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ChEMBL ligand: CHEMBL205596 (Cholalic acid, Cholbam, Cholic acid, Cholic Acid, E1000, Kolbam, NSC-6135, Orphacol) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Farnesoid X receptor/Bile acid receptor FXR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1] | ||||||||
ChEMBL | Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2009) 52: 7958-7961 [PMID:20014870] |
ChEMBL | Agonist activity at GST-tagged FXR-LBD using biotinylated-SRC-1 peptide as substrate preincubated with compound for 30 mins measured after 4 hrs | F | 4 | pEC50 | >100000 | nM | EC50 | ACS Med Chem Lett (2012) 3: 273-277 [PMID:24900463] |
ChEMBL | Agonist activity at GST-tagged FXR-LBD (unknown origin) assessed as biotin-labeled SRC-1 recruitment after 30 mins by Alpha Screen assay | B | 4.35 | pEC50 | 45000 | nM | EC50 | Eur J Med Chem (2018) 144: 349-358 [PMID:29275233] |
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 human TGR5 receptor expressed in HEK293 cells assessed as intracellular cAMP level | F | 5.22 | pIC50 | 6000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 5718-5721 [PMID:20801037] |
ChEMBL | Agonist activity at wild type TGR5 (unknown origin) | B | 4.7 | pEC50 | 19830 | nM | EC50 | ACS Med Chem Lett (2013) 4: 1158-1162 [PMID:24900622] |
ChEMBL | Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay | F | 4.87 | pEC50 | 13600 | nM | EC50 | J Med Chem (2007) 50: 4265-4268 [PMID:17685603] |
ChEMBL | Agonist activity at human TGR5 expressed in CHO cells by luciferase assay | F | 4.87 | pEC50 | 13600 | nM | EC50 | J Med Chem (2008) 51: 1831-1841 [PMID:18307294] |
ChEMBL | Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay | F | 4.87 | pEC50 | 13600 | nM | EC50 | J Med Chem (2009) 52: 7958-7961 [PMID:20014870] |
ChEMBL | Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis | F | 4.87 | pEC50 | 13600 | nM | EC50 | ACS Med Chem Lett (2012) 3: 273-277 [PMID:24900463] |
GtoPdb | - | - | 5 | pEC50 | - | - | - | Biochem Biophys Res Commun (2002) 298: 714-9 [PMID:12419312] |
GPBA receptor/G-protein coupled bile acid receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255150] [GtoPdb: 37] [UniProtKB: Q80SS6] | ||||||||
ChEMBL | Agonist activity at mouse TGR5 receptor expressed in HEK293 cells assessed as intracellular cAMP level | F | 5.28 | pIC50 | 5300 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 5718-5721 [PMID:20801037] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antimalarial activity against Plasmodium falciparum NF54 infected in human erythrocytes assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition measured after 24 hrs by liquid scintillation counting | F | 4.7 | pIC50 | >20000 | nM | IC50 | Medchemcomm (2017) 8: 1152-1157 [PMID:30108825] |
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]