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Literature summary for 2.1.1.100 extracted from

  • Bergman, J.A.; Hahne, K.; Hrycyna, C.A.; Gibbs, R.A.
    Lipid and sulfur substituted prenylcysteine analogs as human Icmt inhibitors (2011), Bioorg. Med. Chem. Lett., 21, 5616-5619.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.1.1.100

Inhibitors

Inhibitors Comment Organism Structure
(2R)-2-(acetylamino)-3-[[(2Z)-3,4-diphenylbut-2-en-1-yl]sulfanyl]propanoic acid 15.7% inhibition at 0.01 mM Homo sapiens
(2R)-2-(acetylamino)-3-[[(2Z)-4-(2-fluorophenyl)-3-phenylbut-2-en-1-yl]sulfanyl]propanoic acid 25.3% inhibition at 0.01 mM Homo sapiens
N-(2-phenoxybenzoyl)-3-[4-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-1H-1,2,3-triazol-1-yl]-L-alanine 35.9% inhibition at 0.01 mM Homo sapiens
N-(5-methoxy-2-nitrobenzoyl)-3-[4-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-1H-1,2,3-triazol-1-yl]-L-alanine 10.1% inhibition at 0.01 mM Homo sapiens
N-(biphenyl-2-ylcarbonyl)-3-[4-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-1H-1,2,3-triazol-1-yl]-L-alanine 17% inhibition at 0.01 mM Homo sapiens
N-acetyl-3-[4-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-1H-1,2,3-triazol-1-yl]-L-alanine 19.5% inhibition at 0.01 mM Homo sapiens
N-acetyl-S-farnesyl-L-cysteine complete inhibition at 0.025 mM Homo sapiens
N-acetyl-S-[(2E)-3-methyl-4-(4-phenoxyphenoxy)but-2-en-1-yl]-L-cysteine 15.5% inhibition at 0.01 mM Homo sapiens
N-acetyl-S-[(2E)-3-methyl-4-[(naphthalen-2-ylamino)oxy]but-2-en-1-yl]-L-cysteine 14.5% inhibition at 0.01 mM Homo sapiens
N-acetyl-S-[(2E)-3-methyl-5-(4-octylphenyl)pent-2-en-1-yl]-L-cysteine 31.1% inhibition at 0.01 mM Homo sapiens
N-acetyl-S-[(2E)-3-methyl-5-(4-pentylphenyl)pent-2-en-1-yl]-L-cysteine 23.1% inhibition at 0.01 mM Homo sapiens
N-acetyl-S-[(2E)-3-methyl-5-(4-propylphenyl)pent-2-en-1-yl]-L-cysteine 20.7% inhibition at 0.01 mM Homo sapiens
N-acetyl-S-[(2E)-3-methyl-7-(4-phenoxyphenoxy)hept-2-en-1-yl]-L-cysteine 19.4% inhibition at 0.01 mM Homo sapiens
N-acetyl-S-[(2E)-3-methyl-7-[(naphthalen-2-ylamino)oxy]hept-2-en-1-yl]-L-cysteine 22.4% inhibition at 0.01 mM Homo sapiens
N-acetyl-S-[(2E)-4-(4-benzylphenoxy)-3-methylbut-2-en-1-yl]-L-cysteine 9.8% inhibition at 0.01 mM Homo sapiens
N-acetyl-S-[(2E)-5-(4-hexylphenyl)-3-methylpent-2-en-1-yl]-L-cysteine 18.8% inhibition at 0.01 mM Homo sapiens
N-acetyl-S-[(2Z)-4-(biphenyl-4-yl)-3-phenylbut-2-en-1-yl]-L-cysteine 26.6% inhibition at 0.01 mM Homo sapiens
N-[3-(phenylsulfonyl)propanoyl]-3-[4-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-1H-1,2,3-triazol-1-yl]-L-alanine 22.7% inhibition at 0.01 mM Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
endoplasmic reticulum
-
 Homo sapiens 5783
-
membrane
-
 Homo sapiens 16020
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
S-adenosyl-L-methionine + N-acetyl-S-[(2E,6E)-farnesyl]-L-cysteine
-
 Homo sapiens S-adenosyl-L-homocysteine + N-acetyl-S-[(2E,6E)-farnesyl]-L-cysteine methyl ester
-
 ir

Synonyms

Synonyms Comment Organism
Icmt
-
 Homo sapiens
isoprenylcysteine carboxyl methyltransferase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0194
-
 pH and temperature not specified in the publication Homo sapiens N-(2-phenoxybenzoyl)-3-[4-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-1H-1,2,3-triazol-1-yl]-L-alanine
0.0346
-
 pH and temperature not specified in the publication Homo sapiens N-acetyl-S-[(2E)-3-methyl-5-(4-octylphenyl)pent-2-en-1-yl]-L-cysteine

General Information

General Information Comment Organism
physiological function methylation of Ras by the enzyme is required for proper localization to the plasma membrane and downstream signaling Homo sapiens