Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
164611803 185089 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 460 6 2 4 4.5 COc1cc(Br)ccc1C(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1016/j.ejmech.2021.113777
CHEMBL4854273 185089 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 460 6 2 4 4.5 COc1cc(Br)ccc1C(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1016/j.ejmech.2021.113777
164624083 185808 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 464 5 2 3 5.2 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Cl)cc1Br 10.1016/j.ejmech.2021.113777
CHEMBL4865504 185808 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 464 5 2 3 5.2 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Cl)cc1Br 10.1016/j.ejmech.2021.113777
172445159 195432 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 508 5 2 3 5.3 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Br)cc1Br 10.1021/acs.jmedchem.3c02030
CHEMBL5403541 195432 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 508 5 2 3 5.3 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Br)cc1Br 10.1021/acs.jmedchem.3c02030
1304207 185855 None 6 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 434 5 2 3 5.4 Cc1ccccc1NS(=O)(=O)c1ccc(NC(=O)c2ccc(Cl)cc2Cl)cc1 10.1016/j.ejmech.2021.113777
CHEMBL4866235 185855 None 6 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 434 5 2 3 5.4 Cc1ccccc1NS(=O)(=O)c1ccc(NC(=O)c2ccc(Cl)cc2Cl)cc1 10.1016/j.ejmech.2021.113777
172470579 197073 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 458 5 2 3 5.1 Cc1cc(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)c(C)cc1Br 10.1021/acs.jmedchem.3c02030
CHEMBL5438097 197073 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 458 5 2 3 5.1 Cc1cc(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)c(C)cc1Br 10.1021/acs.jmedchem.3c02030
169494250 197077 None 4 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 450 6 2 4 4.8 COc1cc(C(F)(F)F)ccc1C(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1021/acs.jmedchem.3c02030
CHEMBL5438150 197077 None 4 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 450 6 2 4 4.8 COc1cc(C(F)(F)F)ccc1C(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1021/acs.jmedchem.3c02030
164614422 184816 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 454 5 2 3 5.7 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)cc1)c1ccc(Cl)cc1Cl 10.1016/j.ejmech.2021.113777
CHEMBL4850296 184816 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 454 5 2 3 5.7 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)cc1)c1ccc(Cl)cc1Cl 10.1016/j.ejmech.2021.113777
1177181 186069 None 11 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR27 expressed in HEK293 cells assessed as induction of beta-arrestin recruitment pretreated with substrate for 45 mins followed by compound addition and measured for 40 mins by NanoLuc luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells assessed as induction of beta-arrestin recruitment pretreated with substrate for 45 mins followed by compound addition and measured for 40 mins by NanoLuc luciferase complementation assay
ChEMBL 427 5 2 5 4.5 O=C(Nc1ccc(S(=O)(=O)Nc2nccs2)cc1)c1ccc(Cl)cc1Cl 10.1016/j.ejmech.2021.113777
CHEMBL4869637 186069 None 11 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR27 expressed in HEK293 cells assessed as induction of beta-arrestin recruitment pretreated with substrate for 45 mins followed by compound addition and measured for 40 mins by NanoLuc luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells assessed as induction of beta-arrestin recruitment pretreated with substrate for 45 mins followed by compound addition and measured for 40 mins by NanoLuc luciferase complementation assay
ChEMBL 427 5 2 5 4.5 O=C(Nc1ccc(S(=O)(=O)Nc2nccs2)cc1)c1ccc(Cl)cc1Cl 10.1016/j.ejmech.2021.113777
164620259 186041 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 422 5 2 3 4.7 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1cc(F)c(Cl)cc1F 10.1016/j.ejmech.2021.113777
CHEMBL4869253 186041 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 422 5 2 3 4.7 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1cc(F)c(Cl)cc1F 10.1016/j.ejmech.2021.113777
172450962 195712 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 416 6 2 4 4.4 COc1cc(Cl)ccc1C(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1021/acs.jmedchem.3c02030
CHEMBL5409423 195712 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 416 6 2 4 4.4 COc1cc(Cl)ccc1C(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1021/acs.jmedchem.3c02030
172465151 196792 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 462 5 2 3 5.0 Cc1cc(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)c(F)cc1Br 10.1021/acs.jmedchem.3c02030
CHEMBL5432356 196792 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 462 5 2 3 5.0 Cc1cc(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)c(F)cc1Br 10.1021/acs.jmedchem.3c02030
164618042 185567 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 395 5 2 4 3.8 N#Cc1ccc(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)c(F)c1 10.1016/j.ejmech.2021.113777
CHEMBL4861825 185567 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 395 5 2 4 3.8 N#Cc1ccc(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)c(F)c1 10.1016/j.ejmech.2021.113777
164619737 185977 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 405 5 2 4 3.9 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Cl)nc1F 10.1016/j.ejmech.2021.113777
CHEMBL4868057 185977 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 405 5 2 4 3.9 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Cl)nc1F 10.1016/j.ejmech.2021.113777
172465450 196620 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 498 5 2 3 5.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(C(F)(F)F)cc1Br 10.1021/acs.jmedchem.3c02030
CHEMBL5428000 196620 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 498 5 2 3 5.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(C(F)(F)F)cc1Br 10.1021/acs.jmedchem.3c02030
49960806 184991 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 434 5 1 3 5.1 CN(c1ccccc1)S(=O)(=O)c1ccc(NC(=O)c2ccc(Cl)cc2Cl)cc1 10.1016/j.ejmech.2021.113777
CHEMBL4852817 184991 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 434 5 1 3 5.1 CN(c1ccccc1)S(=O)(=O)c1ccc(NC(=O)c2ccc(Cl)cc2Cl)cc1 10.1016/j.ejmech.2021.113777
172451996 195645 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 434 5 2 3 5.4 Cc1cc(Cl)c(Cl)cc1C(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1021/acs.jmedchem.3c02030
CHEMBL5407924 195645 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 434 5 2 3 5.4 Cc1cc(Cl)c(Cl)cc1C(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1021/acs.jmedchem.3c02030
172468883 197098 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 414 5 2 3 5.0 Cc1cc(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)c(C)cc1Cl 10.1021/acs.jmedchem.3c02030
CHEMBL5438642 197098 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 414 5 2 3 5.0 Cc1cc(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)c(C)cc1Cl 10.1021/acs.jmedchem.3c02030
172445289 195016 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 460 6 2 4 4.5 COc1ccc(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)c(Br)c1 10.1021/acs.jmedchem.3c02030
CHEMBL5395036 195016 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 460 6 2 4 4.5 COc1ccc(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)c(Br)c1 10.1021/acs.jmedchem.3c02030
1078173 22191 None 5 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 421 5 2 4 4.4 O=C(Nc1ccc(S(=O)(=O)Nc2ccccn2)cc1)c1ccc(Cl)cc1Cl 10.1016/j.ejmech.2021.113777
CHEMBL1322660 22191 None 5 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 421 5 2 4 4.4 O=C(Nc1ccc(S(=O)(=O)Nc2ccccn2)cc1)c1ccc(Cl)cc1Cl 10.1016/j.ejmech.2021.113777
172471781 197166 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 434 5 2 3 5.4 Cc1cc(Cl)c(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)cc1Cl 10.1021/acs.jmedchem.3c02030
CHEMBL5440210 197166 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 434 5 2 3 5.4 Cc1cc(Cl)c(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)cc1Cl 10.1021/acs.jmedchem.3c02030
164625814 186658 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 438 5 2 3 4.9 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(C(F)(F)F)cc1F 10.1016/j.ejmech.2021.113777
CHEMBL4878026 186658 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 438 5 2 3 4.9 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(C(F)(F)F)cc1F 10.1016/j.ejmech.2021.113777
172457671 196186 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 434 5 2 3 5.4 Cc1cc(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)c(Cl)cc1Cl 10.1021/acs.jmedchem.3c02030
CHEMBL5418323 196186 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 434 5 2 3 5.4 Cc1cc(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)c(Cl)cc1Cl 10.1021/acs.jmedchem.3c02030
172470475 197128 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 438 5 2 3 5.2 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1cc(F)c(Cl)cc1Cl 10.1021/acs.jmedchem.3c02030
CHEMBL5439395 197128 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 438 5 2 3 5.2 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1cc(F)c(Cl)cc1Cl 10.1021/acs.jmedchem.3c02030
164619743 185991 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 404 5 2 3 4.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Cl)cc1F 10.1016/j.ejmech.2021.113777
CHEMBL4868300 185991 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 404 5 2 3 4.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Cl)cc1F 10.1016/j.ejmech.2021.113777
172461003 196522 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 466 5 2 3 4.8 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1cc(F)c(Br)cc1F 10.1021/acs.jmedchem.3c02030
CHEMBL5425829 196522 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 466 5 2 3 4.8 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1cc(F)c(Br)cc1F 10.1021/acs.jmedchem.3c02030
172440993 195167 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 388 5 2 3 4.0 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(F)cc1F 10.1021/acs.jmedchem.3c02030
CHEMBL5397942 195167 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 388 5 2 3 4.0 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(F)cc1F 10.1021/acs.jmedchem.3c02030
5157334 185000 None 6 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 420 5 2 3 5.0 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Cl)cc1Cl 10.1016/j.ejmech.2021.113777
CHEMBL4852965 185000 None 6 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 420 5 2 3 5.0 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Cl)cc1Cl 10.1016/j.ejmech.2021.113777
164615573 184820 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 448 5 2 3 4.6 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Br)cc1F 10.1016/j.ejmech.2021.113777
CHEMBL4850346 184820 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 448 5 2 3 4.6 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Br)cc1F 10.1016/j.ejmech.2021.113777
164618091 185464 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 496 5 2 3 4.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(I)cc1F 10.1016/j.ejmech.2021.113777
CHEMBL4860248 185464 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 496 5 2 3 4.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(I)cc1F 10.1016/j.ejmech.2021.113777
172440008 195299 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 462 5 2 3 5.0 Cc1cc(Br)c(F)cc1C(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1021/acs.jmedchem.3c02030
CHEMBL5400267 195299 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 462 5 2 3 5.0 Cc1cc(Br)c(F)cc1C(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1021/acs.jmedchem.3c02030
164620267 186080 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 454 5 2 3 5.7 O=C(Nc1ccc(S(=O)(=O)Nc2cccc(Cl)c2)cc1)c1ccc(Cl)cc1Cl 10.1016/j.ejmech.2021.113777
CHEMBL4869721 186080 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 454 5 2 3 5.7 O=C(Nc1ccc(S(=O)(=O)Nc2cccc(Cl)c2)cc1)c1ccc(Cl)cc1Cl 10.1016/j.ejmech.2021.113777
164624382 186302 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 421 5 2 4 4.4 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ncc(Cl)cc1Cl 10.1016/j.ejmech.2021.113777
CHEMBL4872926 186302 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 421 5 2 4 4.4 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ncc(Cl)cc1Cl 10.1016/j.ejmech.2021.113777
172447923 195846 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 454 5 2 3 5.7 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1cc(Cl)c(Cl)cc1Cl 10.1021/acs.jmedchem.3c02030
CHEMBL5411849 195846 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 454 5 2 3 5.7 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1cc(Cl)c(Cl)cc1Cl 10.1021/acs.jmedchem.3c02030
172467337 196876 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 454 5 2 3 5.7 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Cl)c(Cl)c1Cl 10.1021/acs.jmedchem.3c02030
CHEMBL5433874 196876 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 454 5 2 3 5.7 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Cl)c(Cl)c1Cl 10.1021/acs.jmedchem.3c02030
5157334 185000 None 6 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 420 5 2 3 5.0 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Cl)cc1Cl 10.1021/acs.jmedchem.3c02030
CHEMBL4852965 185000 None 6 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 420 5 2 3 5.0 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Cl)cc1Cl 10.1021/acs.jmedchem.3c02030
172439972 195242 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 454 5 2 3 5.4 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(C(F)(F)F)cc1Cl 10.1021/acs.jmedchem.3c02030
CHEMBL5399326 195242 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 454 5 2 3 5.4 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(C(F)(F)F)cc1Cl 10.1021/acs.jmedchem.3c02030
92380061 196852 None 1 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 380 5 2 3 4.4 Cc1ccc(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)c(C)c1 10.1021/acs.jmedchem.3c02030
CHEMBL5433355 196852 None 1 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 380 5 2 3 4.4 Cc1ccc(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)c(C)c1 10.1021/acs.jmedchem.3c02030
24638090 186236 None 1 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 420 5 2 5 3.8 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1cc2ccccc2oc1=O 10.1016/j.ejmech.2021.113777
CHEMBL4871933 186236 None 1 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 420 5 2 5 3.8 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1cc2ccccc2oc1=O 10.1016/j.ejmech.2021.113777
172451198 195978 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 418 5 2 3 4.8 Cc1cc(Cl)c(F)cc1C(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1021/acs.jmedchem.3c02030
CHEMBL5414526 195978 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 418 5 2 3 4.8 Cc1cc(Cl)c(F)cc1C(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1021/acs.jmedchem.3c02030
164611424 185306 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 444 5 2 3 4.8 Cc1cc(Br)ccc1C(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1016/j.ejmech.2021.113777
CHEMBL4857582 185306 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 444 5 2 3 4.8 Cc1cc(Br)ccc1C(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1016/j.ejmech.2021.113777
164621231 186359 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 402 5 2 3 4.9 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2021.113777
CHEMBL4873758 186359 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 402 5 2 3 4.9 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2021.113777
5157334 185000 None 6 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR27 expressed in HEK293 cells assessed as induction of beta-arrestin recruitment pretreated with substrate for 45 mins followed by compound addition and measured for 40 mins by NanoLuc luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells assessed as induction of beta-arrestin recruitment pretreated with substrate for 45 mins followed by compound addition and measured for 40 mins by NanoLuc luciferase complementation assay
ChEMBL 420 5 2 3 5.0 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Cl)cc1Cl 10.1016/j.ejmech.2021.113777
CHEMBL4852965 185000 None 6 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR27 expressed in HEK293 cells assessed as induction of beta-arrestin recruitment pretreated with substrate for 45 mins followed by compound addition and measured for 40 mins by NanoLuc luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells assessed as induction of beta-arrestin recruitment pretreated with substrate for 45 mins followed by compound addition and measured for 40 mins by NanoLuc luciferase complementation assay
ChEMBL 420 5 2 3 5.0 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccc(Cl)cc1Cl 10.1016/j.ejmech.2021.113777
164624775 186309 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 400 5 2 3 4.7 Cc1cc(Cl)ccc1C(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1016/j.ejmech.2021.113777
CHEMBL4873007 186309 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assayAgonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay
ChEMBL 400 5 2 3 4.7 Cc1cc(Cl)ccc1C(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1016/j.ejmech.2021.113777
172459019 196460 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 436 5 2 3 5.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1cc2ccccc2cc1Cl 10.1021/acs.jmedchem.3c02030
CHEMBL5424423 196460 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 436 5 2 3 5.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1cc2ccccc2cc1Cl 10.1021/acs.jmedchem.3c02030
172455725 196137 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 411 5 2 4 4.3 N#Cc1ccc(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)c(Cl)c1 10.1021/acs.jmedchem.3c02030
CHEMBL5417483 196137 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 411 5 2 4 4.3 N#Cc1ccc(C(=O)Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)c(Cl)c1 10.1021/acs.jmedchem.3c02030


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

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

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