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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL54044 (FTI-276)
  • farnesyltransferase, CAAX box, alpha/Geranylgeranyl transferase type I in Human [ChEMBL: CHEMBL2095164] [GtoPdb: 2825] [UniProtKB: P49354P53609]
There should be some charts here, you may need to enable JavaScript!
  • farnesyltransferase, CAAX box, alpha/farnesyltransferase, CAAX box, beta/Protein farnesyltransferase in Human [ChEMBL: CHEMBL2094108] [GtoPdb: 28252826] [UniProtKB: P49354P49356]
  • Protein farnesyltransferase in Bovine [ChEMBL: CHEMBL2095178] [UniProtKB: P29702P49355]
  • farnesyltransferase, CAAX box, alpha/farnesyltransferase, CAAX box, beta/Protein farnesyltransferase in Mouse [ChEMBL: CHEMBL2096912] [GtoPdb: 28252826] [UniProtKB: Q61239Q8K2I1]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
farnesyltransferase, CAAX box, 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, alpha/farnesyltransferase, CAAX box, 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, alpha/farnesyltransferase, CAAX box, 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]