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Literature summary for 2.1.1.100 extracted from

  • Ramanujulu, P.M.; Yang, T.; Yap, S.Q.; Wong, F.C.; Casey, P.J.; Wang, M.; Go, M.L.
    Functionalized indoleamines as potent, drug-like inhibitors of isoprenylcysteine carboxyl methyltransferase (Icmt) (2013), Eur. J. Med. Chem., 63, 378-386.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Spodoptera frugiperda ovarian membranes Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]sulfanyl]ethanol
-
Homo sapiens
3-(2,2-dimethyloxan-4-yl)-N-[(4-methoxyphenyl)methyl]-3-phenylpropan-1-amine
-
Homo sapiens
3-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]phenol
-
Homo sapiens
4-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]-N-methylbenzene-1-sulfonamide
-
Homo sapiens
5-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]-N,N-dimethylpyridin-2-amine
-
Homo sapiens
5-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]pyrimidin-2-amine
-
Homo sapiens
5-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]pyrimidine-2-carbonitrile
-
Homo sapiens
cysmethynil
-
Homo sapiens
methyl 3-[[(2E)-5-[4-[2-([1,1'-biphenyl]-4-yl)ethyl]-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl]propanoate
-
Homo sapiens
N-(2-phenoxybenzoyl)-S-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-L-cysteine
-
Homo sapiens
N-ethyl-N-([1-octyl-5-[3-(trifluoromethyl)phenyl]-1H-indol-3-yl]methyl)ethanamine
-
Homo sapiens
N-ethyl-N-([5-[4-(methanesulfonyl)phenyl]-1-octyl-1H-indol-3-yl]methyl)ethanamine
-
Homo sapiens
N-ethyl-N-[(4-fluoro-1-octyl-1H-indol-3-yl)methyl]ethanamine
-
Homo sapiens
N-ethyl-N-[(5-fluoro-1-octyl-1H-indol-3-yl)methyl]ethanamine
-
Homo sapiens
N-ethyl-N-[(6-fluoro-1-octyl-1H-indol-3-yl)methyl]ethanamine
-
Homo sapiens
N-ethyl-N-[(7-fluoro-1-octyl-1H-indol-3-yl)methyl]ethanamine
-
Homo sapiens
N-ethyl-N-[[1-octyl-5-(pyridin-3-yl)-1H-indol-3-yl]methyl]ethanamine
-
Homo sapiens
N-ethyl-N-[[1-octyl-5-(pyrimidin-5-yl)-1H-indol-3-yl]methyl]ethanamine
-
Homo sapiens
N-ethyl-N-[[5-(2-fluorophenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
-
Homo sapiens
N-ethyl-N-[[5-(3-fluorophenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
-
Homo sapiens
N-ethyl-N-[[5-(3-fluoropyridin-4-yl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
-
Homo sapiens
N-ethyl-N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
-
Homo sapiens
S-[(2E)-3-[2-([1,1'-biphenyl]-4-yl)ethyl]-6-methylhepta-2,5-dien-1-yl]-N-(2-phenoxybenzoyl)-L-cysteine
-
Homo sapiens
S-[(2E,6E)-8-(3-benzoylphenoxy)-3,7-dimethylocta-2,6-dien-1-yl]-N-([2-[2-([5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl]amino)ethoxy]ethoxy]acetyl)-D-cysteine
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine Homo sapiens
-
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
Hep-G2 cell
-
Homo sapiens
-
IMR-90 cell
-
Homo sapiens
-
MDA-MB-231 cell
-
Homo sapiens
-
Mia PACA 2 cell
-
Homo sapiens
-
PC-3 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
-
Homo sapiens S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
-
?

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00086
-
at pH 7.4 and 37°C Homo sapiens 5-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]pyrimidin-2-amine
0.00096
-
at pH 7.4 and 37°C Homo sapiens N-ethyl-N-[[5-(3-fluoropyridin-4-yl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
0.00158
-
at pH 7.4 and 37°C Homo sapiens N-ethyl-N-[[1-octyl-5-(pyrimidin-5-yl)-1H-indol-3-yl]methyl]ethanamine
0.00161
-
at pH 7.4 and 37°C Homo sapiens N-ethyl-N-[[5-(3-fluorophenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
0.00163
-
at pH 7.4 and 37°C Homo sapiens 5-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]-N,N-dimethylpyridin-2-amine
0.00171
-
at pH 7.4 and 37°C Homo sapiens 4-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]-N-methylbenzene-1-sulfonamide
0.00172
-
at pH 7.4 and 37°C Homo sapiens N-ethyl-N-([5-[4-(methanesulfonyl)phenyl]-1-octyl-1H-indol-3-yl]methyl)ethanamine
0.00175
-
at pH 7.4 and 37°C Homo sapiens N-ethyl-N-[[1-octyl-5-(pyridin-3-yl)-1H-indol-3-yl]methyl]ethanamine
0.0019
-
at pH 7.4 and 37°C Homo sapiens cysmethynil
0.00218
-
at pH 7.4 and 37°C Homo sapiens N-ethyl-N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
0.00222
-
at pH 7.4 and 37°C Homo sapiens N-ethyl-N-[(6-fluoro-1-octyl-1H-indol-3-yl)methyl]ethanamine
0.00226
-
at pH 7.4 and 37°C Homo sapiens 5-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]pyrimidine-2-carbonitrile
0.00227
-
at pH 7.4 and 37°C Homo sapiens N-ethyl-N-[(7-fluoro-1-octyl-1H-indol-3-yl)methyl]ethanamine
0.00245
-
at pH 7.4 and 37°C Homo sapiens 3-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]phenol
0.00256
-
at pH 7.4 and 37°C Homo sapiens N-ethyl-N-[[5-(2-fluorophenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
0.00261
-
at pH 7.4 and 37°C Homo sapiens N-ethyl-N-([1-octyl-5-[3-(trifluoromethyl)phenyl]-1H-indol-3-yl]methyl)ethanamine
0.00442
-
at pH 7.4 and 37°C Homo sapiens N-ethyl-N-[(4-fluoro-1-octyl-1H-indol-3-yl)methyl]ethanamine
0.00483
-
at pH 7.4 and 37°C Homo sapiens N-ethyl-N-[(5-fluoro-1-octyl-1H-indol-3-yl)methyl]ethanamine
0.00543
-
at pH 7.4 and 37°C Homo sapiens S-[(2E,6E)-8-(3-benzoylphenoxy)-3,7-dimethylocta-2,6-dien-1-yl]-N-([2-[2-([5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl]amino)ethoxy]ethoxy]acetyl)-D-cysteine

General Information

General Information Comment Organism
physiological function the enzyme plays an important role in the posttranslational modification of proteins involved in the regulation of cell growth and oncogenesis Homo sapiens