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, 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 Human02468Highcharts.com
  • 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]
Created with Highcharts 10.3.3ValuesChart context menuProtein farnesyltransferasepKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd BovinepKi BovinepIC50 BovinepEC50 BovinepKd MousepKi MousepIC50 MousepEC50 Mouse0246810Highcharts.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 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 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]