ervogastat [Ligand Id: 12241] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4760665 (Pf-06865571) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Alpha-1,3-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4524036] [UniProtKB: P27808] | ||||||||
| ChEMBL | Inhibition of mouse MGAT1 using [1-14C]decanoyl-CoA and 2-oleoylglycerol as substrates assessed as incorporation of [1-14C]decanoyl into diacylglycerol preincubated for 30 mins followed by substrate addition and measured after 30 to 90 mins by scintillation counting method | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2022) 65: 15000-15013 [PMID:36322383] |
| Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321630] [UniProtKB: Q10469] | ||||||||
| ChEMBL | Inhibition of human MGAT2 using [1-14C]decanoyl-CoA and 1-decanoyl-rac-glycerol as substrates assessed as incorporation of [1-14C]decanoyl into diacylglycerol preincubated for 30 mins followed by substrate addition and measured after 30 to 90 mins by scintillation counting method | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2022) 65: 15000-15013 [PMID:36322383] |
| Beta-1,4-mannosyl-glycoprotein 4-beta-N-acetylglucosaminyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2375206] [UniProtKB: Q09327] | ||||||||
| ChEMBL | Inhibition of human MGAT3 using [1-14C]decanoyl-CoA and 1,2-didecanoyl-sn-glycerol as substrates assessed as incorporation of [1-14C]decanoyl into diacylglycerol preincubated for 30 mins followed by substrate addition and measured after 30 to 90 mins by scintillation counting method | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2022) 65: 15000-15013 [PMID:36322383] |
| 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 using [1-14C]decanoyl-CoA and 1,2-didecanoyl-sn-glycerol as substrates assessed as incorporation of [1-14C]decanoyl into diacylglycerol preincubated for 30 mins followed by substrate addition and measured after 30 to 90 mins by scintillation counting method | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2022) 65: 15000-15013 [PMID:36322383] |
| diacylglycerol O-acyltransferase 2/Diacylglycerol O-acyltransferase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5853] [GtoPdb: 3211] [UniProtKB: Q96PD7] | ||||||||
| GtoPdb | - | - | 7.76 | pIC50 | 17.2 | nM | IC50 | J Med Chem (2022) 65: 15000-15013 [PMID:36322383] |
| ChEMBL | Inhibition of human DGAT2 expressed in Sf9 insect cell membrane using [1-14C]decanoyl-CoA and 1,2-didecanoyl-sn-glycerol as substrates assessed as incorporation of [1-14C]decanoyl into triacylglycerol preincubated for 120 mins followed by substrate addition and measured after 40 mins by scintillation counting method | B | 7.76 | pIC50 | 17.2 | nM | IC50 | J Med Chem (2022) 65: 15000-15013 [PMID:36322383] |
| ChEMBL | Inhibition of human DGAT2 using 14C decanoyl-CoA as a substrate pre incubated for 2 hrs followed by substrate addition measured after 40 mins by Trilux Microbeta reader analysis | B | 7.77 | pIC50 | 17 | nM | IC50 | ACS Med Chem Lett (2023) 14: 1427-1433 [PMID:37849537] |
| diacylglycerol O-acyltransferase 2/Diacylglycerol O-acyltransferase 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295847] [GtoPdb: 3211] [UniProtKB: Q5FVP8] | ||||||||
| ChEMBL | Inhibition of rat DGAT2 using [1-14C]decanoyl-CoA and 1,2-didecanoyl-sn-glycerol as substrates assessed as incorporation of [1-14C]decanoyl into triacylglycerol preincubated for 120 mins followed by substrate addition and measured after 40 mins by scintillation counting method | B | 6.08 | pIC50 | 833 | nM | IC50 | J Med Chem (2022) 65: 15000-15013 [PMID:36322383] |
| GtoPdb | - | - | 6.08 | pIC50 | 833 | nM | IC50 | J Med Chem (2022) 65: 15000-15013 [PMID:36322383] |
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]
