -87 86 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
4209 3161 75 3H-MK912 -77 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3161 75 3H-MK912 -77 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3161 75 3H-MK912 -77 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3161 75 3H-MK912 -77 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3161 75 3H-MK912 -77 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3161 75 3H-MK912 -77 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
484 2856 51 35S-GTPGammaS -8 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2856 51 35S-GTPGammaS -8 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2856 51 35S-GTPGammaS -8 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
2865 4141 73 3H-CLONIDINE -64 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4141 73 3H-CLONIDINE -64 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4141 73 3H-CLONIDINE -64 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4141 73 3H-CLONIDINE -64 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4141 73 3H-CLONIDINE -64 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
162265 202272 22 3H-CLONIDINE -8 45 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 202272 22 3H-CLONIDINE -8 45 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 202272 22 3H-CLONIDINE -8 45 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4158 205339 21 None 1 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 205339 21 None 1 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 205339 21 None 1 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
10836 14465 14 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
CHEMBL1201201 14465 14 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
1836 2590 59 None -31 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2590 59 None -31 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2590 59 None -31 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2590 59 None -31 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2590 59 None -31 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
5318 15574 49 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1200348 15574 49 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1221 15574 49 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
1960 2855 67 None -12 26 Mouse 8.2 pKi = 8.2 Binding
Binding affinity to mouse alpha-2C receptor expressed in COS7 cellsBinding affinity to mouse alpha-2C receptor expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
439260 2855 67 None -12 26 Mouse 8.2 pKi = 8.2 Binding
Binding affinity to mouse alpha-2C receptor expressed in COS7 cellsBinding affinity to mouse alpha-2C receptor expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
505 2855 67 None -12 26 Mouse 8.2 pKi = 8.2 Binding
Binding affinity to mouse alpha-2C receptor expressed in COS7 cellsBinding affinity to mouse alpha-2C receptor expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL1437 2855 67 None -12 26 Mouse 8.2 pKi = 8.2 Binding
Binding affinity to mouse alpha-2C receptor expressed in COS7 cellsBinding affinity to mouse alpha-2C receptor expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
DB00368 2855 67 None -12 26 Mouse 8.2 pKi = 8.2 Binding
Binding affinity to mouse alpha-2C receptor expressed in COS7 cellsBinding affinity to mouse alpha-2C receptor expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
68617 205525 62 None -9 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 205525 62 None -9 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 205525 62 None -9 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
2406 100402 89 None -11 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O None
CHEMBL290106 100402 89 None -11 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O None
5353853 17984 47 None -11 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
9556529 17984 47 None -11 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1262 17984 47 None -11 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
3561 19075 39 None -2 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl None
CHEMBL1289 19075 39 None -2 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl None
237 204863 48 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
CHEMBL546257 204863 48 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
CHEMBL554190 204863 48 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
CHEMBL7568 204863 48 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
2600 3777 74 None -4 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
2608 3777 74 None -4 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
5405 3777 74 None -4 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
CHEMBL17157 3777 74 None -4 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
DB00342 3777 74 None -4 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
2342 598 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
331 598 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 598 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 598 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 598 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
1353 1909 93 None -87 86 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 1909 93 None -87 86 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 1909 93 None -87 86 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 1909 93 None -87 86 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 1909 93 None -87 86 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
657255 199082 34 None -8 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
CHEMBL588119 199082 34 None -8 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
1443 2026 34 None -11 11 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
33625 2026 34 None -11 11 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
501 2026 34 None -11 11 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
CHEMBL279516 2026 34 None -11 11 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
DB08950 2026 34 None -11 11 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
191 403 98 None -39 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 403 98 None -39 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 403 98 None -39 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 403 98 None -39 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 403 98 None -39 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
60838 183872 99 None -1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC None
CHEMBL481 183872 99 None -1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC None
463 1404 22 None -48 13 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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 1404 22 None -48 13 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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 1404 22 None -48 13 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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 1404 22 None -48 13 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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 1404 22 None -48 13 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C 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
33630 178955 99 None -9 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expressed in MDCK cells by radioligand binding assayDisplacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expressed in MDCK cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 178955 99 None -9 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expressed in MDCK cells by radioligand binding assayDisplacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expressed in MDCK cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
2435 3588 83 None -104 49 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 3588 83 None -104 49 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 3588 83 None -104 49 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 3588 83 None -104 49 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 3588 83 None -104 49 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
4011 82406 49 None -28 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 82406 49 None -28 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
11079 2731 63 None -2 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
3369 2731 63 None -2 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
4436 2731 63 None -2 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
5509 2731 63 None -2 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
CHEMBL761 2731 63 None -2 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
DB06711 2731 63 None -2 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
214 3858 58 None -60 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 3858 58 None -60 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 3858 58 None -60 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 3858 58 None -60 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 3858 58 None -60 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 3858 58 None -60 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
16362 3123 71 None -263 30 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 3123 71 None -263 30 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 3123 71 None -263 30 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 3123 71 None -263 30 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 3123 71 None -263 30 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
1028 291 71 None -67 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 291 71 None -67 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 291 71 None -67 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 291 71 None -67 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 291 71 None -67 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 291 71 None -67 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
2286 3181 51 None -15 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3181 51 None -15 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3181 51 None -15 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3181 51 None -15 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3181 51 None -15 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
2247 505 81 None -25 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 505 81 None -25 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 505 81 None -25 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 505 81 None -25 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 505 81 None -25 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2335 11846 22 None -2 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 11846 22 None -2 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 11846 22 None -2 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 11846 22 None -2 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
2181 3126 46 None -36 35 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 3126 46 None -36 35 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 3126 46 None -36 35 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 3126 46 None -36 35 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 3126 46 None -36 35 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
3157 1469 71 None -39 12 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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 1469 71 None -39 12 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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 1469 71 None -39 12 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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 1469 71 None -39 12 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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 1469 71 None -39 12 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C 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
11057 176147 23 None -1 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 176147 23 None -1 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 176147 23 None -1 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 176147 23 None -1 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
5524 216462 0 None -2 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 215 1 2 3 1.9 C1CCC2=C(C1)C=CC=C2NC3=NCCN3 None
2162 41512 100 None -1 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl None
CHEMBL1491 41512 100 None -1 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl None
3168 9260 92 None -63 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 9260 92 None -63 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
DB00450 9260 92 None -63 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
1548955 88579 20 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
2800 88579 20 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
CHEMBL2355051 88579 20 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
2398 953 62 None -4 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801 953 62 None -4 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
701 953 62 None -4 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
CHEMBL415 953 62 None -4 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
DB01242 953 62 None -4 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
104870 98878 47 None -3 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 98878 47 None -3 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 98878 47 None -3 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
66265 94011 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 94011 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
277 1300 62 None -42 50 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1300 62 None -42 50 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1300 62 None -42 50 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1300 62 None -42 50 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1300 62 None -42 50 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1830 2588 44 None -6 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 2588 44 None -6 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 2588 44 None -6 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 2588 44 None -6 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 2588 44 None -6 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
5472 205816 75 None -1 3 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 None
CHEMBL1717 205816 75 None -1 3 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 None
CHEMBL833 205816 75 None -1 3 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 None
DB00208 205816 75 None -1 3 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 None
3952 1886 38 None -19 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5353646 1886 38 None -19 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5443 1886 38 None -19 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5702063 1886 38 None -19 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
CHEMBL1331786 1886 38 None -19 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
CHEMBL420 1886 38 None -19 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
DB00629 1886 38 None -19 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
213 3851 55 None -6 44 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 3851 55 None -6 44 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 3851 55 None -6 44 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 3851 55 None -6 44 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 3851 55 None -6 44 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
3151 1461 97 None -40 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
945 1461 97 None -40 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
965 1461 97 None -40 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
CHEMBL219916 1461 97 None -40 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
DB01184 1461 97 None -40 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
3584 3775 64 None -50 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 3775 64 None -50 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 3775 64 None -50 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 3775 64 None -50 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 3775 64 None -50 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
3658 4105 53 None -17 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
517 4105 53 None -17 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
5709 4105 53 None -17 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
CHEMBL312448 4105 53 None -17 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
DB06694 4105 53 None -17 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
240 943 43 None -5 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 943 43 None -5 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 943 43 None -5 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 943 43 None -5 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 943 43 None -5 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 943 43 None -5 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 943 43 None -5 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2351 3284 64 None -4 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
2820 3284 64 None -4 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
5035 3284 64 None -4 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
CHEMBL81 3284 64 None -4 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
DB00481 3284 64 None -4 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
1576 216324 0 3H-CLONIDINE 1 41 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
1222 1662 49 3H-RAUWOLSCINE -34 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1662 49 3H-RAUWOLSCINE -34 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1662 49 3H-RAUWOLSCINE -34 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1662 49 3H-RAUWOLSCINE -34 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1662 49 3H-RAUWOLSCINE -34 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
103 4151 61 3H-CLONIDINE -33 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4151 61 3H-CLONIDINE -33 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4151 61 3H-CLONIDINE -33 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4151 61 3H-CLONIDINE -33 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4151 61 3H-CLONIDINE -33 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2803 954 58 3H-RX821002 -4 19 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 954 58 3H-RX821002 -4 19 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 954 58 3H-RX821002 -4 19 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 954 58 3H-RX821002 -4 19 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 954 58 3H-RX821002 -4 19 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
15897 2860 0 3H-CLONIDINE -29 37 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2860 0 3H-CLONIDINE -29 37 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2860 0 3H-CLONIDINE -29 37 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
2105 3052 37 3H-RX821002 -81 33 Human 7.2 pKi = 7.2 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 3052 37 3H-RX821002 -81 33 Human 7.2 pKi = 7.2 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 3052 37 3H-RX821002 -81 33 Human 7.2 pKi = 7.2 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 3052 37 3H-RX821002 -81 33 Human 7.2 pKi = 7.2 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 3052 37 3H-RX821002 -81 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
2202 3130 96 3H-RX821002 1 21 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 3130 96 3H-RX821002 1 21 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 3130 96 3H-RX821002 1 21 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 3130 96 3H-RX821002 1 21 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 3130 96 3H-RX821002 1 21 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
11141 345 50 None 1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 315 6 2 5 1.3 C=CCN1CCCC1CNC(=O)c1cc2[nH]nnc2cc1OC None
120 345 50 None 1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 315 6 2 5 1.3 C=CCN1CCCC1CNC(=O)c1cc2[nH]nnc2cc1OC None
135413504 345 50 None 1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 315 6 2 5 1.3 C=CCN1CCCC1CNC(=O)c1cc2[nH]nnc2cc1OC None
43008 345 50 None 1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 315 6 2 5 1.3 C=CCN1CCCC1CNC(=O)c1cc2[nH]nnc2cc1OC None
CHEMBL290194 345 50 None 1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 315 6 2 5 1.3 C=CCN1CCCC1CNC(=O)c1cc2[nH]nnc2cc1OC None
DB01425 345 50 None 1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 315 6 2 5 1.3 C=CCN1CCCC1CNC(=O)c1cc2[nH]nnc2cc1OC None
1547484 939 74 None -4 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
654 939 74 None -4 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
9072 939 74 None -4 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL43064 939 74 None -4 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB00568 939 74 None -4 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
103 4151 61 None -33 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4151 61 None -33 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4151 61 None -33 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4151 61 None -33 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4151 61 None -33 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
209 3055 97 None -34 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3055 97 None -34 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3055 97 None -34 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3055 97 None -34 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3055 97 None -34 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2726 918 68 None -31 73 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 918 68 None -31 73 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 918 68 None -31 73 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 918 68 None -31 73 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 918 68 None -31 73 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1613 2346 53 None -6 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2346 53 None -6 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2346 53 None -6 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2346 53 None -6 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2346 53 None -6 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2865 4141 73 None -64 54 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 4141 73 None -64 54 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 4141 73 None -64 54 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 4141 73 None -64 54 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 4141 73 None -64 54 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
100 3803 58 None -27 55 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 3803 58 None -27 55 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 3803 58 None -27 55 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 3803 58 None -27 55 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 3803 58 None -27 55 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
1593 2338 66 None -6 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
Drug Central 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl None
30668 2338 66 None -6 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
Drug Central 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl None
9868 2338 66 None -6 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
Drug Central 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl None
CHEMBL17860 2338 66 None -6 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
Drug Central 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl None
DB04948 2338 66 None -6 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
Drug Central 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl None
1960 2855 67 None -20 26 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
439260 2855 67 None -20 26 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
505 2855 67 None -20 26 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL1437 2855 67 None -20 26 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
DB00368 2855 67 None -20 26 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Alpha-2C adrenergic receptorBinding affinity for human Alpha-2C adrenergic receptor
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
2105 3052 37 None -81 33 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 3052 37 None -81 33 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 3052 37 None -81 33 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 3052 37 None -81 33 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 3052 37 None -81 33 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
2202 3130 96 None 1 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 3130 96 None 1 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 3130 96 None 1 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 3130 96 None 1 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 3130 96 None 1 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
441383 20331 57 None 2 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 20331 57 None 2 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
1222 1662 49 None -34 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1662 49 None -34 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1662 49 None -34 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1662 49 None -34 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1662 49 None -34 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1201549 596 24 None -18 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
333 596 24 None -18 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 596 24 None -18 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 596 24 None -18 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 596 24 None -18 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 596 24 None -18 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
212 3804 47 None -6 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 3804 47 None -6 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 3804 47 None -6 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 3804 47 None -6 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 3804 47 None -6 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
3191 102856 97 None -3 25 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 102856 97 None -3 25 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
DB11742 102856 97 None -3 25 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
228 445 28 None -3 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 445 28 None -3 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 445 28 None -3 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 445 28 None -3 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 445 28 None -3 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
242 470 124 None -23 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 None -23 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 None -23 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 None -23 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 None -23 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
2284 3180 33 None -7 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3180 33 None -7 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3180 33 None -7 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3180 33 None -7 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3180 33 None -7 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
12488 1655 56 None -2 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1655 56 None -2 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1655 56 None -2 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1655 56 None -2 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
2216 446 50 None -3 6 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 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
229 446 50 None -3 6 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 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 446 50 None -3 6 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 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 446 50 None -3 6 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 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 446 50 None -3 6 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 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
1971 2864 38 None -3 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2864 38 None -3 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2864 38 None -3 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2864 38 None -3 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2864 38 None -3 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
1212 1660 50 None -54 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1660 50 None -54 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1660 50 None -54 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1660 50 None -54 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1660 50 None -54 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398745 2912 112 None -30 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2912 112 None -30 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2912 112 None -30 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2912 112 None -30 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
3389 217709 0 None -1 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1 None
133 2494 52 None -26 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2494 52 None -26 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2494 52 None -26 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2494 52 None -26 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2494 52 None -26 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
10219 188794 37 None -2 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 188794 37 None -2 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 188794 37 None -2 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
31101 728 40 None -36 36 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
35 728 40 None -36 36 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
403 728 40 None -36 36 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 728 40 None -36 36 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 728 40 None -36 36 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
4209 3161 75 None -77 33 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3161 75 None -77 33 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3161 75 None -77 33 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3161 75 None -77 33 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3161 75 None -77 33 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3161 75 None -77 33 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
37 777 60 None -5 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
460 777 60 None -5 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 777 60 None -5 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 777 60 None -5 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 777 60 None -5 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
1816 2538 102 None -38 18 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 2538 102 None -38 18 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 2538 102 None -38 18 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 2538 102 None -38 18 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 2538 102 None -38 18 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
3294 2004 111 None -16 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2004 111 None -16 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2004 111 None -16 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2004 111 None -16 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2004 111 None -16 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
26987 948 33 None -107 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 948 33 None -107 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 948 33 None -107 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 948 33 None -107 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 948 33 None -107 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
2585 802 103 None -16 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 802 103 None -16 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 802 103 None -16 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 802 103 None -16 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 802 103 None -16 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
68712 100336 60 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2C 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 100336 60 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2C 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
2274 3171 58 None -4 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3171 58 None -4 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3171 58 None -4 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3171 58 None -4 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3171 58 None -4 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
213046 2383 59 None -10 9 Human 8.1 pKi = 8.1 Binding
antagonist with moderate affinityantagonist with moderate affinity
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 2383 59 None -10 9 Human 8.1 pKi = 8.1 Binding
antagonist with moderate affinityantagonist with moderate affinity
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 2383 59 None -10 9 Human 8.1 pKi = 8.1 Binding
antagonist with moderate affinityantagonist with moderate affinity
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 2383 59 None -10 9 Human 8.1 pKi = 8.1 Binding
antagonist with moderate affinityantagonist with moderate affinity
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 2383 59 None -10 9 Human 8.1 pKi = 8.1 Binding
antagonist with moderate affinityantagonist with moderate affinity
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
25137849 216177 0 3H-CLONIDINE 1 41 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 216177 0 3H-CLONIDINE 1 41 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
124 2979 47 3H-RAUWOLSCINE -104 32 North American opossum 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2979 47 3H-RAUWOLSCINE -104 32 North American opossum 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2979 47 3H-RAUWOLSCINE -104 32 North American opossum 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2979 47 3H-RAUWOLSCINE -104 32 North American opossum 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2979 47 3H-RAUWOLSCINE -104 32 North American opossum 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
100 3803 58 3H-CLONIDINE -27 55 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3803 58 3H-CLONIDINE -27 55 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3803 58 3H-CLONIDINE -27 55 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3803 58 3H-CLONIDINE -27 55 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3803 58 3H-CLONIDINE -27 55 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
100 3803 58 3H-CLONIDINE -27 55 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3803 58 3H-CLONIDINE -27 55 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3803 58 3H-CLONIDINE -27 55 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3803 58 3H-CLONIDINE -27 55 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3803 58 3H-CLONIDINE -27 55 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2683 3832 60 3H-RAUWOLSCINE 1 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
5487 3832 60 3H-RAUWOLSCINE 1 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
7308 3832 60 3H-RAUWOLSCINE 1 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
CHEMBL1079 3832 60 3H-RAUWOLSCINE 1 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
DB00697 3832 60 3H-RAUWOLSCINE 1 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
None 216323 0 3H-CLONIDINE 1 41 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
2865 4141 73 3H-CLONIDINE -64 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2865 4141 73 3H-RAUWOLSCINE -64 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4141 73 3H-CLONIDINE -64 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4141 73 3H-RAUWOLSCINE -64 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4141 73 3H-CLONIDINE -64 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4141 73 3H-RAUWOLSCINE -64 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4141 73 3H-CLONIDINE -64 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4141 73 3H-RAUWOLSCINE -64 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4141 73 3H-CLONIDINE -64 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4141 73 3H-RAUWOLSCINE -64 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
1613 2346 53 3H-CLONIDINE -6 45 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2346 53 3H-CLONIDINE -6 45 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2346 53 3H-CLONIDINE -6 45 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2346 53 3H-CLONIDINE -6 45 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2346 53 3H-CLONIDINE -6 45 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
11750482 147419 0 UNDEFINED 19 3 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 419 6 0 6 5.3 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccco4)cc13)CC2 None
CHEMBL392991 147419 0 UNDEFINED 19 3 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 419 6 0 6 5.3 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccco4)cc13)CC2 None
180 401 56 None -16 40 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 None -16 40 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 None -16 40 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 None -16 40 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 None -16 40 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2142 3094 58 None -7 37 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3094 58 None -7 37 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3094 58 None -7 37 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3094 58 None -7 37 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3094 58 None -7 37 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3094 58 None -7 37 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-2C adrenergic receptor from human clones.Binding affinity against Alpha-2C adrenergic receptor from human clones.
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
129211 3747 78 None -51 16 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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 3747 78 None -51 16 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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 3747 78 None -51 16 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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 3747 78 None -51 16 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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 3747 78 None -51 16 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2C 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
6761 67797 19 None -3 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL1909072 67797 19 None -3 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
115237 55583 119 None -29 55 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 55583 119 None -29 55 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
DB01267 55583 119 None -29 55 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
134551 358 27 None -5 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
271 358 27 None -5 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
885 358 27 None -5 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 358 27 None -5 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
135 2530 43 None -6 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2530 43 None -6 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2530 43 None -6 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2530 43 None -6 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2530 43 None -6 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2389 3329 118 None -10 67 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 3329 118 None -10 67 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 3329 118 None -10 67 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 3329 118 None -10 67 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 3329 118 None -10 67 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
135398737 957 93 None -3 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 957 93 None -3 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 957 93 None -3 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 957 93 None -3 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 957 93 None -3 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
11954224 215951 0 None -4168 60 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
3251 215951 0 None -4168 60 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
CHEMBL1982133 215951 0 None -4168 60 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
DB00696 215951 0 None -4168 60 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
10531 1419 21 None -9 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1419 21 None -9 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1419 21 None -9 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1419 21 None -9 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 1419 21 None -9 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
107715 200943 22 None -7 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 200943 22 None -7 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 200943 22 None -7 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
1613 2346 53 3H-CLONIDINE -6 45 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2346 53 3H-CLONIDINE -6 45 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2346 53 3H-CLONIDINE -6 45 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2346 53 3H-CLONIDINE -6 45 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2346 53 3H-CLONIDINE -6 45 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
10836 14465 14 3H-CLONIDINE -1 9 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
CHEMBL1201201 14465 14 3H-CLONIDINE -1 9 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
135398745 2912 112 3H-RAUWOLSCINE -30 66 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2912 112 3H-RAUWOLSCINE -30 66 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2912 112 3H-RAUWOLSCINE -30 66 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2912 112 3H-RAUWOLSCINE -30 66 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
209 3055 97 3H-CLONIDINE -34 23 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3055 97 3H-CLONIDINE -34 23 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3055 97 3H-CLONIDINE -34 23 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3055 97 3H-CLONIDINE -34 23 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3055 97 3H-CLONIDINE -34 23 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4158 205339 21 125I-Clonidine 1 21 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 205339 21 125I-Clonidine 1 21 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 205339 21 125I-Clonidine 1 21 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
134 2512 24 3H-CLONIDINE -21 68 Human 7.1 pKi = 7.1 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 2512 24 3H-CLONIDINE -21 68 Human 7.1 pKi = 7.1 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 2512 24 3H-CLONIDINE -21 68 Human 7.1 pKi = 7.1 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 2512 24 3H-CLONIDINE -21 68 Human 7.1 pKi = 7.1 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 2512 24 3H-CLONIDINE -21 68 Human 7.1 pKi = 7.1 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
124 2979 47 None -60 32 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2979 47 None -60 32 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2979 47 None -60 32 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2979 47 None -60 32 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2979 47 None -60 32 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
None 216328 0 UNDEFINED -8 28 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
2601 3778 33 None -2 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 3778 33 None -2 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 3778 33 None -2 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 3778 33 None -2 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 3778 33 None -2 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
135398737 957 93 3H-RAUWOLSCINE -3 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 957 93 3H-RAUWOLSCINE -3 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 957 93 3H-RAUWOLSCINE -3 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 957 93 3H-RAUWOLSCINE -3 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 957 93 3H-RAUWOLSCINE -3 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2389 3329 118 3H-RAUWOLSCINE -10 67 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3329 118 3H-RAUWOLSCINE -10 67 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3329 118 3H-RAUWOLSCINE -10 67 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3329 118 3H-RAUWOLSCINE -10 67 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3329 118 3H-RAUWOLSCINE -10 67 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1588 2323 27 None -3 44 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2323 27 None -3 44 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2323 27 None -3 44 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2323 27 None -3 44 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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 2323 27 None -3 44 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] 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
11978813 720 79 None -11 24 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 720 79 None -11 24 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 720 79 None -11 24 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 720 79 None -11 24 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 720 79 None -11 24 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
102 4125 48 None -2 50 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cells
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 4125 48 None -2 50 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cells
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 4125 48 None -2 50 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cells
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 4125 48 None -2 50 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cells
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 4125 48 None -2 50 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cells
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
521 1403 69 None -30 7 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
5311068 1403 69 None -30 7 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
835 1403 69 None -30 7 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
CHEMBL778 1403 69 None -30 7 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
DB00633 1403 69 None -30 7 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
44438161 147139 0 UNDEFINED 22 3 Human 8.0 pKi = 8.0 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 147139 0 UNDEFINED 22 3 Human 8.0 pKi = 8.0 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
44438165 166782 0 UNDEFINED 48 3 Human 8.0 pKi = 8.0 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 166782 0 UNDEFINED 48 3 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 467 9 1 7 3.3 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)NCCN(C)C)cc13)CC2 None
44438148 93488 0 UNDEFINED 14 3 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 430 6 0 6 5.1 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccn4)cc13)CC2 None
CHEMBL246229 93488 0 UNDEFINED 14 3 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 430 6 0 6 5.1 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccn4)cc13)CC2 None
2142 3094 58 3H-RAUWOLSCINE -7 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3094 58 3H-RAUWOLSCINE -7 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3094 58 3H-RAUWOLSCINE -7 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3094 58 3H-RAUWOLSCINE -7 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3094 58 3H-RAUWOLSCINE -7 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3094 58 3H-RAUWOLSCINE -7 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
15897 2860 0 3H-CLONIDINE -29 37 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2860 0 3H-CLONIDINE -29 37 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2860 0 3H-CLONIDINE -29 37 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
68602 205124 80 35S-GTPGammaS -4 8 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C None
CHEMBL77921 205124 80 35S-GTPGammaS -4 8 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C None
15897 2860 0 3H-CLONIDINE -29 37 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2860 0 3H-CLONIDINE -29 37 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2860 0 3H-CLONIDINE -29 37 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
104870 98878 47 35S-GTPGammaS -3 21 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 98878 47 35S-GTPGammaS -3 21 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 98878 47 35S-GTPGammaS -3 21 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
None 216328 0 3H-CLONIDINE -8 28 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
1593 2338 66 None -6 4 Human 7.2 pKi = 7.2 Binding
Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2C</sub>-AR.Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2C</sub>-AR.
Guide to Pharmacology 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 22341244
30668 2338 66 None -6 4 Human 7.2 pKi = 7.2 Binding
Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2C</sub>-AR.Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2C</sub>-AR.
Guide to Pharmacology 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 22341244
9868 2338 66 None -6 4 Human 7.2 pKi = 7.2 Binding
Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2C</sub>-AR.Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2C</sub>-AR.
Guide to Pharmacology 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 22341244
CHEMBL17860 2338 66 None -6 4 Human 7.2 pKi = 7.2 Binding
Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2C</sub>-AR.Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2C</sub>-AR.
Guide to Pharmacology 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 22341244
DB04948 2338 66 None -6 4 Human 7.2 pKi = 7.2 Binding
Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2C</sub>-AR.Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2C</sub>-AR.
Guide to Pharmacology 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 22341244
1816 2538 102 None -38 18 Human 7.4 pKi = 7.4 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 2538 102 None -38 18 Human 7.4 pKi = 7.4 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 2538 102 None -38 18 Human 7.4 pKi = 7.4 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 2538 102 None -38 18 Human 7.4 pKi = 7.4 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 2538 102 None -38 18 Human 7.4 pKi = 7.4 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 2538 102 None -38 18 Human 7.4 pKi = 7.4 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 2538 102 None -38 18 Human 7.4 pKi = 7.4 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 2538 102 None -38 18 Human 7.4 pKi = 7.4 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 2538 102 None -38 18 Human 7.4 pKi = 7.4 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 2538 102 None -38 18 Human 7.4 pKi = 7.4 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 3839 81 None -30 6 Human 5.4 pKi = 5.4 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 3839 81 None -30 6 Human 5.4 pKi = 5.4 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 3839 81 None -30 6 Human 5.4 pKi = 5.4 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 3839 81 None -30 6 Human 5.4 pKi = 5.4 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 3839 81 None -30 6 Human 5.4 pKi = 5.4 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
13129 2964 0 None - 1 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 2 0 3 3.8 C[C@@]1(CCCN2[C@@H]1C3=C(CC2)C4=CC=CC=C4O3)COC 33296042
71301276 2964 0 None - 1 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 2 0 3 3.8 C[C@@]1(CCCN2[C@@H]1C3=C(CC2)C4=CC=CC=C4O3)COC 33296042
CHEMBL4297312 2964 0 None - 1 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 2 0 3 3.8 C[C@@]1(CCCN2[C@@H]1C3=C(CC2)C4=CC=CC=C4O3)COC 33296042
DB12057 2964 0 None - 1 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 2 0 3 3.8 C[C@@]1(CCCN2[C@@H]1C3=C(CC2)C4=CC=CC=C4O3)COC 33296042
12574 2603 88 None -87 6 Human 4.8 pKi = 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
4810 2603 88 None -87 6 Human 4.8 pKi = 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
CHEMBL19236 2603 88 None -87 6 Human 4.8 pKi = 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
DB09242 2603 88 None -87 6 Human 4.8 pKi = 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
523 4104 93 None -2 5 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
523 4104 93 None -2 5 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 9605427
5707 4104 93 None -2 5 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
5707 4104 93 None -2 5 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 9605427
CHEMBL297362 4104 93 None -2 5 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
CHEMBL297362 4104 93 None -2 5 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 9605427
DB11477 4104 93 None -2 5 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
DB11477 4104 93 None -2 5 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 9605427
1028 291 71 None -67 30 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
1028 291 71 None -67 30 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
139148732 291 71 None -67 30 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
139148732 291 71 None -67 30 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
479 291 71 None -67 30 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
479 291 71 None -67 30 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
5816 291 71 None -67 30 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
5816 291 71 None -67 30 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
CHEMBL679 291 71 None -67 30 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
CHEMBL679 291 71 None -67 30 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
DB00668 291 71 None -67 30 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
DB00668 291 71 None -67 30 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
1960 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 25080296
1960 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
1960 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9605427
1960 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9824686
439260 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 25080296
439260 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
439260 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9605427
439260 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9824686
505 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 25080296
505 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
505 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9605427
505 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9824686
CHEMBL1437 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 25080296
CHEMBL1437 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
CHEMBL1437 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9605427
CHEMBL1437 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9824686
DB00368 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 25080296
DB00368 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
DB00368 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9605427
DB00368 2855 67 None -20 26 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9824686
1343 1887 62 None -251 9 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
1343 1887 62 None -251 9 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9605427
3519 1887 62 None -251 9 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
3519 1887 62 None -251 9 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9605427
522 1887 62 None -251 9 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
522 1887 62 None -251 9 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9605427
CHEMBL862 1887 62 None -251 9 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
CHEMBL862 1887 62 None -251 9 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9605427
DB01018 1887 62 None -251 9 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
DB01018 1887 62 None -251 9 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9605427
4508 3137 98 None -199 13 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 9605427
4866774 3137 98 None -199 13 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 9605427
509 3137 98 None -199 13 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 9605427
838 3137 98 None -199 13 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 9605427
CHEMBL1740 3137 98 None -199 13 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 9605427
DB11124 3137 98 None -199 13 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 9605427
11079 2731 63 None -2 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
3369 2731 63 None -2 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
4436 2731 63 None -2 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
5509 2731 63 None -2 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
CHEMBL761 2731 63 None -2 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
DB06711 2731 63 None -2 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
121850 725 0 None -41 3 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 35224877
121850 725 0 None -41 3 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 7996470
525 725 0 None -41 3 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 35224877
525 725 0 None -41 3 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 7996470
CHEMBL216097 725 0 None -41 3 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 35224877
CHEMBL216097 725 0 None -41 3 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 7996470
124 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 25080296
124 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
124 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 7996470
124 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9605427
2032 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 25080296
2032 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
2032 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 7996470
2032 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9605427
4636 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 25080296
4636 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
4636 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 7996470
4636 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9605427
CHEMBL762 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 25080296
CHEMBL762 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
CHEMBL762 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 7996470
CHEMBL762 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9605427
DB00935 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 25080296
DB00935 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
DB00935 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 7996470
DB00935 2979 47 None -60 32 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9605427
2435 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
2435 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9227000
2435 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9605427
2435 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9760042
2435 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9824686
395 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
395 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9227000
395 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9605427
395 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9760042
395 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9824686
520 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
520 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9227000
520 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9605427
520 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9760042
520 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9824686
5386 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
5386 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9227000
5386 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9605427
5386 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9760042
5386 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9824686
CHEMBL844 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
CHEMBL844 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9227000
CHEMBL844 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9605427
CHEMBL844 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9760042
CHEMBL844 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9824686
DB00484 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
DB00484 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9227000
DB00484 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9605427
DB00484 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9760042
DB00484 721 100 None -33 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9824686
2726 918 68 None -31 73 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1353247
2726 918 68 None -31 73 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 35224877
2726 918 68 None -31 73 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908642
621 918 68 None -31 73 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1353247
621 918 68 None -31 73 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 35224877
621 918 68 None -31 73 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908642
83 918 68 None -31 73 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1353247
83 918 68 None -31 73 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 35224877
83 918 68 None -31 73 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908642
CHEMBL71 918 68 None -31 73 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1353247
CHEMBL71 918 68 None -31 73 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 35224877
CHEMBL71 918 68 None -31 73 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908642
DB00477 918 68 None -31 73 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1353247
DB00477 918 68 None -31 73 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 35224877
DB00477 918 68 None -31 73 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908642
2803 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
2803 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9605427
2803 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9760042
2803 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9824686
516 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
516 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9605427
516 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9760042
516 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9824686
704 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
704 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9605427
704 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9760042
704 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9824686
CHEMBL134 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
CHEMBL134 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9605427
CHEMBL134 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9760042
CHEMBL134 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9824686
DB00575 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
DB00575 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9605427
DB00575 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9760042
DB00575 954 58 None -4 19 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9824686
3658 4105 53 None -17 8 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
517 4105 53 None -17 8 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
5709 4105 53 None -17 8 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
CHEMBL312448 4105 53 None -17 8 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
DB06694 4105 53 None -17 8 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
12575 1986 30 None -8 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 1986 30 None -8 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 1986 30 None -8 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
DB12551 1986 30 None -8 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
2105 3052 37 None -81 33 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
47811 3052 37 None -81 33 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
48 3052 37 None -81 33 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
CHEMBL531 3052 37 None -81 33 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
DB01186 3052 37 None -81 33 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
4209 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 1353247
4209 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 35224877
4209 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7908642
4209 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7996470
4893 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 1353247
4893 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 35224877
4893 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7908642
4893 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7996470
503 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 1353247
503 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 35224877
503 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7908642
503 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7996470
5385 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 1353247
5385 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 35224877
5385 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7908642
5385 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7996470
CHEMBL2 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 1353247
CHEMBL2 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 35224877
CHEMBL2 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7908642
CHEMBL2 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7996470
DB00457 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 1353247
DB00457 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 35224877
DB00457 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7908642
DB00457 3161 75 None -77 33 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7996470
2216 446 50 None -3 6 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 36101495
2216 446 50 None -3 6 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 8784451
229 446 50 None -3 6 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 36101495
229 446 50 None -3 6 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 8784451
7117 446 50 None -3 6 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 36101495
7117 446 50 None -3 6 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 8784451
CHEMBL647 446 50 None -3 6 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 36101495
CHEMBL647 446 50 None -3 6 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 8784451
DB00964 446 50 None -3 6 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 36101495
DB00964 446 50 None -3 6 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 8784451
122211 462 0 None -9 6 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C 1353247
122211 462 0 None -9 6 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C 35224877
122211 462 0 None -9 6 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C 7908642
122211 462 0 None -9 6 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C 7996470
524 462 0 None -9 6 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C 1353247
524 462 0 None -9 6 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C 35224877
524 462 0 None -9 6 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C 7908642
524 462 0 None -9 6 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C 7996470
31101 728 40 None -36 36 Human 7.6 pKi = 7.6 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 728 40 None -36 36 Human 7.6 pKi = 7.6 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
35 728 40 None -36 36 Human 7.6 pKi = 7.6 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
35 728 40 None -36 36 Human 7.6 pKi = 7.6 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
403 728 40 None -36 36 Human 7.6 pKi = 7.6 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
403 728 40 None -36 36 Human 7.6 pKi = 7.6 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 728 40 None -36 36 Human 7.6 pKi = 7.6 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 728 40 None -36 36 Human 7.6 pKi = 7.6 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 728 40 None -36 36 Human 7.6 pKi = 7.6 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 728 40 None -36 36 Human 7.6 pKi = 7.6 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
213046 2383 59 None -10 9 Human 7.7 pKi = 7.7 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 2383 59 None -10 9 Human 7.7 pKi = 7.7 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 2383 59 None -10 9 Human 7.7 pKi = 7.7 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 2383 59 None -10 9 Human 7.7 pKi = 7.7 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 2383 59 None -10 9 Human 7.7 pKi = 7.7 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 2383 59 None -10 9 Human 7.7 pKi = 7.7 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 2383 59 None -10 9 Human 7.7 pKi = 7.7 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 2383 59 None -10 9 Human 7.7 pKi = 7.7 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 2383 59 None -10 9 Human 7.7 pKi = 7.7 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 2383 59 None -10 9 Human 7.7 pKi = 7.7 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
2741 350 0 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 5 1 2 4.8 C/C(=C\C=C\C(=C\C(=O)O)\C)/C=C/C1=C(C)C(=O)CCC1(C)C 15771415
6437063 350 0 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 5 1 2 4.8 C/C(=C\C=C\C(=C\C(=O)O)\C)/C=C/C1=C(C)C(=O)CCC1(C)C 15771415
CHEMBL104049 350 0 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 5 1 2 4.8 C/C(=C\C=C\C(=C\C(=O)O)\C)/C=C/C1=C(C)C(=O)CCC1(C)C 15771415
2142 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 1353247
2142 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 35224877
2142 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7908642
4920903 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 1353247
4920903 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 35224877
4920903 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7908642
502 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 1353247
502 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 35224877
502 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7908642
5775 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 1353247
5775 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 35224877
5775 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7908642
CHEMBL597 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 1353247
CHEMBL597 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 35224877
CHEMBL597 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7908642
DB00692 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 1353247
DB00692 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 35224877
DB00692 3094 58 None -7 37 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7908642
11959 1535 0 None -4 4 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 405 5 1 7 3.0 Cn1c(=O)c(c(cn1)NCCN1CCC(CC1)c1noc2c1ccc(c2)F)Cl 22824189
9909267 1535 0 None -4 4 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 405 5 1 7 3.0 Cn1c(=O)c(c(cn1)NCCN1CCC(CC1)c1noc2c1ccc(c2)F)Cl 22824189
521 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
521 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9605427
521 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9760042
521 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9824686
5311068 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
5311068 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9605427
5311068 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9760042
5311068 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9824686
835 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
835 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9605427
835 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9760042
835 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9824686
CHEMBL778 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
CHEMBL778 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9605427
CHEMBL778 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9760042
CHEMBL778 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9824686
DB00633 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
DB00633 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9605427
DB00633 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9760042
DB00633 1403 69 None -30 7 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9824686
108094 3421 27 None -2 4 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 35224877
108094 3421 27 None -2 4 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 7996470
526 3421 27 None -2 4 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 35224877
526 3421 27 None -2 4 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 7996470
528 3421 27 None -2 4 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 35224877
528 3421 27 None -2 4 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 7996470
CHEMBL10332 3421 27 None -2 4 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 35224877
CHEMBL10332 3421 27 None -2 4 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 7996470
12576 514 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 514 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 514 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 514 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
499 4075 18 None -3 15 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 1353247
499 4075 18 None -3 15 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 35224877
499 4075 18 None -3 15 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 7908642
499 4075 18 None -3 15 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 7996470
5685 4075 18 None -3 15 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 1353247
5685 4075 18 None -3 15 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 35224877
5685 4075 18 None -3 15 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 7908642
5685 4075 18 None -3 15 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 7996470
CHEMBL25554 4075 18 None -3 15 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 1353247
CHEMBL25554 4075 18 None -3 15 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 35224877
CHEMBL25554 4075 18 None -3 15 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 7908642
CHEMBL25554 4075 18 None -3 15 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 7996470
5268 3654 40 None -1 18 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 35224877
5268 3654 40 None -1 18 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 7996470
53 3654 40 None -1 18 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 35224877
53 3654 40 None -1 18 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 7996470
CHEMBL300555 3654 40 None -1 18 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 35224877
CHEMBL300555 3654 40 None -1 18 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 7996470
13130 2963 0 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 2 0 3 3.9 [H][C@@]12N(CCC[C@@]1(C)OCC)CCC3=C2OC4=C3C=CC=C4 23718812
171037438 2963 0 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 2 0 3 3.9 [H][C@@]12N(CCC[C@@]1(C)OCC)CCC3=C2OC4=C3C=CC=C4 23718812
102 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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 4125 48 None -2 50 Human 9.0 pKi = 9 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
136 3290 32 None 3 16 Human 9.1 pKi = 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 7996470
223 3290 32 None 3 16 Human 9.1 pKi = 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 7996470
643606 3290 32 None 3 16 Human 9.1 pKi = 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 7996470
CHEMBL10347 3290 32 None 3 16 Human 9.1 pKi = 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 7996470
13128 3398 0 None 3 3 Human 9.4 pKi = 9.4 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 3398 0 None 3 3 Human 9.4 pKi = 9.4 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 3398 0 None 3 3 Human 9.4 pKi = 9.4 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 2323 27 None -3 44 Human 9.6 pKi = 9.6 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 2323 27 None -3 44 Human 9.6 pKi = 9.6 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
1588 2323 27 None -3 44 Human 9.6 pKi = 9.6 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 9227000
28864 2323 27 None -3 44 Human 9.6 pKi = 9.6 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 2323 27 None -3 44 Human 9.6 pKi = 9.6 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 2323 27 None -3 44 Human 9.6 pKi = 9.6 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 9227000
43 2323 27 None -3 44 Human 9.6 pKi = 9.6 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 2323 27 None -3 44 Human 9.6 pKi = 9.6 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 2323 27 None -3 44 Human 9.6 pKi = 9.6 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 9227000
CHEMBL157138 2323 27 None -3 44 Human 9.6 pKi = 9.6 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 2323 27 None -3 44 Human 9.6 pKi = 9.6 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 2323 27 None -3 44 Human 9.6 pKi = 9.6 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 9227000
DB00589 2323 27 None -3 44 Human 9.6 pKi = 9.6 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 2323 27 None -3 44 Human 9.6 pKi = 9.6 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 2323 27 None -3 44 Human 9.6 pKi = 9.6 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 9227000
12577 2561 0 None 15 3 Human 9.9 pKi = 9.9 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 2561 0 None 15 3 Human 9.9 pKi = 9.9 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 2561 0 None 15 3 Human 9.9 pKi = 9.9 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
179 400 115 None -40 51 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 400 115 None -40 51 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
963 400 115 None -40 51 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 400 115 None -40 51 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 400 115 None -40 51 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
162265 202272 22 None -8 45 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 202272 22 None -8 45 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 202272 22 None -8 45 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
3337 206365 27 None -13 41 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 206365 27 None -13 41 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 206365 27 None -13 41 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 206365 27 None -13 41 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 206365 27 None -13 41 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
DB00574 206365 27 None -13 41 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
134 2512 24 None -21 68 Human 8.2 pKi None 8.2 Binding
NoneNone
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 2512 24 None -21 68 Human 8.2 pKi None 8.2 Binding
NoneNone
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 2512 24 None -21 68 Human 8.2 pKi None 8.2 Binding
NoneNone
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 2512 24 None -21 68 Human 8.2 pKi None 8.2 Binding
NoneNone
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 2512 24 None -21 68 Human 8.2 pKi None 8.2 Binding
NoneNone
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
119570 3157 96 None -89 40 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3157 96 None -89 40 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3157 96 None -89 40 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3157 96 None -89 40 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3157 96 None -89 40 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
3036780 107529 20 None -72 54 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
46780481 107529 20 None -72 54 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107529 20 None -72 54 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107529 20 None -72 54 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107529 20 None -72 54 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL504548 107529 20 None -72 54 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
DB06216 107529 20 None -72 54 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
2202 3130 96 None 1 21 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
4850 3130 96 None 1 21 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
49 3130 96 None 1 21 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
CHEMBL1371770 3130 96 None 1 21 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
DB12478 3130 96 None 1 21 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
228 445 28 None -3 24 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
33 445 28 None -3 24 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
6005 445 28 None -3 24 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
CHEMBL53 445 28 None -3 24 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
DB00714 445 28 None -3 24 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
37 777 60 None -5 17 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
460 777 60 None -5 17 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
54746 777 60 None -5 17 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
CHEMBL1201087 777 60 None -5 17 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
DB00248 777 60 None -5 17 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
219050 3371 25 None -10 21 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
52 3371 25 None -10 21 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
CHEMBL431367 3371 25 None -10 21 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
2601 3778 33 None -2 21 Human 9.1 pKi None 9.1 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 3778 33 None -2 21 Human 9.1 pKi None 9.1 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 3778 33 None -2 21 Human 9.1 pKi None 9.1 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 3778 33 None -2 21 Human 9.1 pKi None 9.1 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 3778 33 None -2 21 Human 9.1 pKi None 9.1 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