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Literature summary for 2.5.1.58 extracted from

  • Ryckebusch, A.; Gilleron, P.; Millet, R.; Houssin, R.; Lemoine, A.; Pommery, N.; Grellier, P.; Sergheraert, C.; Henichart, J.P.
    Novel N-(4-piperidinyl)benzamide antimalarials with mammalian protein farnesyltransferase inhibitory activity (2005), Chem. Pharm. Bull., 53, 1324-1326.
    View publication on PubMed
Search for more literature for 2.5.1.58

Inhibitors

Inhibitors Comment Organism Structure
methyl N-(1-cysteinylpiperidin-4-yl)-N-(phenylcarbonyl)-L-methioninate IC50: 22.8 nM Rattus norvegicus
methyl N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]piperidin-4-yl)-N-(phenylcarbonyl)-L-isoleucinate IC50: 32.7 nM Rattus norvegicus
methyl N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]piperidin-4-yl)-N-(phenylcarbonyl)-L-methioninate IC50: 4.6 nM Rattus norvegicus
methyl N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]piperidin-4-yl)-N-(phenylcarbonyl)-L-phenylalaninate IC50: 22 nM Rattus norvegicus
methyl N-(phenylcarbonyl)-N-{1-([1-[4-(trifluoromethyl)benzyl]-1H-imidazol-4-yl]methyl)piperidin-4-yl}-L-methioninate IC50: 43.9 nM Rattus norvegicus
methyl N-benzyl-N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]piperidin-4-yl)-L-methioninate IC50: 2.35 nM Rattus norvegicus
methyl N-[1-[(1-benzyl-1H-imidazol-4-yl)methyl]piperidin-4-yl]-N-(phenylcarbonyl)-L-methioninate IC50: 397 nM Rattus norvegicus

Metals/Ions

Metals/Ions Comment Organism Structure
Zn dependent Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
farnesyl diphosphate + protein-cysteine
-
 Rattus norvegicus diphosphate + S-farnesyl protein
-
 ?

Synonyms

Synonyms Comment Organism
FTase
-
 Rattus norvegicus
PFT
-
 Rattus norvegicus
prenyl transferase
-
 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000235
-
 IC50: 2.35 nM Rattus norvegicus methyl N-benzyl-N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]piperidin-4-yl)-L-methioninate
0.0000046
-
 IC50: 4.6 nM Rattus norvegicus methyl N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]piperidin-4-yl)-N-(phenylcarbonyl)-L-methioninate
0.000022
-
 IC50: 22 nM Rattus norvegicus methyl N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]piperidin-4-yl)-N-(phenylcarbonyl)-L-phenylalaninate
0.0000228
-
 IC50: 22.8 nM Rattus norvegicus methyl N-(1-cysteinylpiperidin-4-yl)-N-(phenylcarbonyl)-L-methioninate
0.0000327
-
 IC50: 32.7 nM Rattus norvegicus methyl N-(1-[[1-(4-cyanobenzyl)-1H-imidazol-4-yl]methyl]piperidin-4-yl)-N-(phenylcarbonyl)-L-isoleucinate
0.0000439
-
 IC50: 43.9 nM Rattus norvegicus methyl N-(phenylcarbonyl)-N-{1-([1-[4-(trifluoromethyl)benzyl]-1H-imidazol-4-yl]methyl)piperidin-4-yl}-L-methioninate
0.000397
-
 IC50: 397 nM Rattus norvegicus methyl N-[1-[(1-benzyl-1H-imidazol-4-yl)methyl]piperidin-4-yl]-N-(phenylcarbonyl)-L-methioninate