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ChEMBL ligand: CHEMBL408701 (Taurolithocholate, Taurolithocholic acid, Tauroursodeoxycholic acid) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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EPH receptor A2/Ephrin type-A receptor 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105859] [GtoPdb: 1822] [UniProtKB: Q03145] | ||||||||
ChEMBL | Displacement of biotinylated ephrin-A1-Fc from recombinant mouse EphA2 receptor preincubated for 1 hr followed by biotinylated ephrin-A1-Fc addition measured after 4 hrs by ELISA method | B | 4.14 | pIC50 | 72000 | nM | IC50 | J Med Chem (2017) 60: 787-796 [PMID:28005388] |
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 recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay | F | 6 | pEC50 | 1005.4 | nM | EC50 | RSC Med Chem (2021) 12: 394-405 [PMID:34046622] |
ChEMBL | Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay | F | 6.07 | pEC50 | 847 | nM | EC50 | J Med Chem (2019) 62: 6824-6830 [PMID:31268316] |
ChEMBL | Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation in presence of 3-isobutyl-1-methylxanthine after 20 mins | F | 6.48 | pEC50 | 330 | nM | EC50 | J Med Chem (2019) 62: 6824-6830 [PMID:31268316] |
ChEMBL | Agonist activity at human TGR5 expressed in CHO cells by luciferase assay | F | 6.54 | pEC50 | 290 | nM | EC50 | J Med Chem (2008) 51: 1831-1841 [PMID:18307294] |
ABCC4/Multidrug resistance-associated protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743128] [GtoPdb: 782] [UniProtKB: O15439] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of E217betaG uptake in membrane vesicles from MRP4-expressing HEK-293 cells | F | 4.7 | pIC50 | 20000 | nM | IC50 | Biochem J (2003) 371: 361-367 [PMID:12523936] |
Vitamin D receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1977] [GtoPdb: 605] [UniProtKB: P11473] | ||||||||
ChEMBL | Antagonist activity against VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as inhibition of 1,25-dihydroxyvitamin D3-induced SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Eur J Med Chem (2016) 109: 238-246 [PMID:26774929] |
ChEMBL | Antagonist activity against VDR-LBD (unknown origin) expressed in Escherichia coli assessed as inhibition of VDR agonist LG190178-induced SRC2-3 coactivator peptide recruitment after 30 mins by fluorescence polarization assay | B | 4.84 | pIC50 | 14500 | nM | IC50 | Eur J Med Chem (2016) 109: 238-246 [PMID:26774929] |
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]