lomitapide [Ligand Id: 7439] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL354541 (AEGR-733, BMS-201038, BMS-201038-01, Lojuxta, Lomitapida, Lomitapide)
  • 5-methyltetrahydrofolate-homocysteine methyltransferase/Methionine synthase in Human [ChEMBL: CHEMBL2150844] [GtoPdb: 3099] [UniProtKB: Q99707]
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  • Microsomal triglyceride transfer protein large subunit in Human [ChEMBL: CHEMBL2569] [UniProtKB: P55157]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-methyltetrahydrofolate-homocysteine methyltransferase/Methionine synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2150844] [GtoPdb: 3099] [UniProtKB: Q99707]
ChEMBL Inhibition of MTR (unknown origin) B 9.3 pIC50 0.5 nM IC50 Eur J Med Chem (2022) 243: 114742-114742 [PMID:36155354]
Microsomal triglyceride transfer protein large subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2569] [UniProtKB: P55157]
ChEMBL In vitro inhibition of human microsomal triglyceride transfer protein using triglyceride transfer assay B 8.1 pIC50 8 nM IC50 J Med Chem (2001) 44: 851-856 [PMID:11300866]
ChEMBL In vitro inhibitory concentration against human Microsomal triglyceride transfer protein F 8.1 pIC50 8 nM IC50 Bioorg Med Chem Lett (2004) 14: 5067-5070 [PMID:15380200]
ChEMBL In vitro inhibition of human microsomal triglyceride transfer protein in HepG2 cells using apoB secretion assay F 9.1 pIC50 0.8 nM IC50 J Med Chem (2001) 44: 851-856 [PMID:11300866]

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]