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 1664 None 37 Human Functional pAC50 = 6 6.0 -23 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1664 None 37 Human Functional pAC50 = 6 6.0 -23 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
3396.0 1664 None 37 Human Functional pAC50 = 6 6.0 -23 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1664 None 37 Human Functional pAC50 = 6 6.0 -23 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1664 None 37 Human Functional pAC50 = 6 6.0 -23 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1664 None 37 Human Functional pAC50 = 6 6.0 -23 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3256 None 51 Human Functional pAC50 = 6 6.0 -8 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3256 None 51 Human Functional pAC50 = 6 6.0 -8 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3256 None 51 Human Functional pAC50 = 6 6.0 -8 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5002.0 3256 None 51 Human Functional pAC50 = 6 6.0 -8 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3256 None 51 Human Functional pAC50 = 6 6.0 -8 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3256 None 51 Human Functional pAC50 = 6 6.0 -8 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 100270 None 65 Human Functional pAC50 = 6 6.0 -1 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 100270 None 65 Human Functional pAC50 = 6 6.0 -1 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 9427 None 34 Human Functional pAC50 = 5 5.0 -1 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 9427 None 34 Human Functional pAC50 = 5 5.0 -1 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 41527 None 58 Human Functional pAC50 = 5 5.0 -3 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 41527 None 58 Human Functional pAC50 = 5 5.0 -3 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78239 None 45 Human Functional pAC50 = 5 5.0 -3311 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78239 None 45 Human Functional pAC50 = 5 5.0 -3311 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3054 None 28 Human Functional pAC50 = 6.0 6.0 -251 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3054 None 28 Human Functional pAC50 = 6.0 6.0 -251 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3054 None 28 Human Functional pAC50 = 6.0 6.0 -251 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3054 None 28 Human Functional pAC50 = 6.0 6.0 -251 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3054 None 28 Human Functional pAC50 = 6.0 6.0 -251 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3163 None 48 Human Functional pAC50 = 7.0 7.0 -891 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3163 None 48 Human Functional pAC50 = 7.0 7.0 -891 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4893.0 3163 None 48 Human Functional pAC50 = 7.0 7.0 -891 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3163 None 48 Human Functional pAC50 = 7.0 7.0 -891 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3163 None 48 Human Functional pAC50 = 7.0 7.0 -891 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3163 None 48 Human Functional pAC50 = 7.0 7.0 -891 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3163 None 48 Human Functional pAC50 = 7.0 7.0 -891 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 208276 None 49 Human Functional pAC50 = 6.0 6.0 -1 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5472.0 208276 None 49 Human Functional pAC50 = 6.0 6.0 -1 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 208276 None 49 Human Functional pAC50 = 6.0 6.0 -1 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 208276 None 49 Human Functional pAC50 = 6.0 6.0 -1 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 208276 None 49 Human Functional pAC50 = 6.0 6.0 -1 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 40 Human Functional pAC50 = 5.0 5.0 -44 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 40 Human Functional pAC50 = 5.0 5.0 -44 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 40 Human Functional pAC50 = 5.0 5.0 -44 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 40 Human Functional pAC50 = 5.0 5.0 -44 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5816.0 291 None 40 Human Functional pAC50 = 5.0 5.0 -44 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 40 Human Functional pAC50 = 5.0 5.0 -44 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 40 Human Functional pAC50 = 5.0 5.0 -44 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1406 None 18 Human Functional pAC50 = 5.0 5.0 -1737 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1406 None 18 Human Functional pAC50 = 5.0 5.0 -1737 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1406 None 18 Human Functional pAC50 = 5.0 5.0 -1737 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1406 None 18 Human Functional pAC50 = 5.0 5.0 -1737 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1406 None 18 Human Functional pAC50 = 5.0 5.0 -1737 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 20210 None 38 Human Functional pAC50 = 5.0 5.0 -6 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2200.0 20210 None 38 Human Functional pAC50 = 5.0 5.0 -6 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 20210 None 38 Human Functional pAC50 = 5.0 5.0 -6 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 20210 None 38 Human Functional pAC50 = 5.0 5.0 -6 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 20210 None 38 Human Functional pAC50 = 5.0 5.0 -6 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 55132 None 30 Human Functional pAC50 = 5.0 5.0 -3 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 55132 None 30 Human Functional pAC50 = 5.0 5.0 -3 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 56869 None 26 Human Functional pAC50 = 5.0 5.0 -32 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 56869 None 26 Human Functional pAC50 = 5.0 5.0 -32 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 56869 None 26 Human Functional pAC50 = 5.0 5.0 -32 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 84404 None 3 Human Functional pAC50 = 5.0 5.0 -3890 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
55645.0 84404 None 3 Human Functional pAC50 = 5.0 5.0 -3890 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 84404 None 3 Human Functional pAC50 = 5.0 5.0 -3890 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 137055 None 20 Human Functional pAC50 = 5.0 5.0 -4 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 137055 None 20 Human Functional pAC50 = 5.0 5.0 -4 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 137055 None 20 Human Functional pAC50 = 5.0 5.0 -4 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206037 None 20 Human Functional pAC50 = 5.0 5.0 -1230 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206037 None 20 Human Functional pAC50 = 5.0 5.0 -1230 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 70 Human Functional pAC50 = 7.0 7.0 -32 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 70 Human Functional pAC50 = 7.0 7.0 -32 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 70 Human Functional pAC50 = 7.0 7.0 -32 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
60795.0 470 None 70 Human Functional pAC50 = 7.0 7.0 -32 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 70 Human Functional pAC50 = 7.0 7.0 -32 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 70 Human Functional pAC50 = 7.0 7.0 -32 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2385 None 44 Human Functional pAC50 = 6.0 6.0 -69 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
213046.0 2385 None 44 Human Functional pAC50 = 6.0 6.0 -69 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2385 None 44 Human Functional pAC50 = 6.0 6.0 -69 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2385 None 44 Human Functional pAC50 = 6.0 6.0 -69 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2385 None 44 Human Functional pAC50 = 6.0 6.0 -69 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2385 None 44 Human Functional pAC50 = 6.0 6.0 -69 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206828 None 60 Human Functional pAC50 = 6.0 6.0 2 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206828 None 60 Human Functional pAC50 = 6.0 6.0 2 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2348 None 42 Human Functional pAC50 = 5.9 5.9 -97 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2348 None 42 Human Functional pAC50 = 5.9 5.9 -97 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2348 None 42 Human Functional pAC50 = 5.9 5.9 -97 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
3964.0 2348 None 42 Human Functional pAC50 = 5.9 5.9 -97 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2348 None 42 Human Functional pAC50 = 5.9 5.9 -97 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2348 None 42 Human Functional pAC50 = 5.9 5.9 -97 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 203394 None 56 Human Functional pAC50 = 5.9 5.9 -1 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 203394 None 56 Human Functional pAC50 = 5.9 5.9 -1 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207555 None 29 Human Functional pAC50 = 5.9 5.9 -7 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207555 None 29 Human Functional pAC50 = 5.9 5.9 -7 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4402 None 68 Human Functional pAC50 = 4.9 4.9 -1737 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4402 None 68 Human Functional pAC50 = 4.9 4.9 -1737 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14429 None 40 Human Functional pAC50 = 4.9 4.9 -1 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14429 None 40 Human Functional pAC50 = 4.9 4.9 -1 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 15398 None 50 Human Functional pAC50 = 4.9 4.9 -4 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 15398 None 50 Human Functional pAC50 = 4.9 4.9 -4 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 15398 None 50 Human Functional pAC50 = 4.9 4.9 -4 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 98850 None 21 Human Functional pAC50 = 4.9 4.9 -331 3
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
11291.0 98850 None 21 Human Functional pAC50 = 4.9 4.9 -331 3
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 98850 None 21 Human Functional pAC50 = 4.9 4.9 -331 3
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 98850 None 21 Human Functional pAC50 = 4.9 4.9 -331 3
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3776 None 69 Human Functional pAC50 = 4.9 4.9 -7079 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3776 None 69 Human Functional pAC50 = 4.9 4.9 -7079 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3776 None 69 Human Functional pAC50 = 4.9 4.9 -7079 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
65999.0 3776 None 69 Human Functional pAC50 = 4.9 4.9 -7079 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3776 None 69 Human Functional pAC50 = 4.9 4.9 -7079 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3776 None 69 Human Functional pAC50 = 4.9 4.9 -7079 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 115628 None 61 Human Functional pAC50 = 4.9 4.9 -33 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 115628 None 61 Human Functional pAC50 = 4.9 4.9 -33 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3330 None 58 Human Functional pAC50 = 4.9 4.9 -1174 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3330 None 58 Human Functional pAC50 = 4.9 4.9 -1174 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3330 None 58 Human Functional pAC50 = 4.9 4.9 -1174 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3330 None 58 Human Functional pAC50 = 4.9 4.9 -1174 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3330 None 58 Human Functional pAC50 = 4.9 4.9 -1174 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14437 None 23 Human Functional pAC50 = 4.9 4.9 -14 4
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14437 None 23 Human Functional pAC50 = 4.9 4.9 -14 4
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 18563 None 62 Human Functional pAC50 = 4.9 4.9 -5 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 18563 None 62 Human Functional pAC50 = 4.9 4.9 -5 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 19387 None 54 Human Functional pAC50 = 4.9 4.9 -14 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 19387 None 54 Human Functional pAC50 = 4.9 4.9 -14 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 52396 None 9 Human Functional pAC50 = 4.9 4.9 -102 3
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
7028.0 52396 None 9 Human Functional pAC50 = 4.9 4.9 -102 3
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 52396 None 9 Human Functional pAC50 = 4.9 4.9 -102 3
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 52396 None 9 Human Functional pAC50 = 4.9 4.9 -102 3
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 67446 None 31 Human Functional pAC50 = 4.9 4.9 -3 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 67446 None 31 Human Functional pAC50 = 4.9 4.9 -3 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 158486 None 71 Human Functional pAC50 = 4.9 4.9 -5 2
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 158486 None 71 Human Functional pAC50 = 4.9 4.9 -5 2
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 189531 None 18 Human Functional pAC50 = 4.9 4.9 -8 3
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 189531 None 18 Human Functional pAC50 = 4.9 4.9 -8 3
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78202 None 29 Human Functional pAC50 = 5.9 5.9 -61 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
68867.0 78202 None 29 Human Functional pAC50 = 5.9 5.9 -61 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78202 None 29 Human Functional pAC50 = 5.9 5.9 -61 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78202 None 29 Human Functional pAC50 = 5.9 5.9 -61 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207584 None 54 Human Functional pAC50 = 5.9 5.9 -11 4
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207584 None 54 Human Functional pAC50 = 5.9 5.9 -11 4
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3834 None 40 Human Functional pAC50 = 5.9 5.9 -5 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3834 None 40 Human Functional pAC50 = 5.9 5.9 -5 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5487.0 3834 None 40 Human Functional pAC50 = 5.9 5.9 -5 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3834 None 40 Human Functional pAC50 = 5.9 5.9 -5 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3834 None 40 Human Functional pAC50 = 5.9 5.9 -5 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3834 None 40 Human Functional pAC50 = 5.9 5.9 -5 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207084 None 54 Human Functional pAC50 = 4.9 4.9 -870 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4066.0 207084 None 54 Human Functional pAC50 = 4.9 4.9 -870 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207084 None 54 Human Functional pAC50 = 4.9 4.9 -870 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207084 None 54 Human Functional pAC50 = 4.9 4.9 -870 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1582 None 6 Human Functional pAC50 = 6.9 6.9 -208 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1582 None 6 Human Functional pAC50 = 6.9 6.9 -208 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1582 None 6 Human Functional pAC50 = 6.9 6.9 -208 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
8223.0 1582 None 6 Human Functional pAC50 = 6.9 6.9 -208 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1582 None 6 Human Functional pAC50 = 6.9 6.9 -208 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1582 None 6 Human Functional pAC50 = 6.9 6.9 -208 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1508 None 46 Human Functional pAC50 = 5.9 5.9 1 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1508 None 46 Human Functional pAC50 = 5.9 5.9 1 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1508 None 46 Human Functional pAC50 = 5.9 5.9 1 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1508 None 46 Human Functional pAC50 = 5.9 5.9 1 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1508 None 46 Human Functional pAC50 = 5.9 5.9 1 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2981 None 32 Human Functional pAC50 = 5.9 5.9 -144 24
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2981 None 32 Human Functional pAC50 = 5.9 5.9 -144 24
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2981 None 32 Human Functional pAC50 = 5.9 5.9 -144 24
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4636.0 2981 None 32 Human Functional pAC50 = 5.9 5.9 -144 24
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2981 None 32 Human Functional pAC50 = 5.9 5.9 -144 24
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2981 None 32 Human Functional pAC50 = 5.9 5.9 -144 24
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3173 None 38 Human Functional pAC50 = 5.9 5.9 -22 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3173 None 38 Human Functional pAC50 = 5.9 5.9 -22 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4917.0 3173 None 38 Human Functional pAC50 = 5.9 5.9 -22 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3173 None 38 Human Functional pAC50 = 5.9 5.9 -22 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3173 None 38 Human Functional pAC50 = 5.9 5.9 -22 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3173 None 38 Human Functional pAC50 = 5.9 5.9 -22 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3806 None 35 Human Functional pAC50 = 5.9 5.9 -524 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3806 None 35 Human Functional pAC50 = 5.9 5.9 -524 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3806 None 35 Human Functional pAC50 = 5.9 5.9 -524 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
941651.0 3806 None 35 Human Functional pAC50 = 5.9 5.9 -524 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3806 None 35 Human Functional pAC50 = 5.9 5.9 -524 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3806 None 35 Human Functional pAC50 = 5.9 5.9 -524 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 31564 None 60 Human Functional pAC50 = 5.9 5.9 3 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 31564 None 60 Human Functional pAC50 = 5.9 5.9 3 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 31564 None 60 Human Functional pAC50 = 5.9 5.9 3 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78241 None 0 Human Functional pAC50 = 5.9 5.9 3 4
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78241 None 0 Human Functional pAC50 = 5.9 5.9 3 4
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78295 None 23 Human Functional pAC50 = 5.9 5.9 -11 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78295 None 23 Human Functional pAC50 = 5.9 5.9 -11 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3202 None 61 Human Functional pAC50 = 4.9 4.9 -1202 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3202 None 61 Human Functional pAC50 = 4.9 4.9 -1202 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
3052762.0 3202 None 61 Human Functional pAC50 = 4.9 4.9 -1202 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3202 None 61 Human Functional pAC50 = 4.9 4.9 -1202 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3202 None 61 Human Functional pAC50 = 4.9 4.9 -1202 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3202 None 61 Human Functional pAC50 = 4.9 4.9 -1202 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 120581 None 50 Human Functional pAC50 = 4.9 4.9 -3 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 120581 None 50 Human Functional pAC50 = 4.9 4.9 -3 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 133578 None 43 Human Functional pAC50 = 4.9 4.9 - 1
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 133578 None 43 Human Functional pAC50 = 4.9 4.9 - 1
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207971 None 50 Human Functional pAC50 = 4.9 4.9 -50 37
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207971 None 50 Human Functional pAC50 = 4.9 4.9 -50 37
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207971 None 50 Human Functional pAC50 = 4.9 4.9 -50 37
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 37 Human Functional pAC50 = 4.8 4.8 -6606 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 37 Human Functional pAC50 = 4.8 4.8 -6606 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 37 Human Functional pAC50 = 4.8 4.8 -6606 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 37 Human Functional pAC50 = 4.8 4.8 -6606 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 37 Human Functional pAC50 = 4.8 4.8 -6606 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 37 Human Functional pAC50 = 4.8 4.8 -6606 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14460 None 44 Human Functional pAC50 = 5.8 5.8 1 4
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14460 None 44 Human Functional pAC50 = 5.8 5.8 1 4
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3187 None 44 Human Functional pAC50 = 4.8 4.8 -9549 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3187 None 44 Human Functional pAC50 = 4.8 4.8 -9549 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3187 None 44 Human Functional pAC50 = 4.8 4.8 -9549 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3187 None 44 Human Functional pAC50 = 4.8 4.8 -9549 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3187 None 44 Human Functional pAC50 = 4.8 4.8 -9549 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3187 None 44 Human Functional pAC50 = 4.8 4.8 -9549 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3187 None 44 Human Functional pAC50 = 4.8 4.8 -9549 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3187 None 44 Human Functional pAC50 = 4.8 4.8 -9549 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 19056 None 55 Human Functional pAC50 = 4.8 4.8 -1 3
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 19056 None 55 Human Functional pAC50 = 4.8 4.8 -1 3
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 127295 None 58 Human Functional pAC50 = 4.8 4.8 -1 3
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 127295 None 58 Human Functional pAC50 = 4.8 4.8 -1 3
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 729 None 28 Human Functional pAC50 = 5.8 5.8 -323 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
31101.0 729 None 28 Human Functional pAC50 = 5.8 5.8 -323 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
35 729 None 28 Human Functional pAC50 = 5.8 5.8 -323 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
403 729 None 28 Human Functional pAC50 = 5.8 5.8 -323 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 729 None 28 Human Functional pAC50 = 5.8 5.8 -323 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 729 None 28 Human Functional pAC50 = 5.8 5.8 -323 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 194927 None 32 Human Functional pAC50 = 6.8 6.8 -13 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5311507.0 194927 None 32 Human Functional pAC50 = 6.8 6.8 -13 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 194927 None 32 Human Functional pAC50 = 6.8 6.8 -13 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 194927 None 32 Human Functional pAC50 = 6.8 6.8 -13 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 111644 None 40 Human Functional pAC50 = 5.8 5.8 -18 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 111644 None 40 Human Functional pAC50 = 5.8 5.8 -18 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 940 None 51 Human Functional pAC50 = 4.8 4.8 -38 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
1547484.0 940 None 51 Human Functional pAC50 = 4.8 4.8 -38 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
654 940 None 51 Human Functional pAC50 = 4.8 4.8 -38 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 940 None 51 Human Functional pAC50 = 4.8 4.8 -38 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 940 None 51 Human Functional pAC50 = 4.8 4.8 -38 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 940 None 51 Human Functional pAC50 = 4.8 4.8 -38 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3779 None 53 Human Functional pAC50 = 4.8 4.8 -223 32
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3779 None 53 Human Functional pAC50 = 4.8 4.8 -223 32
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3779 None 53 Human Functional pAC50 = 4.8 4.8 -223 32
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3779 None 53 Human Functional pAC50 = 4.8 4.8 -223 32
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3779 None 53 Human Functional pAC50 = 4.8 4.8 -223 32
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4781 None 63 Human Functional pAC50 = 4.8 4.8 -165 44
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4781 None 63 Human Functional pAC50 = 4.8 4.8 -165 44
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 5260 None 48 Human Functional pAC50 = 4.8 4.8 -6 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 5260 None 48 Human Functional pAC50 = 4.8 4.8 -6 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 52574 None 20 Human Functional pAC50 = 4.8 4.8 -14 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4260.0 52574 None 20 Human Functional pAC50 = 4.8 4.8 -14 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 52574 None 20 Human Functional pAC50 = 4.8 4.8 -14 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 52574 None 20 Human Functional pAC50 = 4.8 4.8 -14 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 178333 None 41 Human Functional pAC50 = 4.8 4.8 -24 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 178333 None 41 Human Functional pAC50 = 4.8 4.8 -24 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207349 None 24 Human Functional pAC50 = 4.8 4.8 -15 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207349 None 24 Human Functional pAC50 = 4.8 4.8 -15 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207349 None 24 Human Functional pAC50 = 4.8 4.8 -15 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 89164 None 10 Human Functional pAC50 = 7.8 7.8 -1 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 89164 None 10 Human Functional pAC50 = 7.8 7.8 -1 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 599 None 30 Human Functional pAC50 = 5.8 5.8 -5 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
331 599 None 30 Human Functional pAC50 = 5.8 5.8 -5 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 599 None 30 Human Functional pAC50 = 5.8 5.8 -5 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 599 None 30 Human Functional pAC50 = 5.8 5.8 -5 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 599 None 30 Human Functional pAC50 = 5.8 5.8 -5 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2509 None 14 Human Functional pAC50 = 5.8 5.8 -676 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2509 None 14 Human Functional pAC50 = 5.8 5.8 -676 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2509 None 14 Human Functional pAC50 = 5.8 5.8 -676 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
8226.0 2509 None 14 Human Functional pAC50 = 5.8 5.8 -676 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2509 None 14 Human Functional pAC50 = 5.8 5.8 -676 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2509 None 14 Human Functional pAC50 = 5.8 5.8 -676 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 10802 None 64 Human Functional pAC50 = 4.8 4.8 -53 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 10802 None 64 Human Functional pAC50 = 4.8 4.8 -53 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 63203 None 12 Human Functional pAC50 = 4.8 4.8 -74 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5039.0 63203 None 12 Human Functional pAC50 = 4.8 4.8 -74 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 63203 None 12 Human Functional pAC50 = 4.8 4.8 -74 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 63203 None 12 Human Functional pAC50 = 4.8 4.8 -74 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 106225 None 66 Human Functional pAC50 = 4.8 4.8 -7 2
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 106225 None 66 Human Functional pAC50 = 4.8 4.8 -7 2
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 208853 None 39 Human Functional pAC50 = 4.8 4.8 -26 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 208853 None 39 Human Functional pAC50 = 4.8 4.8 -26 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 62505 None 35 Human Functional pAC50 = 4.8 4.8 -8 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 62505 None 35 Human Functional pAC50 = 4.8 4.8 -8 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 62505 None 35 Human Functional pAC50 = 4.8 4.8 -8 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 194838 None 50 Human Functional pAC50 = 5.8 5.8 -16 37
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 194838 None 50 Human Functional pAC50 = 5.8 5.8 -16 37
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1389 None 72 Human Functional pAC50 = 4.8 4.8 -407 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
124087.0 1389 None 72 Human Functional pAC50 = 4.8 4.8 -407 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1389 None 72 Human Functional pAC50 = 4.8 4.8 -407 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1389 None 72 Human Functional pAC50 = 4.8 4.8 -407 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1389 None 72 Human Functional pAC50 = 4.8 4.8 -407 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1389 None 72 Human Functional pAC50 = 4.8 4.8 -407 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 19421 None 48 Human Functional pAC50 = 4.8 4.8 -13 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 19421 None 48 Human Functional pAC50 = 4.8 4.8 -13 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2006 None 61 Human Functional pAC50 = 7.8 7.8 -18 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2006 None 61 Human Functional pAC50 = 7.8 7.8 -18 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
71360.0 2006 None 61 Human Functional pAC50 = 7.8 7.8 -18 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2006 None 61 Human Functional pAC50 = 7.8 7.8 -18 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2006 None 61 Human Functional pAC50 = 7.8 7.8 -18 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2006 None 61 Human Functional pAC50 = 7.8 7.8 -18 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207729 None 57 Human Functional pAC50 = 5.8 5.8 -3 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207729 None 57 Human Functional pAC50 = 5.8 5.8 -3 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207729 None 57 Human Functional pAC50 = 5.8 5.8 -3 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207729 None 57 Human Functional pAC50 = 5.8 5.8 -3 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207729 None 57 Human Functional pAC50 = 5.8 5.8 -3 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207729 None 57 Human Functional pAC50 = 5.8 5.8 -3 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207729 None 57 Human Functional pAC50 = 5.8 5.8 -3 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4153 None 44 Human Functional pAC50 = 5.7 5.7 -316 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4153 None 44 Human Functional pAC50 = 5.7 5.7 -316 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4153 None 44 Human Functional pAC50 = 5.7 5.7 -316 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4153 None 44 Human Functional pAC50 = 5.7 5.7 -316 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4153 None 44 Human Functional pAC50 = 5.7 5.7 -316 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 597 None 17 Human Functional pAC50 = 5.7 5.7 -426 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
1201549.0 597 None 17 Human Functional pAC50 = 5.7 5.7 -426 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
333 597 None 17 Human Functional pAC50 = 5.7 5.7 -426 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 597 None 17 Human Functional pAC50 = 5.7 5.7 -426 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 597 None 17 Human Functional pAC50 = 5.7 5.7 -426 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 597 None 17 Human Functional pAC50 = 5.7 5.7 -426 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 597 None 17 Human Functional pAC50 = 5.7 5.7 -426 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2605 None 60 Human Functional pAC50 = 4.7 4.7 -26 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2605 None 60 Human Functional pAC50 = 4.7 4.7 -26 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4810.0 2605 None 60 Human Functional pAC50 = 4.7 4.7 -26 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2605 None 60 Human Functional pAC50 = 4.7 4.7 -26 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2605 None 60 Human Functional pAC50 = 4.7 4.7 -26 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 15583 None 40 Human Functional pAC50 = 4.7 4.7 -5 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 15583 None 40 Human Functional pAC50 = 4.7 4.7 -5 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 15583 None 40 Human Functional pAC50 = 4.7 4.7 -5 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 33583 None 70 Human Functional pAC50 = 4.7 4.7 -3 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 33583 None 70 Human Functional pAC50 = 4.7 4.7 -3 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
CHEMBL5416410 33583 None 70 Human Functional pAC50 = 4.7 4.7 -3 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 596 None 33 Human Functional pAC50 = 5.7 5.7 -363 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
16363.0 596 None 33 Human Functional pAC50 = 5.7 5.7 -363 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
312 596 None 33 Human Functional pAC50 = 5.7 5.7 -363 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 596 None 33 Human Functional pAC50 = 5.7 5.7 -363 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 596 None 33 Human Functional pAC50 = 5.7 5.7 -363 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 596 None 33 Human Functional pAC50 = 5.7 5.7 -363 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 958 None 57 Human Functional pAC50 = 7.7 7.7 -6 43
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
135398737.0 958 None 57 Human Functional pAC50 = 7.7 7.7 -6 43
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
38 958 None 57 Human Functional pAC50 = 7.7 7.7 -6 43
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
722 958 None 57 Human Functional pAC50 = 7.7 7.7 -6 43
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 958 None 57 Human Functional pAC50 = 7.7 7.7 -6 43
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 958 None 57 Human Functional pAC50 = 7.7 7.7 -6 43
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 34231 None 58 Human Functional pAC50 = 6.7 6.7 -3 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4418.0 34231 None 58 Human Functional pAC50 = 6.7 6.7 -3 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 34231 None 58 Human Functional pAC50 = 6.7 6.7 -3 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 34231 None 58 Human Functional pAC50 = 6.7 6.7 -3 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2757 None 41 Human Functional pAC50 = 5.7 5.7 -660 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2757 None 41 Human Functional pAC50 = 5.7 5.7 -660 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2757 None 41 Human Functional pAC50 = 5.7 5.7 -660 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
189562.0 2757 None 41 Human Functional pAC50 = 5.7 5.7 -660 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2757 None 41 Human Functional pAC50 = 5.7 5.7 -660 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
71301.0 2757 None 41 Human Functional pAC50 = 5.7 5.7 -660 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2757 None 41 Human Functional pAC50 = 5.7 5.7 -660 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2757 None 41 Human Functional pAC50 = 5.7 5.7 -660 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
9844194.0 2757 None 41 Human Functional pAC50 = 5.7 5.7 -660 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2757 None 41 Human Functional pAC50 = 5.7 5.7 -660 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2757 None 41 Human Functional pAC50 = 5.7 5.7 -660 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2757 None 41 Human Functional pAC50 = 5.7 5.7 -660 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2757 None 41 Human Functional pAC50 = 5.7 5.7 -660 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3860 None 43 Human Functional pAC50 = 5.7 5.7 -134 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3860 None 43 Human Functional pAC50 = 5.7 5.7 -134 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3860 None 43 Human Functional pAC50 = 5.7 5.7 -134 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5566.0 3860 None 43 Human Functional pAC50 = 5.7 5.7 -134 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3860 None 43 Human Functional pAC50 = 5.7 5.7 -134 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3860 None 43 Human Functional pAC50 = 5.7 5.7 -134 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3860 None 43 Human Functional pAC50 = 5.7 5.7 -134 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 11852 None 18 Human Functional pAC50 = 5.7 5.7 -14 34
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 11852 None 18 Human Functional pAC50 = 5.7 5.7 -14 34
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 11852 None 18 Human Functional pAC50 = 5.7 5.7 -14 34
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 11852 None 18 Human Functional pAC50 = 5.7 5.7 -14 34
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78169 None 0 Human Functional pAC50 = 4.7 4.7 -3 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2590 None 33 Human Functional pAC50 = 5.7 5.7 -58 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2590 None 33 Human Functional pAC50 = 5.7 5.7 -58 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2590 None 33 Human Functional pAC50 = 5.7 5.7 -58 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
23897.0 2590 None 33 Human Functional pAC50 = 5.7 5.7 -58 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2590 None 33 Human Functional pAC50 = 5.7 5.7 -58 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2590 None 33 Human Functional pAC50 = 5.7 5.7 -58 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3334 None 46 Human Functional pAC50 = 4.7 4.7 -1737 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3334 None 46 Human Functional pAC50 = 4.7 4.7 -1737 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5078.0 3334 None 46 Human Functional pAC50 = 4.7 4.7 -1737 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3334 None 46 Human Functional pAC50 = 4.7 4.7 -1737 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3334 None 46 Human Functional pAC50 = 4.7 4.7 -1737 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3334 None 46 Human Functional pAC50 = 4.7 4.7 -1737 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 67630 None 28 Human Functional pAC50 = 5.7 5.7 -1 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 67630 None 28 Human Functional pAC50 = 5.7 5.7 -1 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2013 None 42 Human Functional pAC50 = 5.7 5.7 -2691 30
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2013 None 42 Human Functional pAC50 = 5.7 5.7 -2691 30
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2013 None 42 Human Functional pAC50 = 5.7 5.7 -2691 30
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2013 None 42 Human Functional pAC50 = 5.7 5.7 -2691 30
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2013 None 42 Human Functional pAC50 = 5.7 5.7 -2691 30
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3095 None 24 Human Functional pAC50 = 5.7 5.7 -41 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3095 None 24 Human Functional pAC50 = 5.7 5.7 -41 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4768.0 3095 None 24 Human Functional pAC50 = 5.7 5.7 -41 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3095 None 24 Human Functional pAC50 = 5.7 5.7 -41 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3095 None 24 Human Functional pAC50 = 5.7 5.7 -41 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3095 None 24 Human Functional pAC50 = 5.7 5.7 -41 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3134 None 58 Human Functional pAC50 = 5.7 5.7 -758 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3134 None 58 Human Functional pAC50 = 5.7 5.7 -758 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
27400.0 3134 None 58 Human Functional pAC50 = 5.7 5.7 -758 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3134 None 58 Human Functional pAC50 = 5.7 5.7 -758 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3134 None 58 Human Functional pAC50 = 5.7 5.7 -758 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3134 None 58 Human Functional pAC50 = 5.7 5.7 -758 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 99367 None 27 Human Functional pAC50 = 5.7 5.7 -3 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 99367 None 27 Human Functional pAC50 = 5.7 5.7 -3 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 102785 None 36 Human Functional pAC50 = 5.7 5.7 -338 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
16351.0 102785 None 36 Human Functional pAC50 = 5.7 5.7 -338 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 102785 None 36 Human Functional pAC50 = 5.7 5.7 -338 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 102785 None 36 Human Functional pAC50 = 5.7 5.7 -338 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 110592 None 24 Human Functional pAC50 = 5.7 5.7 -218 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2780.0 110592 None 24 Human Functional pAC50 = 5.7 5.7 -218 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 110592 None 24 Human Functional pAC50 = 5.7 5.7 -218 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 110592 None 24 Human Functional pAC50 = 5.7 5.7 -218 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78425 None 58 Human Functional pAC50 = 4.7 4.7 -2 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78425 None 58 Human Functional pAC50 = 4.7 4.7 -2 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 120312 None 42 Human Functional pAC50 = 4.7 4.7 -1 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 120312 None 42 Human Functional pAC50 = 4.7 4.7 -1 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 209014 None 51 Human Functional pAC50 = 4.7 4.7 -2 3
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 209014 None 51 Human Functional pAC50 = 4.7 4.7 -2 3
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 59901 None 35 Human Functional pAC50 = 4.7 4.7 -8 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 59901 None 35 Human Functional pAC50 = 4.7 4.7 -8 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78248 None 44 Human Functional pAC50 = 4.7 4.7 -7 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78248 None 44 Human Functional pAC50 = 4.7 4.7 -7 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 722 None 63 Human Functional pAC50 = 5.7 5.7 -7 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2435.0 722 None 63 Human Functional pAC50 = 5.7 5.7 -7 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
395 722 None 63 Human Functional pAC50 = 5.7 5.7 -7 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
520 722 None 63 Human Functional pAC50 = 5.7 5.7 -7 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 722 None 63 Human Functional pAC50 = 5.7 5.7 -7 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 722 None 63 Human Functional pAC50 = 5.7 5.7 -7 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 722 None 63 Human Functional pAC50 = 5.7 5.7 -7 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 28732 None 28 Human Functional pAC50 = 5.7 5.7 -707 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5440.0 28732 None 28 Human Functional pAC50 = 5.7 5.7 -707 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 28732 None 28 Human Functional pAC50 = 5.7 5.7 -707 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 28732 None 28 Human Functional pAC50 = 5.7 5.7 -707 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 178724 None 43 Human Functional pAC50 = 6.7 6.7 4 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 178724 None 43 Human Functional pAC50 = 6.7 6.7 4 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 188904 None 34 Human Functional pAC50 = 6.6 6.6 -1 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 188904 None 34 Human Functional pAC50 = 6.6 6.6 -1 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 188904 None 34 Human Functional pAC50 = 6.6 6.6 -1 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1957 None 46 Human Functional pAC50 = 5.6 5.6 -17 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1957 None 46 Human Functional pAC50 = 5.6 5.6 -17 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
3658.0 1957 None 46 Human Functional pAC50 = 5.6 5.6 -17 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1957 None 46 Human Functional pAC50 = 5.6 5.6 -17 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1957 None 46 Human Functional pAC50 = 5.6 5.6 -17 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1957 None 46 Human Functional pAC50 = 5.6 5.6 -17 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1957 None 46 Human Functional pAC50 = 5.6 5.6 -17 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 44861 None 29 Human Functional pAC50 = 5.6 5.6 -38 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 44861 None 29 Human Functional pAC50 = 5.6 5.6 -38 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 91619 None 25 Human Functional pAC50 = 5.6 5.6 -6 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 91619 None 25 Human Functional pAC50 = 5.6 5.6 -6 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1630 None 10 Human Functional pAC50 = 4.6 4.6 -3235 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1630 None 10 Human Functional pAC50 = 4.6 4.6 -3235 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1630 None 10 Human Functional pAC50 = 4.6 4.6 -3235 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
3345.0 1630 None 10 Human Functional pAC50 = 4.6 4.6 -3235 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1630 None 10 Human Functional pAC50 = 4.6 4.6 -3235 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1630 None 10 Human Functional pAC50 = 4.6 4.6 -3235 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4107 None 38 Human Functional pAC50 = 6.6 6.6 -12 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4107 None 38 Human Functional pAC50 = 6.6 6.6 -12 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4107 None 38 Human Functional pAC50 = 6.6 6.6 -12 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5709.0 4107 None 38 Human Functional pAC50 = 6.6 6.6 -12 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4107 None 38 Human Functional pAC50 = 6.6 6.6 -12 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4107 None 38 Human Functional pAC50 = 6.6 6.6 -12 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 157623 None 57 Human Functional pAC50 = 4.6 4.6 -14 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 157623 None 57 Human Functional pAC50 = 4.6 4.6 -14 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 45 Human Functional pAC50 = 5.6 5.6 -100 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2267.0 559 None 45 Human Functional pAC50 = 5.6 5.6 -100 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 45 Human Functional pAC50 = 5.6 5.6 -100 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 45 Human Functional pAC50 = 5.6 5.6 -100 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 45 Human Functional pAC50 = 5.6 5.6 -100 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 45 Human Functional pAC50 = 5.6 5.6 -100 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 154946 None 18 Human Functional pAC50 = 5.6 5.6 -3 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 154946 None 18 Human Functional pAC50 = 5.6 5.6 -3 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 955 None 40 Human Functional pAC50 = 6.6 6.6 -15 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2803.0 955 None 40 Human Functional pAC50 = 6.6 6.6 -15 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
516 955 None 40 Human Functional pAC50 = 6.6 6.6 -15 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
704 955 None 40 Human Functional pAC50 = 6.6 6.6 -15 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 955 None 40 Human Functional pAC50 = 6.6 6.6 -15 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 955 None 40 Human Functional pAC50 = 6.6 6.6 -15 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 6 Human Functional pAC50 = 5.6 5.6 -13182 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
11434515.0 261 None 6 Human Functional pAC50 = 5.6 5.6 -13182 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 6 Human Functional pAC50 = 5.6 5.6 -13182 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 6 Human Functional pAC50 = 5.6 5.6 -13182 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 6 Human Functional pAC50 = 5.6 5.6 -13182 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 6 Human Functional pAC50 = 5.6 5.6 -13182 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 6 Human Functional pAC50 = 5.6 5.6 -13182 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 57423 None 16 Human Functional pAC50 = 5.6 5.6 -3 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 57423 None 16 Human Functional pAC50 = 5.6 5.6 -3 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 84720 None 41 Human Functional pAC50 = 4.6 4.6 -5 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 84720 None 41 Human Functional pAC50 = 4.6 4.6 -5 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1889 None 43 Human Functional pAC50 = 5.6 5.6 -11 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1889 None 43 Human Functional pAC50 = 5.6 5.6 -11 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
3519.0 1889 None 43 Human Functional pAC50 = 5.6 5.6 -11 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1889 None 43 Human Functional pAC50 = 5.6 5.6 -11 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1889 None 43 Human Functional pAC50 = 5.6 5.6 -11 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1889 None 43 Human Functional pAC50 = 5.6 5.6 -11 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78250 None 62 Human Functional pAC50 = 4.6 4.6 -21 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78250 None 62 Human Functional pAC50 = 4.6 4.6 -21 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78289 None 22 Human Functional pAC50 = 4.6 4.6 -77 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78289 None 22 Human Functional pAC50 = 4.6 4.6 -77 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 142422 None 66 Human Functional pAC50 = 4.6 4.6 -22 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 142422 None 66 Human Functional pAC50 = 4.6 4.6 -22 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1420 None 13 Human Functional pAC50 = 7.6 7.6 -19 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
10531.0 1420 None 13 Human Functional pAC50 = 7.6 7.6 -19 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1420 None 13 Human Functional pAC50 = 7.6 7.6 -19 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1420 None 13 Human Functional pAC50 = 7.6 7.6 -19 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1420 None 13 Human Functional pAC50 = 7.6 7.6 -19 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1420 None 13 Human Functional pAC50 = 7.6 7.6 -19 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2857 None 46 Human Functional pAC50 = 6.6 6.6 -11 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2857 None 46 Human Functional pAC50 = 6.6 6.6 -11 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
439260.0 2857 None 46 Human Functional pAC50 = 6.6 6.6 -11 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2857 None 46 Human Functional pAC50 = 6.6 6.6 -11 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2857 None 46 Human Functional pAC50 = 6.6 6.6 -11 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2857 None 46 Human Functional pAC50 = 6.6 6.6 -11 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 60304 None 49 Human Functional pAC50 = 5.6 5.6 - 1
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5282136.0 60304 None 49 Human Functional pAC50 = 5.6 5.6 - 1
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 60304 None 49 Human Functional pAC50 = 5.6 5.6 - 1
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 60304 None 49 Human Functional pAC50 = 5.6 5.6 - 1
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 204590 None 44 Human Functional pAC50 = 5.6 5.6 -275 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
9429.0 204590 None 44 Human Functional pAC50 = 5.6 5.6 -275 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 204590 None 44 Human Functional pAC50 = 5.6 5.6 -275 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 204590 None 44 Human Functional pAC50 = 5.6 5.6 -275 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3869 None 33 Human Functional pAC50 = 4.6 4.6 -7 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3869 None 33 Human Functional pAC50 = 4.6 4.6 -7 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3869 None 33 Human Functional pAC50 = 4.6 4.6 -7 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3869 None 33 Human Functional pAC50 = 4.6 4.6 -7 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3869 None 33 Human Functional pAC50 = 4.6 4.6 -7 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2324 77126 None 16 Human Functional pAC50 = 4.6 4.6 -17 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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)OC2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL2074972 77126 None 16 Human Functional pAC50 = 4.6 4.6 -17 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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)OC2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL4743867 216518 None 10 Human Functional pAC50 = 6.6 6.6 -89 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 40 Human Functional pAC50 = 5.6 5.6 -44 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 40 Human Functional pAC50 = 5.6 5.6 -44 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 40 Human Functional pAC50 = 5.6 5.6 -44 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 40 Human Functional pAC50 = 5.6 5.6 -44 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5816.0 291 None 40 Human Functional pAC50 = 5.6 5.6 -44 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 40 Human Functional pAC50 = 5.6 5.6 -44 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 40 Human Functional pAC50 = 5.6 5.6 -44 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1462 None 65 Human Functional pAC50 = 5.6 5.6 -602 24
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
3151.0 1462 None 65 Human Functional pAC50 = 5.6 5.6 -602 24
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1462 None 65 Human Functional pAC50 = 5.6 5.6 -602 24
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1462 None 65 Human Functional pAC50 = 5.6 5.6 -602 24
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1462 None 65 Human Functional pAC50 = 5.6 5.6 -602 24
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1462 None 65 Human Functional pAC50 = 5.6 5.6 -602 24
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 26472 None 27 Human Functional pAC50 = 5.6 5.6 1 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 26472 None 27 Human Functional pAC50 = 5.6 5.6 1 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 27995 None 38 Human Functional pAC50 = 5.6 5.6 -1 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 27995 None 38 Human Functional pAC50 = 5.6 5.6 -1 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 98949 None 48 Human Functional pAC50 = 5.6 5.6 -53 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 98949 None 48 Human Functional pAC50 = 5.6 5.6 -53 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 167616 None 49 Human Functional pAC50 = 5.6 5.6 -2 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 167616 None 49 Human Functional pAC50 = 5.6 5.6 -2 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 167616 None 49 Human Functional pAC50 = 5.6 5.6 -2 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 38 Human Functional pAC50 = 6.5 6.5 -281 38
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 38 Human Functional pAC50 = 6.5 6.5 -281 38
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 38 Human Functional pAC50 = 6.5 6.5 -281 38
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2160.0 401 None 38 Human Functional pAC50 = 6.5 6.5 -281 38
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 38 Human Functional pAC50 = 6.5 6.5 -281 38
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 38 Human Functional pAC50 = 6.5 6.5 -281 38
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 210437 None 20 Human Functional pAC50 = 5.5 5.5 -7 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 210437 None 20 Human Functional pAC50 = 5.5 5.5 -7 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 23189 None 39 Human Functional pAC50 = 4.5 4.5 -7079 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 23189 None 39 Human Functional pAC50 = 4.5 4.5 -7079 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3780 None 25 Human Functional pAC50 = 8.5 8.5 1 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3780 None 25 Human Functional pAC50 = 8.5 8.5 1 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3780 None 25 Human Functional pAC50 = 8.5 8.5 1 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3780 None 25 Human Functional pAC50 = 8.5 8.5 1 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3780 None 25 Human Functional pAC50 = 8.5 8.5 1 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4127 None 36 Human Functional pAC50 = 8.5 8.5 -2 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4127 None 36 Human Functional pAC50 = 8.5 8.5 -2 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4127 None 36 Human Functional pAC50 = 8.5 8.5 -2 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
8969.0 4127 None 36 Human Functional pAC50 = 8.5 8.5 -2 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4127 None 36 Human Functional pAC50 = 8.5 8.5 -2 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4127 None 36 Human Functional pAC50 = 8.5 8.5 -2 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
37 778 None 41 Human Functional pAC50 = 6.5 6.5 -63 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
460 778 None 41 Human Functional pAC50 = 6.5 6.5 -63 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 778 None 41 Human Functional pAC50 = 6.5 6.5 -63 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
54746.0 778 None 41 Human Functional pAC50 = 6.5 6.5 -63 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 778 None 41 Human Functional pAC50 = 6.5 6.5 -63 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 778 None 41 Human Functional pAC50 = 6.5 6.5 -63 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3749 None 48 Human Functional pAC50 = 6.5 6.5 -660 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
129211.0 3749 None 48 Human Functional pAC50 = 6.5 6.5 -660 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3749 None 48 Human Functional pAC50 = 6.5 6.5 -660 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3749 None 48 Human Functional pAC50 = 6.5 6.5 -660 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3749 None 48 Human Functional pAC50 = 6.5 6.5 -660 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3749 None 48 Human Functional pAC50 = 6.5 6.5 -660 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 107587 None 16 Human Functional pAC50 = 6.5 6.5 -1513 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
3036780.0 107587 None 16 Human Functional pAC50 = 6.5 6.5 -1513 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 107587 None 16 Human Functional pAC50 = 6.5 6.5 -1513 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 107587 None 16 Human Functional pAC50 = 6.5 6.5 -1513 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
9903970.0 107587 None 16 Human Functional pAC50 = 6.5 6.5 -1513 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 107587 None 16 Human Functional pAC50 = 6.5 6.5 -1513 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 107587 None 16 Human Functional pAC50 = 6.5 6.5 -1513 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 107587 None 16 Human Functional pAC50 = 6.5 6.5 -1513 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 107587 None 16 Human Functional pAC50 = 6.5 6.5 -1513 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2518 None 51 Human Functional pAC50 = 5.5 5.5 -144 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2518 None 51 Human Functional pAC50 = 5.5 5.5 -144 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2518 None 51 Human Functional pAC50 = 5.5 5.5 -144 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4168.0 2518 None 51 Human Functional pAC50 = 5.5 5.5 -144 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2518 None 51 Human Functional pAC50 = 5.5 5.5 -144 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2518 None 51 Human Functional pAC50 = 5.5 5.5 -144 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3183 None 36 Human Functional pAC50 = 5.5 5.5 -602 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3183 None 36 Human Functional pAC50 = 5.5 5.5 -602 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4927.0 3183 None 36 Human Functional pAC50 = 5.5 5.5 -602 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3183 None 36 Human Functional pAC50 = 5.5 5.5 -602 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3183 None 36 Human Functional pAC50 = 5.5 5.5 -602 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3183 None 36 Human Functional pAC50 = 5.5 5.5 -602 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 121354 None 36 Human Functional pAC50 = 5.5 5.5 -269 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 121354 None 36 Human Functional pAC50 = 5.5 5.5 -269 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 919 None 48 Human Functional pAC50 = 5.5 5.5 -501 42
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2726.0 919 None 48 Human Functional pAC50 = 5.5 5.5 -501 42
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
621 919 None 48 Human Functional pAC50 = 5.5 5.5 -501 42
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
83 919 None 48 Human Functional pAC50 = 5.5 5.5 -501 42
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 919 None 48 Human Functional pAC50 = 5.5 5.5 -501 42
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 919 None 48 Human Functional pAC50 = 5.5 5.5 -501 42
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 60 Human Functional pAC50 = 5.5 5.5 -524 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 60 Human Functional pAC50 = 5.5 5.5 -524 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 60 Human Functional pAC50 = 5.5 5.5 -524 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2170.0 403 None 60 Human Functional pAC50 = 5.5 5.5 -524 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 60 Human Functional pAC50 = 5.5 5.5 -524 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 60 Human Functional pAC50 = 5.5 5.5 -524 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 20 Human Functional pAC50 = 5.5 5.5 -758 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 20 Human Functional pAC50 = 5.5 5.5 -758 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 20 Human Functional pAC50 = 5.5 5.5 -758 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
6005.0 445 None 20 Human Functional pAC50 = 5.5 5.5 -758 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 20 Human Functional pAC50 = 5.5 5.5 -758 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 20 Human Functional pAC50 = 5.5 5.5 -758 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 98126 None 43 Human Functional pAC50 = 5.5 5.5 1 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 98126 None 43 Human Functional pAC50 = 5.5 5.5 1 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 194796 None 31 Human Functional pAC50 = 5.5 5.5 1 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 194796 None 31 Human Functional pAC50 = 5.5 5.5 1 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2733 None 38 Human Functional pAC50 = 6.5 6.5 -13 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2733 None 38 Human Functional pAC50 = 6.5 6.5 -13 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2733 None 38 Human Functional pAC50 = 6.5 6.5 -13 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4436.0 2733 None 38 Human Functional pAC50 = 6.5 6.5 -13 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2733 None 38 Human Functional pAC50 = 6.5 6.5 -13 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2733 None 38 Human Functional pAC50 = 6.5 6.5 -13 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2733 None 38 Human Functional pAC50 = 6.5 6.5 -13 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4143 None 47 Human Functional pAC50 = 6.5 6.5 -138 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4143 None 47 Human Functional pAC50 = 6.5 6.5 -138 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4143 None 47 Human Functional pAC50 = 6.5 6.5 -138 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
60854.0 4143 None 47 Human Functional pAC50 = 6.5 6.5 -138 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4143 None 47 Human Functional pAC50 = 6.5 6.5 -138 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4143 None 47 Human Functional pAC50 = 6.5 6.5 -138 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4301 None 35 Human Functional pAC50 = 5.5 5.5 -1 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4301 None 35 Human Functional pAC50 = 5.5 5.5 -1 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 4301 None 35 Human Functional pAC50 = 5.5 5.5 -1 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1470 None 44 Human Functional pAC50 = 6.5 6.5 -446 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
3157.0 1470 None 44 Human Functional pAC50 = 6.5 6.5 -446 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1470 None 44 Human Functional pAC50 = 6.5 6.5 -446 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1470 None 44 Human Functional pAC50 = 6.5 6.5 -446 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1470 None 44 Human Functional pAC50 = 6.5 6.5 -446 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1470 None 44 Human Functional pAC50 = 6.5 6.5 -446 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3805 None 44 Human Functional pAC50 = 5.5 5.5 -162 38
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3805 None 44 Human Functional pAC50 = 5.5 5.5 -162 38
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3805 None 44 Human Functional pAC50 = 5.5 5.5 -162 38
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3805 None 44 Human Functional pAC50 = 5.5 5.5 -162 38
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3805 None 44 Human Functional pAC50 = 5.5 5.5 -162 38
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3777 None 45 Human Functional pAC50 = 6.5 6.5 -1548 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3777 None 45 Human Functional pAC50 = 6.5 6.5 -1548 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5401.0 3777 None 45 Human Functional pAC50 = 6.5 6.5 -1548 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3777 None 45 Human Functional pAC50 = 6.5 6.5 -1548 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3777 None 45 Human Functional pAC50 = 6.5 6.5 -1548 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3777 None 45 Human Functional pAC50 = 6.5 6.5 -1548 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3853 None 34 Human Functional pAC50 = 6.5 6.5 -28 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3853 None 34 Human Functional pAC50 = 6.5 6.5 -28 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3853 None 34 Human Functional pAC50 = 6.5 6.5 -28 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5533.0 3853 None 34 Human Functional pAC50 = 6.5 6.5 -28 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3853 None 34 Human Functional pAC50 = 6.5 6.5 -28 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3853 None 34 Human Functional pAC50 = 6.5 6.5 -28 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2514 None 19 Human Functional pAC50 = 5.5 5.5 -1819 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2514 None 19 Human Functional pAC50 = 5.5 5.5 -1819 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2514 None 19 Human Functional pAC50 = 5.5 5.5 -1819 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
9681.0 2514 None 19 Human Functional pAC50 = 5.5 5.5 -1819 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2514 None 19 Human Functional pAC50 = 5.5 5.5 -1819 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2514 None 19 Human Functional pAC50 = 5.5 5.5 -1819 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2344 None 24 Human Functional pAC50 = 5.4 5.4 -316 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2344 None 24 Human Functional pAC50 = 5.4 5.4 -316 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2344 None 24 Human Functional pAC50 = 5.4 5.4 -316 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2344 None 24 Human Functional pAC50 = 5.4 5.4 -316 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2344 None 24 Human Functional pAC50 = 5.4 5.4 -316 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3653 None 40 Human Functional pAC50 = 6.4 6.4 -6165 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3653 None 40 Human Functional pAC50 = 6.4 6.4 -6165 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3653 None 40 Human Functional pAC50 = 6.4 6.4 -6165 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3653 None 40 Human Functional pAC50 = 6.4 6.4 -6165 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3653 None 40 Human Functional pAC50 = 6.4 6.4 -6165 23
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 51685 None 37 Human Functional pAC50 = 6.4 6.4 -28 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 51685 None 37 Human Functional pAC50 = 6.4 6.4 -28 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 16656 None 34 Human Functional pAC50 = 5.4 5.4 -1 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 16656 None 34 Human Functional pAC50 = 5.4 5.4 -1 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 16656 None 34 Human Functional pAC50 = 5.4 5.4 -1 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 33346 None 22 Human Functional pAC50 = 5.4 5.4 -1 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 33346 None 22 Human Functional pAC50 = 5.4 5.4 -1 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 33346 None 22 Human Functional pAC50 = 5.4 5.4 -1 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206050 None 27 Human Functional pAC50 = 5.4 5.4 -186 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2895.0 206050 None 27 Human Functional pAC50 = 5.4 5.4 -186 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206050 None 27 Human Functional pAC50 = 5.4 5.4 -186 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206050 None 27 Human Functional pAC50 = 5.4 5.4 -186 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207985 None 33 Human Functional pAC50 = 5.4 5.4 -12 30
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207985 None 33 Human Functional pAC50 = 5.4 5.4 -12 30
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 207985 None 33 Human Functional pAC50 = 5.4 5.4 -12 30
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3372 None 50 Human Functional pAC50 = 6.4 6.4 -120 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3372 None 50 Human Functional pAC50 = 6.4 6.4 -120 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
59227.0 3372 None 50 Human Functional pAC50 = 6.4 6.4 -120 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3372 None 50 Human Functional pAC50 = 6.4 6.4 -120 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3372 None 50 Human Functional pAC50 = 6.4 6.4 -120 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3372 None 50 Human Functional pAC50 = 6.4 6.4 -120 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 13001 None 38 Human Functional pAC50 = 5.4 5.4 -3 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 13001 None 38 Human Functional pAC50 = 5.4 5.4 -3 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1324 None 32 Human Functional pAC50 = 6.4 6.4 -407 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1324 None 32 Human Functional pAC50 = 6.4 6.4 -407 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1324 None 32 Human Functional pAC50 = 6.4 6.4 -407 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
444031.0 1324 None 32 Human Functional pAC50 = 6.4 6.4 -407 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1324 None 32 Human Functional pAC50 = 6.4 6.4 -407 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1324 None 32 Human Functional pAC50 = 6.4 6.4 -407 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1324 None 32 Human Functional pAC50 = 6.4 6.4 -407 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2340 None 41 Human Functional pAC50 = 6.4 6.4 -1 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2340 None 41 Human Functional pAC50 = 6.4 6.4 -1 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
30668.0 2340 None 41 Human Functional pAC50 = 6.4 6.4 -1 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2340 None 41 Human Functional pAC50 = 6.4 6.4 -1 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2340 None 41 Human Functional pAC50 = 6.4 6.4 -1 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2340 None 41 Human Functional pAC50 = 6.4 6.4 -1 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 12618 None 11 Human Functional pAC50 = 5.4 5.4 -11 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 12618 None 11 Human Functional pAC50 = 5.4 5.4 -11 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 100668 None 35 Human Functional pAC50 = 5.4 5.4 -4 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 100668 None 35 Human Functional pAC50 = 5.4 5.4 -4 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206466 None 47 Human Functional pAC50 = 5.4 5.4 -38 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206466 None 47 Human Functional pAC50 = 5.4 5.4 -38 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206466 None 47 Human Functional pAC50 = 5.4 5.4 -38 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206077 None 58 Human Functional pAC50 = 5.4 5.4 -100 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206077 None 58 Human Functional pAC50 = 5.4 5.4 -100 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 954 None 43 Human Functional pAC50 = 5.4 5.4 -1819 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 954 None 43 Human Functional pAC50 = 5.4 5.4 -1819 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2801.0 954 None 43 Human Functional pAC50 = 5.4 5.4 -1819 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
701 954 None 43 Human Functional pAC50 = 5.4 5.4 -1819 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 954 None 43 Human Functional pAC50 = 5.4 5.4 -1819 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 954 None 43 Human Functional pAC50 = 5.4 5.4 -1819 36
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14476 None 26 Human Functional pAC50 = 5.4 5.4 -151 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14476 None 26 Human Functional pAC50 = 5.4 5.4 -151 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 98790 None 31 Human Functional pAC50 = 5.4 5.4 -407 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 98790 None 31 Human Functional pAC50 = 5.4 5.4 -407 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2762 None 13 Human Functional pAC50 = 6.3 6.3 -1513 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2762 None 13 Human Functional pAC50 = 6.3 6.3 -1513 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2762 None 13 Human Functional pAC50 = 6.3 6.3 -1513 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3057 None 57 Human Functional pAC50 = 6.3 6.3 -199 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3057 None 57 Human Functional pAC50 = 6.3 6.3 -199 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3057 None 57 Human Functional pAC50 = 6.3 6.3 -199 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4748.0 3057 None 57 Human Functional pAC50 = 6.3 6.3 -199 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3057 None 57 Human Functional pAC50 = 6.3 6.3 -199 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3057 None 57 Human Functional pAC50 = 6.3 6.3 -199 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3286 None 44 Human Functional pAC50 = 6.3 6.3 -93 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3286 None 44 Human Functional pAC50 = 6.3 6.3 -93 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3286 None 44 Human Functional pAC50 = 6.3 6.3 -93 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3286 None 44 Human Functional pAC50 = 6.3 6.3 -93 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3286 None 44 Human Functional pAC50 = 6.3 6.3 -93 27
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3125 None 49 Human Functional pAC50 = 6.3 6.3 -52 35
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
16362.0 3125 None 49 Human Functional pAC50 = 6.3 6.3 -52 35
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3125 None 49 Human Functional pAC50 = 6.3 6.3 -52 35
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3125 None 49 Human Functional pAC50 = 6.3 6.3 -52 35
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3125 None 49 Human Functional pAC50 = 6.3 6.3 -52 35
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3125 None 49 Human Functional pAC50 = 6.3 6.3 -52 35
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 205329 None 22 Human Functional pAC50 = 5.3 5.3 -2 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 205329 None 22 Human Functional pAC50 = 5.3 5.3 -2 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206241 None 47 Human Functional pAC50 = 5.3 5.3 -3 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206241 None 47 Human Functional pAC50 = 5.3 5.3 -3 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206241 None 47 Human Functional pAC50 = 5.3 5.3 -3 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1911 None 63 Human Functional pAC50 = 5.3 5.3 -1047 39
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1911 None 63 Human Functional pAC50 = 5.3 5.3 -1047 39
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
3559.0 1911 None 63 Human Functional pAC50 = 5.3 5.3 -1047 39
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1911 None 63 Human Functional pAC50 = 5.3 5.3 -1047 39
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1911 None 63 Human Functional pAC50 = 5.3 5.3 -1047 39
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1911 None 63 Human Functional pAC50 = 5.3 5.3 -1047 39
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1662 None 37 Human Functional pAC50 = 6.3 6.3 -138 35
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1662 None 37 Human Functional pAC50 = 6.3 6.3 -138 35
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1662 None 37 Human Functional pAC50 = 6.3 6.3 -138 35
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
3372.0 1662 None 37 Human Functional pAC50 = 6.3 6.3 -138 35
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1662 None 37 Human Functional pAC50 = 6.3 6.3 -138 35
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1662 None 37 Human Functional pAC50 = 6.3 6.3 -138 35
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2532 None 33 Human Functional pAC50 = 7.3 7.3 -34 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2532 None 33 Human Functional pAC50 = 7.3 7.3 -34 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2532 None 33 Human Functional pAC50 = 7.3 7.3 -34 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4184.0 2532 None 33 Human Functional pAC50 = 7.3 7.3 -34 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2532 None 33 Human Functional pAC50 = 7.3 7.3 -34 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2532 None 33 Human Functional pAC50 = 7.3 7.3 -34 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3841 None 53 Human Functional pAC50 = 5.3 5.3 -6 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3841 None 53 Human Functional pAC50 = 5.3 5.3 -6 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3841 None 53 Human Functional pAC50 = 5.3 5.3 -6 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3841 None 53 Human Functional pAC50 = 5.3 5.3 -6 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3841 None 53 Human Functional pAC50 = 5.3 5.3 -6 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
240 944 None 25 Human Functional pAC50 = 5.3 5.3 -371 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 944 None 25 Human Functional pAC50 = 5.3 5.3 -371 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 944 None 25 Human Functional pAC50 = 5.3 5.3 -371 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
660 944 None 25 Human Functional pAC50 = 5.3 5.3 -371 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 944 None 25 Human Functional pAC50 = 5.3 5.3 -371 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 944 None 25 Human Functional pAC50 = 5.3 5.3 -371 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 944 None 25 Human Functional pAC50 = 5.3 5.3 -371 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206863 None 31 Human Functional pAC50 = 5.3 5.3 -1905 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2995.0 206863 None 31 Human Functional pAC50 = 5.3 5.3 -1905 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206863 None 31 Human Functional pAC50 = 5.3 5.3 -1905 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206863 None 31 Human Functional pAC50 = 5.3 5.3 -1905 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 206863 None 31 Human Functional pAC50 = 5.3 5.3 -1905 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 949 None 27 Human Functional pAC50 = 6.3 6.3 -190 34
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
26987.0 949 None 27 Human Functional pAC50 = 6.3 6.3 -190 34
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 949 None 27 Human Functional pAC50 = 6.3 6.3 -190 34
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
671 949 None 27 Human Functional pAC50 = 6.3 6.3 -190 34
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 949 None 27 Human Functional pAC50 = 6.3 6.3 -190 34
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 949 None 27 Human Functional pAC50 = 6.3 6.3 -190 34
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 96601 None 25 Human Functional pAC50 = 5.3 5.3 -13 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 96601 None 25 Human Functional pAC50 = 5.3 5.3 -13 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3331 None 72 Human Functional pAC50 = 7.3 7.3 -23 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3331 None 72 Human Functional pAC50 = 7.3 7.3 -23 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5073.0 3331 None 72 Human Functional pAC50 = 7.3 7.3 -23 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3331 None 72 Human Functional pAC50 = 7.3 7.3 -23 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3331 None 72 Human Functional pAC50 = 7.3 7.3 -23 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3331 None 72 Human Functional pAC50 = 7.3 7.3 -23 29
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 67305 None 37 Human Functional pAC50 = 6.3 6.3 3 4
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 67305 None 37 Human Functional pAC50 = 6.3 6.3 3 4
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 55838 None 37 Human Functional pAC50 = 5.3 5.3 -13 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4034.0 55838 None 37 Human Functional pAC50 = 5.3 5.3 -13 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 55838 None 37 Human Functional pAC50 = 5.3 5.3 -13 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 55838 None 37 Human Functional pAC50 = 5.3 5.3 -13 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 84687 None 24 Human Functional pAC50 = 5.3 5.3 -104 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 84687 None 24 Human Functional pAC50 = 5.3 5.3 -104 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2866 None 32 Human Functional pAC50 = 6.3 6.3 -467 32
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2866 None 32 Human Functional pAC50 = 6.3 6.3 -467 32
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2866 None 32 Human Functional pAC50 = 6.3 6.3 -467 32
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4543.0 2866 None 32 Human Functional pAC50 = 6.3 6.3 -467 32
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2866 None 32 Human Functional pAC50 = 6.3 6.3 -467 32
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2866 None 32 Human Functional pAC50 = 6.3 6.3 -467 32
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2540 None 64 Human Functional pAC50 = 6.3 6.3 -43 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2540 None 64 Human Functional pAC50 = 6.3 6.3 -43 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4205.0 2540 None 64 Human Functional pAC50 = 6.3 6.3 -43 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2540 None 64 Human Functional pAC50 = 6.3 6.3 -43 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2540 None 64 Human Functional pAC50 = 6.3 6.3 -43 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2540 None 64 Human Functional pAC50 = 6.3 6.3 -43 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2914 None 65 Human Functional pAC50 = 6.3 6.3 -52 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
135398745.0 2914 None 65 Human Functional pAC50 = 6.3 6.3 -52 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2914 None 65 Human Functional pAC50 = 6.3 6.3 -52 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2914 None 65 Human Functional pAC50 = 6.3 6.3 -52 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2914 None 65 Human Functional pAC50 = 6.3 6.3 -52 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3133 None 50 Human Functional pAC50 = 5.2 5.2 -3981 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3133 None 50 Human Functional pAC50 = 5.2 5.2 -3981 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3133 None 50 Human Functional pAC50 = 5.2 5.2 -3981 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
9948102.0 3133 None 50 Human Functional pAC50 = 5.2 5.2 -3981 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3133 None 50 Human Functional pAC50 = 5.2 5.2 -3981 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3133 None 50 Human Functional pAC50 = 5.2 5.2 -3981 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 803 None 59 Human Functional pAC50 = 7.2 7.2 -95 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2585.0 803 None 59 Human Functional pAC50 = 7.2 7.2 -95 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
522 803 None 59 Human Functional pAC50 = 7.2 7.2 -95 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
551 803 None 59 Human Functional pAC50 = 7.2 7.2 -95 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 803 None 59 Human Functional pAC50 = 7.2 7.2 -95 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 803 None 59 Human Functional pAC50 = 7.2 7.2 -95 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 188518 None 61 Human Functional pAC50 = 5.2 5.2 -14 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 188518 None 61 Human Functional pAC50 = 5.2 5.2 -14 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 138516 None 29 Human Functional pAC50 = 6.2 6.2 -4 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 138516 None 29 Human Functional pAC50 = 6.2 6.2 -4 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2759 None 31 Human Functional pAC50 = 6.2 6.2 -4 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2759 None 31 Human Functional pAC50 = 6.2 6.2 -4 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2759 None 31 Human Functional pAC50 = 6.2 6.2 -4 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2759 None 31 Human Functional pAC50 = 6.2 6.2 -4 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2759 None 31 Human Functional pAC50 = 6.2 6.2 -4 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3590 None 59 Human Functional pAC50 = 5.2 5.2 -1548 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3590 None 59 Human Functional pAC50 = 5.2 5.2 -1548 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3590 None 59 Human Functional pAC50 = 5.2 5.2 -1548 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3590 None 59 Human Functional pAC50 = 5.2 5.2 -1548 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3590 None 59 Human Functional pAC50 = 5.2 5.2 -1548 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 9950 None 29 Human Functional pAC50 = 6.2 6.2 -11 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 9950 None 29 Human Functional pAC50 = 6.2 6.2 -11 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2182 None 36 Human Functional pAC50 = 5.2 5.2 -467 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2182 None 36 Human Functional pAC50 = 5.2 5.2 -467 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
3827.0 2182 None 36 Human Functional pAC50 = 5.2 5.2 -467 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2182 None 36 Human Functional pAC50 = 5.2 5.2 -467 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2182 None 36 Human Functional pAC50 = 5.2 5.2 -467 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2182 None 36 Human Functional pAC50 = 5.2 5.2 -467 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14425 None 55 Human Functional pAC50 = 5.2 5.2 -3 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14425 None 55 Human Functional pAC50 = 5.2 5.2 -3 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2181 None 61 Human Functional pAC50 = 5.2 5.2 -1548 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2181 None 61 Human Functional pAC50 = 5.2 5.2 -1548 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2181 None 61 Human Functional pAC50 = 5.2 5.2 -1548 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
3822.0 2181 None 61 Human Functional pAC50 = 5.2 5.2 -1548 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2181 None 61 Human Functional pAC50 = 5.2 5.2 -1548 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2181 None 61 Human Functional pAC50 = 5.2 5.2 -1548 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 2181 None 61 Human Functional pAC50 = 5.2 5.2 -1548 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 82440 None 34 Human Functional pAC50 = 5.2 5.2 -549 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 82440 None 34 Human Functional pAC50 = 5.2 5.2 -549 26
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 133581 None 40 Human Functional pAC50 = 5.2 5.2 -83 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 133581 None 40 Human Functional pAC50 = 5.2 5.2 -83 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 133581 None 40 Human Functional pAC50 = 5.2 5.2 -83 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 120668 None 8 Human Functional pAC50 = 6.2 6.2 2 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5311017.0 120668 None 8 Human Functional pAC50 = 6.2 6.2 2 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 120668 None 8 Human Functional pAC50 = 6.2 6.2 2 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 120668 None 8 Human Functional pAC50 = 6.2 6.2 2 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 100392 None 40 Human Functional pAC50 = 5.2 5.2 -1 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 100392 None 40 Human Functional pAC50 = 5.2 5.2 -1 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 209699 None 30 Human Functional pAC50 = 6.2 6.2 -1 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 209699 None 30 Human Functional pAC50 = 6.2 6.2 -1 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78430 None 26 Human Functional pAC50 = 5.2 5.2 -457 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 78430 None 26 Human Functional pAC50 = 5.2 5.2 -457 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 72 Human Functional pAC50 = 6.2 6.2 -104 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 72 Human Functional pAC50 = 6.2 6.2 -104 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2159.0 400 None 72 Human Functional pAC50 = 6.2 6.2 -104 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 72 Human Functional pAC50 = 6.2 6.2 -104 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 72 Human Functional pAC50 = 6.2 6.2 -104 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 72 Human Functional pAC50 = 6.2 6.2 -104 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 98934 None 37 Human Functional pAC50 = 6.2 6.2 -2 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 98934 None 37 Human Functional pAC50 = 6.2 6.2 -2 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 98934 None 37 Human Functional pAC50 = 6.2 6.2 -2 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3184 None 43 Human Functional pAC50 = 5.2 5.2 -134 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3184 None 43 Human Functional pAC50 = 5.2 5.2 -134 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3184 None 43 Human Functional pAC50 = 5.2 5.2 -134 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4932.0 3184 None 43 Human Functional pAC50 = 5.2 5.2 -134 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3184 None 43 Human Functional pAC50 = 5.2 5.2 -134 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3184 None 43 Human Functional pAC50 = 5.2 5.2 -134 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 37419 None 62 Human Functional pAC50 = 5.2 5.2 -1 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 37419 None 62 Human Functional pAC50 = 5.2 5.2 -1 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 7074 None 25 Human Functional pAC50 = 6.1 6.1 -165 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
17676.0 7074 None 25 Human Functional pAC50 = 6.1 6.1 -165 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 7074 None 25 Human Functional pAC50 = 6.1 6.1 -165 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 7074 None 25 Human Functional pAC50 = 6.1 6.1 -165 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 7074 None 25 Human Functional pAC50 = 6.1 6.1 -165 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 745 None 38 Human Functional pAC50 = 5.1 5.1 -316 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2477.0 745 None 38 Human Functional pAC50 = 5.1 5.1 -316 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
36 745 None 38 Human Functional pAC50 = 5.1 5.1 -316 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
437 745 None 38 Human Functional pAC50 = 5.1 5.1 -316 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 745 None 38 Human Functional pAC50 = 5.1 5.1 -316 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 745 None 38 Human Functional pAC50 = 5.1 5.1 -316 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 204731 None 11 Human Functional pAC50 = 5.1 5.1 - 1
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 204731 None 11 Human Functional pAC50 = 5.1 5.1 - 1
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 204731 None 11 Human Functional pAC50 = 5.1 5.1 - 1
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 18992 None 63 Human Functional pAC50 = 5.1 5.1 -6 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 18992 None 63 Human Functional pAC50 = 5.1 5.1 -6 13
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 33346 None 22 Human Functional pAC50 = 6.1 6.1 -1 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 33346 None 22 Human Functional pAC50 = 6.1 6.1 -1 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 33346 None 22 Human Functional pAC50 = 6.1 6.1 -1 8
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 189330 None 32 Human Functional pAC50 = 5.1 5.1 -28 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 189330 None 32 Human Functional pAC50 = 5.1 5.1 -28 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 189330 None 32 Human Functional pAC50 = 5.1 5.1 -28 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3773 None 26 Human Functional pAC50 = 6.1 6.1 -263 35
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3773 None 26 Human Functional pAC50 = 6.1 6.1 -263 35
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3773 None 26 Human Functional pAC50 = 6.1 6.1 -263 35
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 187026 None 38 Human Functional pAC50 = 5.1 5.1 -77 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 187026 None 38 Human Functional pAC50 = 5.1 5.1 -77 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 187026 None 38 Human Functional pAC50 = 5.1 5.1 -77 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 15289 None 20 Human Functional pAC50 = 5.1 5.1 -10 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 15289 None 20 Human Functional pAC50 = 5.1 5.1 -10 12
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1454 None 27 Human Functional pAC50 = 6.1 6.1 -28 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
36811.0 1454 None 27 Human Functional pAC50 = 6.1 6.1 -28 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1454 None 27 Human Functional pAC50 = 6.1 6.1 -28 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1454 None 27 Human Functional pAC50 = 6.1 6.1 -28 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1454 None 27 Human Functional pAC50 = 6.1 6.1 -28 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1454 None 27 Human Functional pAC50 = 6.1 6.1 -28 17
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3100 None 45 Human Functional pAC50 = 5.1 5.1 -181 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3100 None 45 Human Functional pAC50 = 5.1 5.1 -181 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3100 None 45 Human Functional pAC50 = 5.1 5.1 -181 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
6041.0 3100 None 45 Human Functional pAC50 = 5.1 5.1 -181 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3100 None 45 Human Functional pAC50 = 5.1 5.1 -181 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3100 None 45 Human Functional pAC50 = 5.1 5.1 -181 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 99377 None 50 Human Functional pAC50 = 5.1 5.1 -363 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2448.0 99377 None 50 Human Functional pAC50 = 5.1 5.1 -363 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 99377 None 50 Human Functional pAC50 = 5.1 5.1 -363 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 99377 None 50 Human Functional pAC50 = 5.1 5.1 -363 15
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 50 Human Functional pAC50 = 6.1 6.1 -14 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 50 Human Functional pAC50 = 6.1 6.1 -14 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2092.0 343 None 50 Human Functional pAC50 = 6.1 6.1 -14 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 50 Human Functional pAC50 = 6.1 6.1 -14 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 50 Human Functional pAC50 = 6.1 6.1 -14 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 50 Human Functional pAC50 = 6.1 6.1 -14 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 56283 None 21 Human Functional pAC50 = 6.1 6.1 -1202 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
3158.0 56283 None 21 Human Functional pAC50 = 6.1 6.1 -1202 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 56283 None 21 Human Functional pAC50 = 6.1 6.1 -1202 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 56283 None 21 Human Functional pAC50 = 6.1 6.1 -1202 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3096 None 36 Human Functional pAC50 = 6.1 6.1 -31 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3096 None 36 Human Functional pAC50 = 6.1 6.1 -31 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3096 None 36 Human Functional pAC50 = 6.1 6.1 -31 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3096 None 36 Human Functional pAC50 = 6.1 6.1 -31 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5775.0 3096 None 36 Human Functional pAC50 = 6.1 6.1 -31 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3096 None 36 Human Functional pAC50 = 6.1 6.1 -31 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3096 None 36 Human Functional pAC50 = 6.1 6.1 -31 18
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 35070 None 5 Human Functional pAC50 = 5.1 5.1 -7 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 35070 None 5 Human Functional pAC50 = 5.1 5.1 -7 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 35070 None 5 Human Functional pAC50 = 5.1 5.1 -7 28
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 198942 None 55 Human Functional pAC50 = 5.1 5.1 -5 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 198942 None 55 Human Functional pAC50 = 5.1 5.1 -5 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3182 None 26 Human Functional pAC50 = 6.1 6.1 -56 34
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3182 None 26 Human Functional pAC50 = 6.1 6.1 -56 34
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3182 None 26 Human Functional pAC50 = 6.1 6.1 -56 34
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3182 None 26 Human Functional pAC50 = 6.1 6.1 -56 34
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3182 None 26 Human Functional pAC50 = 6.1 6.1 -56 34
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 938 None 48 Human Functional pAC50 = 6.1 6.1 -19 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
156419.0 938 None 48 Human Functional pAC50 = 6.1 6.1 -19 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 938 None 48 Human Functional pAC50 = 6.1 6.1 -19 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
647 938 None 48 Human Functional pAC50 = 6.1 6.1 -19 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 938 None 48 Human Functional pAC50 = 6.1 6.1 -19 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 938 None 48 Human Functional pAC50 = 6.1 6.1 -19 20
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14479 None 25 Human Functional pAC50 = 5.1 5.1 -2 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14479 None 25 Human Functional pAC50 = 5.1 5.1 -2 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 103167 None 14 Human Functional pAC50 = 5.1 5.1 -190 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 103167 None 14 Human Functional pAC50 = 5.1 5.1 -190 7
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 93987 None 66 Human Functional pAC50 = 6.1 6.1 -1 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 93987 None 66 Human Functional pAC50 = 6.1 6.1 -1 14
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 29284 None 49 Human Functional pAC50 = 6.1 6.1 -104 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 29284 None 49 Human Functional pAC50 = 6.1 6.1 -104 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4615.0 29284 None 49 Human Functional pAC50 = 6.1 6.1 -104 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 29284 None 49 Human Functional pAC50 = 6.1 6.1 -104 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 29284 None 49 Human Functional pAC50 = 6.1 6.1 -104 19
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 102826 None 36 Human Functional pAC50 = 6.1 6.1 -128 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 102826 None 36 Human Functional pAC50 = 6.1 6.1 -128 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 102826 None 36 Human Functional pAC50 = 6.1 6.1 -128 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
2018 3007 None 26 Human Functional pAC50 = 5.1 5.1 -56234 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
9941444 3007 None 26 Human Functional pAC50 = 5.1 5.1 -56234 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
CHEMBL3349607 3007 None 26 Human Functional pAC50 = 5.1 5.1 -56234 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
DB06663 3007 None 26 Human Functional pAC50 = 5.1 5.1 -56234 22
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
22323 15305 None 29 Human Functional pAC50 = 5.1 5.1 -5 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 15305 None 29 Human Functional pAC50 = 5.1 5.1 -5 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 15305 None 29 Human Functional pAC50 = 5.1 5.1 -5 11
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
21722 17999 None 26 Human Functional pAC50 = 5.1 5.1 -22 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 17999 None 26 Human Functional pAC50 = 5.1 5.1 -22 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 9309 None 36 Human Functional pAC50 = 5.0 5.0 -109 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 9309 None 36 Human Functional pAC50 = 5.0 5.0 -109 5
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3863 None 23 Human Functional pAC50 = 5.0 5.0 -301 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3863 None 23 Human Functional pAC50 = 5.0 5.0 -301 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5587.0 3863 None 23 Human Functional pAC50 = 5.0 5.0 -301 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3863 None 23 Human Functional pAC50 = 5.0 5.0 -301 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3863 None 23 Human Functional pAC50 = 5.0 5.0 -301 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3863 None 23 Human Functional pAC50 = 5.0 5.0 -301 9
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 106524 None 30 Human Functional pAC50 = 5.0 5.0 -354 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 106524 None 30 Human Functional pAC50 = 5.0 5.0 -354 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 208825 None 14 Human Functional pAC50 = 5.0 5.0 -2 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
3337.0 208825 None 14 Human Functional pAC50 = 5.0 5.0 -2 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 208825 None 14 Human Functional pAC50 = 5.0 5.0 -2 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 208825 None 14 Human Functional pAC50 = 5.0 5.0 -2 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 208825 None 14 Human Functional pAC50 = 5.0 5.0 -2 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 208825 None 14 Human Functional pAC50 = 5.0 5.0 -2 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 208825 None 14 Human Functional pAC50 = 5.0 5.0 -2 6
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3132 None 63 Human Functional pAC50 = 6.0 6.0 -16 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3132 None 63 Human Functional pAC50 = 6.0 6.0 -16 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
4850.0 3132 None 63 Human Functional pAC50 = 6.0 6.0 -16 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3132 None 63 Human Functional pAC50 = 6.0 6.0 -16 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3132 None 63 Human Functional pAC50 = 6.0 6.0 -16 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 3132 None 63 Human Functional pAC50 = 6.0 6.0 -16 10
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 9159 None 27 Human Functional pAC50 = 5.0 5.0 -263 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 9159 None 27 Human Functional pAC50 = 5.0 5.0 -263 21
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14499 None 5 Human Functional pAC50 = 5.0 5.0 -3 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14499 None 5 Human Functional pAC50 = 5.0 5.0 -3 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14499 None 5 Human Functional pAC50 = 5.0 5.0 -3 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14499 None 5 Human Functional pAC50 = 5.0 5.0 -3 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14499 None 5 Human Functional pAC50 = 5.0 5.0 -3 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 14499 None 5 Human Functional pAC50 = 5.0 5.0 -3 25
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 102913 None 65 Human Functional pAC50 = 5.0 5.0 -89 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
3191.0 102913 None 65 Human Functional pAC50 = 5.0 5.0 -89 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 102913 None 65 Human Functional pAC50 = 5.0 5.0 -89 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 102913 None 65 Human Functional pAC50 = 5.0 5.0 -89 33
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 55 Human Functional pAC50 = 5.0 5.0 -323 42
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 55 Human Functional pAC50 = 5.0 5.0 -323 42
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 55 Human Functional pAC50 = 5.0 5.0 -323 42
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 55 Human Functional pAC50 = 5.0 5.0 -323 42
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 None 55 Human Functional pAC50 = 5.0 5.0 -323 42
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 41735 None 12 Human Functional pAC50 = 5.0 5.0 -512 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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
5284550.0 41735 None 12 Human Functional pAC50 = 5.0 5.0 -512 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 41735 None 12 Human Functional pAC50 = 5.0 5.0 -512 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 41735 None 12 Human Functional pAC50 = 5.0 5.0 -512 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 41735 None 12 Human Functional pAC50 = 5.0 5.0 -512 16
Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components 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 1404 None 49 Human Functional pEC50 = 9.3 9.3 -4 5
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 1404 None 49 Human Functional pEC50 = 9.3 9.3 -4 5
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
5311068.0 1404 None 49 Human Functional pEC50 = 9.3 9.3 -4 5
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 1404 None 49 Human Functional pEC50 = 9.3 9.3 -4 5
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 1404 None 49 Human Functional pEC50 = 9.3 9.3 -4 5
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 1404 None 49 Human Functional pEC50 = 9.3 9.3 -4 5
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 2340 None 41 Human Functional pEC50 = 8.9 8.9 -1 6
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 2340 None 41 Human Functional pEC50 = 8.9 8.9 -1 6
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
30668.0 2340 None 41 Human Functional pEC50 = 8.9 8.9 -1 6
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 2340 None 41 Human Functional pEC50 = 8.9 8.9 -1 6
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 2340 None 41 Human Functional pEC50 = 8.9 8.9 -1 6
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 2340 None 41 Human Functional pEC50 = 8.9 8.9 -1 6
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 71207 None 0 Human Functional pEC50 = 8.7 8.7 1659 2
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 71207 None 0 Human Functional pEC50 = 8.7 8.7 1659 2
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 71207 None 0 Human Functional pEC50 = 8.7 8.7 1659 2
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 71207 None 0 Human Functional pEC50 = 8.7 8.7 1659 2
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 77701 None 0 Human Functional pEC50 = 8.7 8.7 794 2
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 77701 None 0 Human Functional pEC50 = 8.7 8.7 794 2
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 101537 None 0 Human Functional pEC50 = 8.7 8.7 35 2
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 101537 None 0 Human Functional pEC50 = 8.7 8.7 35 2
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 92343 None 1 Human Functional pEC50 = 8 8.0 - 1
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 92343 None 1 Human Functional pEC50 = 8 8.0 - 1
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 71204 None 0 Human Functional pEC50 = 8 8.0 31 2
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 71204 None 0 Human Functional pEC50 = 8 8.0 31 2
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 187771 None 18 Human Functional pEC50 = 8 8.0 6 3
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 187771 None 18 Human Functional pEC50 = 8 8.0 6 3
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 92343 None 1 Human Functional pEC50 = 8 8.0 - 1
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 92343 None 1 Human Functional pEC50 = 8 8.0 - 1
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 18582 None 0 Human Functional pEC50 = 7 7.0 31 2
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 18582 None 0 Human Functional pEC50 = 7 7.0 31 2
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 84779 None 0 Human Functional pEC50 = 7 7.0 - 1
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 84779 None 0 Human Functional pEC50 = 7 7.0 - 1
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 84779 None 0 Human Functional pEC50 = 7 7.0 - 1
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 84779 None 0 Human Functional pEC50 = 7 7.0 - 1
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 33561 None 0 Human Functional pEC50 = 7 7.0 17 2
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 33561 None 0 Human Functional pEC50 = 7 7.0 17 2
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 49303 None 0 Human Functional pEC50 = 7 7.0 100 2
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 49303 None 0 Human Functional pEC50 = 7 7.0 100 2
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 71213 None 0 Human Functional pEC50 = 7 7.0 -3 3
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 71213 None 0 Human Functional pEC50 = 7 7.0 -3 3
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 103053 None 1 Human Functional pEC50 = 7 7.0 -16 5
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 103053 None 1 Human Functional pEC50 = 7 7.0 -16 5
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 84779 None 0 Human Functional pEC50 = 7 7.0 - 1
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 84779 None 0 Human Functional pEC50 = 7 7.0 - 1
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 187352 None 0 Human Functional pEC50 = 6 6.0 - 1
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 187352 None 0 Human Functional pEC50 = 6 6.0 - 1
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 133675 None 29 Human Functional pEC50 = 5 5.0 -5011 7
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 133675 None 29 Human Functional pEC50 = 5 5.0 -5011 7
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 71208 None 0 Human Functional pEC50 = 5 5.0 -3 2
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 71208 None 0 Human Functional pEC50 = 5 5.0 -3 2
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 207185 None 14 Human Functional pEC50 = 7.0 7.0 -37 3
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 207185 None 14 Human Functional pEC50 = 7.0 7.0 -37 3
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 168125 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 168125 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 92206 None 0 Human Functional pEC50 = 7.0 7.0 257 3
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 92206 None 0 Human Functional pEC50 = 7.0 7.0 257 3
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 92206 None 0 Human Functional pEC50 = 7.0 7.0 257 3
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 92206 None 0 Human Functional pEC50 = 7.0 7.0 257 3
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 206780 None 0 Human Functional pEC50 = 6.0 6.0 -575 3
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 206780 None 0 Human Functional pEC50 = 6.0 6.0 -575 3
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 71206 None 0 Human Functional pEC50 = 6.9 6.9 13 2
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 71206 None 0 Human Functional pEC50 = 6.9 6.9 13 2
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 3834 None 40 Human Functional pEC50 = 5.9 5.9 -5 6
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 3834 None 40 Human Functional pEC50 = 5.9 5.9 -5 6
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
5487.0 3834 None 40 Human Functional pEC50 = 5.9 5.9 -5 6
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 3834 None 40 Human Functional pEC50 = 5.9 5.9 -5 6
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 3834 None 40 Human Functional pEC50 = 5.9 5.9 -5 6
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 3834 None 40 Human Functional pEC50 = 5.9 5.9 -5 6
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 18578 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 18578 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 187511 None 11 Human Functional pEC50 = 6.9 6.9 3 3
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 187511 None 11 Human Functional pEC50 = 6.9 6.9 3 3
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 101175 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 101175 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 3613 None 17 Human Functional pEC50 = 5.9 5.9 -10 3
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 3613 None 17 Human Functional pEC50 = 5.9 5.9 -10 3
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 3613 None 17 Human Functional pEC50 = 5.9 5.9 -10 3
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 187196 None 2 Human Functional pEC50 = 7.9 7.9 -11 3
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 187196 None 2 Human Functional pEC50 = 7.9 7.9 -11 3
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 121783 None 1 Human Functional pEC50 = 3.8 3.8 - 1
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 121783 None 1 Human Functional pEC50 = 3.8 3.8 - 1
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 206629 None 0 Human Functional pEC50 = 7.8 7.8 -2 5
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 206629 None 0 Human Functional pEC50 = 7.8 7.8 -2 5
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 199941 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
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 199941 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
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 84779 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 84779 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 84784 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 84784 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 71203 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
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 71203 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
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 121774 None 1 Human Functional pEC50 = 6.8 6.8 - 1
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 121774 None 1 Human Functional pEC50 = 6.8 6.8 - 1
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 151327 None 0 Human Functional pEC50 = 7.7 7.7 3 3
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 151327 None 0 Human Functional pEC50 = 7.7 7.7 3 3
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 151327 None 0 Human Functional pEC50 = 7.7 7.7 3 3
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 151327 None 0 Human Functional pEC50 = 7.7 7.7 3 3
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 18573 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 18573 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 18573 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 18573 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 100392 None 40 Human Functional pEC50 = 6.7 6.7 -1 7
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 100392 None 40 Human Functional pEC50 = 6.7 6.7 -1 7
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 71214 None 0 Human Functional pEC50 = 6.7 6.7 -3 3
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 71214 None 0 Human Functional pEC50 = 6.7 6.7 -3 3
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 2892 None 6 Human Functional pEC50 = 5.7 5.7 -8 2
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 2892 None 6 Human Functional pEC50 = 5.7 5.7 -8 2
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 2892 None 6 Human Functional pEC50 = 5.7 5.7 -8 2
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 207205 None 0 Human Functional pEC50 = 5.7 5.7 -120 2
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 207205 None 0 Human Functional pEC50 = 5.7 5.7 -120 2
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 207258 None 2 Human Functional pEC50 = 8.7 8.7 -1 3
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 207258 None 2 Human Functional pEC50 = 8.7 8.7 -1 3
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 206638 None 0 Human Functional pEC50 = 8.6 8.6 -6 5
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 206638 None 0 Human Functional pEC50 = 8.6 8.6 -6 5
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 172875 None 0 Human Functional pEC50 = 7.7 7.7 3 3
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 172875 None 0 Human Functional pEC50 = 7.7 7.7 3 3
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 101376 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
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 101376 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
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 103007 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 103007 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 200766 None 0 Human Functional pEC50 = 7.6 7.6 125 2
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 200766 None 0 Human Functional pEC50 = 7.6 7.6 125 2
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 18574 None 0 Human Functional pEC50 = 7.6 7.6 39 2
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 18574 None 0 Human Functional pEC50 = 7.6 7.6 39 2
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 18791 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 18791 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 18574 None 0 Human Functional pEC50 = 7.6 7.6 39 2
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 18574 None 0 Human Functional pEC50 = 7.6 7.6 39 2
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 18792 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 18792 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 188989 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 188989 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 84780 None 0 Human Functional pEC50 = 5.6 5.6 1 2
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 84780 None 0 Human Functional pEC50 = 5.6 5.6 1 2
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 84780 None 0 Human Functional pEC50 = 5.6 5.6 1 2
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 48791 None 0 Human Functional pEC50 = 7.6 7.6 -1 3
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 48791 None 0 Human Functional pEC50 = 7.6 7.6 -1 3
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 51156 None 0 Human Functional pEC50 = 7.6 7.6 -2 3
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 51156 None 0 Human Functional pEC50 = 7.6 7.6 -2 3
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 13057 None 0 Human Functional pEC50 = 7.6 7.6 -8 5
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 13057 None 0 Human Functional pEC50 = 7.6 7.6 -8 5
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 13057 None 0 Human Functional pEC50 = 7.6 7.6 -8 5
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 13687 None 0 Human Functional pEC50 = 7.6 7.6 -5 4
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 13687 None 0 Human Functional pEC50 = 7.6 7.6 -5 4
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 13687 None 0 Human Functional pEC50 = 7.6 7.6 -5 4
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 200847 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
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 200847 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
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 722 None 63 Human Functional pEC50 = 8.5 8.5 -7 10
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
2435.0 722 None 63 Human Functional pEC50 = 8.5 8.5 -7 10
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
395 722 None 63 Human Functional pEC50 = 8.5 8.5 -7 10
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
520 722 None 63 Human Functional pEC50 = 8.5 8.5 -7 10
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 722 None 63 Human Functional pEC50 = 8.5 8.5 -7 10
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 722 None 63 Human Functional pEC50 = 8.5 8.5 -7 10
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 722 None 63 Human Functional pEC50 = 8.5 8.5 -7 10
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 206989 None 20 Human Functional pEC50 = 7.5 7.5 -13 3
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 206989 None 20 Human Functional pEC50 = 7.5 7.5 -13 3
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 71212 None 0 Human Functional pEC50 = 6.5 6.5 1 3
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 71212 None 0 Human Functional pEC50 = 6.5 6.5 1 3
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 77700 None 0 Human Functional pEC50 = 6.5 6.5 12 2
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 77700 None 0 Human Functional pEC50 = 6.5 6.5 12 2
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 192926 None 0 Human Functional pEC50 = 5.5 5.5 7 2
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 192926 None 0 Human Functional pEC50 = 5.5 5.5 7 2
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 77597 None 20 Human Functional pEC50 = 5.5 5.5 - 1
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 77597 None 20 Human Functional pEC50 = 5.5 5.5 - 1
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 10723 None 4 Human Functional pEC50 = 5.5 5.5 -60 2
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 10723 None 4 Human Functional pEC50 = 5.5 5.5 -60 2
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 10723 None 4 Human Functional pEC50 = 5.5 5.5 -60 2
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 22663 None 66 Human Functional pEC50 = 3.5 3.5 - 1
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 22663 None 66 Human Functional pEC50 = 3.5 3.5 - 1
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 3100 None 45 Human Functional pEC50 = 6.5 6.5 -181 14
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 3100 None 45 Human Functional pEC50 = 6.5 6.5 -181 14
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 3100 None 45 Human Functional pEC50 = 6.5 6.5 -181 14
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
6041.0 3100 None 45 Human Functional pEC50 = 6.5 6.5 -181 14
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 3100 None 45 Human Functional pEC50 = 6.5 6.5 -181 14
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 3100 None 45 Human Functional pEC50 = 6.5 6.5 -181 14
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 121776 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 121776 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 18579 None 0 Human Functional pEC50 = 7.5 7.5 89 2
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 18579 None 0 Human Functional pEC50 = 7.5 7.5 89 2
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 187772 None 0 Human Functional pEC50 = 5.5 5.5 8 2
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 187772 None 0 Human Functional pEC50 = 5.5 5.5 8 2
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 85036 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 85036 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 92343 None 1 Human Functional pEC50 = 7.4 7.4 - 1
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 92343 None 1 Human Functional pEC50 = 7.4 7.4 - 1
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 200823 None 0 Human Functional pEC50 = 7.4 7.4 25 2
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 200823 None 0 Human Functional pEC50 = 7.4 7.4 25 2
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 18577 None 0 Human Functional pEC50 = 7.4 7.4 79 2
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 18577 None 0 Human Functional pEC50 = 7.4 7.4 79 2
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 136496 None 0 Human Functional pEC50 = 7.4 7.4 9 3
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 136496 None 0 Human Functional pEC50 = 7.4 7.4 9 3
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 943 None 16 Human Functional pEC50 = 6.4 6.4 -38 7
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
515 943 None 16 Human Functional pEC50 = 6.4 6.4 -38 7
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 943 None 16 Human Functional pEC50 = 6.4 6.4 -38 7
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 943 None 16 Human Functional pEC50 = 6.4 6.4 -38 7
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 97058 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 97058 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 104467 None 0 Human Functional pEC50 = 8.4 8.4 -2 3
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 104467 None 0 Human Functional pEC50 = 8.4 8.4 -2 3
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 101524 None 0 Human Functional pEC50 = 8.4 8.4 -2 3
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 101524 None 0 Human Functional pEC50 = 8.4 8.4 -2 3
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 207163 None 0 Human Functional pEC50 = 6.4 6.4 -10 2
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 207163 None 0 Human Functional pEC50 = 6.4 6.4 -10 2
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 137071 None 0 Human Functional pEC50 = 7.3 7.3 112 2
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 137071 None 0 Human Functional pEC50 = 7.3 7.3 112 2
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 137071 None 0 Human Functional pEC50 = 7.3 7.3 112 2
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 137071 None 0 Human Functional pEC50 = 7.3 7.3 112 2
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 137071 None 0 Human Functional pEC50 = 7.3 7.3 112 2
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 137071 None 0 Human Functional pEC50 = 7.3 7.3 112 2
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 71209 None 0 Human Functional pEC50 = 7.3 7.3 269 2
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 71209 None 0 Human Functional pEC50 = 7.3 7.3 269 2
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 121777 None 0 Human Functional pEC50 = 3.3 3.3 - 1
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 121777 None 0 Human Functional pEC50 = 3.3 3.3 - 1
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 206991 None 1 Human Functional pEC50 = 8.3 8.3 -3 5
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 206991 None 1 Human Functional pEC50 = 8.3 8.3 -3 5
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 10876 None 0 Human Functional pEC50 = 8.3 8.3 1 5
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 10876 None 0 Human Functional pEC50 = 8.3 8.3 1 5
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 10876 None 0 Human Functional pEC50 = 8.3 8.3 1 5
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 200115 None 0 Human Functional pEC50 = 7.3 7.3 19 2
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 200115 None 0 Human Functional pEC50 = 7.3 7.3 19 2
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 187770 None 3 Human Functional pEC50 = 7.3 7.3 - 1
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 187770 None 3 Human Functional pEC50 = 7.3 7.3 - 1
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 136496 None 0 Human Functional pEC50 = 7.3 7.3 9 3
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 136496 None 0 Human Functional pEC50 = 7.3 7.3 9 3
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 187770 None 3 Human Functional pEC50 = 7.3 7.3 - 1
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 187770 None 3 Human Functional pEC50 = 7.3 7.3 - 1
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 187770 None 3 Human Functional pEC50 = 7.3 7.3 - 1
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 187770 None 3 Human Functional pEC50 = 7.3 7.3 - 1
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 136496 None 0 Human Functional pEC50 = 7.3 7.3 9 3
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 136496 None 0 Human Functional pEC50 = 7.3 7.3 9 3
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 84675 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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 84675 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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 169559 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 169559 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 163486 None 0 Human Functional pEC50 = 6.3 6.3 -20 2
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 163486 None 0 Human Functional pEC50 = 6.3 6.3 -20 2
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 206689 None 0 Human Functional pEC50 = 5.3 5.3 -20 2
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 206689 None 0 Human Functional pEC50 = 5.3 5.3 -20 2
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 2733 None 38 Human Functional pEC50 = 7.3 7.3 -13 7
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 2733 None 38 Human Functional pEC50 = 7.3 7.3 -13 7
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 2733 None 38 Human Functional pEC50 = 7.3 7.3 -13 7
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
4436.0 2733 None 38 Human Functional pEC50 = 7.3 7.3 -13 7
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 2733 None 38 Human Functional pEC50 = 7.3 7.3 -13 7
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 2733 None 38 Human Functional pEC50 = 7.3 7.3 -13 7
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 2733 None 38 Human Functional pEC50 = 7.3 7.3 -13 7
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 955 None 40 Human Functional pEC50 = 7.3 7.3 -15 14
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
2803.0 955 None 40 Human Functional pEC50 = 7.3 7.3 -15 14
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
516 955 None 40 Human Functional pEC50 = 7.3 7.3 -15 14
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
704 955 None 40 Human Functional pEC50 = 7.3 7.3 -15 14
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 955 None 40 Human Functional pEC50 = 7.3 7.3 -15 14
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 955 None 40 Human Functional pEC50 = 7.3 7.3 -15 14
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 206624 None 8 Human Functional pEC50 = 7.3 7.3 -4 2
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 206624 None 8 Human Functional pEC50 = 7.3 7.3 -4 2
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 955 None 40 Human Functional pEC50 = 7.3 7.3 -15 14
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
2803.0 955 None 40 Human Functional pEC50 = 7.3 7.3 -15 14
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
516 955 None 40 Human Functional pEC50 = 7.3 7.3 -15 14
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
704 955 None 40 Human Functional pEC50 = 7.3 7.3 -15 14
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 955 None 40 Human Functional pEC50 = 7.3 7.3 -15 14
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 955 None 40 Human Functional pEC50 = 7.3 7.3 -15 14
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 50335 None 0 Human Functional pEC50 = 7.3 7.3 8 2
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 50335 None 0 Human Functional pEC50 = 7.3 7.3 8 2
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 168866 None 4 Human Functional pEC50 = 5.3 5.3 -66 6
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 168866 None 4 Human Functional pEC50 = 5.3 5.3 -66 6
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 955 None 40 Human Functional pEC50 = 7.2 7.2 -15 14
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
2803.0 955 None 40 Human Functional pEC50 = 7.2 7.2 -15 14
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
516 955 None 40 Human Functional pEC50 = 7.2 7.2 -15 14
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
704 955 None 40 Human Functional pEC50 = 7.2 7.2 -15 14
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 955 None 40 Human Functional pEC50 = 7.2 7.2 -15 14
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 955 None 40 Human Functional pEC50 = 7.2 7.2 -15 14
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 18863 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 18863 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 18863 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 18863 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 18863 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 18863 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 18863 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 18863 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 85035 None 0 Human Functional pEC50 = 7.2 7.2 -1 3
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 85035 None 0 Human Functional pEC50 = 7.2 7.2 -1 3
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 18583 None 0 Human Functional pEC50 = 8.2 8.2 9 3
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 18583 None 0 Human Functional pEC50 = 8.2 8.2 9 3
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 103609 None 24 Human Functional pEC50 = 8.2 8.2 1 3
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 103609 None 24 Human Functional pEC50 = 8.2 8.2 1 3
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 85037 None 0 Human Functional pEC50 = 7.2 7.2 1 2
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 85037 None 0 Human Functional pEC50 = 7.2 7.2 1 2
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 85037 None 0 Human Functional pEC50 = 7.2 7.2 1 2
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 85037 None 0 Human Functional pEC50 = 7.2 7.2 1 2
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 184332 None 0 Human Functional pEC50 = 7.2 7.2 -1 2
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 184332 None 0 Human Functional pEC50 = 7.2 7.2 -1 2
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 200096 None 0 Human Functional pEC50 = 7.2 7.2 79 2
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 200096 None 0 Human Functional pEC50 = 7.2 7.2 79 2
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 71210 None 0 Human Functional pEC50 = 6.2 6.2 5 2
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 71210 None 0 Human Functional pEC50 = 6.2 6.2 5 2
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 206636 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 206636 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 121781 None 1 Human Functional pEC50 = 3.2 3.2 - 1
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 121781 None 1 Human Functional pEC50 = 3.2 3.2 - 1
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 206986 None 0 Human Functional pEC50 = 8.1 8.1 -1 4
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 206986 None 0 Human Functional pEC50 = 8.1 8.1 -1 4
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 153340 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 153340 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 153340 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 153340 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 102948 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
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 102948 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
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 193265 None 0 Human Functional pEC50 = 6.1 6.1 1 2
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 193265 None 0 Human Functional pEC50 = 6.1 6.1 1 2
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 71215 None 0 Human Functional pEC50 = 7.1 7.1 2 2
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 71215 None 0 Human Functional pEC50 = 7.1 7.1 2 2
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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
439260.0 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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
439260.0 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 71205 None 0 Human Functional pEC50 = 6.1 6.1 -3 2
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 71205 None 0 Human Functional pEC50 = 6.1 6.1 -3 2
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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
439260.0 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 187459 None 0 Human Functional pEC50 = 6.1 6.1 15 2
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 187459 None 0 Human Functional pEC50 = 6.1 6.1 15 2
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 206620 None 0 Human Functional pEC50 = 6.1 6.1 -281 3
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 206620 None 0 Human Functional pEC50 = 6.1 6.1 -281 3
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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
439260.0 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 2857 None 46 Human Functional pEC50 = 6.1 6.1 -11 18
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 722 None 63 Human Functional pEC50 = 8.1 8.1 -7 10
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
2435.0 722 None 63 Human Functional pEC50 = 8.1 8.1 -7 10
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
395 722 None 63 Human Functional pEC50 = 8.1 8.1 -7 10
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
520 722 None 63 Human Functional pEC50 = 8.1 8.1 -7 10
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 722 None 63 Human Functional pEC50 = 8.1 8.1 -7 10
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 722 None 63 Human Functional pEC50 = 8.1 8.1 -7 10
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 722 None 63 Human Functional pEC50 = 8.1 8.1 -7 10
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 206944 None 0 Human Functional pEC50 = 8.1 8.1 -81 5
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 206944 None 0 Human Functional pEC50 = 8.1 8.1 -81 5
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 166356 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 166356 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 206887 None 0 Human Functional pEC50 = 6.1 6.1 1 2
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 206887 None 0 Human Functional pEC50 = 6.1 6.1 1 2
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 207023 None 1 Human Functional pEC50 = 6.1 6.1 19 2
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 207023 None 1 Human Functional pEC50 = 6.1 6.1 19 2
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 722 None 63 Human Functional pEC50 = 8.0 8.0 -7 10
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
2435.0 722 None 63 Human Functional pEC50 = 8.0 8.0 -7 10
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
395 722 None 63 Human Functional pEC50 = 8.0 8.0 -7 10
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
520 722 None 63 Human Functional pEC50 = 8.0 8.0 -7 10
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 722 None 63 Human Functional pEC50 = 8.0 8.0 -7 10
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 722 None 63 Human Functional pEC50 = 8.0 8.0 -7 10
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 722 None 63 Human Functional pEC50 = 8.0 8.0 -7 10
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 141725 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
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 141725 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
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 20690 None 0 Human Functional pEC50 = 7.0 7.0 4 3
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 20690 None 0 Human Functional pEC50 = 7.0 7.0 4 3
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 141725 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
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 141725 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
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 71211 None 0 Human Functional pEC50 = 5.0 5.0 10 2
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 71211 None 0 Human Functional pEC50 = 5.0 5.0 10 2
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 186711 None 0 Human Functional pIC50 = 10.1 10.1 - 1
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 186711 None 0 Human Functional pIC50 = 10.1 10.1 - 1
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 186474 None 0 Human Functional pIC50 = 9.6 9.6 - 1
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 186474 None 0 Human Functional pIC50 = 9.6 9.6 - 1
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 184941 None 0 Human Functional pIC50 = 9.5 9.5 - 1
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 184941 None 0 Human Functional pIC50 = 9.5 9.5 - 1
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 186531 None 0 Human Functional pIC50 = 9.4 9.4 - 1
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 186531 None 0 Human Functional pIC50 = 9.4 9.4 - 1
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 186016 None 0 Human Functional pIC50 = 9.4 9.4 - 1
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 186016 None 0 Human Functional pIC50 = 9.4 9.4 - 1
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 185864 None 0 Human Functional pIC50 = 9.3 9.3 - 1
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 185864 None 0 Human Functional pIC50 = 9.3 9.3 - 1
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 3292 None 26 Human Functional pIC50 = 7.8 7.8 -1 2
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 3292 None 26 Human Functional pIC50 = 7.8 7.8 -1 2
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 3292 None 26 Human Functional pIC50 = 7.8 7.8 -1 2
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 3292 None 26 Human Functional pIC50 = 7.8 7.8 -1 2
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 168610 None 0 Human Functional pKi = 10.5 10.5 - 0
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 168610 None 0 Human Functional pKi = 10.5 10.5 - 0
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 61014 None 0 Human Functional pKi = 10 10.0 - 0
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 61014 None 0 Human Functional pKi = 10 10.0 - 0
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 63915 None 0 Human Functional pKi = 10 10.0 - 0
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 63915 None 0 Human Functional pKi = 10 10.0 - 0
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 78976 None 0 Human Functional pKi = 10 10.0 - 0
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 78976 None 0 Human Functional pKi = 10 10.0 - 0
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 60564 None 0 Human Functional pKi = 9.7 9.7 - 0
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 60564 None 0 Human Functional pKi = 9.7 9.7 - 0
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 60595 None 0 Human Functional pKi = 9.7 9.7 - 0
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 60595 None 0 Human Functional pKi = 9.7 9.7 - 0
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 60816 None 0 Human Functional pKi = 9.7 9.7 - 0
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 60816 None 0 Human Functional pKi = 9.7 9.7 - 0
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 63300 None 0 Human Functional pKi = 9.7 9.7 - 0
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 63300 None 0 Human Functional pKi = 9.7 9.7 - 0
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 209406 None 0 Human Functional pKi = 9.7 9.7 - 0
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 209406 None 0 Human Functional pKi = 9.7 9.7 - 0
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 60576 None 0 Human Functional pKi = 9.5 9.5 - 0
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 60576 None 0 Human Functional pKi = 9.5 9.5 - 0
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 63880 None 0 Human Functional pKi = 9.3 9.3 - 0
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 63880 None 0 Human Functional pKi = 9.3 9.3 - 0
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 131871 None 0 Human Functional pKi = 9.3 9.3 - 0
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 131871 None 0 Human Functional pKi = 9.3 9.3 - 0
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 166079 None 0 Human Functional pKi = 9.3 9.3 - 0
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 166079 None 0 Human Functional pKi = 9.3 9.3 - 0
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 163467 None 0 Human Functional pKi = 9.2 9.2 - 0
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 163467 None 0 Human Functional pKi = 9.2 9.2 - 0
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 63005 None 0 Human Functional pKi = 8.8 8.8 - 0
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 63005 None 0 Human Functional pKi = 8.8 8.8 - 0
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 78961 None 0 Human Functional pKi = 8.8 8.8 - 0
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 78961 None 0 Human Functional pKi = 8.8 8.8 - 0
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 187201 None 0 Human Functional pKi = 8.8 8.8 - 0
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 187201 None 0 Human Functional pKi = 8.8 8.8 - 0
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 78970 None 0 Human Functional pKi = 8.8 8.8 - 0
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 78970 None 0 Human Functional pKi = 8.8 8.8 - 0
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 189788 None 0 Human Functional pKi = 8.7 8.7 - 0
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 189788 None 0 Human Functional pKi = 8.7 8.7 - 0
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 193418 None 0 Human Functional pKi = 8.7 8.7 - 0
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 193418 None 0 Human Functional pKi = 8.7 8.7 - 0
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 166368 None 0 Human Functional pKi = 8.0 8.0 - 0
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 166368 None 0 Human Functional pKi = 8.0 8.0 - 0
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 78971 None 0 Human Functional pKi = 7.0 7.0 - 0
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 78971 None 0 Human Functional pKi = 7.0 7.0 - 0
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 78968 None 0 Human Functional pKi = 7.9 7.9 - 0
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 78968 None 0 Human Functional pKi = 7.9 7.9 - 0
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 78972 None 0 Human Functional pKi = 7.8 7.8 - 0
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 78972 None 0 Human Functional pKi = 7.8 7.8 - 0
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 78965 None 0 Human Functional pKi = 8.6 8.6 - 0
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 78965 None 0 Human Functional pKi = 8.6 8.6 - 0
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 63437 None 0 Human Functional pKi = 7.7 7.7 - 0
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 63437 None 0 Human Functional pKi = 7.7 7.7 - 0
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 191062 None 3 Human Functional pKi = 7.6 7.6 - 0
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 191062 None 3 Human Functional pKi = 7.6 7.6 - 0
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 78966 None 0 Human Functional pKi = 7.6 7.6 - 0
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 78966 None 0 Human Functional pKi = 7.6 7.6 - 0
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 181920 None 1 Human Functional pKi = 7.6 7.6 - 0
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 181920 None 1 Human Functional pKi = 7.6 7.6 - 0
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 209696 None 0 Human Functional pKi = 8.5 8.5 - 0
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 209696 None 0 Human Functional pKi = 8.5 8.5 - 0
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 78963 None 0 Human Functional pKi = 8.4 8.4 - 0
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 78963 None 0 Human Functional pKi = 8.4 8.4 - 0
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 181650 None 0 Human Functional pKi = 8.4 8.4 - 0
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 181650 None 0 Human Functional pKi = 8.4 8.4 - 0
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 78973 None 0 Human Functional pKi = 8.4 8.4 - 0
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 78973 None 0 Human Functional pKi = 8.4 8.4 - 0
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 181760 None 0 Human Functional pKi = 7.5 7.5 - 0
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 181760 None 0 Human Functional pKi = 7.5 7.5 - 0
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 78969 None 0 Human Functional pKi = 8.4 8.4 - 0
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 78969 None 0 Human Functional pKi = 8.4 8.4 - 0
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 78962 None 0 Human Functional pKi = 8.4 8.4 - 0
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 78962 None 0 Human Functional pKi = 8.4 8.4 - 0
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 189725 None 0 Human Functional pKi = 8.3 8.3 - 0
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 189725 None 0 Human Functional pKi = 8.3 8.3 - 0
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 78974 None 0 Human Functional pKi = 8.3 8.3 - 0
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 78974 None 0 Human Functional pKi = 8.3 8.3 - 0
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 111631 None 0 Human Functional pKi = 8.2 8.2 - 0
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 111631 None 0 Human Functional pKi = 8.2 8.2 - 0
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 78964 None 0 Human Functional pKi = 8.2 8.2 - 0
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 78964 None 0 Human Functional pKi = 8.2 8.2 - 0
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 187200 None 0 Human Functional pKi = 8.2 8.2 - 0
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 187200 None 0 Human Functional pKi = 8.2 8.2 - 0
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 161217 None 20 Human Functional pKi = 6.2 6.2 - 0
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
10073773.0 161217 None 20 Human Functional pKi = 6.2 6.2 - 0
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 161217 None 20 Human Functional pKi = 6.2 6.2 - 0
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 161217 None 20 Human Functional pKi = 6.2 6.2 - 0
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 161217 None 20 Human Functional pKi = 6.2 6.2 - 0
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 111631 None 0 Human Functional pKi = 8.1 8.1 - 0
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 111631 None 0 Human Functional pKi = 8.1 8.1 - 0
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 78975 None 0 Human Functional pKi = 8.0 8.0 - 0
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 78975 None 0 Human Functional pKi = 8.0 8.0 - 0
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 78967 None 0 Human Functional pKi = 8.0 8.0 - 0
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 78967 None 0 Human Functional pKi = 8.0 8.0 - 0
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 1889 None 43 Human Functional pEC50 = 8.3 8.3 -11 12
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
3519 1889 None 43 Human Functional pEC50 = 8.3 8.3 -11 12
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
3519.0 1889 None 43 Human Functional pEC50 = 8.3 8.3 -11 12
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
522 1889 None 43 Human Functional pEC50 = 8.3 8.3 -11 12
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
CHEMBL862 1889 None 43 Human Functional pEC50 = 8.3 8.3 -11 12
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
DB01018 1889 None 43 Human Functional pEC50 = 8.3 8.3 -11 12
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
2683 3834 None 40 Human Functional pEC50 = 8.2 8.2 -5 6
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 3834 None 40 Human Functional pEC50 = 8.2 8.2 -5 6
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
5487.0 3834 None 40 Human Functional pEC50 = 8.2 8.2 -5 6
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 3834 None 40 Human Functional pEC50 = 8.2 8.2 -5 6
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 3834 None 40 Human Functional pEC50 = 8.2 8.2 -5 6
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 3834 None 40 Human Functional pEC50 = 8.2 8.2 -5 6
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 955 None 40 Human Functional pEC50 = 8.2 8.2 -15 14
NoneNone
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
2803.0 955 None 40 Human Functional pEC50 = 8.2 8.2 -15 14
NoneNone
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 955 None 40 Human Functional pEC50 = 8.2 8.2 -15 14
NoneNone
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 955 None 40 Human Functional pEC50 = 8.2 8.2 -15 14
NoneNone
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 955 None 40 Human Functional pEC50 = 8.2 8.2 -15 14
NoneNone
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 955 None 40 Human Functional pEC50 = 8.2 8.2 -15 14
NoneNone
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
2435 722 None 63 Human Functional pEC50 = 8.1 8.1 -7 10
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
2435.0 722 None 63 Human Functional pEC50 = 8.1 8.1 -7 10
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
395 722 None 63 Human Functional pEC50 = 8.1 8.1 -7 10
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
520 722 None 63 Human Functional pEC50 = 8.1 8.1 -7 10
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
5386 722 None 63 Human Functional pEC50 = 8.1 8.1 -7 10
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
CHEMBL844 722 None 63 Human Functional pEC50 = 8.1 8.1 -7 10
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
DB00484 722 None 63 Human Functional pEC50 = 8.1 8.1 -7 10
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
124 2981 None 32 Human Functional pEC50 = 6.9 6.9 -144 24
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 2981 None 32 Human Functional pEC50 = 6.9 6.9 -144 24
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 2981 None 32 Human Functional pEC50 = 6.9 6.9 -144 24
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
4636.0 2981 None 32 Human Functional pEC50 = 6.9 6.9 -144 24
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 2981 None 32 Human Functional pEC50 = 6.9 6.9 -144 24
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 2981 None 32 Human Functional pEC50 = 6.9 6.9 -144 24
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 955 None 40 Human Functional pEC50 = 5.7 5.7 -15 14
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
2803.0 955 None 40 Human Functional pEC50 = 5.7 5.7 -15 14
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
516 955 None 40 Human Functional pEC50 = 5.7 5.7 -15 14
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
704 955 None 40 Human Functional pEC50 = 5.7 5.7 -15 14
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 955 None 40 Human Functional pEC50 = 5.7 5.7 -15 14
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 955 None 40 Human Functional pEC50 = 5.7 5.7 -15 14
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 2605 None 60 Human Functional pEC50 = 5.0 5.0 -26 8
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 2605 None 60 Human Functional pEC50 = 5.0 5.0 -26 8
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
4810.0 2605 None 60 Human Functional pEC50 = 5.0 5.0 -26 8
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 2605 None 60 Human Functional pEC50 = 5.0 5.0 -26 8
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 2605 None 60 Human Functional pEC50 = 5.0 5.0 -26 8
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 1888 None 32 Human Functional pEC50 = 5.9 5.9 -18 21
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 1888 None 32 Human Functional pEC50 = 5.9 5.9 -18 21
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
5353646.0 1888 None 32 Human Functional pEC50 = 5.9 5.9 -18 21
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 1888 None 32 Human Functional pEC50 = 5.9 5.9 -18 21
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 1888 None 32 Human Functional pEC50 = 5.9 5.9 -18 21
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
5702063.0 1888 None 32 Human Functional pEC50 = 5.9 5.9 -18 21
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 1888 None 32 Human Functional pEC50 = 5.9 5.9 -18 21
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 1888 None 32 Human Functional pEC50 = 5.9 5.9 -18 21
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 1888 None 32 Human Functional pEC50 = 5.9 5.9 -18 21
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 722 None 63 Human Functional pEC50 = 6.4 6.4 -7 10
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
2435.0 722 None 63 Human Functional pEC50 = 6.4 6.4 -7 10
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
395 722 None 63 Human Functional pEC50 = 6.4 6.4 -7 10
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
520 722 None 63 Human Functional pEC50 = 6.4 6.4 -7 10
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 722 None 63 Human Functional pEC50 = 6.4 6.4 -7 10
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 722 None 63 Human Functional pEC50 = 6.4 6.4 -7 10
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 722 None 63 Human Functional pEC50 = 6.4 6.4 -7 10
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 2857 None 46 Human Functional pEC50 = 6.3 6.3 -11 18
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 2857 None 46 Human Functional pEC50 = 6.3 6.3 -11 18
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
439260.0 2857 None 46 Human Functional pEC50 = 6.3 6.3 -11 18
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 2857 None 46 Human Functional pEC50 = 6.3 6.3 -11 18
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 2857 None 46 Human Functional pEC50 = 6.3 6.3 -11 18
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 2857 None 46 Human Functional pEC50 = 6.3 6.3 -11 18
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 2605 None 60 Human Functional pEC50 = 6.9 6.9 -26 8
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 2605 None 60 Human Functional pEC50 = 6.9 6.9 -26 8
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
4810.0 2605 None 60 Human Functional pEC50 = 6.9 6.9 -26 8
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 2605 None 60 Human Functional pEC50 = 6.9 6.9 -26 8
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 2605 None 60 Human Functional pEC50 = 6.9 6.9 -26 8
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 4106 None 55 Human Functional pEC50 = 7.1 7.1 -1 5
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
5707 4106 None 55 Human Functional pEC50 = 7.1 7.1 -1 5
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
CHEMBL297362 4106 None 55 Human Functional pEC50 = 7.1 7.1 -1 5
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
DB11477 4106 None 55 Human Functional pEC50 = 7.1 7.1 -1 5
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
1028 291 None 40 Human Functional pEC50 = 7.6 7.6 -44 19
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 None 40 Human Functional pEC50 = 7.6 7.6 -44 19
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 None 40 Human Functional pEC50 = 7.6 7.6 -44 19
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 None 40 Human Functional pEC50 = 7.6 7.6 -44 19
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
5816.0 291 None 40 Human Functional pEC50 = 7.6 7.6 -44 19
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 None 40 Human Functional pEC50 = 7.6 7.6 -44 19
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 None 40 Human Functional pEC50 = 7.6 7.6 -44 19
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 2733 None 38 Human Functional pEC50 = 7.7 7.7 -13 7
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
3369 2733 None 38 Human Functional pEC50 = 7.7 7.7 -13 7
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
4436 2733 None 38 Human Functional pEC50 = 7.7 7.7 -13 7
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
4436.0 2733 None 38 Human Functional pEC50 = 7.7 7.7 -13 7
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
5509 2733 None 38 Human Functional pEC50 = 7.7 7.7 -13 7
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
CHEMBL761 2733 None 38 Human Functional pEC50 = 7.7 7.7 -13 7
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
DB06711 2733 None 38 Human Functional pEC50 = 7.7 7.7 -13 7
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
1960 2857 None 46 Human Functional pEC50 = 7.7 7.7 -11 18
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 2857 None 46 Human Functional pEC50 = 7.7 7.7 -11 18
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
439260.0 2857 None 46 Human Functional pEC50 = 7.7 7.7 -11 18
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 2857 None 46 Human Functional pEC50 = 7.7 7.7 -11 18
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 2857 None 46 Human Functional pEC50 = 7.7 7.7 -11 18
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 2857 None 46 Human Functional pEC50 = 7.7 7.7 -11 18
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 955 None 40 Human Functional pEC50 = 7.8 7.8 -15 14
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
2803.0 955 None 40 Human Functional pEC50 = 7.8 7.8 -15 14
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
516 955 None 40 Human Functional pEC50 = 7.8 7.8 -15 14
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
704 955 None 40 Human Functional pEC50 = 7.8 7.8 -15 14
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
CHEMBL134 955 None 40 Human Functional pEC50 = 7.8 7.8 -15 14
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
DB00575 955 None 40 Human Functional pEC50 = 7.8 7.8 -15 14
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
1343 1889 None 43 Human Functional pEC50 = 8 8.0 -11 12
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 1889 None 43 Human Functional pEC50 = 8 8.0 -11 12
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
3519.0 1889 None 43 Human Functional pEC50 = 8 8.0 -11 12
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 1889 None 43 Human Functional pEC50 = 8 8.0 -11 12
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 1889 None 43 Human Functional pEC50 = 8 8.0 -11 12
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 1889 None 43 Human Functional pEC50 = 8 8.0 -11 12
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 722 None 63 Human Functional pEC50 = 8.2 8.2 -7 10
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
2435.0 722 None 63 Human Functional pEC50 = 8.2 8.2 -7 10
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
395 722 None 63 Human Functional pEC50 = 8.2 8.2 -7 10
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
520 722 None 63 Human Functional pEC50 = 8.2 8.2 -7 10
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
5386 722 None 63 Human Functional pEC50 = 8.2 8.2 -7 10
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
CHEMBL844 722 None 63 Human Functional pEC50 = 8.2 8.2 -7 10
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
DB00484 722 None 63 Human Functional pEC50 = 8.2 8.2 -7 10
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
3952 1888 None 32 Human Functional pEC50 = 8.4 8.4 -18 21
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5353646 1888 None 32 Human Functional pEC50 = 8.4 8.4 -18 21
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5353646.0 1888 None 32 Human Functional pEC50 = 8.4 8.4 -18 21
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5443 1888 None 32 Human Functional pEC50 = 8.4 8.4 -18 21
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5702063 1888 None 32 Human Functional pEC50 = 8.4 8.4 -18 21
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5702063.0 1888 None 32 Human Functional pEC50 = 8.4 8.4 -18 21
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
CHEMBL1331786 1888 None 32 Human Functional pEC50 = 8.4 8.4 -18 21
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
CHEMBL420 1888 None 32 Human Functional pEC50 = 8.4 8.4 -18 21
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
DB00629 1888 None 32 Human Functional pEC50 = 8.4 8.4 -18 21
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
521 1404 None 49 Human Functional pEC50 = 9.6 9.6 -4 5
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
5311068 1404 None 49 Human Functional pEC50 = 9.6 9.6 -4 5
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
5311068.0 1404 None 49 Human Functional pEC50 = 9.6 9.6 -4 5
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
835 1404 None 49 Human Functional pEC50 = 9.6 9.6 -4 5
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
CHEMBL778 1404 None 49 Human Functional pEC50 = 9.6 9.6 -4 5
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
DB00633 1404 None 49 Human Functional pEC50 = 9.6 9.6 -4 5
ERK1/2 phosphorylationERK1/2 phosphorylation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
30699 220190 None 0 Human Functional pIC50 = 8.3 8.3 -1 14
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 3256 None 51 Human Functional pIC50 = 8.2 8.2 -8 29
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 None 51 Human Functional pIC50 = 8.2 8.2 -8 29
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 None 51 Human Functional pIC50 = 8.2 8.2 -8 29
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002.0 3256 None 51 Human Functional pIC50 = 8.2 8.2 -8 29
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 None 51 Human Functional pIC50 = 8.2 8.2 -8 29
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 None 51 Human Functional pIC50 = 8.2 8.2 -8 29
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1225 1471 None 18 Human Functional pIC50 = 8.2 8.2 -3 11
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 None 18 Human Functional pIC50 = 8.2 8.2 -3 11
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 None 18 Human Functional pIC50 = 8.2 8.2 -3 11
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477.0 1471 None 18 Human Functional pIC50 = 8.2 8.2 -3 11
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 None 18 Human Functional pIC50 = 8.2 8.2 -3 11
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 None 18 Human Functional pIC50 = 8.2 8.2 -3 11
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
1816 2540 None 64 Human Functional pIC50 = 6.7 6.7 -43 12
UnclassifiedUnclassified
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10636247
4205 2540 None 64 Human Functional pIC50 = 6.7 6.7 -43 12
UnclassifiedUnclassified
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10636247
4205.0 2540 None 64 Human Functional pIC50 = 6.7 6.7 -43 12
UnclassifiedUnclassified
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10636247
7241 2540 None 64 Human Functional pIC50 = 6.7 6.7 -43 12
UnclassifiedUnclassified
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10636247
CHEMBL654 2540 None 64 Human Functional pIC50 = 6.7 6.7 -43 12
UnclassifiedUnclassified
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10636247
DB00370 2540 None 64 Human Functional pIC50 = 6.7 6.7 -43 12
UnclassifiedUnclassified
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10636247
102 4127 None 36 Human Functional pIC50 = 7.4 7.4 -2 20
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 4127 None 36 Human Functional pIC50 = 7.4 7.4 -2 20
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 4127 None 36 Human Functional pIC50 = 7.4 7.4 -2 20
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
8969.0 4127 None 36 Human Functional pIC50 = 7.4 7.4 -2 20
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 4127 None 36 Human Functional pIC50 = 7.4 7.4 -2 20
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 4127 None 36 Human Functional pIC50 = 7.4 7.4 -2 20
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 2563 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 2563 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 2563 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 2605 None 60 Human Functional pIC50 = 6.5 6.5 -26 8
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 2605 None 60 Human Functional pIC50 = 6.5 6.5 -26 8
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 2605 None 60 Human Functional pIC50 = 6.5 6.5 -26 8
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 2605 None 60 Human Functional pIC50 = 6.5 6.5 -26 8
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
4810.0 2605 None 60 Human Functional pIC50 = 6.5 6.5 -26 8
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
4810.0 2605 None 60 Human Functional pIC50 = 6.5 6.5 -26 8
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 2605 None 60 Human Functional pIC50 = 6.5 6.5 -26 8
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 2605 None 60 Human Functional pIC50 = 6.5 6.5 -26 8
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 2605 None 60 Human Functional pIC50 = 6.5 6.5 -26 8
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 2605 None 60 Human Functional pIC50 = 6.5 6.5 -26 8
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 None 40 Human Functional pIC50 = 6.7 6.7 -44 19
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 None 40 Human Functional pIC50 = 6.7 6.7 -44 19
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 None 40 Human Functional pIC50 = 6.7 6.7 -44 19
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 None 40 Human Functional pIC50 = 6.7 6.7 -44 19
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
5816.0 291 None 40 Human Functional pIC50 = 6.7 6.7 -44 19
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 None 40 Human Functional pIC50 = 6.7 6.7 -44 19
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 None 40 Human Functional pIC50 = 6.7 6.7 -44 19
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 4106 None 55 Human Functional pIC50 = 6.8 6.8 -1 5
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
5707 4106 None 55 Human Functional pIC50 = 6.8 6.8 -1 5
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
CHEMBL297362 4106 None 55 Human Functional pIC50 = 6.8 6.8 -1 5
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
DB11477 4106 None 55 Human Functional pIC50 = 6.8 6.8 -1 5
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
3952 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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
5353646.0 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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
5353646.0 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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
5702063.0 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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
5702063.0 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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 1888 None 32 Human Functional pIC50 = 7.0 7.0 -18 21
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 2733 None 38 Human Functional pIC50 = 7.1 7.1 -13 7
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
3369 2733 None 38 Human Functional pIC50 = 7.1 7.1 -13 7
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
4436 2733 None 38 Human Functional pIC50 = 7.1 7.1 -13 7
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
4436.0 2733 None 38 Human Functional pIC50 = 7.1 7.1 -13 7
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
5509 2733 None 38 Human Functional pIC50 = 7.1 7.1 -13 7
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
CHEMBL761 2733 None 38 Human Functional pIC50 = 7.1 7.1 -13 7
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
DB06711 2733 None 38 Human Functional pIC50 = 7.1 7.1 -13 7
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
1343 1889 None 43 Human Functional pIC50 = 7.2 7.2 -11 12
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 1889 None 43 Human Functional pIC50 = 7.2 7.2 -11 12
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
3519.0 1889 None 43 Human Functional pIC50 = 7.2 7.2 -11 12
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 1889 None 43 Human Functional pIC50 = 7.2 7.2 -11 12
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 1889 None 43 Human Functional pIC50 = 7.2 7.2 -11 12
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 1889 None 43 Human Functional pIC50 = 7.2 7.2 -11 12
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 4107 None 38 Human Functional pIC50 = 7.2 7.2 -12 18
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 4107 None 38 Human Functional pIC50 = 7.2 7.2 -12 18
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 4107 None 38 Human Functional pIC50 = 7.2 7.2 -12 18
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
5709.0 4107 None 38 Human Functional pIC50 = 7.2 7.2 -12 18
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 4107 None 38 Human Functional pIC50 = 7.2 7.2 -12 18
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 4107 None 38 Human Functional pIC50 = 7.2 7.2 -12 18
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 2857 None 46 Human Functional pIC50 = 7.6 7.6 -11 18
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 2857 None 46 Human Functional pIC50 = 7.6 7.6 -11 18
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 2857 None 46 Human Functional pIC50 = 7.6 7.6 -11 18
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 2857 None 46 Human Functional pIC50 = 7.6 7.6 -11 18
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
439260.0 2857 None 46 Human Functional pIC50 = 7.6 7.6 -11 18
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
439260.0 2857 None 46 Human Functional pIC50 = 7.6 7.6 -11 18
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 2857 None 46 Human Functional pIC50 = 7.6 7.6 -11 18
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 2857 None 46 Human Functional pIC50 = 7.6 7.6 -11 18
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 2857 None 46 Human Functional pIC50 = 7.6 7.6 -11 18
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 2857 None 46 Human Functional pIC50 = 7.6 7.6 -11 18
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 2857 None 46 Human Functional pIC50 = 7.6 7.6 -11 18
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 2857 None 46 Human Functional pIC50 = 7.6 7.6 -11 18
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 955 None 40 Human Functional pIC50 = 7.6 7.6 -15 14
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 25080296
2803 955 None 40 Human Functional pIC50 = 7.6 7.6 -15 14
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
2803.0 955 None 40 Human Functional pIC50 = 7.6 7.6 -15 14
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 25080296
2803.0 955 None 40 Human Functional pIC50 = 7.6 7.6 -15 14
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
516 955 None 40 Human Functional pIC50 = 7.6 7.6 -15 14
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 25080296
516 955 None 40 Human Functional pIC50 = 7.6 7.6 -15 14
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
704 955 None 40 Human Functional pIC50 = 7.6 7.6 -15 14
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 25080296
704 955 None 40 Human Functional pIC50 = 7.6 7.6 -15 14
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
CHEMBL134 955 None 40 Human Functional pIC50 = 7.6 7.6 -15 14
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 25080296
CHEMBL134 955 None 40 Human Functional pIC50 = 7.6 7.6 -15 14
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
DB00575 955 None 40 Human Functional pIC50 = 7.6 7.6 -15 14
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 25080296
DB00575 955 None 40 Human Functional pIC50 = 7.6 7.6 -15 14
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
124 2981 None 32 Human Functional pIC50 = 7.8 7.8 -144 24
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 2981 None 32 Human Functional pIC50 = 7.8 7.8 -144 24
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 2981 None 32 Human Functional pIC50 = 7.8 7.8 -144 24
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 2981 None 32 Human Functional pIC50 = 7.8 7.8 -144 24
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 2981 None 32 Human Functional pIC50 = 7.8 7.8 -144 24
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 2981 None 32 Human Functional pIC50 = 7.8 7.8 -144 24
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
4636.0 2981 None 32 Human Functional pIC50 = 7.8 7.8 -144 24
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
4636.0 2981 None 32 Human Functional pIC50 = 7.8 7.8 -144 24
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 2981 None 32 Human Functional pIC50 = 7.8 7.8 -144 24
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 2981 None 32 Human Functional pIC50 = 7.8 7.8 -144 24
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 2981 None 32 Human Functional pIC50 = 7.8 7.8 -144 24
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 2981 None 32 Human Functional pIC50 = 7.8 7.8 -144 24
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 722 None 63 Human Functional pIC50 = 8.3 8.3 -7 10
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
2435 722 None 63 Human Functional pIC50 = 8.3 8.3 -7 10
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
2435.0 722 None 63 Human Functional pIC50 = 8.3 8.3 -7 10
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
2435.0 722 None 63 Human Functional pIC50 = 8.3 8.3 -7 10
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
395 722 None 63 Human Functional pIC50 = 8.3 8.3 -7 10
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
395 722 None 63 Human Functional pIC50 = 8.3 8.3 -7 10
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
520 722 None 63 Human Functional pIC50 = 8.3 8.3 -7 10
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
520 722 None 63 Human Functional pIC50 = 8.3 8.3 -7 10
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
5386 722 None 63 Human Functional pIC50 = 8.3 8.3 -7 10
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
5386 722 None 63 Human Functional pIC50 = 8.3 8.3 -7 10
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
CHEMBL844 722 None 63 Human Functional pIC50 = 8.3 8.3 -7 10
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
CHEMBL844 722 None 63 Human Functional pIC50 = 8.3 8.3 -7 10
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
DB00484 722 None 63 Human Functional pIC50 = 8.3 8.3 -7 10
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 25080296
DB00484 722 None 63 Human Functional pIC50 = 8.3 8.3 -7 10
inhibition of cAMP productioninhibition of cAMP production
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
521 1404 None 49 Human Functional pIC50 = 9.2 9.2 -4 5
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 1404 None 49 Human Functional pIC50 = 9.2 9.2 -4 5
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
5311068.0 1404 None 49 Human Functional pIC50 = 9.2 9.2 -4 5
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 1404 None 49 Human Functional pIC50 = 9.2 9.2 -4 5
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 1404 None 49 Human Functional pIC50 = 9.2 9.2 -4 5
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 1404 None 49 Human Functional pIC50 = 9.2 9.2 -4 5
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 2151 None 37 Human Functional pKB = 7.4 7.4 28 3
UnclassifiedUnclassified
Guide to Pharmacology 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 17220913
3930 2151 None 37 Human Functional pKB = 7.4 7.4 28 3
UnclassifiedUnclassified
Guide to Pharmacology 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 35224877
540335 2151 None 37 Human Functional pKB = 7.4 7.4 28 3
UnclassifiedUnclassified
Guide to Pharmacology 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 17220913
540335 2151 None 37 Human Functional pKB = 7.4 7.4 28 3
UnclassifiedUnclassified
Guide to Pharmacology 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 35224877
CHEMBL106525 2151 None 37 Human Functional pKB = 7.4 7.4 28 3
UnclassifiedUnclassified
Guide to Pharmacology 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 17220913
CHEMBL106525 2151 None 37 Human Functional pKB = 7.4 7.4 28 3
UnclassifiedUnclassified
Guide to Pharmacology 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 35224877
13130 2965 None 0 Human Functional pKB = 9.8 9.8 - 1
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 2965 None 0 Human Functional pKB = 9.8 9.8 - 1
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
Sel. page Common
name
GPCRdb
ID
Reference
ligand
Vendors

Species

Assay
Type
Activity
Type
Activity
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Activity
Value
p-value
(-log)
Fold
selectivity
Tested
GPCRs
Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

57345628 71207 None 0 Human Binding pEC50 = 8.7 8.7 -26 4
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 71207 None 0 Human Binding pEC50 = 8.7 8.7 -26 4
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 77701 None 0 Human Binding pEC50 = 8.7 8.7 -47 4
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 77701 None 0 Human Binding pEC50 = 8.7 8.7 -47 4
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 71204 None 0 Human Binding pEC50 = 8 8.0 -12 4
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 71204 None 0 Human Binding pEC50 = 8 8.0 -12 4
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 92541 None 0 Human Binding pEC50 = 6 6.0 -10 4
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 92541 None 0 Human Binding pEC50 = 6 6.0 -10 4
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 142814 None 0 Human Binding pEC50 = 6.9 6.9 - 0
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 142814 None 0 Human Binding pEC50 = 6.9 6.9 - 0
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 18578 None 0 Human Binding pEC50 = 6.9 6.9 -2 3
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 18578 None 0 Human Binding pEC50 = 6.9 6.9 -2 3
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 116872 None 0 Human Binding pEC50 = 6.8 6.8 - 0
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 116872 None 0 Human Binding pEC50 = 6.8 6.8 - 0
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 30350 None 0 Human Binding pEC50 = 6.8 6.8 -10 4
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 218 5 1 3 2.0 CCCc1ccccc1OCC1=NCCN1 10.1021/ml400232p
CHEMBL13917 30350 None 0 Human Binding pEC50 = 6.8 6.8 -10 4
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 218 5 1 3 2.0 CCCc1ccccc1OCC1=NCCN1 10.1021/ml400232p
134156190 151454 None 0 Human Binding pEC50 = 6.8 6.8 - 0
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 151454 None 0 Human Binding pEC50 = 6.8 6.8 - 0
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 18573 None 0 Human Binding pEC50 = 6.7 6.7 -1 3
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 18573 None 0 Human Binding pEC50 = 6.7 6.7 -1 3
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 144282 None 1 Human Binding pEC50 = 7.7 7.7 - 0
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 144282 None 1 Human Binding pEC50 = 7.7 7.7 - 0
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 189562 None 1 Human Binding pEC50 = 6.7 6.7 - 1
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 189562 None 1 Human Binding pEC50 = 6.7 6.7 - 1
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 92542 None 0 Human Binding pEC50 = 6.6 6.6 -8 4
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 92542 None 0 Human Binding pEC50 = 6.6 6.6 -8 4
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 18574 None 0 Human Binding pEC50 = 7.6 7.6 -1 4
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 18574 None 0 Human Binding pEC50 = 7.6 7.6 -1 4
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 92543 None 0 Human Binding pEC50 = 7.6 7.6 -10 4
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 92543 None 0 Human Binding pEC50 = 7.6 7.6 -10 4
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 77700 None 0 Human Binding pEC50 = 6.5 6.5 -5 4
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 77700 None 0 Human Binding pEC50 = 6.5 6.5 -5 4
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 18579 None 0 Human Binding pEC50 = 7.5 7.5 -10 4
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 18579 None 0 Human Binding pEC50 = 7.5 7.5 -10 4
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 18577 None 0 Human Binding pEC50 = 7.4 7.4 -10 4
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 18577 None 0 Human Binding pEC50 = 7.4 7.4 -10 4
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 943 None 16 Human Binding pEC50 = 6.4 6.4 -15 9
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
515 943 None 16 Human Binding pEC50 = 6.4 6.4 -15 9
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 943 None 16 Human Binding pEC50 = 6.4 6.4 -15 9
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 943 None 16 Human Binding pEC50 = 6.4 6.4 -15 9
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 71209 None 0 Human Binding pEC50 = 7.3 7.3 -45 4
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 71209 None 0 Human Binding pEC50 = 7.3 7.3 -45 4
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 187770 None 3 Human Binding pEC50 = 7.3 7.3 -3 4
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 187770 None 3 Human Binding pEC50 = 7.3 7.3 -3 4
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 32361 None 0 Human Binding pEC50 = 7.2 7.2 -1 4
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 32361 None 0 Human Binding pEC50 = 7.2 7.2 -1 4
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 92539 None 1 Human Binding pEC50 = 7.0 7.0 -4 4
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 254 3 1 3 1.8 Brc1ccccc1OCC1=NCCN1 10.1021/ml400232p
CHEMBL2431279 92539 None 1 Human Binding pEC50 = 7.0 7.0 -4 4
Agonist activity at human alpha2C ARAgonist activity at human alpha2C AR
ChEMBL 254 3 1 3 1.8 Brc1ccccc1OCC1=NCCN1 10.1021/ml400232p
44376984 56239 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 56239 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 57437 None 1 Human Binding pIC50 = 9.2 9.2 - 0
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 57437 None 1 Human Binding pIC50 = 9.2 9.2 - 0
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 56061 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 56061 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 120220 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 120220 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 55756 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 55756 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 56443 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 56443 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 57496 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 57496 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 55937 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 55937 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 120194 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 120194 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 56500 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 56500 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 56284 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 56284 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 56075 None 31 Human Binding pIC50 = 8.8 8.8 - 0
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 56075 None 31 Human Binding pIC50 = 8.8 8.8 - 0
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 1420 None 13 Human Binding pIC50 = 8 8.0 -16 30
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
10531.0 1420 None 13 Human Binding pIC50 = 8 8.0 -16 30
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 1420 None 13 Human Binding pIC50 = 8 8.0 -16 30
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 1420 None 13 Human Binding pIC50 = 8 8.0 -16 30
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 1420 None 13 Human Binding pIC50 = 8 8.0 -16 30
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 1420 None 13 Human Binding pIC50 = 8 8.0 -16 30
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 1462 None 65 Human Binding pIC50 = 6 6.0 -40 26
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
3151.0 1462 None 65 Human Binding pIC50 = 6 6.0 -40 26
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 1462 None 65 Human Binding pIC50 = 6 6.0 -40 26
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 1462 None 65 Human Binding pIC50 = 6 6.0 -40 26
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 1462 None 65 Human Binding pIC50 = 6 6.0 -40 26
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 1462 None 65 Human Binding pIC50 = 6 6.0 -40 26
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 56283 None 21 Human Binding pIC50 = 6.0 6.0 -1047 20
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
3158.0 56283 None 21 Human Binding pIC50 = 6.0 6.0 -1047 20
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 56283 None 21 Human Binding pIC50 = 6.0 6.0 -1047 20
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 56283 None 21 Human Binding pIC50 = 6.0 6.0 -1047 20
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 189769 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 189769 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 3096 None 36 Human Binding pIC50 = 7.0 7.0 -7 36
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 3096 None 36 Human Binding pIC50 = 7.0 7.0 -7 36
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 3096 None 36 Human Binding pIC50 = 7.0 7.0 -7 36
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 3096 None 36 Human Binding pIC50 = 7.0 7.0 -7 36
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
5775.0 3096 None 36 Human Binding pIC50 = 7.0 7.0 -7 36
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 3096 None 36 Human Binding pIC50 = 7.0 7.0 -7 36
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 3096 None 36 Human Binding pIC50 = 7.0 7.0 -7 36
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 83572 None 1 Human Binding pIC50 = 5.0 5.0 - 0
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 83572 None 1 Human Binding pIC50 = 5.0 5.0 - 0
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 1888 None 32 Human Binding pIC50 = 6.0 6.0 -19 12
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 1888 None 32 Human Binding pIC50 = 6.0 6.0 -19 12
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
5353646.0 1888 None 32 Human Binding pIC50 = 6.0 6.0 -19 12
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 1888 None 32 Human Binding pIC50 = 6.0 6.0 -19 12
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 1888 None 32 Human Binding pIC50 = 6.0 6.0 -19 12
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
5702063.0 1888 None 32 Human Binding pIC50 = 6.0 6.0 -19 12
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 1888 None 32 Human Binding pIC50 = 6.0 6.0 -19 12
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 1888 None 32 Human Binding pIC50 = 6.0 6.0 -19 12
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 1888 None 32 Human Binding pIC50 = 6.0 6.0 -19 12
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 208467 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 208467 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 208276 None 49 Human Binding pIC50 = 5.9 5.9 -1 3
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
5472.0 208276 None 49 Human Binding pIC50 = 5.9 5.9 -1 3
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 208276 None 49 Human Binding pIC50 = 5.9 5.9 -1 3
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 208276 None 49 Human Binding pIC50 = 5.9 5.9 -1 3
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 208276 None 49 Human Binding pIC50 = 5.9 5.9 -1 3
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 1582 None 6 Human Binding pIC50 = 7.9 7.9 -19 27
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 1582 None 6 Human Binding pIC50 = 7.9 7.9 -19 27
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 1582 None 6 Human Binding pIC50 = 7.9 7.9 -19 27
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
8223.0 1582 None 6 Human Binding pIC50 = 7.9 7.9 -19 27
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 1582 None 6 Human Binding pIC50 = 7.9 7.9 -19 27
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 1582 None 6 Human Binding pIC50 = 7.9 7.9 -19 27
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 1301 None 39 Human Binding pIC50 = 5.9 5.9 -42 49
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 1301 None 39 Human Binding pIC50 = 5.9 5.9 -42 49
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
2913.0 1301 None 39 Human Binding pIC50 = 5.9 5.9 -42 49
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 1301 None 39 Human Binding pIC50 = 5.9 5.9 -42 49
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 1301 None 39 Human Binding pIC50 = 5.9 5.9 -42 49
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 1301 None 39 Human Binding pIC50 = 5.9 5.9 -42 49
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 216737 None 3 Human Binding pIC50 = 4.9 4.9 - 0
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 57392 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 57392 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 156397 None 49 Human Binding pIC50 = 4.9 4.9 - 0
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 156397 None 49 Human Binding pIC50 = 4.9 4.9 - 0
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 None 9 Human Binding pIC50 = 4.9 4.9 - 6
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 None 9 Human Binding pIC50 = 4.9 4.9 - 6
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 None 9 Human Binding pIC50 = 4.9 4.9 - 6
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 3054 None 28 Human Binding pIC50 = 5.9 5.9 -81 33
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 3054 None 28 Human Binding pIC50 = 5.9 5.9 -81 33
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 3054 None 28 Human Binding pIC50 = 5.9 5.9 -81 33
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 3054 None 28 Human Binding pIC50 = 5.9 5.9 -81 33
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 3054 None 28 Human Binding pIC50 = 5.9 5.9 -81 33
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 954 None 43 Human Binding pIC50 = 5.9 5.9 -4 28
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 954 None 43 Human Binding pIC50 = 5.9 5.9 -4 28
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
2801.0 954 None 43 Human Binding pIC50 = 5.9 5.9 -4 28
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
701 954 None 43 Human Binding pIC50 = 5.9 5.9 -4 28
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 954 None 43 Human Binding pIC50 = 5.9 5.9 -4 28
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 954 None 43 Human Binding pIC50 = 5.9 5.9 -4 28
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 71142 None 57 Human Binding pIC50 = 4.9 4.9 1 10
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 71142 None 57 Human Binding pIC50 = 4.9 4.9 1 10
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 210138 None 21 Human Binding pIC50 = 5.8 5.8 1 17
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 210138 None 21 Human Binding pIC50 = 5.8 5.8 1 17
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 102943 None 17 Human Binding pIC50 = 5.8 5.8 -30 16
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 102943 None 17 Human Binding pIC50 = 5.8 5.8 -30 16
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 102943 None 17 Human Binding pIC50 = 5.8 5.8 -30 16
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 160344 None 54 Human Binding pIC50 = 4.8 4.8 -21 25
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 160344 None 54 Human Binding pIC50 = 4.8 4.8 -21 25
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 1662 None 37 Human Binding pIC50 = 6.8 6.8 -54 65
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 1662 None 37 Human Binding pIC50 = 6.8 6.8 -54 65
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 1662 None 37 Human Binding pIC50 = 6.8 6.8 -54 65
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
3372.0 1662 None 37 Human Binding pIC50 = 6.8 6.8 -54 65
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 1662 None 37 Human Binding pIC50 = 6.8 6.8 -54 65
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 1662 None 37 Human Binding pIC50 = 6.8 6.8 -54 65
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 177282 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 177282 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 67820 None 12 Human Binding pIC50 = 5.8 5.8 -295 15
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 67820 None 12 Human Binding pIC50 = 5.8 5.8 -295 15
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 189057 None 54 Human Binding pIC50 = 5.8 5.8 -3 13
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 189057 None 54 Human Binding pIC50 = 5.8 5.8 -3 13
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 29624 None 14 Human Binding pIC50 = 7.8 7.8 -3 17
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 29624 None 14 Human Binding pIC50 = 7.8 7.8 -3 17
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 3805 None 44 Human Binding pIC50 = 6.8 6.8 -27 55
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 3805 None 44 Human Binding pIC50 = 6.8 6.8 -27 55
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 3805 None 44 Human Binding pIC50 = 6.8 6.8 -27 55
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 3805 None 44 Human Binding pIC50 = 6.8 6.8 -27 55
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 3805 None 44 Human Binding pIC50 = 6.8 6.8 -27 55
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 9264 None 62 Human Binding pIC50 = 5.8 5.8 -63 21
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
3168.0 9264 None 62 Human Binding pIC50 = 5.8 5.8 -63 21
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 9264 None 62 Human Binding pIC50 = 5.8 5.8 -63 21
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 9264 None 62 Human Binding pIC50 = 5.8 5.8 -63 21
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 2532 None 33 Human Binding pIC50 = 6.8 6.8 -6 57
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 2532 None 33 Human Binding pIC50 = 6.8 6.8 -6 57
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 2532 None 33 Human Binding pIC50 = 6.8 6.8 -6 57
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
4184.0 2532 None 33 Human Binding pIC50 = 6.8 6.8 -6 57
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 2532 None 33 Human Binding pIC50 = 6.8 6.8 -6 57
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 2532 None 33 Human Binding pIC50 = 6.8 6.8 -6 57
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 177400 None 1 Human Binding pIC50 = 6.8 6.8 - 0
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 177400 None 1 Human Binding pIC50 = 6.8 6.8 - 0
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 41527 None 58 Human Binding pIC50 = 5.8 5.8 -1 6
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 41527 None 58 Human Binding pIC50 = 5.8 5.8 -1 6
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 188904 None 34 Human Binding pIC50 = 6.7 6.7 -2 5
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 188904 None 34 Human Binding pIC50 = 6.7 6.7 -2 5
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 188904 None 34 Human Binding pIC50 = 6.7 6.7 -2 5
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 1911 None 63 Human Binding pIC50 = 5.7 5.7 -87 85
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 1911 None 63 Human Binding pIC50 = 5.7 5.7 -87 85
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
3559.0 1911 None 63 Human Binding pIC50 = 5.7 5.7 -87 85
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 1911 None 63 Human Binding pIC50 = 5.7 5.7 -87 85
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 1911 None 63 Human Binding pIC50 = 5.7 5.7 -87 85
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 1911 None 63 Human Binding pIC50 = 5.7 5.7 -87 85
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 208308 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 208308 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 176253 None 16 Human Binding pIC50 = 5.7 5.7 -1 20
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 176253 None 16 Human Binding pIC50 = 5.7 5.7 -1 20
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 176253 None 16 Human Binding pIC50 = 5.7 5.7 -1 20
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 176253 None 16 Human Binding pIC50 = 5.7 5.7 -1 20
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 2496 None 39 Human Binding pIC50 = 6.7 6.7 -26 42
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 2496 None 39 Human Binding pIC50 = 6.7 6.7 -26 42
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 2496 None 39 Human Binding pIC50 = 6.7 6.7 -26 42
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 2496 None 39 Human Binding pIC50 = 6.7 6.7 -26 42
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 2496 None 39 Human Binding pIC50 = 6.7 6.7 -26 42
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 3853 None 34 Human Binding pIC50 = 5.7 5.7 -3 43
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 3853 None 34 Human Binding pIC50 = 5.7 5.7 -3 43
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 3853 None 34 Human Binding pIC50 = 5.7 5.7 -3 43
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
5533.0 3853 None 34 Human Binding pIC50 = 5.7 5.7 -3 43
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 3853 None 34 Human Binding pIC50 = 5.7 5.7 -3 43
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 3853 None 34 Human Binding pIC50 = 5.7 5.7 -3 43
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 None 55 Human Binding pIC50 = 5.7 5.7 -25 41
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 None 55 Human Binding pIC50 = 5.7 5.7 -25 41
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 None 55 Human Binding pIC50 = 5.7 5.7 -25 41
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 None 55 Human Binding pIC50 = 5.7 5.7 -25 41
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 None 55 Human Binding pIC50 = 5.7 5.7 -25 41
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 11852 None 18 Human Binding pIC50 = 5.7 5.7 -2 12
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 11852 None 18 Human Binding pIC50 = 5.7 5.7 -2 12
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 11852 None 18 Human Binding pIC50 = 5.7 5.7 -2 12
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 11852 None 18 Human Binding pIC50 = 5.7 5.7 -2 12
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 2540 None 64 Human Binding pIC50 = 6.7 6.7 -38 17
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 2540 None 64 Human Binding pIC50 = 6.7 6.7 -38 17
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
4205.0 2540 None 64 Human Binding pIC50 = 6.7 6.7 -38 17
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 2540 None 64 Human Binding pIC50 = 6.7 6.7 -38 17
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 2540 None 64 Human Binding pIC50 = 6.7 6.7 -38 17
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 2540 None 64 Human Binding pIC50 = 6.7 6.7 -38 17
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 57164 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 57164 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 56002 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 56002 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 217275 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 2866 None 32 Human Binding pIC50 = 6.7 6.7 -2 29
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 2866 None 32 Human Binding pIC50 = 6.7 6.7 -2 29
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 2866 None 32 Human Binding pIC50 = 6.7 6.7 -2 29
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
4543.0 2866 None 32 Human Binding pIC50 = 6.7 6.7 -2 29
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 2866 None 32 Human Binding pIC50 = 6.7 6.7 -2 29
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 2866 None 32 Human Binding pIC50 = 6.7 6.7 -2 29
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 201381 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 201381 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 217237 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 1657 None 39 Human Binding pIC50 = 6.7 6.7 -2 23
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 1657 None 39 Human Binding pIC50 = 6.7 6.7 -2 23
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 1657 None 39 Human Binding pIC50 = 6.7 6.7 -2 23
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 1657 None 39 Human Binding pIC50 = 6.7 6.7 -2 23
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 3832 None 11 Human Binding pIC50 = 4.6 4.6 - 0
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 3832 None 11 Human Binding pIC50 = 4.6 4.6 - 0
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 3832 None 11 Human Binding pIC50 = 4.6 4.6 - 0
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 40052 None 36 Human Binding pIC50 = 4.6 4.6 -1 12
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
28417.0 40052 None 36 Human Binding pIC50 = 4.6 4.6 -1 12
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 40052 None 36 Human Binding pIC50 = 4.6 4.6 -1 12
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 40052 None 36 Human Binding pIC50 = 4.6 4.6 -1 12
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 3183 None 36 Human Binding pIC50 = 5.6 5.6 -21 29
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 3183 None 36 Human Binding pIC50 = 5.6 5.6 -21 29
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
4927.0 3183 None 36 Human Binding pIC50 = 5.6 5.6 -21 29
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 3183 None 36 Human Binding pIC50 = 5.6 5.6 -21 29
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 3183 None 36 Human Binding pIC50 = 5.6 5.6 -21 29
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 3183 None 36 Human Binding pIC50 = 5.6 5.6 -21 29
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 None 40 Human Binding pIC50 = 5.6 5.6 -85 29
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 None 40 Human Binding pIC50 = 5.6 5.6 -85 29
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 None 40 Human Binding pIC50 = 5.6 5.6 -85 29
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 None 40 Human Binding pIC50 = 5.6 5.6 -85 29
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
5816.0 291 None 40 Human Binding pIC50 = 5.6 5.6 -85 29
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 None 40 Human Binding pIC50 = 5.6 5.6 -85 29
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 None 40 Human Binding pIC50 = 5.6 5.6 -85 29
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 99430 None 48 Human Binding pIC50 = 4.6 4.6 1 3
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 99430 None 48 Human Binding pIC50 = 4.6 4.6 1 3
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 3182 None 26 Human Binding pIC50 = 6.6 6.6 -7 28
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 3182 None 26 Human Binding pIC50 = 6.6 6.6 -7 28
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 3182 None 26 Human Binding pIC50 = 6.6 6.6 -7 28
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 3182 None 26 Human Binding pIC50 = 6.6 6.6 -7 28
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 3182 None 26 Human Binding pIC50 = 6.6 6.6 -7 28
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 2981 None 32 Human Binding pIC50 = 5.6 5.6 -60 32
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 2981 None 32 Human Binding pIC50 = 5.6 5.6 -60 32
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 2981 None 32 Human Binding pIC50 = 5.6 5.6 -60 32
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
4636.0 2981 None 32 Human Binding pIC50 = 5.6 5.6 -60 32
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 2981 None 32 Human Binding pIC50 = 5.6 5.6 -60 32
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 2981 None 32 Human Binding pIC50 = 5.6 5.6 -60 32
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 4127 None 36 Human Binding pIC50 = 7.6 7.6 -23 50
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 4127 None 36 Human Binding pIC50 = 7.6 7.6 -23 50
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 4127 None 36 Human Binding pIC50 = 7.6 7.6 -23 50
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
8969.0 4127 None 36 Human Binding pIC50 = 7.6 7.6 -23 50
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 4127 None 36 Human Binding pIC50 = 7.6 7.6 -23 50
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 4127 None 36 Human Binding pIC50 = 7.6 7.6 -23 50
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 57480 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 57480 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 102913 None 65 Human Binding pIC50 = 6.6 6.6 -3 25
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
3191.0 102913 None 65 Human Binding pIC50 = 6.6 6.6 -3 25
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 102913 None 65 Human Binding pIC50 = 6.6 6.6 -3 25
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 102913 None 65 Human Binding pIC50 = 6.6 6.6 -3 25
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 101166 None 49 Human Binding pIC50 = 5.6 5.6 -1 4
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 101166 None 49 Human Binding pIC50 = 5.6 5.6 -1 4
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 101166 None 49 Human Binding pIC50 = 5.6 5.6 -1 4
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 55653 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 55653 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 216937 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 82440 None 34 Human Binding pIC50 = 5.5 5.5 -28 23
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 82440 None 34 Human Binding pIC50 = 5.5 5.5 -28 23
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 15618 None 4 Human Binding pIC50 = 5.5 5.5 -47 8
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 15618 None 4 Human Binding pIC50 = 5.5 5.5 -47 8
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 183980 None 58 Human Binding pIC50 = 5.5 5.5 -1 2
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 183980 None 58 Human Binding pIC50 = 5.5 5.5 -1 2
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 None 60 Human Binding pIC50 = 5.5 5.5 -39 28
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 None 60 Human Binding pIC50 = 5.5 5.5 -39 28
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 None 60 Human Binding pIC50 = 5.5 5.5 -39 28
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
2170.0 403 None 60 Human Binding pIC50 = 5.5 5.5 -39 28
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 None 60 Human Binding pIC50 = 5.5 5.5 -39 28
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 None 60 Human Binding pIC50 = 5.5 5.5 -39 28
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
5354 155746 None 16 Human Binding pIC50 = 5.5 5.5 -5 14
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 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 nan
CHEMBL404849 155746 None 16 Human Binding pIC50 = 5.5 5.5 -5 14
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 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 nan
102 4127 None 36 Human Binding pIC50 = 7.4 7.4 -23 50
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 4127 None 36 Human Binding pIC50 = 7.4 7.4 -23 50
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 4127 None 36 Human Binding pIC50 = 7.4 7.4 -23 50
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
8969.0 4127 None 36 Human Binding pIC50 = 7.4 7.4 -23 50
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 4127 None 36 Human Binding pIC50 = 7.4 7.4 -23 50
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 4127 None 36 Human Binding pIC50 = 7.4 7.4 -23 50
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 919 None 48 Human Binding pIC50 = 6.4 6.4 -31 72
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
2726.0 919 None 48 Human Binding pIC50 = 6.4 6.4 -31 72
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
621 919 None 48 Human Binding pIC50 = 6.4 6.4 -31 72
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
83 919 None 48 Human Binding pIC50 = 6.4 6.4 -31 72
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 919 None 48 Human Binding pIC50 = 6.4 6.4 -31 72
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 919 None 48 Human Binding pIC50 = 6.4 6.4 -31 72
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 3779 None 53 Human Binding pIC50 = 5.4 5.4 -4 13
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 3779 None 53 Human Binding pIC50 = 5.4 5.4 -4 13
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 3779 None 53 Human Binding pIC50 = 5.4 5.4 -4 13
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 3779 None 53 Human Binding pIC50 = 5.4 5.4 -4 13
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 3779 None 53 Human Binding pIC50 = 5.4 5.4 -4 13
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 None 18 Human Binding pIC50 = 7.4 7.4 -5 21
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 None 18 Human Binding pIC50 = 7.4 7.4 -5 21
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 None 18 Human Binding pIC50 = 7.4 7.4 -5 21
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 None 18 Human Binding pIC50 = 7.4 7.4 -5 21
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 207323 None 37 Human Binding pIC50 = 5.4 5.4 -1 13
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 207323 None 37 Human Binding pIC50 = 5.4 5.4 -1 13
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 207323 None 37 Human Binding pIC50 = 5.4 5.4 -1 13
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 207323 None 37 Human Binding pIC50 = 5.4 5.4 -1 13
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 192355 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 192355 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 211059 None 4 Human Binding pIC50 = 5.4 5.4 -1 8
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 597 None 17 Human Binding pIC50 = 6.4 6.4 -18 20
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
1201549.0 597 None 17 Human Binding pIC50 = 6.4 6.4 -18 20
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
333 597 None 17 Human Binding pIC50 = 6.4 6.4 -18 20
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 597 None 17 Human Binding pIC50 = 6.4 6.4 -18 20
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 597 None 17 Human Binding pIC50 = 6.4 6.4 -18 20
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 597 None 17 Human Binding pIC50 = 6.4 6.4 -18 20
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 597 None 17 Human Binding pIC50 = 6.4 6.4 -18 20
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 2325 None 21 Human Binding pIC50 = 8.4 8.4 -3 43
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 2325 None 21 Human Binding pIC50 = 8.4 8.4 -3 43
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
28864.0 2325 None 21 Human Binding pIC50 = 8.4 8.4 -3 43
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 2325 None 21 Human Binding pIC50 = 8.4 8.4 -3 43
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 2325 None 21 Human Binding pIC50 = 8.4 8.4 -3 43
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 2325 None 21 Human Binding pIC50 = 8.4 8.4 -3 43
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 19084 None 29 Human Binding pIC50 = 5.4 5.4 -2 11
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 19084 None 29 Human Binding pIC50 = 5.4 5.4 -2 11
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 17993 None 30 Human Binding pIC50 = 5.4 5.4 -11 15
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 17993 None 30 Human Binding pIC50 = 5.4 5.4 -11 15
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 17993 None 30 Human Binding pIC50 = 5.4 5.4 -11 15
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 20340 None 41 Human Binding pIC50 = 6.4 6.4 -3 17
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 20340 None 41 Human Binding pIC50 = 6.4 6.4 -3 17
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 2532 None 33 Human Binding pIC50 = 7.4 7.4 -6 57
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 2532 None 33 Human Binding pIC50 = 7.4 7.4 -6 57
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 2532 None 33 Human Binding pIC50 = 7.4 7.4 -6 57
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
4184.0 2532 None 33 Human Binding pIC50 = 7.4 7.4 -6 57
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 2532 None 33 Human Binding pIC50 = 7.4 7.4 -6 57
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 2532 None 33 Human Binding pIC50 = 7.4 7.4 -6 57
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 3256 None 51 Human Binding pIC50 = 6.4 6.4 -10 62
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 3256 None 51 Human Binding pIC50 = 6.4 6.4 -10 62
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 3256 None 51 Human Binding pIC50 = 6.4 6.4 -10 62
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
5002.0 3256 None 51 Human Binding pIC50 = 6.4 6.4 -10 62
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 3256 None 51 Human Binding pIC50 = 6.4 6.4 -10 62
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 3256 None 51 Human Binding pIC50 = 6.4 6.4 -10 62
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 100458 None 56 Human Binding pIC50 = 5.4 5.4 -11 12
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 100458 None 56 Human Binding pIC50 = 5.4 5.4 -11 12
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 207985 None 33 Human Binding pIC50 = 5.4 5.4 -9 25
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 207985 None 33 Human Binding pIC50 = 5.4 5.4 -9 25
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 207985 None 33 Human Binding pIC50 = 5.4 5.4 -9 25
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 67821 None 11 Human Binding pIC50 = 7.4 7.4 -3 18
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 67821 None 11 Human Binding pIC50 = 7.4 7.4 -3 18
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 15583 None 40 Human Binding pIC50 = 5.3 5.3 -1 13
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 15583 None 40 Human Binding pIC50 = 5.3 5.3 -1 13
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 15583 None 40 Human Binding pIC50 = 5.3 5.3 -1 13
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 189074 None 0 Human Binding pIC50 = 5.3 5.3 -25 6
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 729 None 28 Human Binding pIC50 = 6.3 6.3 -36 35
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
31101.0 729 None 28 Human Binding pIC50 = 6.3 6.3 -36 35
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
35 729 None 28 Human Binding pIC50 = 6.3 6.3 -36 35
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
403 729 None 28 Human Binding pIC50 = 6.3 6.3 -36 35
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 729 None 28 Human Binding pIC50 = 6.3 6.3 -36 35
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 729 None 28 Human Binding pIC50 = 6.3 6.3 -36 35
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 2592 None 44 Human Binding pIC50 = 5.3 5.3 -31 15
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 2592 None 44 Human Binding pIC50 = 5.3 5.3 -31 15
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 2592 None 44 Human Binding pIC50 = 5.3 5.3 -31 15
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
5281040.0 2592 None 44 Human Binding pIC50 = 5.3 5.3 -31 15
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 2592 None 44 Human Binding pIC50 = 5.3 5.3 -31 15
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 2592 None 44 Human Binding pIC50 = 5.3 5.3 -31 15
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 1988 None 24 Human Binding pIC50 = 7.3 7.3 -8 16
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 1988 None 24 Human Binding pIC50 = 7.3 7.3 -8 16
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
54459.0 1988 None 24 Human Binding pIC50 = 7.3 7.3 -8 16
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 1988 None 24 Human Binding pIC50 = 7.3 7.3 -8 16
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 1988 None 24 Human Binding pIC50 = 7.3 7.3 -8 16
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 2914 None 65 Human Binding pIC50 = 6.3 6.3 -30 65
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
135398745.0 2914 None 65 Human Binding pIC50 = 6.3 6.3 -30 65
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 2914 None 65 Human Binding pIC50 = 6.3 6.3 -30 65
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 2914 None 65 Human Binding pIC50 = 6.3 6.3 -30 65
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 2914 None 65 Human Binding pIC50 = 6.3 6.3 -30 65
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 29093 None 45 Human Binding pIC50 = 4.3 4.3 -3 6
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 29093 None 45 Human Binding pIC50 = 4.3 4.3 -3 6
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 55561 None 1 Human Binding pIC50 = 7.2 7.2 - 0
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 55561 None 1 Human Binding pIC50 = 7.2 7.2 - 0
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 None 38 Human Binding pIC50 = 7.2 7.2 -16 39
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 None 38 Human Binding pIC50 = 7.2 7.2 -16 39
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 None 38 Human Binding pIC50 = 7.2 7.2 -16 39
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
2160.0 401 None 38 Human Binding pIC50 = 7.2 7.2 -16 39
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 None 38 Human Binding pIC50 = 7.2 7.2 -16 39
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 None 38 Human Binding pIC50 = 7.2 7.2 -16 39
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 57491 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 57491 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 3777 None 45 Human Binding pIC50 = 5.2 5.2 -50 14
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 3777 None 45 Human Binding pIC50 = 5.2 5.2 -50 14
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
5401.0 3777 None 45 Human Binding pIC50 = 5.2 5.2 -50 14
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 3777 None 45 Human Binding pIC50 = 5.2 5.2 -50 14
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 3777 None 45 Human Binding pIC50 = 5.2 5.2 -50 14
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 3777 None 45 Human Binding pIC50 = 5.2 5.2 -50 14
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
141 1427 None 18 Human Binding pIC50 = 5.2 5.2 -50 28
Displacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2c receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysisDisplacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2c receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
6089 1427 None 18 Human Binding pIC50 = 5.2 5.2 -50 28
Displacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2c receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysisDisplacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2c receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
CHEMBL12420 1427 None 18 Human Binding pIC50 = 5.2 5.2 -50 28
Displacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2c receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysisDisplacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2c receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
DB01488 1427 None 18 Human Binding pIC50 = 5.2 5.2 -50 28
Displacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2c receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysisDisplacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2c receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
1343 1889 None 43 Human Binding pIC50 = 5.2 5.2 -251 9
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 1889 None 43 Human Binding pIC50 = 5.2 5.2 -251 9
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
3519.0 1889 None 43 Human Binding pIC50 = 5.2 5.2 -251 9
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 1889 None 43 Human Binding pIC50 = 5.2 5.2 -251 9
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 1889 None 43 Human Binding pIC50 = 5.2 5.2 -251 9
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 1889 None 43 Human Binding pIC50 = 5.2 5.2 -251 9
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 3163 None 48 Human Binding pIC50 = 6.2 6.2 -239 35
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 3163 None 48 Human Binding pIC50 = 6.2 6.2 -239 35
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
4893.0 3163 None 48 Human Binding pIC50 = 6.2 6.2 -239 35
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 3163 None 48 Human Binding pIC50 = 6.2 6.2 -239 35
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 3163 None 48 Human Binding pIC50 = 6.2 6.2 -239 35
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 3163 None 48 Human Binding pIC50 = 6.2 6.2 -239 35
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 3163 None 48 Human Binding pIC50 = 6.2 6.2 -239 35
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 940 None 51 Human Binding pIC50 = 6.2 6.2 -4 20
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
1547484.0 940 None 51 Human Binding pIC50 = 6.2 6.2 -4 20
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
654 940 None 51 Human Binding pIC50 = 6.2 6.2 -4 20
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 940 None 51 Human Binding pIC50 = 6.2 6.2 -4 20
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 940 None 51 Human Binding pIC50 = 6.2 6.2 -4 20
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 940 None 51 Human Binding pIC50 = 6.2 6.2 -4 20
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
42611190 3156 None 14 Human Binding pIC50 = 5.2 5.2 -2511 22
Adrenergic alpha2C Eurofins-Panlabs radioligand binding assayAdrenergic alpha2C Eurofins-Panlabs radioligand binding assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL4507292
5802 3156 None 14 Human Binding pIC50 = 5.2 5.2 -2511 22
Adrenergic alpha2C Eurofins-Panlabs radioligand binding assayAdrenergic alpha2C Eurofins-Panlabs radioligand binding assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL4507292
CHEMBL1800685 3156 None 14 Human Binding pIC50 = 5.2 5.2 -2511 22
Adrenergic alpha2C Eurofins-Panlabs radioligand binding assayAdrenergic alpha2C Eurofins-Panlabs radioligand binding assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL4507292
3598 187927 None 45 Human Binding pIC50 = 5.2 5.2 -1 7
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 187927 None 45 Human Binding pIC50 = 5.2 5.2 -1 7
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 958 None 57 Human Binding pIC50 = 8.1 8.1 -3 91
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
135398737.0 958 None 57 Human Binding pIC50 = 8.1 8.1 -3 91
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
38 958 None 57 Human Binding pIC50 = 8.1 8.1 -3 91
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
722 958 None 57 Human Binding pIC50 = 8.1 8.1 -3 91
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 958 None 57 Human Binding pIC50 = 8.1 8.1 -3 91
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 958 None 57 Human Binding pIC50 = 8.1 8.1 -3 91
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 15293 None 53 Human Binding pIC50 = 5.2 5.2 -18 3
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 15293 None 53 Human Binding pIC50 = 5.2 5.2 -18 3
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 3286 None 44 Human Binding pIC50 = 6.1 6.1 -4 21
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 3286 None 44 Human Binding pIC50 = 6.1 6.1 -4 21
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 3286 None 44 Human Binding pIC50 = 6.1 6.1 -4 21
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 3286 None 44 Human Binding pIC50 = 6.1 6.1 -4 21
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 3286 None 44 Human Binding pIC50 = 6.1 6.1 -4 21
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 179055 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 179055 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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
240 944 None 25 Human Binding pIC50 = 6.1 6.1 -5 25
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 944 None 25 Human Binding pIC50 = 6.1 6.1 -5 25
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 944 None 25 Human Binding pIC50 = 6.1 6.1 -5 25
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
660 944 None 25 Human Binding pIC50 = 6.1 6.1 -5 25
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 944 None 25 Human Binding pIC50 = 6.1 6.1 -5 25
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 944 None 25 Human Binding pIC50 = 6.1 6.1 -5 25
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 944 None 25 Human Binding pIC50 = 6.1 6.1 -5 25
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 56360 None 12 Human Binding pIC50 = 5.1 5.1 -1 6
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 56360 None 12 Human Binding pIC50 = 5.1 5.1 -1 6
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 203402 None 16 Human Binding pIC50 = 8.1 8.1 -7 21
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 203402 None 16 Human Binding pIC50 = 8.1 8.1 -7 21
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 203402 None 16 Human Binding pIC50 = 8.1 8.1 -7 21
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 3173 None 38 Human Binding pIC50 = 7.1 7.1 -4 32
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 3173 None 38 Human Binding pIC50 = 7.1 7.1 -4 32
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
4917.0 3173 None 38 Human Binding pIC50 = 7.1 7.1 -4 32
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 3173 None 38 Human Binding pIC50 = 7.1 7.1 -4 32
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 3173 None 38 Human Binding pIC50 = 7.1 7.1 -4 32
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 3173 None 38 Human Binding pIC50 = 7.1 7.1 -4 32
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 216972 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 107125 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 107125 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 190556 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 190556 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 217352 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 3331 None 72 Human Binding pIC50 = 8.0 8.0 -10 67
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 3331 None 72 Human Binding pIC50 = 8.0 8.0 -10 67
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
5073.0 3331 None 72 Human Binding pIC50 = 8.0 8.0 -10 67
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 3331 None 72 Human Binding pIC50 = 8.0 8.0 -10 67
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 3331 None 72 Human Binding pIC50 = 8.0 8.0 -10 67
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 3331 None 72 Human Binding pIC50 = 8.0 8.0 -10 67
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 803 None 59 Human Binding pIC50 = 7.1 7.1 -20 22
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
2585.0 803 None 59 Human Binding pIC50 = 7.1 7.1 -20 22
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
522 803 None 59 Human Binding pIC50 = 7.1 7.1 -20 22
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
551 803 None 59 Human Binding pIC50 = 7.1 7.1 -20 22
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 803 None 59 Human Binding pIC50 = 7.1 7.1 -20 22
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 803 None 59 Human Binding pIC50 = 7.1 7.1 -20 22
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
141 1427 None 18 Human Binding pIC50 = 5.0 5.0 -50 28
Displacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2c receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysisDisplacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2c receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
6089 1427 None 18 Human Binding pIC50 = 5.0 5.0 -50 28
Displacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2c receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysisDisplacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2c receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
CHEMBL12420 1427 None 18 Human Binding pIC50 = 5.0 5.0 -50 28
Displacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2c receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysisDisplacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2c receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
DB01488 1427 None 18 Human Binding pIC50 = 5.0 5.0 -50 28
Displacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2c receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysisDisplacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2c receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
26987 949 None 27 Human Binding pIC50 = 7.0 7.0 -107 21
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
26987.0 949 None 27 Human Binding pIC50 = 7.0 7.0 -107 21
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 949 None 27 Human Binding pIC50 = 7.0 7.0 -107 21
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
671 949 None 27 Human Binding pIC50 = 7.0 7.0 -107 21
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 949 None 27 Human Binding pIC50 = 7.0 7.0 -107 21
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 949 None 27 Human Binding pIC50 = 7.0 7.0 -107 21
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
46209194 167813 None 6 Human Binding pKd = 8.4 8.4 6 3
Binding affinity to alpha2C receptor (unknown origin)Binding affinity to alpha2C receptor (unknown origin)
ChEMBL 355 5 0 6 2.2 COCc1cccnc1N1CCN(C[C@H]2COc3ccccc3O2)CC1 10.1021/acs.jmedchem.2c01965
CHEMBL4297337 167813 None 6 Human Binding pKd = 8.4 8.4 6 3
Binding affinity to alpha2C receptor (unknown origin)Binding affinity to alpha2C receptor (unknown origin)
ChEMBL 355 5 0 6 2.2 COCc1cccnc1N1CCN(C[C@H]2COc3ccccc3O2)CC1 10.1021/acs.jmedchem.2c01965
CHEMBL4302506 167813 None 6 Human Binding pKd = 8.4 8.4 6 3
Binding affinity to alpha2C receptor (unknown origin)Binding affinity to alpha2C receptor (unknown origin)
ChEMBL 355 5 0 6 2.2 COCc1cccnc1N1CCN(C[C@H]2COc3ccccc3O2)CC1 10.1021/acs.jmedchem.2c01965
136019934 144618 None 0 Human Binding pKi = 10 10.0 7 3
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 144618 None 0 Human Binding pKi = 10 10.0 7 3
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 209406 None 0 Human Binding pKi = 10 10.0 5 7
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 209406 None 0 Human Binding pKi = 10 10.0 5 7
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 209406 None 0 Human Binding pKi = 10 10.0 5 7
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 209406 None 0 Human Binding pKi = 10 10.0 5 7
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 17212 None 0 Human Binding pKi = 9.9 9.9 -3 4
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 17212 None 0 Human Binding pKi = 9.9 9.9 -3 4
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 17159 None 0 Human Binding pKi = 9.8 9.8 -1 4
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 17159 None 0 Human Binding pKi = 9.8 9.8 -1 4
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 17212 None 0 Human Binding pKi = 9.8 9.8 -3 4
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 17212 None 0 Human Binding pKi = 9.8 9.8 -3 4
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 4320 None 0 Human Binding pKi = 9.7 9.7 1 2
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 4320 None 0 Human Binding pKi = 9.7 9.7 1 2
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 4437 None 0 Human Binding pKi = 9.7 9.7 5 2
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 4437 None 0 Human Binding pKi = 9.7 9.7 5 2
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 96673 None 0 Human Binding pKi = 9.7 9.7 5 2
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 96673 None 0 Human Binding pKi = 9.7 9.7 5 2
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 107788 None 0 Human Binding pKi = 9.7 9.7 1 2
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 107788 None 0 Human Binding pKi = 9.7 9.7 1 2
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 163467 None 0 Human Binding pKi = 9.7 9.7 2 4
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 163467 None 0 Human Binding pKi = 9.7 9.7 2 4
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 209406 None 0 Human Binding pKi = 9.7 9.7 5 7
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 209406 None 0 Human Binding pKi = 9.7 9.7 5 7
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 210691 None 0 Human Binding pKi = 9.7 9.7 8 2
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 210691 None 0 Human Binding pKi = 9.7 9.7 8 2
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 163467 None 0 Human Binding pKi = 9.7 9.7 2 4
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 163467 None 0 Human Binding pKi = 9.7 9.7 2 4
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 209739 None 0 Human Binding pKi = 9.7 9.7 3 3
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 209739 None 0 Human Binding pKi = 9.7 9.7 3 3
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 163467 None 0 Human Binding pKi = 9.7 9.7 2 4
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 163467 None 0 Human Binding pKi = 9.7 9.7 2 4
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 17212 None 0 Human Binding pKi = 9.6 9.6 -3 4
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 17212 None 0 Human Binding pKi = 9.6 9.6 -3 4
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 107497 None 2 Human Binding pKi = 9.6 9.6 5 7
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 107497 None 2 Human Binding pKi = 9.6 9.6 5 7
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 17205 None 0 Human Binding pKi = 9.5 9.5 -1 4
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 17205 None 0 Human Binding pKi = 9.5 9.5 -1 4
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 111645 None 0 Human Binding pKi = 9.5 9.5 4 2
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 111645 None 0 Human Binding pKi = 9.5 9.5 4 2
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 210677 None 0 Human Binding pKi = 9.5 9.5 9 2
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 210677 None 0 Human Binding pKi = 9.5 9.5 9 2
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 108138 None 0 Human Binding pKi = 9.4 9.4 1 2
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 108138 None 0 Human Binding pKi = 9.4 9.4 1 2
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 210885 None 0 Human Binding pKi = 9.4 9.4 2 2
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 210885 None 0 Human Binding pKi = 9.4 9.4 2 2
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 17160 None 0 Human Binding pKi = 9.4 9.4 -1 4
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 17160 None 0 Human Binding pKi = 9.4 9.4 -1 4
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 181760 None 0 Human Binding pKi = 9.3 9.3 13 3
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 181760 None 0 Human Binding pKi = 9.3 9.3 13 3
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 4127 None 36 Human Binding pKi = 9.3 9.3 -23 50
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 4127 None 36 Human Binding pKi = 9.3 9.3 -23 50
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 4127 None 36 Human Binding pKi = 9.3 9.3 -23 50
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
8969.0 4127 None 36 Human Binding pKi = 9.3 9.3 -23 50
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 4127 None 36 Human Binding pKi = 9.3 9.3 -23 50
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 4127 None 36 Human Binding pKi = 9.3 9.3 -23 50
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 4127 None 36 Human Binding pKi = 9.3 9.3 -23 50
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 4127 None 36 Human Binding pKi = 9.3 9.3 -23 50
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 4127 None 36 Human Binding pKi = 9.3 9.3 -23 50
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
8969.0 4127 None 36 Human Binding pKi = 9.3 9.3 -23 50
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 4127 None 36 Human Binding pKi = 9.3 9.3 -23 50
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 4127 None 36 Human Binding pKi = 9.3 9.3 -23 50
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 210893 None 0 Human Binding pKi = 9.3 9.3 3 2
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 210893 None 0 Human Binding pKi = 9.3 9.3 3 2
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 111631 None 0 Human Binding pKi = 9.3 9.3 2 5
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 111631 None 0 Human Binding pKi = 9.3 9.3 2 5
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 111631 None 0 Human Binding pKi = 9.3 9.3 2 5
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 111631 None 0 Human Binding pKi = 9.3 9.3 2 5
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 17258 None 0 Human Binding pKi = 9.3 9.3 -2 4
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 17258 None 0 Human Binding pKi = 9.3 9.3 -2 4
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 181650 None 0 Human Binding pKi = 9.2 9.2 8 3
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 181650 None 0 Human Binding pKi = 9.2 9.2 8 3
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 112255 None 0 Human Binding pKi = 9.2 9.2 3 2
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 112255 None 0 Human Binding pKi = 9.2 9.2 3 2
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 111586 None 0 Human Binding pKi = 9.2 9.2 2 3
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 111586 None 0 Human Binding pKi = 9.2 9.2 2 3
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 2325 None 21 Human Binding pKi = 9.2 9.2 -3 43
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 2325 None 21 Human Binding pKi = 9.2 9.2 -3 43
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
28864.0 2325 None 21 Human Binding pKi = 9.2 9.2 -3 43
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 2325 None 21 Human Binding pKi = 9.2 9.2 -3 43
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 2325 None 21 Human Binding pKi = 9.2 9.2 -3 43
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 2325 None 21 Human Binding pKi = 9.2 9.2 -3 43
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 71707 None 0 Human Binding pKi = 9.2 9.2 44 3
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 71707 None 0 Human Binding pKi = 9.2 9.2 44 3
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 107497 None 2 Human Binding pKi = 9.2 9.2 5 7
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 107497 None 2 Human Binding pKi = 9.2 9.2 5 7
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 107497 None 2 Human Binding pKi = 9.2 9.2 5 7
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 107497 None 2 Human Binding pKi = 9.2 9.2 5 7
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 163470 None 0 Human Binding pKi = 9.2 9.2 4 2
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 163470 None 0 Human Binding pKi = 9.2 9.2 4 2
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 210097 None 0 Human Binding pKi = 9.2 9.2 8 2
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 210097 None 0 Human Binding pKi = 9.2 9.2 8 2
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 3423 None 24 Human Binding pKi = 9.1 9.1 -2 4
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 3423 None 24 Human Binding pKi = 9.1 9.1 -2 4
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 3423 None 24 Human Binding pKi = 9.1 9.1 -2 4
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 3423 None 24 Human Binding pKi = 9.1 9.1 -2 4
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 4077 None 13 Human Binding pKi = 9.1 9.1 -3 14
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 4077 None 13 Human Binding pKi = 9.1 9.1 -3 14
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 4077 None 13 Human Binding pKi = 9.1 9.1 -3 14
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 189725 None 0 Human Binding pKi = 9.1 9.1 6 3
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 189725 None 0 Human Binding pKi = 9.1 9.1 6 3
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 189788 None 0 Human Binding pKi = 9.1 9.1 25 3
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 189788 None 0 Human Binding pKi = 9.1 9.1 25 3
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 149058 None 0 Human Binding pKi = 9.1 9.1 52 3
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 149058 None 0 Human Binding pKi = 9.1 9.1 52 3
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 4127 None 36 Human Binding pKi = 9.1 9.1 -23 50
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 4127 None 36 Human Binding pKi = 9.1 9.1 -23 50
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 4127 None 36 Human Binding pKi = 9.1 9.1 -23 50
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
8969.0 4127 None 36 Human Binding pKi = 9.1 9.1 -23 50
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 4127 None 36 Human Binding pKi = 9.1 9.1 -23 50
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 4127 None 36 Human Binding pKi = 9.1 9.1 -23 50
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 111718 None 0 Human Binding pKi = 9.1 9.1 11 2
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 111718 None 0 Human Binding pKi = 9.1 9.1 11 2
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 209696 None 0 Human Binding pKi = 9.1 9.1 2 5
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 209696 None 0 Human Binding pKi = 9.1 9.1 2 5
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 209696 None 0 Human Binding pKi = 9.1 9.1 2 5
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 209696 None 0 Human Binding pKi = 9.1 9.1 2 5
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 4127 None 36 Human Binding pKi = 9.1 9.1 -23 50
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 4127 None 36 Human Binding pKi = 9.1 9.1 -23 50
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 4127 None 36 Human Binding pKi = 9.1 9.1 -23 50
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
8969.0 4127 None 36 Human Binding pKi = 9.1 9.1 -23 50
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 4127 None 36 Human Binding pKi = 9.1 9.1 -23 50
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 4127 None 36 Human Binding pKi = 9.1 9.1 -23 50
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 193418 None 0 Human Binding pKi = 9.1 9.1 16 3
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 193418 None 0 Human Binding pKi = 9.1 9.1 16 3
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 4395 None 0 Human Binding pKi = 9.1 9.1 5 2
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 4395 None 0 Human Binding pKi = 9.1 9.1 5 2
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 144618 None 0 Human Binding pKi = 9.0 9.0 7 3
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 144618 None 0 Human Binding pKi = 9.0 9.0 7 3
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 2981 None 32 Human Binding pKi = 9 9.0 -60 32
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 2981 None 32 Human Binding pKi = 9 9.0 -60 32
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 2981 None 32 Human Binding pKi = 9 9.0 -60 32
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
4636.0 2981 None 32 Human Binding pKi = 9 9.0 -60 32
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 2981 None 32 Human Binding pKi = 9 9.0 -60 32
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 2981 None 32 Human Binding pKi = 9 9.0 -60 32
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 3292 None 26 Human Binding pKi = 9 9.0 3 18
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 3292 None 26 Human Binding pKi = 9 9.0 3 18
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 3292 None 26 Human Binding pKi = 9 9.0 3 18
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 3292 None 26 Human Binding pKi = 9 9.0 3 18
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 132807 None 0 Human Binding pKi = 9.0 9.0 - 1
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 132807 None 0 Human Binding pKi = 9.0 9.0 - 1
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 958 None 57 Human Binding pKi = 8.9 8.9 -3 91
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
135398737.0 958 None 57 Human Binding pKi = 8.9 8.9 -3 91
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
38 958 None 57 Human Binding pKi = 8.9 8.9 -3 91
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
722 958 None 57 Human Binding pKi = 8.9 8.9 -3 91
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 958 None 57 Human Binding pKi = 8.9 8.9 -3 91
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 958 None 57 Human Binding pKi = 8.9 8.9 -3 91
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 17165 None 0 Human Binding pKi = 8.9 8.9 -1 4
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 17165 None 0 Human Binding pKi = 8.9 8.9 -1 4
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 203402 None 16 Human Binding pKi = 8.9 8.9 -7 21
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 203402 None 16 Human Binding pKi = 8.9 8.9 -7 21
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 203402 None 16 Human Binding pKi = 8.9 8.9 -7 21
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 17259 None 0 Human Binding pKi = 8.9 8.9 -2 4
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 17259 None 0 Human Binding pKi = 8.9 8.9 -2 4
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 3331 None 72 Human Binding pKi = 8.9 8.9 -10 67
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 3331 None 72 Human Binding pKi = 8.9 8.9 -10 67
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
5073.0 3331 None 72 Human Binding pKi = 8.9 8.9 -10 67
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 3331 None 72 Human Binding pKi = 8.9 8.9 -10 67
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 3331 None 72 Human Binding pKi = 8.9 8.9 -10 67
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 3331 None 72 Human Binding pKi = 8.9 8.9 -10 67
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 120545 None 0 Rat Binding pKi = 8.9 8.9 - 1
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 120545 None 0 Rat Binding pKi = 8.9 8.9 - 1
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 120545 None 0 Rat Binding pKi = 8.9 8.9 - 1
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 209406 None 0 Human Binding pKi = 8.9 8.9 5 7
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 209406 None 0 Human Binding pKi = 8.9 8.9 5 7
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 17150 None 0 Human Binding pKi = 8.8 8.8 -1 4
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 17150 None 0 Human Binding pKi = 8.8 8.8 -1 4
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 1420 None 13 Human Binding pKi = 8.8 8.8 -16 30
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
10531.0 1420 None 13 Human Binding pKi = 8.8 8.8 -16 30
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 1420 None 13 Human Binding pKi = 8.8 8.8 -16 30
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 1420 None 13 Human Binding pKi = 8.8 8.8 -16 30
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 1420 None 13 Human Binding pKi = 8.8 8.8 -16 30
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 1420 None 13 Human Binding pKi = 8.8 8.8 -16 30
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 17248 None 0 Human Binding pKi = 8.8 8.8 2 4
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 17248 None 0 Human Binding pKi = 8.8 8.8 2 4
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 209371 None 0 Human Binding pKi = 8.8 8.8 -1 3
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 209371 None 0 Human Binding pKi = 8.8 8.8 -1 3
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 1582 None 6 Human Binding pKi = 8.7 8.7 -19 27
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 1582 None 6 Human Binding pKi = 8.7 8.7 -19 27
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 1582 None 6 Human Binding pKi = 8.7 8.7 -19 27
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
8223.0 1582 None 6 Human Binding pKi = 8.7 8.7 -19 27
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 1582 None 6 Human Binding pKi = 8.7 8.7 -19 27
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 1582 None 6 Human Binding pKi = 8.7 8.7 -19 27
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 187201 None 0 Human Binding pKi = 8.7 8.7 5 3
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 187201 None 0 Human Binding pKi = 8.7 8.7 5 3
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 4127 None 36 Human Binding pKi = 8.7 8.7 -23 50
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 4127 None 36 Human Binding pKi = 8.7 8.7 -23 50
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 4127 None 36 Human Binding pKi = 8.7 8.7 -23 50
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
8969.0 4127 None 36 Human Binding pKi = 8.7 8.7 -23 50
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 4127 None 36 Human Binding pKi = 8.7 8.7 -23 50
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 4127 None 36 Human Binding pKi = 8.7 8.7 -23 50
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 112182 None 0 Human Binding pKi = 8.7 8.7 -3 12
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 112182 None 0 Human Binding pKi = 8.7 8.7 -3 12
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 209245 None 0 Human Binding pKi = 8.7 8.7 -3 3
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 209245 None 0 Human Binding pKi = 8.7 8.7 -3 3
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 209275 None 0 Human Binding pKi = 8.7 8.7 13 3
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 209275 None 0 Human Binding pKi = 8.7 8.7 13 3
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 17221 None 0 Human Binding pKi = 8.7 8.7 -3 4
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 17221 None 0 Human Binding pKi = 8.7 8.7 -3 4
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 3331 None 72 Human Binding pKi = 8 8.0 -10 67
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 3331 None 72 Human Binding pKi = 8 8.0 -10 67
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
5073.0 3331 None 72 Human Binding pKi = 8 8.0 -10 67
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 3331 None 72 Human Binding pKi = 8 8.0 -10 67
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 3331 None 72 Human Binding pKi = 8 8.0 -10 67
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 3331 None 72 Human Binding pKi = 8 8.0 -10 67
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 107497 None 2 Human Binding pKi = 8 8.0 5 7
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 107497 None 2 Human Binding pKi = 8 8.0 5 7
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 4403 None 0 Human Binding pKi = 8 8.0 6 2
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 4403 None 0 Human Binding pKi = 8 8.0 6 2
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 163467 None 0 Human Binding pKi = 8 8.0 2 4
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 163467 None 0 Human Binding pKi = 8 8.0 2 4
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 17247 None 0 Human Binding pKi = 8.0 8.0 -3 4
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 17247 None 0 Human Binding pKi = 8.0 8.0 -3 4
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 1163 None 35 Human Binding pKi = 8.0 8.0 -2 8
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 1163 None 35 Human Binding pKi = 8.0 8.0 -2 8
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 1163 None 35 Human Binding pKi = 8.0 8.0 -2 8
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 1163 None 35 Human Binding pKi = 8.0 8.0 -2 8
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 1163 None 35 Human Binding pKi = 8.0 8.0 -2 8
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 1163 None 35 Human Binding pKi = 8.0 8.0 -2 8
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 179391 None 0 Human Binding pKi = 8.0 8.0 -7 3
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 179391 None 0 Human Binding pKi = 8.0 8.0 -7 3
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 None 70 Human Binding pKi = 7 7.0 -23 51
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 None 70 Human Binding pKi = 7 7.0 -23 51
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 None 70 Human Binding pKi = 7 7.0 -23 51
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
60795.0 470 None 70 Human Binding pKi = 7 7.0 -23 51
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 None 70 Human Binding pKi = 7 7.0 -23 51
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 None 70 Human Binding pKi = 7 7.0 -23 51
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 958 None 57 Human Binding pKi = 7 7.0 -3 91
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
135398737.0 958 None 57 Human Binding pKi = 7 7.0 -3 91
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
38 958 None 57 Human Binding pKi = 7 7.0 -3 91
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
722 958 None 57 Human Binding pKi = 7 7.0 -3 91
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 958 None 57 Human Binding pKi = 7 7.0 -3 91
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 958 None 57 Human Binding pKi = 7 7.0 -3 91
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 2914 None 65 Human Binding pKi = 7 7.0 -30 65
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
135398745.0 2914 None 65 Human Binding pKi = 7 7.0 -30 65
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 2914 None 65 Human Binding pKi = 7 7.0 -30 65
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 2914 None 65 Human Binding pKi = 7 7.0 -30 65
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 2914 None 65 Human Binding pKi = 7 7.0 -30 65
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 3256 None 51 Human Binding pKi = 7 7.0 -10 62
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 3256 None 51 Human Binding pKi = 7 7.0 -10 62
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 3256 None 51 Human Binding pKi = 7 7.0 -10 62
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
5002.0 3256 None 51 Human Binding pKi = 7 7.0 -10 62
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 3256 None 51 Human Binding pKi = 7 7.0 -10 62
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 3256 None 51 Human Binding pKi = 7 7.0 -10 62
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 169284 None 0 Human Binding pKi = 7 7.0 10 3
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 169284 None 0 Human Binding pKi = 7 7.0 10 3
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 101819 None 5 Human Binding pKi = 7 7.0 -12 6
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 101819 None 5 Human Binding pKi = 7 7.0 -12 6
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 101819 None 5 Human Binding pKi = 7 7.0 -12 6
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 169284 None 0 Human Binding pKi = 7 7.0 10 3
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 169284 None 0 Human Binding pKi = 7 7.0 10 3
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
42611190 3156 None 14 Human Binding pKi = 6 6.0 -2511 22
Adrenergic alpha2C Eurofins-Panlabs radioligand binding assayAdrenergic alpha2C Eurofins-Panlabs radioligand binding assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL4507292
5802 3156 None 14 Human Binding pKi = 6 6.0 -2511 22
Adrenergic alpha2C Eurofins-Panlabs radioligand binding assayAdrenergic alpha2C Eurofins-Panlabs radioligand binding assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL4507292
CHEMBL1800685 3156 None 14 Human Binding pKi = 6 6.0 -2511 22
Adrenergic alpha2C Eurofins-Panlabs radioligand binding assayAdrenergic alpha2C Eurofins-Panlabs radioligand binding assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL4507292
10793665 107008 None 0 Human Binding pKi = 6 6.0 -562 6
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 107008 None 0 Human Binding pKi = 6 6.0 -562 6
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 15293 None 53 Human Binding pKi = 6 6.0 -18 3
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 15293 None 53 Human Binding pKi = 6 6.0 -18 3
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 171207 None 0 Human Binding pKi = 6 6.0 -158 6
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 171207 None 0 Human Binding pKi = 6 6.0 -158 6
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 917 None 54 Human Binding pKi = 5 5.0 -6 11
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 917 None 54 Human Binding pKi = 5 5.0 -6 11
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
607 917 None 54 Human Binding pKi = 5 5.0 -6 11
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 917 None 54 Human Binding pKi = 5 5.0 -6 11
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 917 None 54 Human Binding pKi = 5 5.0 -6 11
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 158328 None 19 Human Binding pKi = 5 5.0 -1 7
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 158328 None 19 Human Binding pKi = 5 5.0 -1 7
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
72901200 119841 None 26 Human Binding pKi = 5 5.0 -6918 33
GPCRScan assay: inhibition of Alpha2CGPCRScan assay: inhibition of Alpha2C
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL4507309
CHEMBL3480577 119841 None 26 Human Binding pKi = 5 5.0 -6918 33
GPCRScan assay: inhibition of Alpha2CGPCRScan assay: inhibition of Alpha2C
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL4507309
CHEMBL4578164 216492 None 2 Human Binding pKi = 5 5.0 -478 6
GPCRScan assay: inhibition of Alpha2CGPCRScan assay: inhibition of Alpha2C
ChEMBL None None None CC(=O)c1c(NS(C)(=O)=O)c2cc(-c3ccc(Cl)cc3)c(-c3ccc(Cl)cc3Cl)nc2n(C)c1=O 10.6019/CHEMBL4507287
3598 187927 None 45 Human Binding pKi = 6.0 6.0 -1 7
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 187927 None 45 Human Binding pKi = 6.0 6.0 -1 7
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 209002 None 0 Human Binding pKi = 6.0 6.0 -63 6
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 209002 None 0 Human Binding pKi = 6.0 6.0 -63 6
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
60785 208351 None 35 Human Binding pKi = 6.0 6.0 -2454 19
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.6019/CHEMBL5442175
CHEMBL83894 208351 None 35 Human Binding pKi = 6.0 6.0 -2454 19
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.6019/CHEMBL5442175
132584404 143436 None 0 Human Binding pKi = 6.0 6.0 -2 5
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 143436 None 0 Human Binding pKi = 6.0 6.0 -2 5
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 121780 None 2 Human Binding pKi = 5.0 5.0 - 1
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 121780 None 2 Human Binding pKi = 5.0 5.0 - 1
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 3286 None 44 Human Binding pKi = 7.0 7.0 -4 21
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 3286 None 44 Human Binding pKi = 7.0 7.0 -4 21
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 3286 None 44 Human Binding pKi = 7.0 7.0 -4 21
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 3286 None 44 Human Binding pKi = 7.0 7.0 -4 21
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 3286 None 44 Human Binding pKi = 7.0 7.0 -4 21
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 121776 None 0 Human Binding pKi = 6.0 6.0 - 1
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 121776 None 0 Human Binding pKi = 6.0 6.0 - 1
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 166262 None 0 Human Binding pKi = 7.0 7.0 -269 13
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 166262 None 0 Human Binding pKi = 7.0 7.0 -269 13
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 82547 None 0 Human Binding pKi = 7.0 7.0 5 3
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 82547 None 0 Human Binding pKi = 7.0 7.0 5 3
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 100568 None 0 Human Binding pKi = 6.0 6.0 -575 7
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 100568 None 0 Human Binding pKi = 6.0 6.0 -575 7
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 137501 None 0 Human Binding pKi = 6.0 6.0 -34 19
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 137501 None 0 Human Binding pKi = 6.0 6.0 -34 19
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 192825 None 16 Human Binding pKi = 8.0 8.0 -6 3
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 192825 None 16 Human Binding pKi = 8.0 8.0 -6 3
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 148301 None 0 Human Binding pKi = 8.0 8.0 27 3
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 148301 None 0 Human Binding pKi = 8.0 8.0 27 3
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 121969 None 0 Human Binding pKi = 7.9 7.9 - 1
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 121969 None 0 Human Binding pKi = 7.9 7.9 - 1
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 82547 None 0 Human Binding pKi = 7.0 7.0 5 3
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 82547 None 0 Human Binding pKi = 7.0 7.0 5 3
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 16264 None 0 Human Binding pKi = 6.0 6.0 -5 7
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 16264 None 0 Human Binding pKi = 6.0 6.0 -5 7
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
171357206 193917 None 0 Human Binding pKi = 6.0 6.0 1 5
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
CHEMBL5274312 193917 None 0 Human Binding pKi = 6.0 6.0 1 5
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 4520 None 1 Human Binding pKi = 6.0 6.0 -11 3
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 4520 None 1 Human Binding pKi = 6.0 6.0 -11 3
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 18792 None 0 Human Binding pKi = 7.0 7.0 -1 3
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 18792 None 0 Human Binding pKi = 7.0 7.0 -1 3
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
240 944 None 25 Human Binding pKi = 7.0 7.0 -5 25
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 944 None 25 Human Binding pKi = 7.0 7.0 -5 25
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 944 None 25 Human Binding pKi = 7.0 7.0 -5 25
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
660 944 None 25 Human Binding pKi = 7.0 7.0 -5 25
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 944 None 25 Human Binding pKi = 7.0 7.0 -5 25
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 944 None 25 Human Binding pKi = 7.0 7.0 -5 25
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 944 None 25 Human Binding pKi = 7.0 7.0 -5 25
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 75518 None 9 Human Binding pKi = 6.0 6.0 -1 3
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 75518 None 9 Human Binding pKi = 6.0 6.0 -1 3
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 206991 None 1 Human Binding pKi = 6.9 6.9 -18 6
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 206991 None 1 Human Binding pKi = 6.9 6.9 -18 6
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 83835 None 0 Human Binding pKi = 5.9 5.9 1 12
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 83835 None 0 Human Binding pKi = 5.9 5.9 1 12
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 83835 None 0 Human Binding pKi = 5.9 5.9 1 12
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 83835 None 0 Human Binding pKi = 5.9 5.9 1 12
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 56360 None 12 Human Binding pKi = 5.9 5.9 -1 6
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 56360 None 12 Human Binding pKi = 5.9 5.9 -1 6
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 107098 None 0 Human Binding pKi = 5.9 5.9 -162 6
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 107098 None 0 Human Binding pKi = 5.9 5.9 -162 6
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 207193 None 0 Human Binding pKi = 4.9 4.9 1 5
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 207193 None 0 Human Binding pKi = 4.9 4.9 1 5
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
1028 291 None 40 Human Binding pKi = 5.9 5.9 -85 29
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.6019/CHEMBL5442175
139148732 291 None 40 Human Binding pKi = 5.9 5.9 -85 29
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.6019/CHEMBL5442175
479 291 None 40 Human Binding pKi = 5.9 5.9 -85 29
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.6019/CHEMBL5442175
5816 291 None 40 Human Binding pKi = 5.9 5.9 -85 29
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.6019/CHEMBL5442175
5816.0 291 None 40 Human Binding pKi = 5.9 5.9 -85 29
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.6019/CHEMBL5442175
CHEMBL679 291 None 40 Human Binding pKi = 5.9 5.9 -85 29
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.6019/CHEMBL5442175
DB00668 291 None 40 Human Binding pKi = 5.9 5.9 -85 29
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.6019/CHEMBL5442175
10220337 202907 None 29 Human Binding pKi = 5.9 5.9 - 1
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 202907 None 29 Human Binding pKi = 5.9 5.9 - 1
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 3173 None 38 Human Binding pKi = 7.9 7.9 -4 32
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 3173 None 38 Human Binding pKi = 7.9 7.9 -4 32
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
4917.0 3173 None 38 Human Binding pKi = 7.9 7.9 -4 32
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 3173 None 38 Human Binding pKi = 7.9 7.9 -4 32
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 3173 None 38 Human Binding pKi = 7.9 7.9 -4 32
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 3173 None 38 Human Binding pKi = 7.9 7.9 -4 32
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 207258 None 2 Human Binding pKi = 7.9 7.9 -5 4
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 207258 None 2 Human Binding pKi = 7.9 7.9 -5 4
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 100392 None 40 Human Binding pKi = 7.9 7.9 -1 5
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 100392 None 40 Human Binding pKi = 7.9 7.9 -1 5
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 70588 None 0 Human Binding pKi = 7.9 7.9 1 6
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 70588 None 0 Human Binding pKi = 7.9 7.9 1 6
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 187384 None 0 Human Binding pKi = 6.9 6.9 -12 3
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 187384 None 0 Human Binding pKi = 6.9 6.9 -12 3
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 115189 None 0 Human Binding pKi = 5.9 5.9 -18 3
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 115189 None 0 Human Binding pKi = 5.9 5.9 -18 3
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 176322 None 35 Human Binding pKi = 5.9 5.9 2 3
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 176322 None 35 Human Binding pKi = 5.9 5.9 2 3
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 101376 None 0 Human Binding pKi = 6.9 6.9 -4 3
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 101376 None 0 Human Binding pKi = 6.9 6.9 -4 3
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 184332 None 0 Human Binding pKi = 6.9 6.9 -3 3
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 184332 None 0 Human Binding pKi = 6.9 6.9 -3 3
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 84651 None 0 Human Binding pKi = 5.9 5.9 -7 3
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 84651 None 0 Human Binding pKi = 5.9 5.9 -7 3
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 18578 None 0 Human Binding pKi = 6.9 6.9 -2 3
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 18578 None 0 Human Binding pKi = 6.9 6.9 -2 3
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 18578 None 0 Human Binding pKi = 6.9 6.9 -2 3
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 18578 None 0 Human Binding pKi = 6.9 6.9 -2 3
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 18583 None 0 Human Binding pKi = 6.9 6.9 -2 3
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 18583 None 0 Human Binding pKi = 6.9 6.9 -2 3
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 112106 None 1 Human Binding pKi = 6.9 6.9 -32 12
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 112106 None 1 Human Binding pKi = 6.9 6.9 -32 12
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 187324 None 0 Human Binding pKi = 5.9 5.9 -3 3
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 187324 None 0 Human Binding pKi = 5.9 5.9 -3 3
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 84453 None 0 Human Binding pKi = 5.9 5.9 -1 3
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 84453 None 0 Human Binding pKi = 5.9 5.9 -1 3
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
662 3680 None 7 Human Binding pKi = 5.9 5.9 -1778 6
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 756 14 2 8 6.3 COc1ccc2c(c1)ccc(c2)S(=O)(=O)N[C@@H](c1ccc2c(c1)OCO2)CC(=O)N[C@@H](C(=O)N(C(C)C)C)Cc1ccc(cc1)CN1[C@H](C)CCC[C@@H]1C 10.6019/CHEMBL5442175
9853583 3680 None 7 Human Binding pKi = 5.9 5.9 -1778 6
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 756 14 2 8 6.3 COc1ccc2c(c1)ccc(c2)S(=O)(=O)N[C@@H](c1ccc2c(c1)OCO2)CC(=O)N[C@@H](C(=O)N(C(C)C)C)Cc1ccc(cc1)CN1[C@H](C)CCC[C@@H]1C 10.6019/CHEMBL5442175
CHEMBL2021721 3680 None 7 Human Binding pKi = 5.9 5.9 -1778 6
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 756 14 2 8 6.3 COc1ccc2c(c1)ccc(c2)S(=O)(=O)N[C@@H](c1ccc2c(c1)OCO2)CC(=O)N[C@@H](C(=O)N(C(C)C)C)Cc1ccc(cc1)CN1[C@H](C)CCC[C@@H]1C 10.6019/CHEMBL5442175
56852956 112106 None 1 Human Binding pKi = 6.9 6.9 -32 12
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 112106 None 1 Human Binding pKi = 6.9 6.9 -32 12
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 50335 None 0 Human Binding pKi = 6.9 6.9 -7 3
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 50335 None 0 Human Binding pKi = 6.9 6.9 -7 3
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 803 None 59 Human Binding pKi = 7.9 7.9 -20 22
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
2585.0 803 None 59 Human Binding pKi = 7.9 7.9 -20 22
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
522 803 None 59 Human Binding pKi = 7.9 7.9 -20 22
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
551 803 None 59 Human Binding pKi = 7.9 7.9 -20 22
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 803 None 59 Human Binding pKi = 7.9 7.9 -20 22
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 803 None 59 Human Binding pKi = 7.9 7.9 -20 22
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 209842 None 0 Human Binding pKi = 7.9 7.9 5 3
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 209842 None 0 Human Binding pKi = 7.9 7.9 5 3
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
136 3292 None 26 Human Binding pKi = 7.9 7.9 3 18
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
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 10.6019/CHEMBL5442175
223 3292 None 26 Human Binding pKi = 7.9 7.9 3 18
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
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 10.6019/CHEMBL5442175
643606 3292 None 26 Human Binding pKi = 7.9 7.9 3 18
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
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 10.6019/CHEMBL5442175
CHEMBL10347 3292 None 26 Human Binding pKi = 7.9 7.9 3 18
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
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 10.6019/CHEMBL5442175
213041 17140 None 24 Human Binding pKi = 7.9 7.9 -2 4
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 17140 None 24 Human Binding pKi = 7.9 7.9 -2 4
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 216454 None 39 Human Binding pKi = 6.9 6.9 -1 22
GPCRScan assay: inhibition of Alpha2CGPCRScan assay: inhibition of Alpha2C
ChEMBL None None None CNCc1ccccc1-c1csc([C@@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL4507273
CHEMBL4535474 216454 None 39 Human Binding pKi = 6.9 6.9 -1 22
GPCRScan assay: inhibition of Alpha2CGPCRScan assay: inhibition of Alpha2C
ChEMBL None None None CNCc1ccccc1-c1csc([C@@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL4507273
CHEMBL4535474 216454 None 39 Human Binding pKi = 6.9 6.9 -1 22
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 None 23 Human Binding pKi = 6.9 6.9 -380 12
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 None 23 Human Binding pKi = 6.9 6.9 -380 12
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 None 23 Human Binding pKi = 6.9 6.9 -380 12
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 141725 None 0 Human Binding pKi = 6.9 6.9 -2 3
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 141725 None 0 Human Binding pKi = 6.9 6.9 -2 3
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 141725 None 0 Human Binding pKi = 6.9 6.9 -2 3
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 141725 None 0 Human Binding pKi = 6.9 6.9 -2 3
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 83283 None 0 Human Binding pKi = 6.9 6.9 4 3
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 83283 None 0 Human Binding pKi = 6.9 6.9 4 3
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 83283 None 0 Human Binding pKi = 6.9 6.9 4 3
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 83283 None 0 Human Binding pKi = 6.9 6.9 4 3
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 174178 None 0 Human Binding pKi = 5.9 5.9 -7 3
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 174178 None 0 Human Binding pKi = 5.9 5.9 -7 3
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 172667 None 8 Human Binding pKi = 5.9 5.9 -724 6
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 172667 None 8 Human Binding pKi = 5.9 5.9 -724 6
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
CHEMBL5483012 172667 None 8 Human Binding pKi = 5.9 5.9 -724 6
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 82487 None 0 Human Binding pKi = 6.9 6.9 5 3
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 82487 None 0 Human Binding pKi = 6.9 6.9 5 3
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 82487 None 0 Human Binding pKi = 6.9 6.9 5 3
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 82487 None 0 Human Binding pKi = 6.9 6.9 5 3
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 83833 None 0 Human Binding pKi = 5.9 5.9 1 3
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 83833 None 0 Human Binding pKi = 5.9 5.9 1 3
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
4223 3992 None 57 Human Binding pKi = 5.9 5.9 -512 17
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442175
6918314 3992 None 57 Human Binding pKi = 5.9 5.9 -512 17
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442175
6918314.0 3992 None 57 Human Binding pKi = 5.9 5.9 -512 17
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442175
7427 3992 None 57 Human Binding pKi = 5.9 5.9 -512 17
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442175
CHEMBL439849 3992 None 57 Human Binding pKi = 5.9 5.9 -512 17
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442175
DB06684 3992 None 57 Human Binding pKi = 5.9 5.9 -512 17
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442175
42656257 121784 None 0 Human Binding pKi = 4.9 4.9 - 1
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 121784 None 0 Human Binding pKi = 4.9 4.9 - 1
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 949 None 27 Human Binding pKi = 7.9 7.9 -107 21
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
26987.0 949 None 27 Human Binding pKi = 7.9 7.9 -107 21
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 949 None 27 Human Binding pKi = 7.9 7.9 -107 21
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
671 949 None 27 Human Binding pKi = 7.9 7.9 -107 21
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 949 None 27 Human Binding pKi = 7.9 7.9 -107 21
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 949 None 27 Human Binding pKi = 7.9 7.9 -107 21
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 187555 None 36 Human Binding pKi = 5.9 5.9 -6 6
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 187555 None 36 Human Binding pKi = 5.9 5.9 -6 6
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 78253 None 0 Human Binding pKi = 6.8 6.8 -158 14
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 78253 None 0 Human Binding pKi = 6.8 6.8 -158 14
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 181680 None 0 Human Binding pKi = 6.8 6.8 3 10
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 181680 None 0 Human Binding pKi = 6.8 6.8 3 10
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 10876 None 0 Human Binding pKi = 6.8 6.8 -12 6
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 10876 None 0 Human Binding pKi = 6.8 6.8 -12 6
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 10876 None 0 Human Binding pKi = 6.8 6.8 -12 6
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 169470 None 0 Human Binding pKi = 5.8 5.8 -5 3
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 169470 None 0 Human Binding pKi = 5.8 5.8 -5 3
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 1462 None 65 Human Binding pKi = 6.8 6.8 -40 26
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
3151.0 1462 None 65 Human Binding pKi = 6.8 6.8 -40 26
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 1462 None 65 Human Binding pKi = 6.8 6.8 -40 26
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 1462 None 65 Human Binding pKi = 6.8 6.8 -40 26
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 1462 None 65 Human Binding pKi = 6.8 6.8 -40 26
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 1462 None 65 Human Binding pKi = 6.8 6.8 -40 26
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 92543 None 0 Human Binding pKi = 6.8 6.8 -10 4
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 92543 None 0 Human Binding pKi = 6.8 6.8 -10 4
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 200766 None 0 Human Binding pKi = 6.8 6.8 -2 3
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 200766 None 0 Human Binding pKi = 6.8 6.8 -2 3
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 168525 None 0 Human Binding pKi = 5.8 5.8 -7413 7
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 168525 None 0 Human Binding pKi = 5.8 5.8 -7413 7
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 90779 None 28 Human Binding pKi = 5.8 5.8 -22 18
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 90779 None 28 Human Binding pKi = 5.8 5.8 -22 18
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 155239 None 0 Human Binding pKi = 6.8 6.8 -2 12
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 155239 None 0 Human Binding pKi = 6.8 6.8 -2 12
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 171039 None 0 Human Binding pKi = 5.8 5.8 -85 4
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 171039 None 0 Human Binding pKi = 5.8 5.8 -85 4
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 83834 None 0 Human Binding pKi = 5.8 5.8 -2 8
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 83834 None 0 Human Binding pKi = 5.8 5.8 -2 8
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 91869 None 12 Human Binding pKi = 7.8 7.8 -100 44
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 91869 None 12 Human Binding pKi = 7.8 7.8 -100 44
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 96598 None 0 Human Binding pKi = 7.8 7.8 54 3
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 96598 None 0 Human Binding pKi = 7.8 7.8 54 3
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 96598 None 0 Human Binding pKi = 7.8 7.8 54 3
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 96598 None 0 Human Binding pKi = 7.8 7.8 54 3
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 181673 None 0 Human Binding pKi = 7.8 7.8 1 3
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 181673 None 0 Human Binding pKi = 7.8 7.8 1 3
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 56283 None 21 Human Binding pKi = 6.8 6.8 -1047 20
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
3158.0 56283 None 21 Human Binding pKi = 6.8 6.8 -1047 20
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 56283 None 21 Human Binding pKi = 6.8 6.8 -1047 20
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 56283 None 21 Human Binding pKi = 6.8 6.8 -1047 20
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 103831 None 0 Human Binding pKi = 5.8 5.8 -11 3
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 103831 None 0 Human Binding pKi = 5.8 5.8 -11 3
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 118801 None 0 Human Binding pKi = 5.8 5.8 -489 3
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 118801 None 0 Human Binding pKi = 5.8 5.8 -489 3
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 92584 None 0 Human Binding pKi = 5.8 5.8 -2 5
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 92584 None 0 Human Binding pKi = 5.8 5.8 -2 5
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 118567 None 76 Human Binding pKi = 5.8 5.8 - 1
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 118567 None 76 Human Binding pKi = 5.8 5.8 - 1
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 22663 None 66 Human Binding pKi = 4.8 4.8 - 1
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 22663 None 66 Human Binding pKi = 4.8 4.8 - 1
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 187102 None 0 Human Binding pKi = 6.8 6.8 3 13
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 187102 None 0 Human Binding pKi = 6.8 6.8 3 13
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 83731 None 5 Human Binding pKi = 5.8 5.8 -1 4
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 83731 None 5 Human Binding pKi = 5.8 5.8 -1 4
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 121781 None 1 Human Binding pKi = 4.8 4.8 - 1
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 121781 None 1 Human Binding pKi = 4.8 4.8 - 1
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 121782 None 0 Human Binding pKi = 4.8 4.8 - 1
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 121782 None 0 Human Binding pKi = 4.8 4.8 - 1
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
156419 938 None 48 Human Binding pKi = 5.8 5.8 -39 15
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.6019/CHEMBL5442175
156419.0 938 None 48 Human Binding pKi = 5.8 5.8 -39 15
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.6019/CHEMBL5442175
3308 938 None 48 Human Binding pKi = 5.8 5.8 -39 15
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.6019/CHEMBL5442175
647 938 None 48 Human Binding pKi = 5.8 5.8 -39 15
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.6019/CHEMBL5442175
CHEMBL1201284 938 None 48 Human Binding pKi = 5.8 5.8 -39 15
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.6019/CHEMBL5442175
DB01012 938 None 48 Human Binding pKi = 5.8 5.8 -39 15
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.6019/CHEMBL5442175
10651654 111546 None 0 Human Binding pKi = 6.8 6.8 -85 6
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 111546 None 0 Human Binding pKi = 6.8 6.8 -85 6
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
158797 3771 None 19 Human Binding pKi = 5.8 5.8 -37 14
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 10.6019/CHEMBL5442175
718 3771 None 19 Human Binding pKi = 5.8 5.8 -37 14
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 10.6019/CHEMBL5442175
CHEMBL292376 3771 None 19 Human Binding pKi = 5.8 5.8 -37 14
PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 10.6019/CHEMBL5442175
24906202 187323 None 0 Human Binding pKi = 5.8 5.8 -5 3
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 187323 None 0 Human Binding pKi = 5.8 5.8 -5 3
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 46258 None 54 Human Binding pKi = 4.8 4.8 -2 9
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 46258 None 54 Human Binding pKi = 4.8 4.8 -2 9
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 82166 None 0 Human Binding pKi = 7.8 7.8 77 3
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 82166 None 0 Human Binding pKi = 7.8 7.8 77 3
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 3096 None 36 Human Binding pKi = 7.8 7.8 -7 36
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 3096 None 36 Human Binding pKi = 7.8 7.8 -7 36
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 3096 None 36 Human Binding pKi = 7.8 7.8 -7 36
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 3096 None 36 Human Binding pKi = 7.8 7.8 -7 36
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
5775.0 3096 None 36 Human Binding pKi = 7.8 7.8 -7 36
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 3096 None 36 Human Binding pKi = 7.8 7.8 -7 36
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 3096 None 36 Human Binding pKi = 7.8 7.8 -7 36
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 82166 None 0 Human Binding pKi = 7.8 7.8 77 3
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 82166 None 0 Human Binding pKi = 7.8 7.8 77 3
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 42725 None 1 Human Binding pKi = 7.8 7.8 -1 12
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 42725 None 1 Human Binding pKi = 7.8 7.8 -1 12
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 156356 None 2 Human Binding pKi = 7.8 7.8 -35 15
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 156356 None 2 Human Binding pKi = 7.8 7.8 -35 15
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 85037 None 0 Human Binding pKi = 7.8 7.8 -1 3
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 85037 None 0 Human Binding pKi = 7.8 7.8 -1 3
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 85037 None 0 Human Binding pKi = 7.8 7.8 -1 3
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 85037 None 0 Human Binding pKi = 7.8 7.8 -1 3
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 955 None 40 Human Binding pKi = 6.8 6.8 -5 21
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
2803.0 955 None 40 Human Binding pKi = 6.8 6.8 -5 21
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
516 955 None 40 Human Binding pKi = 6.8 6.8 -5 21
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
704 955 None 40 Human Binding pKi = 6.8 6.8 -5 21
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 955 None 40 Human Binding pKi = 6.8 6.8 -5 21
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 955 None 40 Human Binding pKi = 6.8 6.8 -5 21
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 193095 None 0 Human Binding pKi = 6.8 6.8 -407 19
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 193095 None 0 Human Binding pKi = 6.8 6.8 -407 19
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 193095 None 0 Human Binding pKi = 6.8 6.8 -407 19
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 1888 None 32 Human Binding pKi = 6.8 6.8 -19 12
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 1888 None 32 Human Binding pKi = 6.8 6.8 -19 12
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
5353646.0 1888 None 32 Human Binding pKi = 6.8 6.8 -19 12
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 1888 None 32 Human Binding pKi = 6.8 6.8 -19 12
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 1888 None 32 Human Binding pKi = 6.8 6.8 -19 12
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
5702063.0 1888 None 32 Human Binding pKi = 6.8 6.8 -19 12
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 1888 None 32 Human Binding pKi = 6.8 6.8 -19 12
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 1888 None 32 Human Binding pKi = 6.8 6.8 -19 12
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 1888 None 32 Human Binding pKi = 6.8 6.8 -19 12
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 106598 None 26 Human Binding pKi = 6.8 6.8 -1 6
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 106598 None 26 Human Binding pKi = 6.8 6.8 -1 6
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 99024 None 0 Human Binding pKi = 5.8 5.8 -1479 10
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 99024 None 0 Human Binding pKi = 5.8 5.8 -1479 10
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 136646 None 0 Human Binding pKi = 5.8 5.8 -5 3
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 136646 None 0 Human Binding pKi = 5.8 5.8 -5 3
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 163165 None 0 Human Binding pKi = 5.8 5.8 -9 5
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 163165 None 0 Human Binding pKi = 5.8 5.8 -9 5
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 98979 None 0 Human Binding pKi = 6.8 6.8 -93 7
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 98979 None 0 Human Binding pKi = 6.8 6.8 -93 7
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 13687 None 0 Human Binding pKi = 6.8 6.8 -2 6
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 13687 None 0 Human Binding pKi = 6.8 6.8 -2 6
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 13687 None 0 Human Binding pKi = 6.8 6.8 -2 6
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 98979 None 0 Human Binding pKi = 6.8 6.8 -93 7
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 98979 None 0 Human Binding pKi = 6.8 6.8 -93 7
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 207275 None 2 Human Binding pKi = 4.8 4.8 -1 3
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 207275 None 2 Human Binding pKi = 4.8 4.8 -1 3
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 206638 None 0 Human Binding pKi = 6.8 6.8 -36 6
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 206638 None 0 Human Binding pKi = 6.8 6.8 -36 6
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 82508 None 3 Human Binding pKi = 5.8 5.8 -2 3
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 82508 None 3 Human Binding pKi = 5.8 5.8 -2 3
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 1988 None 24 Human Binding pKi = 7.8 7.8 -8 16
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 1988 None 24 Human Binding pKi = 7.8 7.8 -8 16
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
54459.0 1988 None 24 Human Binding pKi = 7.8 7.8 -8 16
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 1988 None 24 Human Binding pKi = 7.8 7.8 -8 16
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 1988 None 24 Human Binding pKi = 7.8 7.8 -8 16
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 137071 None 0 Human Binding pKi = 7.8 7.8 1 3
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 137071 None 0 Human Binding pKi = 7.8 7.8 1 3
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 1988 None 24 Human Binding pKi = 7.8 7.8 -8 16
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 1988 None 24 Human Binding pKi = 7.8 7.8 -8 16
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
54459.0 1988 None 24 Human Binding pKi = 7.8 7.8 -8 16
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 1988 None 24 Human Binding pKi = 7.8 7.8 -8 16
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 1988 None 24 Human Binding pKi = 7.8 7.8 -8 16
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 137071 None 0 Human Binding pKi = 7.8 7.8 1 3
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 137071 None 0 Human Binding pKi = 7.8 7.8 1 3
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 137071 None 0 Human Binding pKi = 7.8 7.8 1 3
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 137071 None 0 Human Binding pKi = 7.8 7.8 1 3
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(Oc1ccc