Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
164611803 191762 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 191762 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 192481 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 192481 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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
1304207 192528 9 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 192528 9 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
164614422 191489 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 191489 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 192742 17 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 192742 17 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 192714 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 192714 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
164618042 192240 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 192240 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 192650 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 192650 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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
49960806 191664 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 191664 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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
1078173 28956 9 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 28956 9 None - 1 Human 5.5 pEC50 = 5.5 Functional
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
164625814 193331 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 193331 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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
164619743 192664 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 192664 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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
5157334 191673 8 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 191673 8 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 191493 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 191493 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 192137 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 192137 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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
164620267 192753 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 192753 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 192975 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 192975 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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
24638090 192909 1 None - 1 Human 5.1 pEC50 = 5.1 Functional
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 192909 1 None - 1 Human 5.1 pEC50 = 5.1 Functional
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
164611424 191979 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 191979 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 193032 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
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 193032 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
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 191673 8 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 191673 8 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 192982 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 192982 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI