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Literature summary for 2.1.1.100 extracted from

  • Bergman, J.A.; Hahne, K.; Song, J.; Hrycyna, C.A.; Gibbs, R.A.
    S-farnesyl-thiopropionic acid (FTPA) triazoles as potent inhibitors of isoprenylcysteine carboxyl methyltransferase (2012), ACS Med. Chem. Lett., 3, 15-19.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.1.1.100

Inhibitors

Inhibitors Comment Organism Structure
3-([(2E)-3-methyl-5-[4-(2-phenylethyl)-1H-1,2,3-triazol-1-yl]pent-2-en-1-yl]sulfanyl)propanoic acid 75% residual activity at 0.01 mM Homo sapiens
3-([(2E)-3-methyl-5-[4-(3-methylbutyl)-1H-1,2,3-triazol-1-yl]pent-2-en-1-yl]sulfanyl)propanoic acid modest inhibitor, 72% residual activity at 0.01 mM Homo sapiens
3-([(2E)-3-methyl-5-[4-(naphthalen-1-yl)-1H-1,2,3-triazol-1-yl]pent-2-en-1-yl]sulfanyl)propanoic acid poor inhibitor, 77% residual activity at 0.01 mM Homo sapiens
3-([(2E)-3-methyl-5-[4-(phenoxymethyl)-1H-1,2,3-triazol-1-yl]pent-2-en-1-yl]sulfanyl)propanoic acid 89% residual activity at 0.01 mM Homo sapiens
3-([(2E)-3-methyl-5-[4-(thiophen-3-yl)-1H-1,2,3-triazol-1-yl]pent-2-en-1-yl]sulfanyl)propanoic acid poor inhibitor, 80% residual activity at 0.01 mM Homo sapiens
3-([(2E)-5-[4-(4-methoxyphenyl)-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl)propanoic acid poor inhibitor, 87% residual activity at 0.01 mM Homo sapiens
3-([(2E)-5-[4-(4-tert-butylphenyl)-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl)propanoic acid poor inhibitor, 88% residual activity at 0.01 mM Homo sapiens
3-[4-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-1H-1,2,3-triazol-1-yl]propanoic acid modest inhibitor, 53% residual activity at 0.01 mM Homo sapiens
3-[4-[(3E)-4,8-dimethylnona-3,7-dien-1-yl]-1H-1,2,3-triazol-1-yl]propanoic acid modest inhibitor, 75% residual activity at 0.01 mM Homo sapiens
3-[4-[(3E,7E)-4,8,12-trimethyltrideca-3,7,11-trien-1-yl]-1H-1,2,3-triazol-1-yl]propanoic acid modest inhibitor, 69% residual activity at 0.01 mM Homo sapiens
3-[[(2E)-3-methyl-5-(4-pentyl-1H-1,2,3-triazol-1-yl)pent-2-en-1-yl]sulfanyl]propanoic acid modest inhibitor, 77% residual activity at 0.01 mM Homo sapiens
3-[[(2E)-3-methyl-5-(4-phenyl-1H-1,2,3-triazol-1-yl)pent-2-en-1-yl]sulfanyl]propanoic acid poor inhibitor, 88% residual activity at 0.01 mM Homo sapiens
3-[[(2E)-3-methyl-5-(4-[2-[4-(thiophen-2-yl)phenyl]ethyl]-1H-1,2,3-triazol-1-yl)pent-2-en-1-yl]sulfanyl]propanoic acid 63% residual activity at 0.01 mM Homo sapiens
3-[[(2E)-3-methyl-5-[4-[2-(tetrahydro-2H-pyran-2-yloxy)ethyl]-1H-1,2,3-triazol-1-yl]pent-2-en-1-yl]sulfanyl]propanoic acid 90% residual activity at 0.01 mM Homo sapiens
3-[[(2E)-5-(4-benzyl-1H-1,2,3-triazol-1-yl)-3-methylpent-2-en-1-yl]sulfanyl]propanoic acid 82% residual activity at 0.01 mM Homo sapiens
3-[[(2E)-5-[4-[(biphenyl-4-yloxy)methyl]-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl]propanoic acid 75% residual activity at 0.01 mM Homo sapiens
3-[[(2E)-5-[4-[2-(3'-cyanobiphenyl-4-yl)ethyl]-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl]propanoic acid 74% residual activity at 0.01 mM Homo sapiens
3-[[(2E)-5-[4-[2-(4'-fluorobiphenyl-4-yl)ethyl]-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl]propanoic acid 42% residual activity at 0.01 mM Homo sapiens
3-[[(2E)-5-[4-[2-(biphenyl-3-yl)ethyl]-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl]propanoic acid 74% residual activity at 0.01 mM Homo sapiens
3-[[(2E)-5-[4-[2-(biphenyl-4-yl)ethyl]-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl]propanoic acid 43% residual activity at 0.01 mM Homo sapiens
4-[4-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-1H-1,2,3-triazol-1-yl]butanoic acid modest inhibitor, 83% residual activity at 0.01 mM Homo sapiens
4-[4-[(3E)-4,8-dimethylnona-3,7-dien-1-yl]-1H-1,2,3-triazol-1-yl]butanoic acid modest inhibitor, 90% residual activity at 0.01 mM Homo sapiens
5-[4-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-1H-1,2,3-triazol-1-yl]pentanoic acid modest inhibitor, 73% residual activity at 0.01 mM Homo sapiens
methyl 3-([(2E)-3-methyl-5-[4-(2-phenylethyl)-1H-1,2,3-triazol-1-yl]pent-2-en-1-yl]sulfanyl)propanoate 69% residual activity at 0.01 mM Homo sapiens
methyl 3-([(2E)-3-methyl-5-[4-(3-methylbutyl)-1H-1,2,3-triazol-1-yl]pent-2-en-1-yl]sulfanyl)propanoate modest inhibitor, 77% residual activity at 0.01 mM Homo sapiens
methyl 3-([(2E)-3-methyl-5-[4-(naphthalen-1-yl)-1H-1,2,3-triazol-1-yl]pent-2-en-1-yl]sulfanyl)propanoate poor inhibitor, 82% residual activity at 0.01 mM Homo sapiens
methyl 3-([(2E)-3-methyl-5-[4-(phenoxymethyl)-1H-1,2,3-triazol-1-yl]pent-2-en-1-yl]sulfanyl)propanoate 89% residual activity at 0.01 mM Homo sapiens
methyl 3-([(2E)-3-methyl-5-[4-(thiophen-3-yl)-1H-1,2,3-triazol-1-yl]pent-2-en-1-yl]sulfanyl)propanoate poor inhibitor, 82% residual activity at 0.01 mM Homo sapiens
methyl 3-([(2E)-5-[4-(4-methoxyphenyl)-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl)propanoate poor inhibitor, 91% residual activity at 0.01 mM Homo sapiens
methyl 3-([(2E)-5-[4-(4-tert-butylphenyl)-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl)propanoate poor inhibitor, 84% residual activity at 0.01 mM Homo sapiens
methyl 3-[[(2E)-3-methyl-5-(4-nonyl-1H-1,2,3-triazol-1-yl)pent-2-en-1-yl]sulfanyl]propanoate modest inhibitor, 67% residual activity at 0.01 mM Homo sapiens
methyl 3-[[(2E)-3-methyl-5-(4-pentyl-1H-1,2,3-triazol-1-yl)pent-2-en-1-yl]sulfanyl]propanoate modest inhibitor, 76% residual activity at 0.01 mM Homo sapiens
methyl 3-[[(2E)-3-methyl-5-(4-phenyl-1H-1,2,3-triazol-1-yl)pent-2-en-1-yl]sulfanyl]propanoate poor inhibitor, 89% residual activity at 0.01 mM Homo sapiens
methyl 3-[[(2E)-3-methyl-5-(4-[2-[4-(thiophen-2-yl)phenyl]ethyl]-1H-1,2,3-triazol-1-yl)pent-2-en-1-yl]sulfanyl]propanoate 57% residual activity at 0.01 mM Homo sapiens
methyl 3-[[(2E)-3-methyl-5-[4-[2-(1,1':4',1''-terphenyl-4-yl)ethyl]-1H-1,2,3-triazol-1-yl]pent-2-en-1-yl]sulfanyl]propanoate 79% residual activity at 0.01 mM Homo sapiens
methyl 3-[[(2E)-3-methyl-5-[4-[2-(tetrahydro-2H-pyran-2-yloxy)ethyl]-1H-1,2,3-triazol-1-yl]pent-2-en-1-yl]sulfanyl]propanoate 80% residual activity at 0.01 mM Homo sapiens
methyl 3-[[(2E)-5-(4-benzyl-1H-1,2,3-triazol-1-yl)-3-methylpent-2-en-1-yl]sulfanyl]propanoate 80% residual activity at 0.01 mM Homo sapiens
methyl 3-[[(2E)-5-[4-[(3E)-4,8-dimethylnona-3,7-dien-1-yl]-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl]propanoate modest inhibitor, 59% residual activity at 0.01 mM Homo sapiens
methyl 3-[[(2E)-5-[4-[(biphenyl-4-yloxy)methyl]-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl]propanoate 67% residual activity at 0.01 mM Homo sapiens
methyl 3-[[(2E)-5-[4-[2-(3'-cyanobiphenyl-4-yl)ethyl]-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl]propanoate 30% residual activity at 0.01 mM Homo sapiens
methyl 3-[[(2E)-5-[4-[2-(4'-fluorobiphenyl-4-yl)ethyl]-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl]propanoate 28% residual activity at 0.01 mM Homo sapiens
methyl 3-[[(2E)-5-[4-[2-(biphenyl-2-yl)ethyl]-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl]propanoate 74% residual activity at 0.01 mM Homo sapiens
methyl 3-[[(2E)-5-[4-[2-(biphenyl-3-yl)ethyl]-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl]propanoate 65% residual activity at 0.01 mM Homo sapiens
methyl 3-[[(2E)-5-[4-[2-(biphenyl-4-yl)ethyl]-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl]propanoate potent competitive inhibitor, 14% residual activity at 0.01 mM Homo sapiens
[4-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-1H-1,2,3-triazol-1-yl]acetic acid modest inhibitor, 65% residual activity at 0.01 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
S-adenosyl-L-methionine + S-[(2E,6E)-farnesyl]-3-sulfanylpropanoic acid
-
 Homo sapiens S-adenosyl-L-homocysteine + methyl S-[(2E,6E)-farnesyl]-3-sulfanylpropanoate
-
 ?

Synonyms

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

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0004
-
 methyl 3-[[(2E)-5-[4-[2-(biphenyl-4-yl)ethyl]-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl]propanoate pH and temperature not specified in the publication Homo sapiens