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Literature summary for 2.1.1.100 extracted from

  • Majmudar, J.D.; Hodges-Loaiza, H.B.; Hahne, K.; Donelson, J.L.; Song, J.; Shrestha, L.; Harrison, M.L.; Hrycyna, C.A.; Gibbs, R.A.
    Amide-modified prenylcysteine based Icmt inhibitors: Structure-activity relationships, kinetic analysis and cellular characterization (2012), Bioorg. Med. Chem., 20, 283-295.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(R)-2-(2-((benzyloxy)methyl)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)-thio)propanoic acid
-
Homo sapiens
(R)-2-(2-(phenoxymethyl)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
Homo sapiens
(R)-2-(2-(phenylthio)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
Homo sapiens
(R)-2-(2-benzylbenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
Homo sapiens
(R)-2-(2-phenoxybenzamido)-3-(((2E,6E,10E)-3,7,11,15-tetramethylhexadeca-2,6,10,14-tetraen-1-yl)thio)propanoic acid
-
Homo sapiens
(R)-2-(2-phenoxybenzamido)-3-(undecylthio)propanoic acid
-
Homo sapiens
(R)-2-(3-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
Homo sapiens
(R)-2-(4-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
Homo sapiens
(R)-2-(dibenzo[b,d]furan-4-carboxamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)-propanoic acid
-
Homo sapiens
(R)-2-(N-methyl-2-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
Homo sapiens
(R,E)-3-((3,7-dimethylocta-2,6-dien-1-yl)thio)-2-(2-phenoxybenzamido)propanoic acid
-
Homo sapiens
(S)-2-(2-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
Homo sapiens
2-phenoxy-phenylfarnesylcysteine low micromolar inhibitor Homo sapiens
N-[2-(benzyloxy)benzoyl]-S-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-L-cysteine
-
Homo sapiens
S-{(2E)-3-[2-(biphenyl-4-yl)ethyl]-6-methylhepta-2,5-dien-1-yl}-N-(2-phenoxybenzoyl)-L-homocysteine low micromolar inhibitor Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
JURKAT cell
-
Homo sapiens
-

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0025
-
in 100 mM Tris-HCl, pH 7.5, at 30°C Homo sapiens S-{(2E)-3-[2-(biphenyl-4-yl)ethyl]-6-methylhepta-2,5-dien-1-yl}-N-(2-phenoxybenzoyl)-L-homocysteine
0.0062
-
in 100 mM Tris-HCl, pH 7.5, at 30°C Homo sapiens 2-phenoxy-phenylfarnesylcysteine
0.0067
-
in 100 mM Tris-HCl, pH 7.5, at 30°C Homo sapiens (R)-2-(N-methyl-2-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
0.0078
-
in 100 mM Tris-HCl, pH 7.5, at 30°C Homo sapiens (S)-2-(2-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
0.0134
-
in 100 mM Tris-HCl, pH 7.5, at 30°C Homo sapiens N-[2-(benzyloxy)benzoyl]-S-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-L-cysteine
0.0147
-
in 100 mM Tris-HCl, pH 7.5, at 30°C Homo sapiens (R)-2-(2-(phenylthio)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
0.0226
-
in 100 mM Tris-HCl, pH 7.5, at 30°C Homo sapiens (R)-2-(3-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
0.038
-
in 100 mM Tris-HCl, pH 7.5, at 30°C Homo sapiens (R)-2-(2-benzylbenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
0.038
-
in 100 mM Tris-HCl, pH 7.5, at 30°C Homo sapiens (R)-2-(2-phenoxybenzamido)-3-(((2E,6E,10E)-3,7,11,15-tetramethylhexadeca-2,6,10,14-tetraen-1-yl)thio)propanoic acid
0.049
-
in 100 mM Tris-HCl, pH 7.5, at 30°C Homo sapiens (R)-2-(2-((benzyloxy)methyl)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)-thio)propanoic acid
0.058
-
in 100 mM Tris-HCl, pH 7.5, at 30°C Homo sapiens (R)-2-(dibenzo[b,d]furan-4-carboxamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)-propanoic acid
0.063
-
in 100 mM Tris-HCl, pH 7.5, at 30°C Homo sapiens (R)-2-(4-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
0.075
-
in 100 mM Tris-HCl, pH 7.5, at 30°C Homo sapiens (R)-2-(2-(phenoxymethyl)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
0.149
-
in 100 mM Tris-HCl, pH 7.5, at 30°C Homo sapiens (R,E)-3-((3,7-dimethylocta-2,6-dien-1-yl)thio)-2-(2-phenoxybenzamido)propanoic acid
0.21
-
in 100 mM Tris-HCl, pH 7.5, at 30°C Homo sapiens (R)-2-(2-phenoxybenzamido)-3-(undecylthio)propanoic acid

General Information

General Information Comment Organism
metabolism the enzyme is responsible for the last common step of the posttranslational processing pathway of CaaX proteins Homo sapiens