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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] | ||||||||
ChEMBL | Competitive binding affinity to Nluc-fused human GPR35 expressed in CHO-K1 cells assessed as inhibition constant using furimazine as substrate incubated for 30 mins followed by substrate addition by in presence of 10-(4-(2-(4-(4-((2,8-dicarboxy-6-hydroxy-10-methylpyrido[3,2-g]quinolin-4-yl)oxy)butyl)-1H-1,2,3-triazol-1-yl)ethoxy)phenyl)-5,5-difluoro-2,7,9-trimethyl-5H-imidazo[1,2-c]pyrrolo[2,1-f][1,3,2]diazaborinin-6-ium-5-uide | B | 6.63 | pKi | 236 | nM | Ki | ACS Med Chem Lett (2023) 14: 411-416 [PMID:37077394] |
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] |
ChEMBL | Antagonist activity at GPR-35 (unknown origin) by beta-arrestin assay | B | 6.7 | pIC50 | 200 | nM | IC50 | ACS Med Chem Lett (2023) 14: 411-416 [PMID:37077394] |
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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]