pradigastat [Ligand Id: 7830] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2364624 (Lcq-908, Lcq908 - dgat-1-inhibitor, LCQ-908-NXA, LCQ-908NXA, LCQ908-NXA, Pradigastat) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| diacylglycerol O-acyltransferase 1/Diacylglycerol O-acyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6009] [GtoPdb: 2821] [UniProtKB: O75907] | ||||||||
| ChEMBL | Inhibition of human DGAT1 in serum starved HEK293 cells assessed as inhibition of triglyceride synthesis incubated for 20 mins followed by 13C-addition of 13C-oleic acid pre-complexed with BSA for 120 mins by LC-MS-based mass spectrophotometric analysis | B | 7.18 | pIC50 | 66 | nM | IC50 | Bioorg Med Chem Lett (2022) 62: 128632-128632 [PMID:35189320] |
| ChEMBL | Inhibition of recombinant human his-tagged DGAT1 expressed in Sf9 insect cells using oleoyl-CoA and diolein as substrates incubated for 30 mins by LC/MS/MS analysis | B | 7.26 | pIC50 | 55 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1128-1133 [PMID:31413796] |
| diacylglycerol O-acyltransferase 1/Diacylglycerol O-acyltransferase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075284] [GtoPdb: 2821] [UniProtKB: Q9Z2A7] | ||||||||
| ChEMBL | Inhibition of DGAT1 in mouse C2C12 cells assessed as reduction in intracellular triglyceride production incubated for 2 hrs in presence of BSA-complexed oleate by LC/MS/MS analysis | B | 7.15 | pEC50 | 71 | nM | EC50 | ACS Med Chem Lett (2019) 10: 1128-1133 [PMID:31413796] |
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]
