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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 |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]