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) |
---|
There should be some charts here, you may need to enable JavaScript!
|
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, subunit alpha/Geranylgeranyl transferase type I in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095164] [GtoPdb: 2825] [UniProtKB: P49354, P53609] | ||||||||
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: 2825, 2826] [UniProtKB: P49354, P49356] | ||||||||
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: P29702, P49355] | ||||||||
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: 2825, 2826] [UniProtKB: Q61239, Q8K2I1] | ||||||||
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]