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Human FTase Assay from Article 10.3109/14756366.2011.643302: "New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis."
Assay data:5 Active, 1 Activity ≤ 1 µM, 23 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
In Vitro PFT Activity Assay from Article 10.1016/j.chembiol.2009.01.014: "Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase."
Assay data:5 Active, 3 Activity ≤ 1 µM, 5 Tested
GGTase-I Activity Assay from Article 10.1016/S0960-894X(03)00095-7: "Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives."
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
FTase Activity Assay from Article 10.1016/S0960-894X(03)00095-7: "Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives."
Assay data:11 Active, 3 Activity ≤ 1 nM, 11 Activity ≤ 1 µM, 11 Tested
FTase Scintillation Proximity Assay from Article : "Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro."
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
In Vitro FTase/GGTase-1 Inhibition Assay from Article 10.1074/jbc.M600168200: "A novel protein geranylgeranyltransferase-I inhibitor with high potency, selectivity, and cellular activity."
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
In Vitro Enzyme Assay of FPT from Article 10.1021/jm980462b: "(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent."
Assay data:18 Active, 25 Activity ≤ 1 µM, 25 Tested
FTase Activity Assay from Article 10.1016/j.bmcl.2005.02.062: "Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors."
Assay data:16 Active, 4 Activity ≤ 1 nM, 21 Activity ≤ 1 µM, 21 Tested
FTase Activity Assay from Article 10.1016/j.bmcl.2005.03.049: "Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity."
Assay data:18 Active, 2 Activity ≤ 1 nM, 17 Activity ≤ 1 µM, 18 Tested
In Vitro FTase Inhibition Assay from Article 10.1021/jm010531d: "3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency."
Assay data:26 Active, 3 Activity ≤ 1 nM, 25 Activity ≤ 1 µM, 26 Tested
Enzyme Inhibition Assay from Article 10.1021/jm030434f: "Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors."
Assay data:45 Active, 20 Activity ≤ 1 nM, 45 Activity ≤ 1 µM, 45 Tested
PFT IC50 Determination from Article 10.1021/jm0506165: "Synthesis, pharmacological evaluation, and molecular modeling studies of novel peptidic CAAX analogues as farnesyl-protein-transferase inhibitors."
Assay data:9 Active, 3 Activity ≤ 1 µM, 16 Tested
PfPFT and Rat PFT IC50 Determination from Article 10.1021/jm0491039: "Protein farnesyltransferase inhibitors exhibit potent antimalarial activity."
Assay data:24 Active, 5 Activity ≤ 1 nM, 25 Activity ≤ 1 µM, 25 Tested
PFT IC50 Determination from Article 10.1021/jm060081v: "Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites."
Assay data:11 Active, 2 Activity ≤ 1 nM, 12 Activity ≤ 1 µM, 12 Tested
Scintillation proximity assay (SPA)
Assay data:1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, activity ≤ 1 µMRelated BioAssays by Target
Displacement of (1-(2-aminoethyl)-3,5-dimethyl-1H-pyrazol-4-yl)(4-((1-neopentyl-1H-benzo[d]imidazol-2-yl)methyl)piperazin-1-yl)methanone from FNTA in vorinostat-stimulated human Jurkat 2C4 cells infected with latent HIV-1 by pull-down experiment based competitive binding assay
Displacement of (4-((1-neopentyl-1H-benzo[d]imidazol-2-yl)methyl)piperazin-1-yl)(1,3,5-trimethyl-1H-pyrazol-4-yl)methanone from FNTA in vorinostat-stimulated human Jurkat 2C4 cells infected with latent HIV-1 by pull-down experiment based competitive binding assay
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of FTase in HEK293 cells assessed as reduction in H-ras farnesylation at 5 to 20 to 10 uM incubated for 48 hrs by SDS-PAGE and immunoblot analysis
SummaryRelated BioAssays by Target
Inhibition of rat recombinant FTase alpha/beta expressed in Escherichia coli at 100000 nM using K-Ras4B as a substrate as and [3H]farnesyl pyrophosphate incubated for 30 mins by scintillation counting assay
Inhibition of FTase in HEK293 cells assessed as reduction in H-ras farnesylation at 5 uM incubated for 48 hrs by SDS-PAGE and immunoblot analysis
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