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Literature summary extracted from

  • Clark, M.K.; Scott, S.A.; Wojtkowiak, J.; Chirco, R.; Mathieu, P.; Reiners, J.J.; Mattingly, R.R.; Borch, R.F.; Gibbs, R.A.
    Synthesis, biochemical, and cellular evaluation of farnesyl monophosphate prodrugs as farnesyltransferase inhibitors (2007), J. Med. Chem., 50, 3274-3282.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.58 (2Z,6E)-3-(3-methylbut-2-enyl)-7,11-dimethyldodeca-2,6,10-triene monophosphate IC50: 16 nM Homo sapiens
2.5.1.58 (2Z,6E)-3-allyl-7,11-dimethyldodeca-2,6,10-trien-1-yl 5-nitrofurfuryl N-methyl-N-(4-chlorobutyl)phosphoramidate
-
 Homo sapiens
2.5.1.58 (2Z,6E)-3-allyl-7,11-dimethyldodeca-2,6,10-triene monophosphate
-
 Homo sapiens
2.5.1.58 (2Z,6E)-3-tert-butyl-7,11-dimethyldodeca-2,6,10-trien-1-yl 5-nitrofurfuryl N-methyl-N-(4-chlorobutyl)phosphoramidate
-
 Homo sapiens
2.5.1.58 (2Z,6E)-3-tert-butyl-7,11-dimethyldodeca-2,6,10-triene monophosphate IC50: 13 nM Homo sapiens
2.5.1.58 (2Z,6E,10E)-3-(3-methyl-1-but-2-enyl)-7,11-dimethyldodeca-2,6,10-trien-1-yl 5-nitrofurfuryl N-methyl-N-(4-chlorobutyl)phosphoramidate
-
 Homo sapiens
2.5.1.58 3-allylfarnesol potent inhibitor Homo sapiens
2.5.1.58 3-allylfarnesyl diphosphate IC50: 189 nM Homo sapiens
2.5.1.58 3-tert-butylfarnesyl diphosphate IC50: 31 nM Homo sapiens
2.5.1.58 R-115777
-
 Homo sapiens
2.5.1.58 SCH66336
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.58 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.5.1.58 Schwann cell line
-
 Homo sapiens
-
2.5.1.58 STS-26T cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.5.1.58 farnesyl diphosphate + protein-cysteine
-
 Homo sapiens diphosphate + S-farnesyl protein
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.5.1.58 FTase
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.5.1.58 0.000013
-
 IC50: 13 nM Homo sapiens (2Z,6E)-3-tert-butyl-7,11-dimethyldodeca-2,6,10-triene monophosphate
2.5.1.58 0.000016
-
 IC50: 16 nM Homo sapiens (2Z,6E)-3-(3-methylbut-2-enyl)-7,11-dimethyldodeca-2,6,10-triene monophosphate
2.5.1.58 0.000031
-
 IC50: 31 nM Homo sapiens 3-tert-butylfarnesyl diphosphate
2.5.1.58 0.000189
-
 IC50: 189 nM Homo sapiens 3-allylfarnesyl diphosphate