pamoic acid [Ligand Id: 2920] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL177880 (Pamoic Acid)
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
DNA polymerase beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2392] [GtoPdb: 3231] [UniProtKB: P06746]
ChEMBL Inhibition of DNA polymerase beta (unknown origin) B 5.05 pIC50 9000 nM IC50 J Med Chem (2013) 56: 5182-5197 [PMID:23713606]
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 7.64 pKi 23 nM Ki ACS Med Chem Lett (2023) 14: 411-416 [PMID:37077394]
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 20 nM 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 7.83 pKi 14.9 nM Ki ACS Med Chem Lett (2023) 14: 411-416 [PMID:37077394]
ChEMBL Displacement of [3H]PSB-13253 from human recombinant GPR35 exprssed in CHO cells by liquid scintillation counting analysis B 7.94 pKi 11.5 nM Ki J Med Chem (2013) 56: 7084-7099 [PMID:23888932]
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 50 nM 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 7.99 pKi 10.3 nM Ki ACS Med Chem Lett (2023) 14: 411-416 [PMID:37077394]
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 100 nM 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 8.02 pKi 9.6 nM Ki ACS Med Chem Lett (2023) 14: 411-416 [PMID:37077394]
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 40 nM 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 8.05 pKi 8.9 nM Ki ACS Med Chem Lett (2023) 14: 411-416 [PMID:37077394]
ChEMBL Agonist activity at C-terminal beta-galactosidase tagged human recombinant GPR35 expressed in CHO cells after 90 mins by beta-arrestin recruitment assay B 5.92 pEC50 1200 nM EC50 J Med Chem (2013) 56: 7084-7099 [PMID:23888932]
ChEMBL Agonist activity at GPR-35 (unknown origin) by beta-arrestin assay B 5.92 pEC50 1200 nM EC50 ACS Med Chem Lett (2023) 14: 411-416 [PMID:37077394]
ChEMBL Agonist activity at human GPR35 receptor expressed in HEK293T cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment by BRET assay F 6.3 pEC50 500 nM EC50 J Med Chem (2021) 64: 2634-2647 [PMID:33630609]
ChEMBL Agonist activity at human GPR35 expressed in CHO-K1 cells after 90 mins by beta-arrestin 2 recruitment assay B 6.3 pEC50 500 nM EC50 J Med Chem (2017) 60: 362-372 [PMID:27976894]
GtoPdb - - 7.29 pEC50 - - - Biochem J (2010) 432: 451-9 [PMID:20919992]
ChEMBL Agonist activity at human GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay B 7.3 pEC50 50 nM EC50 J Med Chem (2013) 56: 5182-5197 [PMID:23713606]
ChEMBL Agonist activity at GPR-35 (unknown origin) expressed in HT-29 cells by DMR assay B 8.52 pEC50 3 nM EC50 ACS Med Chem Lett (2023) 14: 411-416 [PMID:37077394]
ChEMBL Agonist activity at human GPR35 by DMR assay B 8.68 pEC50 2.1 nM EC50 J Med Chem (2013) 56: 7084-7099 [PMID:23888932]
ChEMBL Agonist activity at human GPR35 expressed in CHO-K1 cells by DMR assay B 8.7 pEC50 2 nM EC50 J Med Chem (2017) 60: 362-372 [PMID:27976894]
ChEMBL Agonist activity at human GPR35 receptor expressed in HT-29 cells assessed as dynamic mass redistribution response measured for 60 mins by DMR assay F 8.7 pEC50 2 nM EC50 J Med Chem (2021) 64: 2634-2647 [PMID:33630609]
GPR35 in Rat [GtoPdb: 102] [UniProtKB: Q33BM1]
GtoPdb - - 5 pEC50 - - - Biochem J (2010) 432: 451-9 [PMID:20919992]

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]