BMS-214662 [Ligand Id: 8026] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL351706 (Bms 214662, Bms-214662, BMS-214662)
  • farnesyltransferase, CAAX box, subunit alpha/Geranylgeranyl transferase type I in Human [ChEMBL: CHEMBL2095164] [GtoPdb: 2825] [UniProtKB: P49354P53609]
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  • farnesyltransferase, CAAX box, subunit alpha/farnesyltransferase, CAAX box, subunit beta/Protein farnesyltransferase in Human [ChEMBL: CHEMBL2094108] [GtoPdb: 28252826] [UniProtKB: P49354P49356]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
farnesyltransferase, CAAX box, subunit alpha/Geranylgeranyl transferase type I in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095164] [GtoPdb: 2825] [UniProtKB: P49354P53609]
ChEMBL Inhibition of geranylgeranyl transferase (GGT1) using K-Ras as substrate B 5.64 pIC50 2300 nM IC50 J Med Chem (2000) 43: 3587-3595 [PMID:11020273]
ChEMBL Inhibition of geranylgeranyl transferase (GGT1) using Ras-CVLL as substrate B 5.89 pIC50 1300 nM IC50 J Med Chem (2000) 43: 3587-3595 [PMID:11020273]
farnesyltransferase, CAAX box, subunit alpha/farnesyltransferase, CAAX box, subunit beta/Protein farnesyltransferase in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094108] [GtoPdb: 28252826] [UniProtKB: P49354P49356]
ChEMBL Inhibition of farnesyltransferase (unknown origin) assessed as KRAS farnesylation B 8.08 pIC50 8.4 nM IC50 J Med Chem (2013) 56: 5219-5230 [PMID:23566315]
ChEMBL Inhibitory concentration against farnesyltransferase was determined B 8.85 pIC50 1.4 nM IC50 J Med Chem (2004) 47: 1869-1878 [PMID:15055985]
ChEMBL Inhibition of human FTase B 8.85 pIC50 1.4 nM IC50 Bioorg Med Chem Lett (2012) 22: 6896-6902 [PMID:23036952]
ChEMBL Inhibition of human recombinant FTase B 8.87 pIC50 1.35 nM IC50 J Med Chem (2018) 61: 3239-3252 [PMID:28505447]
ChEMBL Inhibition of purified recombinant human farnesyltransferase (FT) B 8.87 pIC50 1.35 nM IC50 J Med Chem (2000) 43: 3587-3595 [PMID:11020273]
GtoPdb - - 8.87 pIC50 1.35 nM IC50 J Med Chem (2000) 43: 3587-95 [PMID:11020273]
ChEMBL Inhibition of farnesyltransferase B 8.89 pIC50 1.3 nM IC50 Bioorg Med Chem Lett (2004) 14: 767-771 [PMID:14741286]
ChEMBL Inhibition of farnesyltransferase (unknown origin) assessed as HRAS farnesylation B 8.89 pIC50 1.3 nM IC50 J Med Chem (2013) 56: 5219-5230 [PMID:23566315]
ChEMBL Inhibition of Farnesyltransferase B 9.15 pIC50 0.7 nM IC50 J Med Chem (2004) 47: 612-626 [PMID:14736242]

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]