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Literature summary for 2.5.1.58 extracted from

  • Puntambekar, D.S.; Giridhar, R.; Yadav, M.R.
    Inhibition of farnesyltransferase: a rational approach to treat cancer? (2007), J. Enzyme Inhib. Med. Chem., 22, 127-140.
    View publication on PubMed
Search for more literature for 2.5.1.58

Inhibitors

Inhibitors Comment Organism Structure
1-(1H-imidazol-5-ylmethyl)-7-pyridin-4-yl-4-[[2-(trifluoromethoxy)phenyl]carbonyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine
-
 Homo sapiens
18-oxa-2,5,9,11-tetraazahexacyclo[17.6.2.22,5.113,17.07,11.022,26]triaconta-1(26),7,9,13(28),14,16,19,21,22,24,26-undecaene-16-carbonitrile
-
 Homo sapiens
2-amino-3-[2-butyl-4-(naphthalen-1-ylcarbonyl)piperazin-1-yl]propane-1-thiol
-
 Homo sapiens
29-oxo-18-oxa-2,6,9,11-tetraazahexacyclo[17.5.3.12,5.113,17.07,11.022,26]nonacosa-7,9,13(28),14,16,19,21,26-octaene-16-carbonitrile
-
 Homo sapiens
6-[(4-hydroxyphenyl)(1H-imidazol-1-yl)methyl]-4-phenyl-1,2-dihydroquinolin-2-ol
-
 Homo sapiens
AZD3409
-
 Homo sapiens
BMS-214662
-
 Homo sapiens
FTI-2153
-
 Homo sapiens
FTI-276
-
 Homo sapiens
FTI-277
-
 Homo sapiens
L-739,749
-
 Homo sapiens
L-739,750
-
 Homo sapiens
L-744,832
-
 Homo sapiens
L-788,123
-
 Homo sapiens
methyl N-([3-[methyl(1-methylidene-2,3-disulfanylpropyl)amino]-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-1-yl]acetyl)methioninate
-
 Homo sapiens
methyl N-[(6E)-2-benzyl-5-(1-methylethyl)-8-(sulfanylmethyl)dec-6-enoyl]methioninate
-
 Homo sapiens
N-[(6E)-2-benzyl-5-(1-methylethyl)-8-(sulfanylmethyl)dec-6-enoyl]methionine
-
 Homo sapiens
N-[2-([2-[(2-amino-3-sulfanylpropyl)amino]-3-methylbutyl]amino)-3-phenylpropyl]methionine
-
 Homo sapiens
N-[2-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]acetyl]amino)-3-methylpentyl]-N-(naphthalen-1-ylmethyl)glycylmethionine
-
 Homo sapiens
R115777 tipifarnid, Zarnestra Homo sapiens
SCH-37370
-
 Homo sapiens
SCH-44342
-
 Homo sapiens
SCH-66336 lonafarnib, Sarasar Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
farnesyl diphosphate + Ras-Cys-Val-Ile-Met
-
 Homo sapiens diphosphate + Ras-S-farnesyl-Cys-Val-Ile-Met
-
 ?

Synonyms

Synonyms Comment Organism
FTase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000015
-
-
 Homo sapiens N-[2-([[1-(4-cyanobenzyl)-1H-imidazol-5-yl]acetyl]amino)-3-methylpentyl]-N-(naphthalen-1-ylmethyl)glycylmethionine
0.0000002
-
-
 Homo sapiens 18-oxa-2,5,9,11-tetraazahexacyclo[17.6.2.22,5.113,17.07,11.022,26]triaconta-1(26),7,9,13(28),14,16,19,21,22,24,26-undecaene-16-carbonitrile
0.0000006
-
-
 Homo sapiens FTI-276
0.00000086
-
-
 Homo sapiens R115777
0.000001
-
 IC50 less than 0.000001 mM Homo sapiens 2-amino-3-[2-butyl-4-(naphthalen-1-ylcarbonyl)piperazin-1-yl]propane-1-thiol
0.000001
-
 IC50 less than 0.000001 mM Homo sapiens 29-oxo-18-oxa-2,6,9,11-tetraazahexacyclo[17.5.3.12,5.113,17.07,11.022,26]nonacosa-7,9,13(28),14,16,19,21,26-octaene-16-carbonitrile
0.0000014
-
-
 Homo sapiens BMS-214662
0.0000018
-
-
 Homo sapiens L-739,750
0.0000019
-
-
 Homo sapiens SCH-66336
0.000002
-
-
 Homo sapiens L-788,123
0.0000021
-
-
 Homo sapiens N-[2-([2-[(2-amino-3-sulfanylpropyl)amino]-3-methylbutyl]amino)-3-phenylpropyl]methionine
0.000024
-
-
 Homo sapiens 1-(1H-imidazol-5-ylmethyl)-7-pyridin-4-yl-4-[[2-(trifluoromethoxy)phenyl]carbonyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine
0.00018
-
-
 Homo sapiens 6-[(4-hydroxyphenyl)(1H-imidazol-1-yl)methyl]-4-phenyl-1,2-dihydroquinolin-2-ol
0.00025
-
-
 Homo sapiens SCH-44342
0.027
-
-
 Homo sapiens SCH-37370