Information on EC 2.1.1.100 - protein-S-isoprenylcysteine O-methyltransferase

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The expected taxonomic range for this enzyme is: Eukaryota, Archaea

EC NUMBER
COMMENTARY
2.1.1.100
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RECOMMENDED NAME
GeneOntology No.
protein-S-isoprenylcysteine O-methyltransferase
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine = S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
kinetic mechanism
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S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine = S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
ordered bi bi mechanism, S-adenosyl-L-methionine binds first, S-adenosyl-L-homocysteine departs last
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
methyl group transfer
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PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
Biosynthesis of antibiotics
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Terpenoid backbone biosynthesis
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SYSTEMATIC NAME
IUBMB Comments
S-adenosyl-L-methionine:protein-C-terminal-S-farnesyl-L-cysteine O-methyltransferase
C-terminal S-geranylgeranylcysteine and S-geranylcysteine residues are also methylated, but more slowly.
SYNONYMS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
farnesyl cysteine C-terminal methyltransferase
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farnesyl-protein carboxymethyltransferase
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farnesylated protein C-terminal O-methyltransferase
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isoprenylated protein methyltransferase
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methyltransferase, protein C-terminal farnesylcysteine O-
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prenylated protein methyltransferase
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protein S-farnesylcysteine C-terminal methyltransferase
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S-farnesylcysteine methyltransferase
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CAS REGISTRY NUMBER
COMMENTARY
130731-20-3
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GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
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cell migration and adhesion are impaired by enzyme inhibition (the actin cytoskeleton remains unorganized and lacks peripgeral actin filaments and stress fiber formation in the interior of the cell)
metabolism
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methylation of the C-terminus by Icmt is the final step in the prenylation pathway. The prenylation pathway consists of three enzymatic steps, the final processed protein is isoprenoid modified and methylated on the C-terminal cysteine. This protein modification pathway plays a significant role in cancer biology because many oncogenic proteins undergo prenylation
metabolism
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the enzyme is involved in the farnesyl metabolism, overview
metabolism
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the enzyme is responsible for the last common step of the posttranslational processing pathway of CaaX proteins
physiological function
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isoprenylcysteine methylation and demethylation positively regulate abscisic acid signaling in Arabidopsis thaliana via feedback mechanism involving demethylation and inactivation of isoprenylated negative regulators of abscisic acid signaling
physiological function
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isoprenylcysteine carboxylmethyltransferase plays a role in cell migration and adhesion
physiological function
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methylation of Ras by the enzyme is required for proper localization to the plasma membrane and downstream signaling
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
S-adenosyl-L-methionine + (RhoAA) C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + (RhoA) C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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the enzyme modulates endothelial monolayer per meability by altering RhoA carboxyl methylation and activation, thus changing the organization of intercellular junctions. Carboxy methylation of RhoA may modulate endothelial barrier function
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?
S-adenosyl-L-methionine + biotin-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + biotin-farnesyl-L-cysteine methyl ester
show the reaction diagram
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-
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?
S-adenosyl-L-methionine + farnesylated and Rce1-proteolyzed K-Ras protein
?
show the reaction diagram
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?
S-adenosyl-L-methionine + N-acetyl-S-(3-(3-methylbut-2-enyl)-7,11-dimethyldodeca-2Z,6E,10-trien-1-yl)-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-(3-(3-methylbut-2-enyl)-7,11-dimethyldodeca-2Z,6E,10-trien-1-yl)-L-cysteine methyl ester
show the reaction diagram
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relatively good substrate for the human Icmt enzyme
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?
S-adenosyl-L-methionine + N-acetyl-S-(E)-geranyl-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-(E)-geranyl-L-cysteine methyl ester
show the reaction diagram
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-
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?
S-adenosyl-L-methionine + N-acetyl-S-all trans-geranylgeranyl-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-all trans-geranylgeranyl-L-cysteine methyl ester
show the reaction diagram
Q93W54
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S-adenosyl-L-methionine + N-acetyl-S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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-
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?
S-adenosyl-L-methionine + N-acetyl-S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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?
S-adenosyl-L-methionine + N-acetyl-S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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isoprenoid moiety as a key substrate recognition element for Icmt
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?
S-adenosyl-L-methionine + N-acetyl-S-geranylgeranyl-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-geranylgeranyl-L-cysteine methyl ester
show the reaction diagram
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?
S-adenosyl-L-methionine + N-acetyl-S-geranylgeranyl-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-geranylgeranyl-L-cysteine methyl ester
show the reaction diagram
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-
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?
S-adenosyl-L-methionine + N-acetyl-S-geranylgeranyl-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-geranylgeranyl-L-cysteine methyl ester
show the reaction diagram
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?
S-adenosyl-L-methionine + N-acetyl-S-geranylgeranyl-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-geranylgeranyl-L-cysteine methyl ester
show the reaction diagram
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-
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?
S-adenosyl-L-methionine + N-acetyl-S-geranylgeranyl-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-geranylgeranyl-L-cysteine methyl ester
show the reaction diagram
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-
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S-adenosyl-L-methionine + N-acetyl-S-geranylgeranyl-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-geranylgeranyl-L-cysteine methyl ester
show the reaction diagram
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?
S-adenosyl-L-methionine + N-acetyl-S-geranylgeranyl-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-geranylgeranyl-L-cysteine methyl ester
show the reaction diagram
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?
S-adenosyl-L-methionine + N-acetyl-S-geranylgeranyl-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-geranylgeranyl-L-cysteine methyl ester
show the reaction diagram
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?
S-adenosyl-L-methionine + N-acetyl-S-geranylgeranyl-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-geranylgeranyl-L-cysteine methyl ester
show the reaction diagram
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no activity with N-acetyl-S-trans-geranyl-L-cysteine
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?
S-adenosyl-L-methionine + N-acetyl-S-geranylgeranyl-L-cysteine methyl ester
S-adenosyl-L-homocysteine + N-acetyl-S-geranylgeranyl-L-cysteine methyl ester
show the reaction diagram
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?
S-adenosyl-L-methionine + N-acetyl-S-geranylgeranyl-L-cysteinyl-L-alanyl-S-geranylgeranyl-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-geranylgeranyl-L-cysteinyl-L-alanyl-S-geranylgeranyl-L-cysteine methyl ester
show the reaction diagram
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no activity with + N-acetyl-S-geranylgeranyl-L-cysteinyl-S-geranylgeranyl-L-cysteine
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?
S-adenosyl-L-methionine + N-acetyl-S-trans,trans-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-trans,trans-farnesyl-L-cysteine methyl ester
show the reaction diagram
Q93W54
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S-adenosyl-L-methionine + N-acetyl-S-[(2E,6E)-farnesyl]-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-[(2E,6E)-farnesyl]-L-cysteine methyl ester
show the reaction diagram
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ir
S-adenosyl-L-methionine + N-acetyl-S-[(2E,6E)-farnesyl]-L-cysteine
S-adenosyl-L-homocysteine + N-acetyl-S-[(2E,6E)-farnesyl]-L-cysteine methyl ester
show the reaction diagram
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?
S-adenosyl-L-methionine + N-biotinyl-S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + N-biotinyl-S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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S-adenosyl-L-methionine + N-biotinyl-S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + N-biotinyl-S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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S-adenosyl-L-homocysteine is the final product released
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?
S-adenosyl-L-methionine + N-biotinyl-S-farnesyl-L-cysteine peptide
S-adenosyl-L-homocysteine + biotin S-farnesyl-L-cysteine peptide methyl ester
show the reaction diagram
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S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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-
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?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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-
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?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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-
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?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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-
-
?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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-
-
?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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gamma-subunit of heterotrimeric G-proteins
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?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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ras-proteins
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?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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ras-proteins
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?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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ras-proteins
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?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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enzyme can methylate both peptides and proteins
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?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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21000-24000 Da GTP-binding proteins
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?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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methyl esterification of proteins containing a C-terminal-CXXX sequence requires not only the removal of the 3 terminal amino acids but the isoprenylation of the sulfhydryl group as well
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?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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fusion protein of heat-inducible ubiquitin and the 11 C-terminal amino acid sequence of Ha-ras protein
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?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
methylation of a 23000 Da small G protein is indicated
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S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
a-factor, Ras1 and Ras2
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?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
carboxyl methylation may play a role in the regulation of receptor mediated signal transduction processes in eukaryotic cells
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S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
a-factor mating pheromone, Ras1 and Ras2 are putative substrates of the enzyme
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?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
reversible methylation of ras-proteins may play an important role in the modulation of their signaling properties
-
?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
the protein is involved in posttranslational modifications of Ras proteins
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?
S-adenosyl-L-methionine + Ras2p
S-adenosyl-L-homocysteine + ?
show the reaction diagram
-
-
-
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?
S-adenosyl-L-methionine + S-[(2E,6E)-farnesyl]-3-sulfanylpropanoic acid
S-adenosyl-L-homocysteine + methyl S-[(2E,6E)-farnesyl]-3-sulfanylpropanoate
show the reaction diagram
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-
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?
S-adenosyl-L-methionine + S-[(2E,6E)-farnesyl]-sulfanylacetic acid
S-adenosyl-L-homocysteine + methyl S-[(2E,6E)-farnesyl]-sulfanylacetate
show the reaction diagram
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-
-
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?
S-adenosylmethionine + N-((benzoylglycyl)glycyl)-S-farnesyl-L-cysteine
S-adenosylhomocysteine + N-((benzoylglycyl)glycyl)-S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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-
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?
S-adenosylmethionine + N-(benzoylglycyl)-S-farnesyl-L-cysteine
S-adenosylhomocysteine + N-(benzoylglycyl)-S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
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?
S-adenosylmethionine + N-acetyl-S-(E,E)-farnesyl-D-cysteine
S-adenosylhomocysteine + N-acetyl-S-(E,E)-farnesyl-D-cysteine methyl ester
show the reaction diagram
-
-
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?
S-adenosylmethionine + N-acetyl-S-(E,E)-farnesyl-L-cysteine
S-adenosylhomocysteine + N-acetyl-S-(E,E)-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
-
-
?
S-adenosylmethionine + N-acetyl-S-(E,E)-farnesyl-L-cysteine
S-adenosylhomocysteine + N-acetyl-S-(E,E)-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
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?
S-adenosylmethionine + N-acetyl-S-(E,E)-farnesyl-L-cysteine
S-adenosylhomocysteine + N-acetyl-S-(E,E)-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
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S-adenosylmethionine + N-acetyl-S-(E,E)-farnesyl-L-cysteine
S-adenosylhomocysteine + N-acetyl-S-(E,E)-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
-
?
S-adenosylmethionine + N-acetyl-S-(E,E)-farnesyl-L-cysteine
S-adenosylhomocysteine + N-acetyl-S-(E,E)-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
-
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S-adenosylmethionine + N-acetyl-S-(E,E)-farnesyl-L-cysteine
S-adenosylhomocysteine + N-acetyl-S-(E,E)-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
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S-adenosylmethionine + N-acetyl-S-(E,E)-farnesyl-L-cysteine
S-adenosylhomocysteine + N-acetyl-S-(E,E)-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
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S-adenosylmethionine + N-acetyl-S-(E,E)-farnesyl-L-cysteine
S-adenosylhomocysteine + N-acetyl-S-(E,E)-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
-
?
S-adenosylmethionine + N-acetyl-S-(E,E)-farnesyl-L-cysteine
S-adenosylhomocysteine + N-acetyl-S-(E,E)-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
-
?
S-adenosylmethionine + N-acetyl-S-(E,E)-farnesyl-L-cysteine
S-adenosylhomocysteine + N-acetyl-S-(E,E)-farnesyl-L-cysteine methyl ester
show the reaction diagram
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-
-
?
S-adenosylmethionine + N-acetyl-S-(E,E)-farnesyl-L-cysteine
S-adenosylhomocysteine + N-acetyl-S-(E,E)-farnesyl-L-cysteine methyl ester
show the reaction diagram
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recombinant enzyme: 50fold higher activity than with N-acetyl-S-geranylgeranyl-L-cysteine, native enzyme: 40fold higher activity than with N-acetyl-S-geranylgeranyl-L-cysteine
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?
S-adenosylmethionine + N-acetyl-S-3,3-dimethylallyl-L-cysteine
S-adenosylhomocysteine + N-acetyl-S-3,3-dimethylallyl-L-cysteine methyl ester
show the reaction diagram
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-
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?
S-adenosylmethionine + N-isobutyryl-S-farnesyl-L-cysteine
S-adenosylhomocysteine + N-isobutyryl-S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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-
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?
S-adenosylmethionine + N-isovaleryl-S-farnesyl-L-cysteine
S-adenosylhomocysteine + N-isovaleryl-S-farnesyl-L-cysteine methyl ester
show the reaction diagram
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-
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?
S-adenosylmethionine + S-decyl-Leu-Ala-Arg-Tyr-Lys-Cys
S-adenosylhomocysteine + S-decyl-Leu-Ala-Arg-Tyr-Lys-Cys methyl ester
show the reaction diagram
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-
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?
S-adenosylmethionine + S-farnesyl-Leu-Ala-Arg-Tyr-Lys-Cys
S-adenosylhomocysteine + S-farnesyl-Leu-Ala-Arg-Tyr-Lys-Cys methyl ester
show the reaction diagram
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?
S-adenosylmethionine + S-farnesyl-Leu-Ala-Arg-Tyr-Lys-Cys
S-adenosylhomocysteine + S-farnesyl-Leu-Ala-Arg-Tyr-Lys-Cys methyl ester
show the reaction diagram
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?
S-adenosylmethionine + S-farnesyl-Leu-Ala-Arg-Tyr-Lys-Cys
S-adenosylhomocysteine + S-farnesyl-Leu-Ala-Arg-Tyr-Lys-Cys methyl ester
show the reaction diagram
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-
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?
S-adenosylmethionine + S-farnesyl-Leu-Ala-Arg-Tyr-Lys-Cys
S-adenosylhomocysteine + S-farnesyl-Leu-Ala-Arg-Tyr-Lys-Cys methyl ester
show the reaction diagram
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-
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?
S-adenosylmethionine + S-farnesyl-Leu-Ala-Arg-Tyr-Lys-Cys
S-adenosylhomocysteine + S-farnesyl-Leu-Ala-Arg-Tyr-Lys-Cys methyl ester
show the reaction diagram
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-
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?
S-adenosylmethionine + S-geranyl-Leu-Ala-Arg-Tyr-Lys-Cys
S-adenosylhomocysteine + S-geranyl-Leu-Ala-Arg-Tyr-Lys-Cys methyl ester
show the reaction diagram
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-
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?
S-adenosylmethionine + S-geranylgeranyl-Leu-Ala-Arg-Tyr-Lys-Cys
S-adenosylhomocysteine + S-geranylgeranyl-Leu-Ala-Arg-Tyr-Lys-Cys methyl ester
show the reaction diagram
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?
S-adenosylmethionine + S-octyl-Leu-Ala-Arg-Tyr-Lys-Cys
S-adenosylhomocysteine + S-octyl-Leu-Ala-Arg-Tyr-Lys-Cys methyl ester
show the reaction diagram
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?
S-adenosylmethionine + S-pentadecyl-Leu-Ala-Arg-Tyr-Lys-Cys
S-adenosylhomocysteine + S-pentadecyl-Leu-Ala-Arg-Tyr-Lys-Cys methyl ester
show the reaction diagram
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-
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?
S-adenosylmethionine + S-tridecyl-Leu-Ala-Arg-Tyr-Lys-Cys
S-adenosylhomocysteine + S-tridecyl-Leu-Ala-Arg-Tyr-Lys-Cys methyl ester
show the reaction diagram
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?
additional information
?
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overexpression of the enzyme may protect against endothelial cell apoptosis by enhancing, the carboxyl methylation posttranslational modification, activity, and subsequent intracellular signalling pathway of Ras GTPase
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additional information
?
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the enzyme regulates Rac1 activity by controlling the interaction of Rac1 activity by controlling the interaction of Rac1 with Rho guanine nucleotide dissociation inhibitor, the enzyme regulates membrane accumulation and GTP loading of Rac1
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additional information
?
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inhibition of Icmt significantly decreases the activation of both RhoA and Rac1 involving Rho GDP-dissociation inhibitor, RhoGDI, overview. Icmt inhibition impairs RhoGTPase activation
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additional information
?
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Q93W54
the ICMT isozyme catalyzes the methylation of C-terminal isoprenylcysteines
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additional information
?
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Pseudoceratina sp.
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isoprenylcysteine carboxyl methyltransferase methylates the carboxyl-terminal isoprenylcysteine of CAAX proteins
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additional information
?
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Q93W54
isozyme substrate specificity, no activity with N-acetyl-S-trans-geranyl-L-cysteine, overview
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additional information
?
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Pseudoceratina sp. 1247
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isoprenylcysteine carboxyl methyltransferase methylates the carboxyl-terminal isoprenylcysteine of CAAX proteins
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NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
S-adenosyl-L-methionine + (RhoAA) C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + (RhoA) C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
the enzyme modulates endothelial monolayer per meability by altering RhoA carboxyl methylation and activation, thus changing the organization of intercellular junctions. Carboxy methylation of RhoA may modulate endothelial barrier function
-
-
?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
carboxyl methylation may play a role in the regulation of receptor mediated signal transduction processes in eukaryotic cells
-
-
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
a-factor mating pheromone, Ras1 and Ras2 are putative substrates of the enzyme
-
?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
reversible methylation of ras-proteins may play an important role in the modulation of their signaling properties
-
?
S-adenosyl-L-methionine + protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
the protein is involved in posttranslational modifications of Ras proteins
-
-
?
additional information
?
-
-
overexpression of the enzyme may protect against endothelial cell apoptosis by enhancing, the carboxyl methylation posttranslational modification, activity, and subsequent intracellular signalling pathway of Ras GTPase
-
-
-
additional information
?
-
-
the enzyme regulates Rac1 activity by controlling the interaction of Rac1 activity by controlling the interaction of Rac1 with Rho guanine nucleotide dissociation inhibitor, the enzyme regulates membrane accumulation and GTP loading of Rac1
-
-
-
additional information
?
-
-
inhibition of Icmt significantly decreases the activation of both RhoA and Rac1 involving Rho GDP-dissociation inhibitor, RhoGDI, overview. Icmt inhibition impairs RhoGTPase activation
-
-
-
additional information
?
-
Q93W54
the ICMT isozyme catalyzes the methylation of C-terminal isoprenylcysteines
-
-
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
S-adenosyl-L-methionine
-
-
S-adenosyl-L-methionine
Q93W54
;
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Li+
-
slight stimulation
additional information
-
metal ions are required
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(2R)-2-(acetylamino)-3-[[(2Z)-3,4-diphenylbut-2-en-1-yl]sulfanyl]propanoic acid
-
15.7% inhibition at 0.01 mM
(2R)-2-(acetylamino)-3-[[(2Z)-4-(2-fluorophenyl)-3-phenylbut-2-en-1-yl]sulfanyl]propanoic acid
-
25.3% inhibition at 0.01 mM
(3,5-difluoro-4-methoxyphenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
-
-
-
(3-chloro-4-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
-
-
-
(3-chlorophenyl)-[2-(2,2-dimethyl-4-thiophen-2-yltetrahydropyran-4-yl)ethyl]amine
-
-
-
(4-chloro-3-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
-
-
-
(5-chloro-2-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
-
-
-
(R)-2-(2-((benzyloxy)methyl)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)-thio)propanoic acid
-
-
-
(R)-2-(2-(phenoxymethyl)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
-
-
(R)-2-(2-(phenylthio)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
-
-
(R)-2-(2-benzylbenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
-
-
(R)-2-(2-phenoxybenzamido)-3-(((2E,6E,10E)-3,7,11,15-tetramethylhexadeca-2,6,10,14-tetraen-1-yl)thio)propanoic acid
-
-
-
(R)-2-(2-phenoxybenzamido)-3-(undecylthio)propanoic acid
-
-
-
(R)-2-(3-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
-
-
(R)-2-(4-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
-
-
(R)-2-(dibenzo[b,d]furan-4-carboxamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)-propanoic acid
-
-
-
(R)-2-(N-methyl-2-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
-
-
(R,E)-3-((3,7-dimethylocta-2,6-dien-1-yl)thio)-2-(2-phenoxybenzamido)propanoic acid
-
-
-
(S)-2-(2-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
-
-
(S)-glabrol
-
structure determination, overview
1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-fluorophenyl)thiourea
-
-
-
1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-methoxphenyl)urea
-
-
-
1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-methoxyphenyl)thiourea
-
-
-
1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-phenylthiourea
-
-
-
1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-3-(morpholin-4-ylmethyl)-1H-indole
-
-
1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-3-(piperidin-1-ylmethyl)-1H-indole
-
-
1-(3-chlorophenyl)-3-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)thiourea
-
-
-
1-(3-chlorophenyl)-3-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)urea
-
-
-
1-(3-methylbut-2-enyl)-5-m-tolyl-1H-indole
-
-
-
1-(octyl-5-m-tolyl-1H-indol-3-yl)methanamine
-
-
-
1-ethyl-3-(3-dimethylaminopropyl)carbodiimide
-
22% inhibition
1-octyl-5-(3-methylphenyl)-1H-indole
-
a cysmethynil analogue
1-octyl-5-m-tolyl-1H-indole
-
-
-
1-octyl-5-m-tolyl-1H-indole-3-carboxamide
-
-
-
2'-methoxy-3',3''-diprenyl-licodione
-
isolated from Hovea parvicalyx, collected in Australia, structure determination, overview
2'-methoxy-3'-prenyllicodione
-
isolated from Hovea parvicalyx, collected in Australia, structure determination, overview
2-(1-octyl-1H-indol-3-yl)acetamide
-
-
2-(1-octyl-5-phenyl-1H-indol-3-yl)acetamide
-
-
2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-N-(3-methoxyphenyl)acetamide
-
-
-
2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-N-phenylacetamide
-
-
-
2-(5-(3-ethoxyphenyl)-1-octyl-1H-indol-3-yl)-N,N-diethylacetamide
-
-
-
2-(5-fluoro-1-(3-methylbut-2-enyl)-1H-indol-3-yl)acetamide
-
-
-
2-(5-fluoro-1-octyl-1H-indol-3-yl)acetamide
-
-
2-Carboxy-2'-hydroxy-5'-sulfoformazylbenzene
-
IC50: 1.1 mM
2-phenoxy-phenylfarnesylcysteine
-
low micromolar inhibitor
2-[5-(2-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
-
2-[5-(3-ethoxyphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
-
2-[5-(3-methoxyphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
-
2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(4-methylpiperazin-1-yl)ethanone
-
-
2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(piperidin-1-yl)ethanone
-
-
2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[5-(3-methylphenyl)-1-[3-(trifluoromethyl)benzyl]-1H-indol-3-yl]acetamide
-
-
2-[5-(3-methylphenyl)-1H-indol-3-yl]acetamide
-
-
2-[5-(4-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
-
2-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl](phenyl)amino]-1-(furan-2-yl)ethanone
-
-
2584 Da liver peptide
-
0.000071 mM, 50% inhibition
-
3,4-dichloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2Hpyran-4-yl)ethyl]aniline
-
-
-
3,5-dichloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
-
-
-
3-(1-octyl-5-m-tolyl-1H-indol-3-yl)propanamide
-
-
-
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
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
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
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
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
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
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
3-chloro-4-methyl-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)ethyl]aniline
-
-
-
3-chloro-4-methyl-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]aniline
-
-
-
3-chloro-N-(3-chlorophenyl)-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydropyran-4-yl)ethyl]aniline
-
-
-
3-chloro-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)-ethyl]aniline
-
-
-
3-chloro-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydrothiopyran-4-yl)ethyl]aniline
-
-
-
3-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-4-methylaniline
-
-
-
3-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
-
-
-
3-chloro-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
-
-
-
3-fluoro-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)-ethyl]aniline
-
-
-
3-fluoro-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
-
-
-
3-methoxy-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)-ethyl]aniline
-
-
-
3-methoxy-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydropyran-4-yl)ethyl]aniline
-
-
-
3-methoxy-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydrothiopyran-4-yl)ethyl]aniline
-
-
-
3-methoxy-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
-
-
-
3-methoxy-N-[2-[4-(4-methoxyphenyl)-2,2-dimethyltetrahydro-2H-pyran-4-yl]ethyl]aniline
-
-
-
3-methyl-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
-
-
-
3-tert-butyl-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
-
-
-
3-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethylamino]benzoic acid
-
-
-
3-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethylamino]phenol
-
-
-
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
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
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
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
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
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
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
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
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
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
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
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
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
3-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]-N,N-dimethylbenzenesulfonamide
-
-
-
3-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]benzonitrile
-
-
-
4-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-3-methylaniline
-
-
-
4-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
-
-
-
4-hydroxyphenylglyoxal
-
48% inhibition
4-tert-butyl-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
-
-
-
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
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
4-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]benzenesulfonamide
-
-
-
4-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]benzonitrile
-
-
-
5'-deoxymethylthioadenosine
-
-
5-(3-methylphenyl)-1-octyl-3-(piperidin-1-ylmethyl)-1H-indole
-
-
5-(3-methylphenyl)-1-octyl-3-(pyrrolidin-1-ylmethyl)-1H-indole
-
-
5-(3-methylphenyl)-3-(morpholin-4-ylmethyl)-1-octyl-1H-indole
-
-
5-(3-methylphenyl)-3-[(4-methylpiperazin-1-yl)methyl]-1-octyl-1H-indole
-
-
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
adenosine
-
plus homocysteine
aplysamine 6
Pseudoceratina sp.
-
i.e. (2E)-N-{2-[4-(3-aminopropoxy)-3,5-dibromophenyl]ethyl}-3-(3-bromo-4-methoxyphenyl)acrylamide
aplysamine 6
-
-
Ca2+
-
moderate inhibition
CTAB
-
0.1%, more than 90% inhibition
Cu2+
-
complete inhibition
cysmethynil
-
time-dependent inhibitor, competitive inhibitor with respect to the isoprenylated cysteine substrate and a noncompetitive inhibitor with respect to S-adenosyl-L-methionine
cysmethynil
-
most potent time-dependent inhibitor, inhibition of cell growth in an Icmt-dependent fashion
cysmethynil
-
specific inhibitor, is also able to inhibit Ras-mediated signaling, cell growth, and oncogenesis, and it affects cell adhesion and cell spreading
cysmethynil
-
-
cysmethynil
-
relatively potent in vitro inhibitor
deoxycholate
-
0.1%, 51% inhibition
Diethylpyrocarbonate
-
96% inhibition
dimethylsulfoxid
-
more than 4% cause inhibition
ethyl 4-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]amino]benzoate
-
-
-
ethyl [5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetate
-
-
FTI-2628
-
-
-
Hg2+
-
complete inhibition
iodoacetic acid
-
16% inhibition
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
methyl ester of N-acetyl-S-farnesyl-L-cysteine
-
-
methyl [5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetate
-
-
methylthioadenosine
-
0.9 mM, 50% inhibition
Mg2+
-
inhibition of 23000 Da protein methylation
Mg2+
-
moderate inhibition
Mn2+
-
moderate inhibition
N'-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N,N-dimethylbenzene-1,3-diamine
-
-
-
N,N'-dicyclohexylcarbodiimide
-
76% inhibition
N,N-diethyl-2-(5-(3-methoxyphenyl)-1-octyl-1H-indol-3-yl)acetamide
-
-
-
N,N-diethyl-2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
-
N,N-dimethyl-1-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methanamine
-
-
N,N-dimethyl-2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
-
N-((1-octyl-5-m-tolyl-1H-indol-3-yl)methyl)methanesulfonamide
-
-
-
N-(2-methylidenebut-3-en-1-yl)-2-[5-(3-methylphenyl)-1-[3-(trifluoromethyl)benzyl]-1H-indol-3-yl]acetamide
-
-
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
N-(3-chlorophenyl)-2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)acetamide
-
-
-
N-(3-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]phenyl)acetamide
-
-
-
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
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
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
N-Acetyl-S-(3-(3-methylbut-2-enyl)-5-(4-phenyl)phenylpent-2Z-en-1-yl)-L-cysteine
-
shows a mix of competitive and uncompetitive inhibition
N-acetyl-S-(3-(3-methylbut-2-enyl)-7,11-dimethyldodeca-2Z,6E,10-trien-1-yl)-L-cysteine
-
competitive inhibitor of overexpressed yeast Icmt
N-acetyl-S-(E,E)-farnesyl-L-cysteine
-
-
N-acetyl-S-(E,E)-farnesyl-L-cysteine methyl ester
-
mixed-type vs. N-acetyl-S-(E,E)-farnesyl-L-cysteine
N-acetyl-S-(E,E)-geranylgeranyl-L-cysteine
-
-
N-acetyl-S-farnesyl-L-cysteine
-
-
N-acetyl-S-farnesyl-L-cysteine
-
complete inhibition at 0.025 mM
N-acetyl-S-farnesyl-L-cysteine methyl ester
-
-
N-acetyl-S-farnesyl-L-cysteine methylester
-
noncompetitive inhibition with respect to biotin-S-farnesyl-L-cysteine, mixed type inhibition with respect to S-adenosyl-L-methionine
N-acetyl-S-geranylgeranyl-L-cysteine
-
inhibition of N-acetyl-S-farnesyl-L-cysteine methylation
N-acetyl-S-geranylgeranyl-L-cysteine
-
-
N-acetyl-S-[(2E)-3-methyl-4-(4-phenoxyphenoxy)but-2-en-1-yl]-L-cysteine
-
15.5% inhibition at 0.01 mM
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
N-acetyl-S-[(2E)-3-methyl-5-(4-octylphenyl)pent-2-en-1-yl]-L-cysteine
-
31.1% inhibition at 0.01 mM
N-acetyl-S-[(2E)-3-methyl-5-(4-pentylphenyl)pent-2-en-1-yl]-L-cysteine
-
23.1% inhibition at 0.01 mM
N-acetyl-S-[(2E)-3-methyl-5-(4-propylphenyl)pent-2-en-1-yl]-L-cysteine
-
20.7% inhibition at 0.01 mM
N-acetyl-S-[(2E)-3-methyl-7-(4-phenoxyphenoxy)hept-2-en-1-yl]-L-cysteine
-
19.4% inhibition at 0.01 mM
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
N-acetyl-S-[(2E)-4-(4-benzylphenoxy)-3-methylbut-2-en-1-yl]-L-cysteine
-
9.8% inhibition at 0.01 mM
N-acetyl-S-[(2E)-5-(4-hexylphenyl)-3-methylpent-2-en-1-yl]-L-cysteine
-
18.8% inhibition at 0.01 mM
N-acetyl-S-[(2Z)-4-(biphenyl-4-yl)-3-phenylbut-2-en-1-yl]-L-cysteine
-
26.6% inhibition at 0.01 mM
N-benzyl-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]furan-2-carboxamide
-
-
N-bromosuccinimide
-
56% inhibition in the presence of S-adenosyl-L-homocysteine, 87% inhibition in the absence of S-adenosyl-L-homocysteine
N-ethyl-N-((1-(3-methylbut-2-enyl)-1H-indol-3-yl)methyl) ethanamine
-
-
-
N-ethyl-N-((5-fluoro-1-(3-methylbut-2-enyl)-1H-indol-3-yl)methyl)ethanamine
-
-
-
N-ethyl-N-[(5-fluoro-1-octyl-1H-indol-3-yl)methyl]-ethanamine
-
-
-
N-ethyl-N-[[1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-1H-indol-3-yl]methyl]ethanamine
-
-
N-ethyl-N-[[5-(2-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
-
-
N-ethyl-N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
-
-
N-ethyl-N-[[5-(4-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
-
-
N-ethylmaleimide
-
2 mM, 94% inhibition after preincubation for 30 min, 45% inhibition in the presence of S-adenosyl-L-homocysteine
N-ethylmaleimide
-
moderate inhibition
N-methyl-N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]propan-2-amine
-
-
n-octyl beta-glucoside
-
0.2%, 55-75% inhibition
N-[(1-octyl-5-m-tolyl-1H-indol-3-yl)methyl]acetamide
-
-
-
N-[(2E)-3,7-dimethylocta-2,6-dien-1-yl]-2-[5-(3-methylphenyl)-1-[3-(trifluoromethyl)benzyl]-1H-indol-3-yl]acetamide
-
-
N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydropyran-4-yl)-ethyl]aniline
-
-
-
N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydrothiopyran-4-yl)ethyl]aniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-2-methylaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3,4-dimethoxyaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3,5-dimethylaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-(trifluoromethoxy)aniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-(trifluoromethyl)aniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-ethylaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-fluoroaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-isopropylaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-methoxy-4-methylaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-methoxyaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-methylaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-(trifluoromethoxy)aniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-fluoroaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-isopropylaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-methoxyaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-methylaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N,3-dimethylaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N-methylaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N-phenylacetamide
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]aniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-3,4-dimethylaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-3-nitroaniline
-
-
-
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-4-nitroaniline
-
-
-
N-[2-(benzyloxy)benzoyl]-S-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-L-cysteine
-
-
N-[3-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-3-(2-methoxyphenyl)propyl]-N-(4-methoxybenzyl)furan-2-carboxamide
-
the inhibitor is competitive with respect to a prenylated methyl acceptor substrate but noncompetitive toward the S-adenosyl-L-methionine
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
N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]-N-(propan-2-yl)propan-2-amine
-
-
N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]-N-propylpropan-1-amine
-
-
Nonidet P40
-
0.1%, 73% inhibition
Phenylglyoxal
-
74% inhibition, inhibition increases with the alkanity of the preincubation medium, S-adenosyl-L-methionine protects against inhibition
retinoic acid
-
20% decrease of N-acetyl-S-(E,E)-farnesyl-L-cysteine methylation in cells treated with 0.01 mM retinoic acid
S-(Geranylgeranyl-2-thio)acetic acid
-
-
S-adenosyl-L-homocysteine
-
-
S-adenosyl-L-homocysteine
-
competitive vs. S-adenosyl-L-methionine, mixed-type vs. N-acetyl-S-(E,E)-farnesyl-L-cysteine
S-adenosyl-L-homocysteine
-
-
S-adenosyl-L-homocysteine
-
-
S-adenosyl-L-homocysteine
-
0.02 mM, 50% inhibition
S-adenosyl-L-homocysteine
-
0.025 mM; 50% inhibition
S-adenosyl-L-homocysteine
-
0.005 mM, 50% inhibition
S-adenosyl-L-homocysteine
-
0.2 mM, 67% inhibition of the endogenous methylation of 21000-25000 Da proteins
S-adenosyl-L-homocysteine
-
competitive inhibitor with respect to S-adenosyl-L-methionine
S-adenosylethionine
-
-
S-farnesyl thiosalicylic acid
-
-
S-farnesyl thiosalicylic acid
-
0.05 mM, 50% inhibition
S-farnesyl-4-chlorothiosalicylic acid
-
-
S-farnesyl-4-fluorothiosalicylic acid
-
-
S-farnesyl-5-chlorothiosalicylic acid
-
-
S-farnesyl-5-fluorothiosalicylic acid
-
-
S-Farnesylthioacetic acid
-
competitive vs. N-acetyl-S-(E,E)-farnesyl-L-cysteine
S-Farnesylthioacetic acid
-
-
S-Farnesylthioacetic acid
-
-
S-Farnesylthioacetic acid
-
0.048 mM, 50% inhibition
S-Farnesylthioacetic acid
-
dead-end inhibitor
S-{(2E)-3-[2-(biphenyl-4-yl)ethyl]-6-methylhepta-2,5-dien-1-yl}-N-(2-phenoxybenzoyl)-L-homocysteine
-
low micromolar inhibitor
sinefungin
-
-
sinefungin
-
-
sinefungin
-
0.0009 mM, 50% inhibition
sinefungin
-
0.00002 mM; 50% inhibition, competitive vs. S-adenosyl-L-methionine
sinefungin
-
0.0035 mM, 50% inhibition
spermatinamine
-
-
Triton X-100
-
0.1%, 63% inhibition
Tween 80
-
0.1%, 33% inhibition
Zn2+
-
complete inhibition
[2-(2,2-dimethyl-4-p-tolyltetrahydropyran-4-yl)ethyl]-(3-methoxyphenyl)amine
-
-
-
[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-(2-fluorophenyl)amine
-
-
-
[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]-(2-fluoro-4-methylphenyl)amine
-
-
-
[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]-(3-fluoro-4-methoxyphenyl)amine
-
-
-
[2-(2,2-dimethyl-4-thiophen-2-yltetrahydropyran-4-yl)-ethyl]-(3-methoxyphenyl)amine
-
-
-
[2-(2,2-dimethyl-4-thiophen-2-yltetrahydropyran-4-yl)-ethyl]phenylamine
-
-
-
[2-[4-(3-chlorophenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
-
-
-
[2-[4-(3-fluoro-phenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
-
-
-
[2-[4-(4-chlorophenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
-
-
-
[2-[4-(4-fluorophenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
-
-
-
[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
mono iodoacetate
-
moderate inhibition
additional information
-
decrease in the length versus hydrophobicity of the indole nitrogen substituent is accompanied by loss of the time-dependent properties of this indole class of Icmt inhibitors
-
additional information
-
FC analogs containing larger R-groups inhibit Icmt more effectively than those with smaller R-groups, in particular, an adamantyl analog is the most potent inhibitor. Also compounds containing 3,5-disubstituted phenyl rings, with the exception of a difluoro compound, exhibit inhibitory activity, whereas the corresponding 2,4-disubstituted analogs do not
-
additional information
-
good inhibitory activity is determined largely by the characteristics of the substituent attached to the indole nitrogen, which should be a lipophilic residue with fairly wide dimensions. In contrast, the substituted phenyl ring attached to the indole ring must be of limited dimensions and lipophilicity
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
formyl-methionine-leucine-phenylalanine
-
stimulation of carboxyl methylation of GTP-binding proteins through a substrate-dependent mechanism
-
guanosine 5'-[gamma-thio]-triphosphate
-
2 mM, 40fold increase in activity
guanosine 5'-[gamma-thio]-triphosphate
-
stimulation of 23000 Da protein methylation
guanosine 5'-[gamma-thio]-triphosphate
-
stimulation of carboxymethylation of endogenous substrates
additional information
-
no increase in methyltransferase activity in cell-free preparations by guanosine 5'-[gamma-thio]-triphosphate
-
additional information
-
no increase in N-acetyl-S-(E,E)-farnesyl-L-cysteine methylation
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0021
biotin-S-farnesyl-L-cysteine
-
-
0.0029
farnesylated and Rce1-proteolyzed K-Ras protein
-
-
-
0.0105
N-((benzoylglycyl)glycyl)-S-farnesyl-L-cysteine
-
-
0.00255
N-(benzoylglycyl)-S-farnesyl-L-cysteine
-
-
1
N-acetyl-S-(E)-geranyl-L-cysteine
-
-
0.04
N-acetyl-S-(E,E)-farnesyl-D-cysteine
-
-
0.00017
N-acetyl-S-(E,E)-farnesyl-L-cysteine
-
recombinant enzyme
0.0014
N-acetyl-S-(E,E)-farnesyl-L-cysteine
-
native enzyme
0.0115
N-acetyl-S-(E,E)-farnesyl-L-cysteine
-
native enzyme
0.0116
N-acetyl-S-(E,E)-farnesyl-L-cysteine
-
-
0.018
N-acetyl-S-(E,E)-farnesyl-L-cysteine
-
enzyme from endometrial carcinoma
0.02
N-acetyl-S-(E,E)-farnesyl-L-cysteine
-
-
0.02
N-acetyl-S-(E,E)-farnesyl-L-cysteine
-
-
0.02
N-acetyl-S-(E,E)-farnesyl-L-cysteine
-
enzyme from endometrium
0.03
N-acetyl-S-(E,E)-farnesyl-L-cysteine
-
-
0.0565
N-acetyl-S-(E,E)-farnesyl-L-cysteine
-
-
0.06
N-acetyl-S-(E,E)-farnesyl-L-cysteine
-
-
0.073
N-acetyl-S-(E,E)-farnesyl-L-cysteine
-
-
0.09
N-acetyl-S-(E,E)-farnesyl-L-cysteine
-
-
11.1
N-acetyl-S-(E,E)-farnesyl-L-cysteine
-
-
5
N-acetyl-S-3,3-dimethylalkyl-L-cysteine
-
-
0.003
N-acetyl-S-farnesyl-L-cysteine
-
-
0.0223
N-acetyl-S-farnesyl-L-cysteine
-
-
0.0014
N-acetyl-S-geranylgeranyl-L-cysteine
-
-
0.0023
N-acetyl-S-geranylgeranyl-L-cysteine
-
recombinant enzyme
0.004
N-acetyl-S-geranylgeranyl-L-cysteine
-
native enzyme
0.0116
N-acetyl-S-geranylgeranyl-L-cysteine
-
native enzyme
0.0192
N-acetyl-S-geranylgeranyl-L-cysteine
-
-
0.021
N-acetyl-S-geranylgeranyl-L-cysteine
-
-
0.052
N-acetyl-S-geranylgeranyl-L-cysteine
-
-
0.166
N-acetyl-S-geranylgeranyl-L-cysteine
-
-
0.0032
N-acetyl-S-geranylgeranyl-L-cysteine methyl ester
-
-
0.594
N-acetyl-S-geranylgeranyl-L-cysteinyl-L-alanyl-S-geranylgeranyl-L-cysteine
-
-
0.00295
N-isobutyryl-S-farnesyl-L-cysteine
-
-
0.00255
N-isovaleryl-S-farnesyl-L-cysteine
-
-
0.00013
S-adenosyl-L-methionine
-
-
0.0013
S-adenosyl-L-methionine
-
-
0.0021
S-adenosyl-L-methionine
-
-
0.0036
S-adenosyl-L-methionine
-
-
0.0038
S-adenosyl-L-methionine
-
-
0.004
S-adenosyl-L-methionine
-
-
0.0071
S-adenosyl-L-methionine
-
-
0.0078
S-adenosyl-L-methionine
-
-
3.8
S-adenosyl-L-methionine
-
-
0.48
S-decyl-Leu-Ala-Arg-Tyr-Lys-Cys
-
-
0.0022
S-farnesyl-Leu-Ala-Arg-Tyr-Lys-Cys
-
-
0.389
S-geranyl-Leu-Ala-Arg-Tyr-Lys-Cys
-
-
0.0109
S-geranylgeranyl-Leu-Ala-Arg-Tyr-Lys-Cys
-
-
1.76
S-octyl-Leu-Ala-Arg-Tyr-Lys-Cys
-
-
1.12
S-pentadecyl-Leu-Ala-Arg-Tyr-Lys-Cys
-
-
0.64
S-tridecyl-Leu-Ala-Arg-Tyr-Lys-Cys
-
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
3.95
5'-deoxymethylthioadenosine
-
-
0.0022
cysmethynil
-
with respect to farnesylated and Rce1-proteolyzed K-Ras protein as substrate
0.00239
cysmethynil
-
with respect to S-adenosyl-L-methionine as substrate
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
0.0354
N-Acetyl-S-(3-(3-methylbut-2-enyl)-5-(4-phenyl)phenylpent-2Z-en-1-yl)-L-cysteine
-
competitive inhibition
0.1193
N-Acetyl-S-(3-(3-methylbut-2-enyl)-5-(4-phenyl)phenylpent-2Z-en-1-yl)-L-cysteine
-
competitive inhibition
0.3772
N-Acetyl-S-(3-(3-methylbut-2-enyl)-5-(4-phenyl)phenylpent-2Z-en-1-yl)-L-cysteine
-
uncompetitive inhibition
0.6144
N-Acetyl-S-(3-(3-methylbut-2-enyl)-5-(4-phenyl)phenylpent-2Z-en-1-yl)-L-cysteine
-
uncompetitive inhibition
0.0171
N-acetyl-S-(3-(3-methylbut-2-enyl)-7,11-dimethyldodeca-2Z,6E,10-trien-1-yl)-L-cysteine
-
-
0.0026
N-acetyl-S-(E,E)-farnesyl-L-cysteine
-
competitive vs. N-acetyl-S-(E,E)-geranylgeranyl-L-cysteine
0.041
N-acetyl-S-(E,E)-farnesyl-L-cysteine methyl ester
-
-
0.0023
N-acetyl-S-(E,E)-geranylgeranyl-L-cysteine
-
competitive vs. N-acetyl-S-(E,E)-farnesyl-L-cysteine
0.00207
N-acetyl-S-farnesyl-L-cysteine methyl ester
-
mixed-type vs. N-acetyl-S-farnesyl-L-cysteine
0.0021
N-acetyl-S-farnesyl-L-cysteine methyl ester
-
with respect to biotin-S-farnesyl-L-cysteine
0.00243
N-acetyl-S-farnesyl-L-cysteine methyl ester
-
with respect to S-adenosyl-L-methionine
0.005
N-acetyl-S-farnesyl-L-cysteine methyl ester
-
competitive vs. S-adenosyl-L-methionine
0.0039
S-(Geranylgeranyl-2-thio)acetic acid
-
competitive vs. N-acetyl-S-(E,E)-farnesyl-L-cysteine
0.00157
S-adenosyl-L-homocysteine
-
-
0.0019
S-adenosyl-L-homocysteine
-
vs. S-adenosyl-L-methionine
0.0033
S-adenosyl-L-homocysteine
-
vs. N-acetyl-S-(E,E)-farnesyl-L-cysteine
0.00354
S-adenosyl-L-homocysteine
-
with respect to S-adenosyl-L-methionine
0.00359
S-adenosyl-L-homocysteine
-
with respect to biotin-S-farnesyl-L-cysteine
0.00413
S-adenosyl-L-homocysteine
-
competitive vs. S-adenosyl-L-methionine
0.0044
S-adenosyl-L-homocysteine
-
mixed-type vs. N-acetyl-S-farnesyl-L-cysteine
0.00658
S-adenosyl-L-homocysteine
-
inhibition of N-acetyl-S-(E,E)-farnesyl-L-cysteine methylation
0.0092
S-adenosyl-L-homocysteine
-
-
0.0115
S-adenosyl-L-homocysteine
-
inhibition of N-acetyl-S-geranylgeranyl-L-cysteinyl-L-alanyl-S-geranylgeranyl-L-cysteine
1.8
S-adenosyl-L-homocysteine
-
-
0.00645
S-adenosylethionine
-
inhibition of N-acetyl-S-(E,E)-farnesyl-L-cysteine methylation
0.0218
S-adenosylethionine
-
inhibition of N-acetyl-S-geranylgeranyl-L-cysteinyl-L-alanyl-S-geranylgeranyl-L-cysteine
0.0028
S-farnesyl thiosalicylic acid
-
-
0.028
S-farnesyl-4-chlorothiosalicylic acid
-
-
0.023
S-farnesyl-4-fluorothiosalicylic acid
-
-
0.0085
S-farnesyl-5-chlorothiosalicylic acid
-
-
0.0063
S-farnesyl-5-fluorothiosalicylic acid
-
-
0.00117
S-Farnesylthioacetic acid
-
-
0.0012
S-Farnesylthioacetic acid
-
-
0.002
S-Farnesylthioacetic acid
-
-
0.0046
S-Farnesylthioacetic acid
-
competitive vs. N-acetyl-S-(E,E)-farnesyl-L-cysteine
0.0112
S-Farnesylthioacetic acid
-
inhibition of N-acetyl-S-(E,E)-farnesyl-L-cysteine methylation
0.0137
S-Farnesylthioacetic acid
-
competitive vs. N-acetyl-S-farnesyl-L-cysteine
0.00007
sinefungin
-
-
0.000296
sinefungin
-
inhibition of N-acetyl-S-geranylgeranyl-L-cysteinyl-L-alanyl-S-geranylgeranyl-L-cysteine
0.000318
sinefungin
-
inhibition of N-acetyl-S-(E,E)-farnesyl-L-cysteine methylation
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000031
(3,5-difluoro-4-methoxyphenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000025
(3-chloro-4-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.0000038
(3-chlorophenyl)-[2-(2,2-dimethyl-4-thiophen-2-yltetrahydropyran-4-yl)ethyl]amine
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00047
(4-chloro-3-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000032
(5-chloro-2-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.049
(R)-2-(2-((benzyloxy)methyl)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)-thio)propanoic acid
-
in 100 mM Tris-HCl, pH 7.5, at 30C
-
0.075
(R)-2-(2-(phenoxymethyl)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
in 100 mM Tris-HCl, pH 7.5, at 30C
-
0.0147
(R)-2-(2-(phenylthio)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
in 100 mM Tris-HCl, pH 7.5, at 30C
-
0.038
(R)-2-(2-benzylbenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid, (R)-2-(2-phenoxybenzamido)-3-(((2E,6E,10E)-3,7,11,15-tetramethylhexadeca-2,6,10,14-tetraen-1-yl)thio)propanoic acid
-
in 100 mM Tris-HCl, pH 7.5, at 30C
-
0.21
(R)-2-(2-phenoxybenzamido)-3-(undecylthio)propanoic acid
-
in 100 mM Tris-HCl, pH 7.5, at 30C
-
0.0226
(R)-2-(3-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
in 100 mM Tris-HCl, pH 7.5, at 30C
-
0.063
(R)-2-(4-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
in 100 mM Tris-HCl, pH 7.5, at 30C
-
0.058
(R)-2-(dibenzo[b,d]furan-4-carboxamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)-propanoic acid
-
in 100 mM Tris-HCl, pH 7.5, at 30C
-
0.0067
(R)-2-(N-methyl-2-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
in 100 mM Tris-HCl, pH 7.5, at 30C
-
0.149
(R,E)-3-((3,7-dimethylocta-2,6-dien-1-yl)thio)-2-(2-phenoxybenzamido)propanoic acid
-
in 100 mM Tris-HCl, pH 7.5, at 30C
-
0.0078
(S)-2-(2-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
-
in 100 mM Tris-HCl, pH 7.5, at 30C
-
0.025
(S)-glabrol
-
-
0.001
1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-fluorophenyl)thiourea, 1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-methoxphenyl)urea
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
1
1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-methoxyphenyl)thiourea
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.001
1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-phenylthiourea
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.002
1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-3-(morpholin-4-ylmethyl)-1H-indole
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0021
1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-3-(piperidin-1-ylmethyl)-1H-indole
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
1
1-(3-chlorophenyl)-3-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)thiourea, 1-(3-chlorophenyl)-3-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)urea
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.1
1-(3-methylbut-2-enyl)-5-m-tolyl-1H-indole
-
IC50 above 0.1 mM, in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
-
0.0007
1-(octyl-5-m-tolyl-1H-indol-3-yl)methanamine
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
-
0.1
1-octyl-5-m-tolyl-1H-indole
-
IC50 above 0.1 mM, in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
-
0.03
1-octyl-5-m-tolyl-1H-indole-3-carboxamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
-
0.017
2'-methoxy-3',3''-diprenyl-licodione
-
-
0.03
2'-methoxy-3'-prenyllicodione
-
-
0.0065
2-(1-octyl-1H-indol-3-yl)acetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0018
2-(1-octyl-5-phenyl-1H-indol-3-yl)acetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.005
2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-N-(3-methoxyphenyl)acetamide, 2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-N-phenylacetamide
-
IC50 above 0.005 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.001
2-(5-(3-ethoxyphenyl)-1-octyl-1H-indol-3-yl)-N,N-diethylacetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
-
0.069
2-(5-fluoro-1-(3-methylbut-2-enyl)-1H-indol-3-yl)acetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
-
0.007
2-(5-fluoro-1-octyl-1H-indol-3-yl)acetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
1.1
2-Carboxy-2'-hydroxy-5'-sulfoformazylbenzene
-
IC50: 1.1 mM
0.0062
2-phenoxy-phenylfarnesylcysteine
-
in 100 mM Tris-HCl, pH 7.5, at 30C
0.001
2-[5-(2-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0013
2-[5-(3-ethoxyphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0019
2-[5-(3-methoxyphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0017
2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(4-methylpiperazin-1-yl)ethanone
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0018
2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(piperidin-1-yl)ethanone
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0012
2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(pyrrolidin-1-yl)ethanone
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0025
2-[5-(3-methylphenyl)-1-[3-(trifluoromethyl)benzyl]-1H-indol-3-yl]acetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.033
2-[5-(3-methylphenyl)-1H-indol-3-yl]acetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.001
2-[5-(4-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.00031
2-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl](phenyl)amino]-1-(furan-2-yl)ethanone
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
0.000181
3,4-dichloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2Hpyran-4-yl)ethyl]aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00017
3,5-dichloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.0012
3-(1-octyl-5-m-tolyl-1H-indol-3-yl)propanamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
-
0.001
3-chloro-4-methyl-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)ethyl]aniline
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00046
3-chloro-4-methyl-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.005
3-chloro-N-(3-chlorophenyl)-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydropyran-4-yl)ethyl]aniline
-
IC50 above 0.005 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.001
3-chloro-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)-ethyl]aniline
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00249
3-chloro-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydrothiopyran-4-yl)ethyl]aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000049
3-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-4-methylaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000025
3-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00383
3-chloro-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.001
3-fluoro-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)-ethyl]aniline
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00325
3-fluoro-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.001
3-methoxy-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)-ethyl]aniline
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.0000013
3-methoxy-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydropyran-4-yl)ethyl]aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00042
3-methoxy-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydrothiopyran-4-yl)ethyl]aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000777
3-methoxy-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.0125
3-methoxy-N-[2-[4-(4-methoxyphenyl)-2,2-dimethyltetrahydro-2H-pyran-4-yl]ethyl]aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00325
3-methyl-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000556
3-tert-butyl-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.005
3-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethylamino]benzoic acid, 3-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethylamino]phenol
-
IC50 above 0.005 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00383
3-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]-N,N-dimethylbenzenesulfonamide
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000066
3-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]benzonitrile
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000308
4-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-3-methylaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00036
4-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00076
4-tert-butyl-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.0131
4-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]benzenesulfonamide
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000123
4-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]benzonitrile
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.0007
5-(3-methylphenyl)-1-octyl-3-(piperidin-1-ylmethyl)-1H-indole
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0005
5-(3-methylphenyl)-1-octyl-3-(pyrrolidin-1-ylmethyl)-1H-indole
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0027
5-(3-methylphenyl)-3-(morpholin-4-ylmethyl)-1-octyl-1H-indole
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0009
5-(3-methylphenyl)-3-[(4-methylpiperazin-1-yl)methyl]-1-octyl-1H-indole
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0015
cysmethynil
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.00288
ethyl 4-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]amino]benzoate
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.1
ethyl [5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetate
-
IC50 above 0.1 mM, in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.076
methyl [5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetate
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.000131
N'-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N,N-dimethylbenzene-1,3-diamine
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.0008
N,N-diethyl-2-(5-(3-methoxyphenyl)-1-octyl-1H-indol-3-yl)acetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
-
0.0014
N,N-diethyl-2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0013
N,N-dimethyl-1-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methanamine
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0015
N,N-dimethyl-2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0012
N-((1-octyl-5-m-tolyl-1H-indol-3-yl)methyl)methanesulfonamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
-
0.0077
N-(2-methylidenebut-3-en-1-yl)-2-[5-(3-methylphenyl)-1-[3-(trifluoromethyl)benzyl]-1H-indol-3-yl]acetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0194
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
-
pH and temperature not specified in the publication
0.005
N-(3-chlorophenyl)-2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)acetamide
-
IC50 above 0.005 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00135
N-(3-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]phenyl)acetamide
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.0346
N-acetyl-S-[(2E)-3-methyl-5-(4-octylphenyl)pent-2-en-1-yl]-L-cysteine
-
pH and temperature not specified in the publication
0.00012
N-benzyl-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]furan-2-carboxamide
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
0.067
N-ethyl-N-((1-(3-methylbut-2-enyl)-1H-indol-3-yl)methyl) ethanamine
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
-
0.035
N-ethyl-N-((5-fluoro-1-(3-methylbut-2-enyl)-1H-indol-3-yl)methyl)ethanamine
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
-
0.0041
N-ethyl-N-[(5-fluoro-1-octyl-1H-indol-3-yl)methyl]-ethanamine
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
-
0.0024
N-ethyl-N-[[1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-1H-indol-3-yl]methyl]ethanamine
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0006
N-ethyl-N-[[5-(2-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0007
N-ethyl-N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0006
N-ethyl-N-[[5-(4-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0009
N-methyl-N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]propan-2-amine
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0018
N-[(1-octyl-5-m-tolyl-1H-indol-3-yl)methyl]acetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
-
0.0011
N-[(2E)-3,7-dimethylocta-2,6-dien-1-yl]-2-[5-(3-methylphenyl)-1-[3-(trifluoromethyl)benzyl]-1H-indol-3-yl]acetamide
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.000015
N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydropyran-4-yl)-ethyl]aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.001
N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydrothiopyran-4-yl)ethyl]aniline
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.0036
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-2-methylaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000652
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3,4-dimethoxyaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000054
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3,5-dimethylaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00009
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-(trifluoromethoxy)aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00038
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-(trifluoromethyl)aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00004
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-ethylaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000052
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-fluoroaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000167
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-isopropylaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00009
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-methoxy-4-methylaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000015
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-methoxyaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000031
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-methylaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000184
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-(trifluoromethoxy)aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000168
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-fluoroaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000132
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-isopropylaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00027
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-methoxyaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000031
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-methylaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00985
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N,3-dimethylaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.01
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N-methylaniline
-
IC50 above 0.01 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00234
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N-phenylacetamide
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.0027
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]aniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000069
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-3,4-dimethylaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000026
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-3-nitroaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000682
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-4-nitroaniline
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.0134
N-[2-(benzyloxy)benzoyl]-S-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-L-cysteine
-
in 100 mM Tris-HCl, pH 7.5, at 30C
0.0035
N-[3-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-3-(2-methoxyphenyl)propyl]-N-(4-methoxybenzyl)furan-2-carboxamide
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
0.0017
N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]-N-(propan-2-yl)propan-2-amine
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0008
N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]-N-propylpropan-1-amine
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37C
0.0025
S-{(2E)-3-[2-(biphenyl-4-yl)ethyl]-6-methylhepta-2,5-dien-1-yl}-N-(2-phenoxybenzoyl)-L-homocysteine
-
in 100 mM Tris-HCl, pH 7.5, at 30C
0.00419
[2-(2,2-dimethyl-4-p-tolyltetrahydropyran-4-yl)ethyl]-(3-methoxyphenyl)amine
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00055
[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-(2-fluorophenyl)amine
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.0003
[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]-(2-fluoro-4-methylphenyl)amine
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00016
[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]-(3-fluoro-4-methoxyphenyl)amine
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000019
[2-(2,2-dimethyl-4-thiophen-2-yltetrahydropyran-4-yl)-ethyl]-(3-methoxyphenyl)amine
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00027
[2-(2,2-dimethyl-4-thiophen-2-yltetrahydropyran-4-yl)-ethyl]phenylamine
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00019
[2-[4-(3-chlorophenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.000008
[2-[4-(3-fluoro-phenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.00063
[2-[4-(4-chlorophenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
0.0001
[2-[4-(4-fluorophenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22C
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
0.000143
-
-
0.755
-
wild type enzyme, at pH and C
additional information
-
activities of wild-type and mutant enzymes expressed in HEK-293 cells
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7.4
-
assay at
pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
5.6 - 8.6
-
-
7.4 - 8
-
-
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
22
-
assay at room temperature
TEMPERATURE RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
10 - 44
-
for the Escherichia coli polar lipid (control), Ste14p activity remains essentially constant when the assay temperature is maintained at 10, 16, 32, or 44C, activity in DMPC is unchanged below (16 C) and above (32 C) its phase transition temperature, yielding activity levels that are the same as the Escherichia coli polar lipid values within experimental error, for C20-BAS activity is only 5% of that observed for the Escherichia coli polar lipid above (32 C) and below (10 C) the phase transition temperature of C20BAS
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
adrenal chromaffin cells
Manually annotated by BRENDA team
-
insulin-secreting
Manually annotated by BRENDA team
-
light membrane fraction
Manually annotated by BRENDA team
-
stably overexpressing isoprenylcysteine carboxyl methyltransferase/GFP cDNA
Manually annotated by BRENDA team
-
outer segment
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
-
integral membrane protein with 6 transmembrane segments, determination and analysis of membrane topology using recombinant Icmt expressed in COS-1 cells, overview
Manually annotated by BRENDA team
-
integral membrane protein
Manually annotated by BRENDA team
-
an integral membrane protein
Manually annotated by BRENDA team
-
an integral membrane protein
Manually annotated by BRENDA team
-
48% of the activity
Manually annotated by BRENDA team
-
Ste14p activity is lost in vesicles composed of 75-100 mol% C20BAS and 0-100 mol% C32BAS but retained in vesicles with 0-50 mol% C20BAS and 0-100 mol% C32phytBAS
Manually annotated by BRENDA team
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
24000
-
radiation inactivation
485029
30000
-
gel filtration, photoaffinity labelling
485040
86000
-
PAGE, gel filtration
485035
86000
-
non denaturing PAGE
485040
98000
-
radiation inactivation
485029
180000
-
gel filtration
485027
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
?
-
x * 30000, SDS-PAGE
?
-
x * 28301, deduced from nucleotide sequence
homodimer
-
2 * 23000, untagged enzyme, SDS-PAGE, 2 * 35000, His-tagged enzyme, SDS-PAGE
monomer
-
1 * 24000, deduced from nucleotide sequence
additional information
-
enzyme may be a homotetramer
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
5.5 - 9.5
-
stable
485037
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
complete loss of activity after exposure to detergent e.g. CHAPS, octyl-beta-glucoside and sodium deoxycholate, activity can be reconstituted by removal of the detergent in the presence of phospholipid
-
the membrane-associated activity is highly stable even upon repeated freeze-thaw cycles
-
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-70C, 6 months
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
acid treatment, DEAE-cellulose, Superose 6, Superdex 75, partially purified
-
Ni-NTA column chromatography, ion exchange column chromatography, and gel filtration
-
Q-Sepharose, partially purified
-
by Talon metal affinity chromatography
-
Talon metal affinity bead chromatography
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
the ICMT isozyme is encoded by the STE14A ICMT gene; the ICMT isozyme is encoded by the STE14B ICMT gene
Q93W54
expressed in Sf9 insect cells
-
Icmt, expression in HEK-293 cells and Cos-1 cells
-
into the pCHH10m3N vector, overexpressed in Saccharomyces cerevisiae
-
overepression in tissue culture cells
-
expressed in Escherichia coli C41(DE3) cells
-
expressed in Saccharomyces cerevisiae strain SM1188
-
expression of TrpE-STE14 methyl transferase fusion protein in Escherichia coli
-
His-Ste14p, which encodes Ste14p with a 10 x histidine tag followed by a triply iterated myc epitope repeat at the N terminus under the constitutive control of the phosphoglycerate kinase promoter, overexpressed in Saccharomyces cerevisiae
-
His10myc3-tagged Ste14p expressed in Saccharomyces cereVisiae
-
expression in Sf9 cells
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
abscisic acid promotes abscisic acid responsiveness of plant cells via induction of ICME expression
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
D122A
-
site-directed mutagenesis, the mutant shows decreased activity compared to the wild-type enzyme, comparison of membrane topology
E107A
-
site-directed mutagenesis, the mutant shows decreased activity compared to the wild-type enzyme, comparison of membrane topology
E142A
-
site-directed mutagenesis, the mutant shows decreased activity compared to the wild-type enzyme, comparison of membrane topology
E146A
-
site-directed mutagenesis, the mutant shows decreased activity compared to the wild-type enzyme, comparison of membrane topology
E251A
-
site-directed mutagenesis, the mutant shows decreased activity compared to the wild-type enzyme, comparison of membrane topology
E252A
-
site-directed mutagenesis, the mutant shows decreased activity compared to the wild-type enzyme, comparison of membrane topology
F124A
-
site-directed mutagenesis, the mutant shows decreased activity compared to the wild-type enzyme, comparison of membrane topology
F124R
-
site-directed mutagenesis, the mutant shows decreased activity compared to the wild-type enzyme, comparison of membrane topology
F258A
-
site-directed mutagenesis, the mutant shows decreased activity compared to the wild-type enzyme, comparison of membrane topology
P275A
-
site-directed mutagenesis, the mutant shows decreased activity compared to the wild-type enzyme, comparison of membrane topology
R209A
-
site-directed mutagenesis, the mutant shows activity similar to the wild-type enzyme, comparison of membrane topology
R63A
-
site-directed mutagenesis, the mutant shows decreased activity compared to the wild-type enzyme, comparison of membrane topology
RH209/210A
-
site-directed mutagenesis, the mutant shows decreased activity compared to the wild-type enzyme, comparison of membrane topology
S123A
-
site-directed mutagenesis, the mutant shows decreased activity compared to the wild-type enzyme, comparison of membrane topology
W241A
-
site-directed mutagenesis, the mutant shows decreased activity compared to the wild-type enzyme, comparison of membrane topology
Y266A
-
site-directed mutagenesis, the mutant shows increased activity comapred to the wild-type enzyme, comparison of membrane topology
E167A
-
the mutation leads to strongly reduced activity compared to the wild type enzyme
H113A
-
the mutation leads to strongly reduced activity compared to the wild type enzyme
H126A
-
the mutation leads to strongly reduced activity compared to the wild type enzyme
R163A
-
the mutation leads to strongly reduced activity compared to the wild type enzyme
E213Q
-
the mutant is enzymatically almost inactive (5% activity compared to the wild type)
L81F
-
the mutant shows little to no in vitro methyltransferase activity
additional information
-
transgenic plants overproducing ICME exhibit abscisic acid hypersensitivity in stomatal closure and seed germination assays. Induction leads to demethylation and inactivation of isoprenylated negative regulators of abscisic acid signaling
F72A
-
site-directed mutagenesis, the mutant shows decreased activity compared to the wild-type enzyme, comparison of membrane topology
additional information
-
construction of various CFP-Icmt C-terminal truncation mutants, overview, comparison of membrane topology
additional information
-
enzyme knockout by siRNA in MDA-MB 231 cells, phenotype, overview
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
biotechnology
-
the enzyme is a target for metabolic engineering of crop species for drought tolerance by targeted alterations in isoprenylcysteine methylation
analysis
-
approaches to establish the quantitative structureactivity relationship of indoloacetamides as inhibitors of ICMT
drug development
-
the enzyme is a target for anticancer drug design
medicine
-
development of Icmt inhibitors as another approach to anticancer drug development
medicine
-
generation of Icmt inhibitors based on the structure of the minimal Icmt substrate N-acetyl-S-farnesyl-L-cysteine in hopes of developing potent anticancer agents
medicine
-
inhibition of the enzyme results in Ras mislocalization and loss of cellular transformation ability, making it an attractive and novel anticancer target
pharmacology
-
the enzyme is a target in anticancer therapy
analysis
-
highly sensitive capillary electrophoresis method for monitoring of the enzymic activity
medicine
-
inhibition of the enzyme results in Ras mislocalization and loss of cellular transformation ability, making it an attractive and novel anticancer target
medicine
-
target in anticancer drug design