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