CID2745687 [Ligand Id: 9741] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1708510 (CID 27456)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GPR35/G-protein coupled receptor 35 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97]
GtoPdb In a competition radiologand binding assay membranes preapred from CHO cells recombinantly expressing human GPR35. - 7.37 pKi 42.2 nM Ki J Med Chem (2013) 56: 7084-99 [PMID:23888932]
ChEMBL Displacement of [3H]PSB-13253 from human recombinant GPR35 exprssed in CHO cells by liquid scintillation counting analysis B 7.37 pKi 42.2 nM Ki J. Med. Chem. (2013) 56: 7084-7099 [PMID:23888932]
GtoPdb Antagonism of the GPR35 response to 1 μM pamoic acid in a βarrestin2-GFP trafficking assay. - 7.89 pKi 12.8 nM Ki Mol Pharmacol (2010) 78: 560-8 [PMID:20826425]
GtoPdb Antagonism of zaprinast-mediated activation of GPR35 in a dynamic mass redistribution assay. - 4.98 pIC50 10400 nM IC50 J Med Chem (2013) 56: 7084-99 [PMID:23888932]
ChEMBL Antagonist activity at human GPR35 expressed in human HT29 cells after 1 hr by DMR assay B 4.98 pIC50 10400 nM IC50 J. Med. Chem. (2013) 56: 7084-7099 [PMID:23888932]
ChEMBL Antagonist activity at C-terminal beta-galactosidase tagged human recombinant GPR35 expressed in CHO cells after 90 mins by beta-arrestin recruitment assay B 6.24 pIC50 574 nM IC50 J. Med. Chem. (2013) 56: 7084-7099 [PMID:23888932]
ChEMBL Antagonist activity at human Gal4-VP16 fused GPR35 expressed in human U2OS cells assessed as beta arrestin translocation by reporter gene assay B 6.7 pIC50 200 nM IC50 J. Med. Chem. (2013) 56: 7084-7099 [PMID:23888932]
GtoPdb Antagonism of zaprinast-mediated activation of GPR35 in a β-arrestin assay. - 6.7 pIC50 200 nM IC50 J Med Chem (2013) 56: 7084-99 [PMID:23888932]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]