BMS-963272 [Ligand Id: 12738] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3912712
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  • Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase in Human [ChEMBL: CHEMBL2321630] [UniProtKB: Q10469]
  • Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase in Mouse [ChEMBL: CHEMBL2375203] [UniProtKB: Q921V5]
  • Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase in Rat [ChEMBL: CHEMBL4879456] [UniProtKB: Q09326]
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  • Beta-1,4-mannosyl-glycoprotein 4-beta-N-acetylglucosaminyltransferase in Human [ChEMBL: CHEMBL2375206] [UniProtKB: Q09327]
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  • diacylglycerol O-acyltransferase 1/Diacylglycerol O-acyltransferase 1 in Human [ChEMBL: CHEMBL6009] [GtoPdb: 2821] [UniProtKB: O75907]
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  • monoacylglycerol O-acyltransferase 2 in Human [GtoPdb: 2881] [UniProtKB: Q3SYC2]
  • monoacylglycerol O-acyltransferase 2 in Mouse [GtoPdb: 2881] [UniProtKB: Q80W94]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acyl-CoA wax alcohol acyltransferase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2375204] [UniProtKB: Q6E213]
ChEMBL Inhibition of human AWAT2 B 4.48 pIC50 >33000 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321630] [UniProtKB: Q10469]
ChEMBL Inhibition of human MGAT2 in mouse STC-1 cell based assay B 7.48 pIC50 33 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
ChEMBL Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay B 8.15 pIC50 7.1 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2375203] [UniProtKB: Q921V5]
ChEMBL Inhibition of mouse MGAT2 in mouse STC-1 cell based assay B 7.06 pIC50 88 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
ChEMBL Inhibition of mouse recombinant MGAT2 expressed in Sf9 cell membrane using 2-oleoylglycerol and oleoyl-CoA as substrates incubated for 10 mins by LCMS assay B 7.74 pIC50 18 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879456] [UniProtKB: Q09326]
ChEMBL Inhibition of rat recombinant MGAT2 expressed in Sf9 cell membrane using 2-oleoylglycerol and oleoyl-CoA as substrates incubated for 10 mins by LCMS assay B 8 pIC50 10 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
Beta-1,4-mannosyl-glycoprotein 4-beta-N-acetylglucosaminyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2375206] [UniProtKB: Q09327]
ChEMBL Inhibition of human MGAT3 B 6.09 pIC50 >820 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
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 B 4.48 pIC50 >33000 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
monoacylglycerol O-acyltransferase 2 in Human [GtoPdb: 2881] [UniProtKB: Q3SYC2]
GtoPdb - - 8.15 pIC50 7.1 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
monoacylglycerol O-acyltransferase 2 in Mouse [GtoPdb: 2881] [UniProtKB: Q80W94]
GtoPdb - - 7.74 pIC50 18 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]

ChEMBL data shown on this page come from version 35:

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]