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ChEMBL ligand: CHEMBL54044 (FTI-276) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 34:
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]