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ChEMBL ligand: CHEMBL1835919 (Pf-04620110, PF-04620110, PF-4620110) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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diacylglycerol O-acyltransferase 1/Diacylglycerol O-acyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6009] [GtoPdb: 2821] [UniProtKB: O75907] | ||||||||
ChEMBL | Inhibition of recombinant human DGAT-1 expressed in Hep3B cell lysate using didecanoyl glycerol and [14C]decanoyl-CoA as substrate after 60 mins by liquid scintillation counting analysis | B | 7.05 | pIC50 | 90 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 4713-4718 [PMID:23810496] |
GtoPdb | - | - | 7.72 | pIC50 | 19 | nM | IC50 | ACS Med Chem Lett (2011) 2: 407-12 [PMID:24900321] |
ChEMBL | Inhibition of human full length DGAT-1 expressed in insect sf9 cells using [14C]decanoylCoA as substrate after 1.5 hrs by scintillation spectrometry | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem (2013) 21: 5081-5097 [PMID:23871442] |
ChEMBL | Inhibition of full length human microsomal DGAT-1 expressed in baculovirus infected insect Sf9 cells using [14C]decanoylCoA as substrate after 1.5 hrs by scintillation counting | B | 7.72 | pIC50 | 19 | nM | IC50 | ACS Med Chem Lett (2011) 2: 407-412 [PMID:24900321] |
ChEMBL | Inhibition of human DGAT1 | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6122-6125 [PMID:21908190] |
ChEMBL | Inhibition of human DGAT-1-mediated triglyceride synthesis in the HT-29 cells by whole cell assay | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6122-6125 [PMID:21908190] |
ChEMBL | Inhibition of DGAT1-mediated triglyceride synthesis in human HT-29 cells using [3H]glycerol as substrate after 6 hrs by beta counting | B | 8.1 | pIC50 | 8 | nM | IC50 | ACS Med Chem Lett (2011) 2: 407-412 [PMID:24900321] |
ChEMBL | Inhibition of DGAT-1-mediated triglyceride synthesis in human HT-29 cells using [3H]-glycerol as substrate incubated for 1 hr prior to substrate addition measured after 5 hrs by scintillation counting analysis | B | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem (2013) 21: 5081-5097 [PMID:23871442] |
diacylglycerol O-acyltransferase 1/Diacylglycerol O-acyltransferase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075284] [GtoPdb: 2821] [UniProtKB: Q9Z2A7] | ||||||||
ChEMBL | Inhibition of DGAT-1 in mouse liver microsomes using didecanoyl glycerol and [14C]decanoyl-CoA as substrate after 60 mins by liquid scintillation counting analysis | B | 7.06 | pIC50 | 88 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 4713-4718 [PMID:23810496] |
diacylglycerol O-acyltransferase 1/Diacylglycerol O-acyltransferase 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6129] [GtoPdb: 2821] [UniProtKB: Q9ERM3] | ||||||||
ChEMBL | Inhibition of rat DGAT-1 | B | 7.19 | pIC50 | 64 | nM | IC50 | ACS Med Chem Lett (2011) 2: 407-412 [PMID:24900321] |
diacylglycerol O-acyltransferase 2/Diacylglycerol O-acyltransferase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5853] [GtoPdb: 3211] [UniProtKB: Q96PD7] | ||||||||
ChEMBL | Inhibition of human DGAT-2 | B | 4.52 | pIC50 | >30000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 407-412 [PMID:24900321] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]