PF-04620110 [Ligand Id: 7829] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1835919 (Pf-04620110, PF-04620110, PF-4620110)
  • diacylglycerol O-acyltransferase 1/Diacylglycerol O-acyltransferase 1 in Human [ChEMBL: CHEMBL6009] [GtoPdb: 2821] [UniProtKB: O75907]
  • diacylglycerol O-acyltransferase 1/Diacylglycerol O-acyltransferase 1 in Mouse [ChEMBL: CHEMBL1075284] [GtoPdb: 2821] [UniProtKB: Q9Z2A7]
  • diacylglycerol O-acyltransferase 1/Diacylglycerol O-acyltransferase 1 in Rat [ChEMBL: CHEMBL6129] [GtoPdb: 2821] [UniProtKB: Q9ERM3]
There should be some charts here, you may need to enable JavaScript!
  • diacylglycerol O-acyltransferase 2/Diacylglycerol O-acyltransferase 2 in Human [ChEMBL: CHEMBL5853] [GtoPdb: 3211] [UniProtKB: Q96PD7]
There should be some charts here, you may need to enable JavaScript!
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 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]