tauroursodeoxycholic acid [Ligand Id: 4746] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL272427 (Tauroursodeoxycholic acid, Tauroursodesoxycholic acid, Taurursodiol, Ur-906, Ursodeoxy Cholic Acid, Ursodeoxycholyltaurine, Ursodoxicoltaurine)
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  • GPBA receptor/G-protein coupled bile acid receptor 1 in Human [ChEMBL: CHEMBL5409] [GtoPdb: 37] [UniProtKB: Q8TDU6]
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  • Sodium/bile acid and sulphated solute cotransporter 2/Ileal bile acid transporter in Human [ChEMBL: CHEMBL2778] [GtoPdb: 960] [UniProtKB: Q12908]
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  • sPLA2-1B/Phospholipase A2 group 1B in Human [ChEMBL: CHEMBL4426] [GtoPdb: 1416] [UniProtKB: P04054]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
autotaxin/Autotaxin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3691] [GtoPdb: 2901] [UniProtKB: Q13822]
ChEMBL Inhibition of human ATX expressed in HEK293 Flp-In cells assessed as decrease in choline release from LPC measured every 30 secs for 90 mins by HVA based fluorescence assay B 4.99 pIC50 10300 nM IC50 J Med Chem (2017) 60: 2006-2017 [PMID:28165241]
GPBA receptor/G-protein coupled bile acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5409] [GtoPdb: 37] [UniProtKB: Q8TDU6]
ChEMBL Agonist activity at wild type human TGR5 expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assay F 4.3 pEC50 50500 nM EC50 Eur. J. Med. Chem. (2015) 104: 57-72 [PMID:26435512]
ChEMBL Agonist activity at human TGR5 expressed in CHO cells by luciferase assay F 4.52 pEC50 30000 nM EC50 J. Med. Chem. (2008) 51: 1831-1841 [PMID:18307294]
Sodium/bile acid and sulphated solute cotransporter 2/Ileal bile acid transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2778] [GtoPdb: 960] [UniProtKB: Q12908]
ChEMBL TP_TRANSPORTER: inhibition of Taurocholate uptake in ASBT-expressing COS cells F 4.55 pKi 28000 nM Ki Am. J. Physiol. (1998) 274: G157-G169 [PMID:9458785]
sPLA2-1B/Phospholipase A2 group 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4426] [GtoPdb: 1416] [UniProtKB: P04054]
ChEMBL Binding affinity to human pancreatic recombinant 1B PLA2 expressed in Escherichia coli by resonance energy transfer assay in presence of trimethyl-ammonium-diphenylhexatriene B 5 pKd 10000 nM Kd J. Nat. Prod. (2009) 72: 24-28 [PMID:19102680]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]