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Literature summary extracted from

  • Carrico, D.; Blaskovich, M.A.; Bucher, C.J.; Sebti, S.M.; Hamilton, A.D.
    Design, synthesis, and evaluation of potent and selective benzoyleneurea-based inhibitors of protein geranylgeranyltransferase-I (2005), Bioorg. Med. Chem., 13, 677-688.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.5.1.59 medicine potential target in anticancer drug research Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.59 1-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-cyclohexanecarboxylic acid IC50: 6525 nM Homo sapiens
2.5.1.59 1-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-cyclohexanecarboxylic acid methyl ester IC50: above 0.01 mM Homo sapiens
2.5.1.59 2-aryl-4-aminobenzoic acid IC50: 21 nM Homo sapiens
2.5.1.59 2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-N-(3-methyl-butyl)-acetamide IC50: above 0.01 mM Homo sapiens
2.5.1.59 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl] acetylamino}-4-methyl-pentanoic acid methyl ester IC50: above 0.01 mM Homo sapiens
2.5.1.59 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-3-phenyl-propionic acid IC50: 0.0063 mM; IC50: 170 nM Homo sapiens
2.5.1.59 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-3-phenyl-propionic acid methyl ester IC50: 4500 nM; IC50: above 0.01 mM Homo sapiens
2.5.1.59 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-4-methyl-pentanoic acid IC50: 2700 nM; IC50: 580 nM Homo sapiens
2.5.1.59 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-4-methyl-pentanoic acid methyl ester IC50: above 0.01 mM Homo sapiens
2.5.1.59 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-4-methylsulfanyl-butyric acid IC50: 3350 nM Homo sapiens
2.5.1.59 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-4-methylsulfanyl-butyric acid methyl ester IC50: above 0.01 mM Homo sapiens
2.5.1.59 [3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetic acid benzyl ester IC50: above 0.01 mM Homo sapiens
2.5.1.59 {2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-acetic acid IC50: above 0.01 mM Homo sapiens
2.5.1.59 {2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-acetic acid methyl ester IC50: above 0.01 mM Homo sapiens

Organism

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.5.1.59 geranylgeranyl diphosphate + H-Ras-CVLL
-
 Homo sapiens S-geranylgeranyl-protein + ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.5.1.59 PGGTase-I
-
 Homo sapiens
2.5.1.59 protein geranylgeranyltransferase-I
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.5.1.59 0.000021
-
 IC50: 21 nM Homo sapiens 2-aryl-4-aminobenzoic acid
2.5.1.59 0.00017
-
 IC50: 170 nM Homo sapiens 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-3-phenyl-propionic acid
2.5.1.59 0.00058
-
 IC50: 580 nM Homo sapiens 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-4-methyl-pentanoic acid
2.5.1.59 0.0027
-
 IC50: 2700 nM Homo sapiens 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-4-methyl-pentanoic acid
2.5.1.59 0.00335
-
 IC50: 3350 nM Homo sapiens 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-4-methylsulfanyl-butyric acid
2.5.1.59 0.0045
-
 IC50: 4500 nM Homo sapiens 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-3-phenyl-propionic acid methyl ester
2.5.1.59 0.0063
-
 IC50: 0.0063 mM Homo sapiens 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-3-phenyl-propionic acid
2.5.1.59 0.006525
-
 IC50: 6525 nM Homo sapiens 1-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-cyclohexanecarboxylic acid
2.5.1.59 0.01
-
 IC50: above 0.01 mM Homo sapiens 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-3-phenyl-propionic acid methyl ester
2.5.1.59 0.01
-
 IC50: above 0.01 mM Homo sapiens 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-4-methyl-pentanoic acid methyl ester
2.5.1.59 0.01
-
 IC50: above 0.01 mM Homo sapiens 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl] acetylamino}-4-methyl-pentanoic acid methyl ester
2.5.1.59 0.01
-
 IC50: above 0.01 mM Homo sapiens 1-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-cyclohexanecarboxylic acid methyl ester
2.5.1.59 0.01
-
 IC50: above 0.01 mM Homo sapiens 2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-4-methylsulfanyl-butyric acid methyl ester
2.5.1.59 0.01
-
 IC50: above 0.01 mM Homo sapiens {2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-acetic acid
2.5.1.59 0.01
-
 IC50: above 0.01 mM Homo sapiens {2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-acetic acid methyl ester
2.5.1.59 0.01
-
 IC50: above 0.01 mM Homo sapiens [3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetic acid benzyl ester
2.5.1.59 0.01
-
 IC50: above 0.01 mM Homo sapiens 2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-N-(3-methyl-butyl)-acetamide