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Literature summary for 2.1.1.100 extracted from

  • Go, M.L.; Leow, J.L.; Gorla, S.K.; Schueller, A.P.; Wang, M.; Casey, P.J.
    Amino derivatives of indole as potent inhibitors of isoprenylcysteine carboxyl methyltransferase (2010), J. Med. Chem., 53, 6838-6850.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Sf9 insect cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(1-octyl-5-m-tolyl-1H-indol-3-yl)methanamine
-
Homo sapiens
1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-3-(morpholin-4-ylmethyl)-1H-indole
-
Homo sapiens
1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-3-(piperidin-1-ylmethyl)-1H-indole
-
Homo sapiens
1-(3-methylbut-2-enyl)-5-m-tolyl-1H-indole
-
Homo sapiens
1-octyl-5-m-tolyl-1H-indole
-
Homo sapiens
1-octyl-5-m-tolyl-1H-indole-3-carboxamide
-
Homo sapiens
2-(1-octyl-1H-indol-3-yl)acetamide
-
Homo sapiens
2-(1-octyl-5-phenyl-1H-indol-3-yl)acetamide
-
Homo sapiens
2-(5-(3-ethoxyphenyl)-1-octyl-1H-indol-3-yl)-N,N-diethylacetamide
-
Homo sapiens
2-(5-fluoro-1-(3-methylbut-2-enyl)-1H-indol-3-yl)acetamide
-
Homo sapiens
2-(5-fluoro-1-octyl-1H-indol-3-yl)acetamide
-
Homo sapiens
2-[5-(2-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
Homo sapiens
2-[5-(3-ethoxyphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
Homo sapiens
2-[5-(3-methoxyphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
Homo sapiens
2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(4-methylpiperazin-1-yl)ethanone
-
Homo sapiens
2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(piperidin-1-yl)ethanone
-
Homo sapiens
2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(pyrrolidin-1-yl)ethanone
-
Homo sapiens
2-[5-(3-methylphenyl)-1-[3-(trifluoromethyl)benzyl]-1H-indol-3-yl]acetamide
-
Homo sapiens
2-[5-(3-methylphenyl)-1H-indol-3-yl]acetamide
-
Homo sapiens
2-[5-(4-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
Homo sapiens
3-(1-octyl-5-m-tolyl-1H-indol-3-yl)propanamide
-
Homo sapiens
5-(3-methylphenyl)-1-octyl-3-(piperidin-1-ylmethyl)-1H-indole
-
Homo sapiens
5-(3-methylphenyl)-1-octyl-3-(pyrrolidin-1-ylmethyl)-1H-indole
-
Homo sapiens
5-(3-methylphenyl)-3-(morpholin-4-ylmethyl)-1-octyl-1H-indole
-
Homo sapiens
5-(3-methylphenyl)-3-[(4-methylpiperazin-1-yl)methyl]-1-octyl-1H-indole
-
Homo sapiens
cysmethynil
-
Homo sapiens
ethyl [5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetate
-
Homo sapiens
methyl [5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetate
-
Homo sapiens
N,N-diethyl-2-(5-(3-methoxyphenyl)-1-octyl-1H-indol-3-yl)acetamide
-
Homo sapiens
N,N-diethyl-2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
Homo sapiens
N,N-dimethyl-1-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methanamine
-
Homo sapiens
N,N-dimethyl-2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
Homo sapiens
N-((1-octyl-5-m-tolyl-1H-indol-3-yl)methyl)methanesulfonamide
-
Homo sapiens
N-(2-methylidenebut-3-en-1-yl)-2-[5-(3-methylphenyl)-1-[3-(trifluoromethyl)benzyl]-1H-indol-3-yl]acetamide
-
Homo sapiens
N-ethyl-N-((1-(3-methylbut-2-enyl)-1H-indol-3-yl)methyl) ethanamine
-
Homo sapiens
N-ethyl-N-((5-fluoro-1-(3-methylbut-2-enyl)-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-[[1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-1H-indol-3-yl]methyl]ethanamine
-
Homo sapiens
N-ethyl-N-[[5-(2-methylphenyl)-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
N-ethyl-N-[[5-(4-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
-
Homo sapiens
N-methyl-N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]propan-2-amine
-
Homo sapiens
N-[(1-octyl-5-m-tolyl-1H-indol-3-yl)methyl]acetamide
-
Homo sapiens
N-[(2E)-3,7-dimethylocta-2,6-dien-1-yl]-2-[5-(3-methylphenyl)-1-[3-(trifluoromethyl)benzyl]-1H-indol-3-yl]acetamide
-
Homo sapiens
N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]-N-(propan-2-yl)propan-2-amine
-
Homo sapiens
N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]-N-propylpropan-1-amine
-
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 + biotin-farnesyl-L-cysteine
-
Homo sapiens S-adenosyl-L-homocysteine + biotin-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
0.0005
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 5-(3-methylphenyl)-1-octyl-3-(pyrrolidin-1-ylmethyl)-1H-indole
0.0006
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N-ethyl-N-[[5-(2-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
0.0006
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N-ethyl-N-[[5-(4-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
0.0007
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N-ethyl-N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
0.0007
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 5-(3-methylphenyl)-1-octyl-3-(piperidin-1-ylmethyl)-1H-indole
0.0007
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens (1-octyl-5-m-tolyl-1H-indol-3-yl)methanamine
0.0008
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]-N-propylpropan-1-amine
0.0008
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N,N-diethyl-2-(5-(3-methoxyphenyl)-1-octyl-1H-indol-3-yl)acetamide
0.0009
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N-methyl-N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]propan-2-amine
0.0009
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 5-(3-methylphenyl)-3-[(4-methylpiperazin-1-yl)methyl]-1-octyl-1H-indole
0.001
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 2-[5-(2-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
0.001
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 2-[5-(4-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
0.001
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 2-(5-(3-ethoxyphenyl)-1-octyl-1H-indol-3-yl)-N,N-diethylacetamide
0.0011
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N-[(2E)-3,7-dimethylocta-2,6-dien-1-yl]-2-[5-(3-methylphenyl)-1-[3-(trifluoromethyl)benzyl]-1H-indol-3-yl]acetamide
0.0012
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(pyrrolidin-1-yl)ethanone
0.0012
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 3-(1-octyl-5-m-tolyl-1H-indol-3-yl)propanamide
0.0012
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N-((1-octyl-5-m-tolyl-1H-indol-3-yl)methyl)methanesulfonamide
0.0013
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 2-[5-(3-ethoxyphenyl)-1-octyl-1H-indol-3-yl]acetamide
0.0013
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N,N-dimethyl-1-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methanamine
0.0014
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N,N-diethyl-2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
0.0015
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens cysmethynil
0.0015
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N,N-dimethyl-2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
0.0017
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]-N-(propan-2-yl)propan-2-amine
0.0017
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(4-methylpiperazin-1-yl)ethanone
0.0018
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(piperidin-1-yl)ethanone
0.0018
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 2-(1-octyl-5-phenyl-1H-indol-3-yl)acetamide
0.0018
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N-[(1-octyl-5-m-tolyl-1H-indol-3-yl)methyl]acetamide
0.0019
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 2-[5-(3-methoxyphenyl)-1-octyl-1H-indol-3-yl]acetamide
0.002
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-3-(morpholin-4-ylmethyl)-1H-indole
0.0021
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-3-(piperidin-1-ylmethyl)-1H-indole
0.0024
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N-ethyl-N-[[1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-1H-indol-3-yl]methyl]ethanamine
0.0025
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 2-[5-(3-methylphenyl)-1-[3-(trifluoromethyl)benzyl]-1H-indol-3-yl]acetamide
0.0027
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 5-(3-methylphenyl)-3-(morpholin-4-ylmethyl)-1-octyl-1H-indole
0.0041
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N-ethyl-N-[(5-fluoro-1-octyl-1H-indol-3-yl)methyl]-ethanamine
0.0065
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 2-(1-octyl-1H-indol-3-yl)acetamide
0.007
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 2-(5-fluoro-1-octyl-1H-indol-3-yl)acetamide
0.0077
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N-(2-methylidenebut-3-en-1-yl)-2-[5-(3-methylphenyl)-1-[3-(trifluoromethyl)benzyl]-1H-indol-3-yl]acetamide
0.03
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 1-octyl-5-m-tolyl-1H-indole-3-carboxamide
0.033
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 2-[5-(3-methylphenyl)-1H-indol-3-yl]acetamide
0.035
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N-ethyl-N-((5-fluoro-1-(3-methylbut-2-enyl)-1H-indol-3-yl)methyl)ethanamine
0.067
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens N-ethyl-N-((1-(3-methylbut-2-enyl)-1H-indol-3-yl)methyl) ethanamine
0.069
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 2-(5-fluoro-1-(3-methylbut-2-enyl)-1H-indol-3-yl)acetamide
0.076
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens methyl [5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetate
0.1
-
IC50 above 0.1 mM, in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens ethyl [5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetate
0.1
-
IC50 above 0.1 mM, in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 1-octyl-5-m-tolyl-1H-indole
0.1
-
IC50 above 0.1 mM, in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C Homo sapiens 1-(3-methylbut-2-enyl)-5-m-tolyl-1H-indole