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]
Created with Highcharts 10.3.3ValuesChart context menuGeranylgeranyl transferase type IpKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuGTPase KRaspKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • farnesyltransferase, CAAX box, subunit alpha/farnesyltransferase, CAAX box, subunit beta/Protein farnesyltransferase in Human [ChEMBL: CHEMBL2094108] [GtoPdb: 28252826] [UniProtKB: P49354P49356]
Created with Highcharts 10.3.3ValuesChart context menuProtein farnesyltransferasepKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • HRAS/Transforming protein p21/H-Ras-1 in Human [ChEMBL: CHEMBL2167] [GtoPdb: 2822] [UniProtKB: P01112]
Created with Highcharts 10.3.3ValuesChart context menuTransforming protein p21/H-Ras-1pKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
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]
KRAS/GTPase KRas in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189121] [GtoPdb: 2824] [UniProtKB: P01116]
ChEMBL Inhibition of K-Ras (unknown origin) geranylgeranylation B 5.64 pIC50 2300 nM IC50 Eur J Med Chem (2021) 211: 113006-113006 [PMID:33228976]
ChEMBL Inhibition of K-Ras (unknown origin) farnesylation B 8.08 pIC50 8.4 nM IC50 Eur J Med Chem (2021) 211: 113006-113006 [PMID:33228976]
ChEMBL Inhibition of human K-ras B 8.08 pIC50 8.4 nM IC50 Eur J Med Chem (2021) 226: 113877-113877 [PMID:34624823]
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]
HRAS/Transforming protein p21/H-Ras-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2167] [GtoPdb: 2822] [UniProtKB: P01112]
ChEMBL Inhibition of HRAS (unknown origin) farnesylation B 8.89 pIC50 1.3 nM IC50 Eur J Med Chem (2021) 211: 113006-113006 [PMID:33228976]
ChEMBL Inhibition of human H-ras B 8.89 pIC50 1.3 nM IC50 Eur J Med Chem (2021) 226: 113877-113877 [PMID:34624823]

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]