FTI 276 [Ligand Id: 6531] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL54044 (FTI-276)
  • 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]
  • Protein farnesyltransferase in Bovine [ChEMBL: CHEMBL2095178] [UniProtKB: P29702P49355]
  • farnesyltransferase, CAAX box, subunit alpha/farnesyltransferase, CAAX box, subunit beta/Protein farnesyltransferase in Mouse [ChEMBL: CHEMBL2096912] [GtoPdb: 28252826] [UniProtKB: Q61239Q8K2I1]
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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 human GGTase1 in human Burkitt lymphoma (Daudi) cell supernatant using [3H]geranylgeranyl B 7.3 pIC50 50 nM IC50 Medchemcomm (2013) 4: 476-492 [PMID:25530833]
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 human FTase after 15 mins by fluorimetric analysis B 7.82 pIC50 15 nM IC50 Bioorg Med Chem Lett (2011) 21: 1261-1264 [PMID:21256013]
ChEMBL Inhibition of human recombinant farnesyltransferase using farnesylpyrophosphate and dansyl-GCVLS as substrate measured for 15 mins by fluorescence assay B 8.15 pIC50 7 nM IC50 Bioorg Med Chem Lett (2016) 26: 3730-3734 [PMID:27282741]
ChEMBL Inhibition of Trypanosoma brucei protein farnesyltransferase B 8.77 pIC50 1.7 nM IC50 J Med Chem (2004) 47: 432-445 [PMID:14711313]
ChEMBL Inhibition of farnesyltransferase from human Burkitt lymphoma (Daudi) cells B 9.21 pIC50 0.61 nM IC50 J Med Chem (2002) 45: 177-188 [PMID:11754590]
ChEMBL Inhibitory concentration against farnesyltransferase was determined B 9.22 pIC50 0.6 nM IC50 J Med Chem (2004) 47: 1869-1878 [PMID:15055985]
ChEMBL Inhibitory activity against farnesyltransferase (FT) using SPA assay B 9.29 pIC50 0.51 nM IC50 Bioorg Med Chem Lett (1999) 9: 703-708 [PMID:10201832]
GtoPdb - - 9.3 pIC50 0.5 nM IC50 J Biol Chem (1995) 270: 26802-6 [PMID:7592920]
ChEMBL Inhibition of mammalian Farnesyltransferase B 9.3 pIC50 0.5 nM IC50 Bioorg Med Chem Lett (2001) 11: 761-764 [PMID:11277514]
ChEMBL Inhibition of mammalian protein farnesyltransferase B 9.3 pIC50 0.5 nM IC50 J Med Chem (2004) 47: 432-445 [PMID:14711313]
ChEMBL In vitro inhibitory activity was evaluated against farnesyltransferase (FTase) B 9.3 pIC50 0.5 nM IC50 Bioorg Med Chem Lett (1999) 9: 1069-1074 [PMID:10328287]
ChEMBL Inhibition of human recombinant FTase using [3H]farnesyldiphosphate B 9.3 pIC50 0.5 nM IC50 Medchemcomm (2013) 4: 476-492 [PMID:25530833]
ChEMBL Inhibition of FTase isolated from human Burkitt's lymphoma cells assessed as decrease in transfer of [3H]farnesyl from [3H]farnesyl PPi to H-Ras-CVLS B 9.3 pIC50 0.5 nM IC50 J Med Chem (2018) 61: 3239-3252 [PMID:28505447]
ChEMBL Inhibition of [3H]FPP incorporation into Ha-ras protein by Farnesyltransferase F 9.3 pIC50 0.5 nM IC50 Bioorg Med Chem Lett (2001) 11: 2963-2965 [PMID:11677136]
Protein farnesyltransferase in Bovine (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095178] [UniProtKB: P29702P49355]
ChEMBL In vitro inhibition of farnesyltransferase from bovine brain B 9.3 pIC50 0.5 nM IC50 J Med Chem (1998) 41: 4288-4300 [PMID:9784104]
farnesyltransferase, CAAX box, subunit alpha/farnesyltransferase, CAAX box, subunit beta/Protein farnesyltransferase in Mouse (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096912] [GtoPdb: 28252826] [UniProtKB: Q61239Q8K2I1]
ChEMBL Inhibition of mammalian H-Ras processing in NIH 3T3 cells F 6 pIC50 1000 nM IC50 Bioorg Med Chem Lett (2001) 11: 761-764 [PMID:11277514]

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]