linerixibat [Ligand Id: 14439] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2387408 (GSK2330672, Gsk-2330672, Gsk2330672, Linerixibat) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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| Sodium/bile acid and sulphated solute cotransporter 2/Ileal sodium/bile acid cotransporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2778] [GtoPdb: 960] [UniProtKB: Q12908] | ||||||||
| ChEMBL | Inhibition Assay: On the day of the uptake experiment, 10 mM HEPES was added to Hank's Balanced Salt Solution, and the pH was adjusted to 7.4 with TRIS (HBSSH). The assay buffer was prepared by adding 100 uM [3H]-taurocholate and 10 uM cold taurocholate to room temperature HBSSH. A separate washing buffer was prepared by adding 10 uM cold taurocholate to HBSSH (30 ml per assay plate) and placed on ice. Using 100% DMSO, 8 point, 3-fold dilution curves for each test compound was prepared starting at 200 uM. Similarly, an 8 point dose response curve was prepared of the control compound [(3R,5R)-3-butyl-3-ethyl-7,8-bis(methyloxy)-5-phenyl-2,3,4,5-tetrahydro-1,4-benzothiazepine 1,1-dioxide (Brieaddy, L. E. WO9605188, 1996)] starting at 1.8 mM. Drug plates were created by adding 3 uL of each concentration to a v-bottom 96-well plate then diluted 60-fold with 177 uL of assay buffer. Plates were removed from the incubator and allowed to cool to ambient temperature. | B | 7.37 | pIC50 | 43 | nM | IC50 | US-9040518-B2. Chemical compounds (2015) |
| ChEMBL | Inhibition of human ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (2013) 56: 5094-5114 [PMID:23678871] |
| GtoPdb | Determined as inhibition of 3H-taurocholate uptake in HEK293 cells expressing hASBT | - | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (2013) 56: 5094-114 [PMID:23678871] |
| Sodium/bile acid and sulphated solute cotransporter 2/Ileal sodium/bile acid cotransporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073708] [GtoPdb: 960] [UniProtKB: P70172] | ||||||||
| ChEMBL | Inhibition of mouse ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis | B | 8.68 | pIC50 | 2.1 | nM | IC50 | J Med Chem (2013) 56: 5094-5114 [PMID:23678871] |
| Sodium/bile acid and sulphated solute cotransporter 2/Ileal sodium/bile acid cotransporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073686] [GtoPdb: 960] [UniProtKB: Q62633] | ||||||||
| ChEMBL | Inhibition of rat ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis | B | 8.72 | pIC50 | 1.9 | nM | IC50 | J Med Chem (2013) 56: 5094-5114 [PMID:23678871] |
ChEMBL data shown on this page come from version 37:
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]
