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Information on EC 2.1.1.100 - protein-S-isoprenylcysteine O-methyltransferase and Organism(s) Homo sapiens and UniProt Accession O60725

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EC Tree
IUBMB Comments
C-terminal S-geranylgeranylcysteine and S-geranylcysteine residues are also methylated, but more slowly.
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Select one or more organisms in this record: ?
This record set is specific for:
Homo sapiens
UNIPROT: O60725
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria, Archaea
Synonyms
ste14p, isoprenylcysteine carboxyl methyltransferase, isoprenylcysteine carboxylmethyltransferase, prenylated protein methyltransferase, isoprenylated protein methyltransferase, protein-s-isoprenylcysteine o-methyltransferase, isoprenylcysteine methylesterase, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
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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isoprenylcysteine carboxyl methyltransferase
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isoprenylcysteine carboxylmethyltransferase
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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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REACTION
REACTION DIAGRAM
COMMENTARY hide
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
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 hide
LITERATURE
methyl group transfer
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-
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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.
CAS REGISTRY NUMBER
COMMENTARY hide
130731-20-3
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
S-adenosyl-L-methionine + 4-benzoyl-N-([2-[2-([5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl]amino)ethoxy]ethoxy]acetyl)-L-phenylalanyl-S-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-L-cysteine
S-adenosyl-L-homocysteine + ?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + biotin-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + biotin-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + biotin-Peg4-YIIKGVFWDPAC(C10-meta-Bp)
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + biotin-Peg4-YIIKGVFWDPAC(C10-para-Bp)
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + biotin-Peg4-YIIKGVFWDPAC(C5-meta-Bp)
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + biotin-Peg4-YIIKGVFWDPAC(C5-para-Bp)
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + biotin-S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + biotin-S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
-
-
?
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
-
relatively good substrate for the human Icmt enzyme
-
-
?
S-adenosyl-L-methionine + N-acetyl-S-farnesyl-L-cysteine
?
show the reaction diagram
-
-
-
-
?
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
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
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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-
-
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ir
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
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
-
-
-
-
?
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
S-adenosyl-L-methionine + Ras protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + Ras protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + S-[(2E,6E)-8-(3-benzoylphenoxy)-3,7-dimethylocta-2,6-dien-1-yl]-N-([2-[2-([5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl]amino)ethoxy]ethoxy]acetyl)-D-cysteine
S-adenosyl-L-homocysteine + ?
show the reaction diagram
-
-
-
-
?
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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-
-
-
?
S-adenosylmethionine + N-((benzoylglycyl)glycyl)-S-farnesyl-L-cysteine
S-adenosylhomocysteine + N-((benzoylglycyl)glycyl)-S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
-
?
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-L-cysteine
S-adenosylhomocysteine + N-acetyl-S-(E,E)-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
-
?
S-adenosylmethionine + N-isobutyryl-S-farnesyl-L-cysteine
S-adenosylhomocysteine + N-isobutyryl-S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
-
?
S-adenosylmethionine + N-isovaleryl-S-farnesyl-L-cysteine
S-adenosylhomocysteine + N-isovaleryl-S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
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
-
-
-
-
?
S-adenosyl-L-methionine + Ras protein C-terminal S-farnesyl-L-cysteine
S-adenosyl-L-homocysteine + Ras protein C-terminal S-farnesyl-L-cysteine methyl ester
show the reaction diagram
-
-
-
-
?
additional information
?
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COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
S-adenosyl-L-methionine
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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
4-[(naphthalen-2-yl)(thiophen-2-yl)methylidene]oxane
competitive with the prenylated peptide substrate, N-acetyl-S-farnesyl cysteine and non-competitive with SAM
cysmethynil
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(1-octyl-5-m-tolyl-1H-indol-3-yl)methanamine
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(2R)-2-(acetylamino)-3-[[(2Z)-3,4-diphenylbut-2-en-1-yl]sulfanyl]propanoic acid
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15.7% inhibition at 0.01 mM
(2R)-2-(acetylamino)-3-[[(2Z)-4-(2-fluorophenyl)-3-phenylbut-2-en-1-yl]sulfanyl]propanoic acid
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25.3% inhibition at 0.01 mM
(3,5-difluoro-4-methoxyphenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
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(3-chloro-4-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
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(3-chlorophenyl)-[2-(2,2-dimethyl-4-thiophen-2-yltetrahydropyran-4-yl)ethyl]amine
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(4-chloro-3-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
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(5-chloro-2-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
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(R)-2-(2-((benzyloxy)methyl)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)-thio)propanoic acid
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(R)-2-(2-(phenoxymethyl)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
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(R)-2-(2-(phenylthio)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
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(R)-2-(2-benzylbenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
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(R)-2-(2-phenoxybenzamido)-3-(((2E,6E,10E)-3,7,11,15-tetramethylhexadeca-2,6,10,14-tetraen-1-yl)thio)propanoic acid
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(R)-2-(2-phenoxybenzamido)-3-(undecylthio)propanoic acid
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(R)-2-(3-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
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(R)-2-(4-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
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(R)-2-(dibenzo[b,d]furan-4-carboxamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)-propanoic acid
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(R)-2-(N-methyl-2-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
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(R,E)-3-((3,7-dimethylocta-2,6-dien-1-yl)thio)-2-(2-phenoxybenzamido)propanoic acid
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(S)-2-(2-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
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(S)-glabrol
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structure determination, overview
1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-fluorophenyl)thiourea
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1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-methoxphenyl)urea
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1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-methoxyphenyl)thiourea
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1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-phenylthiourea
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1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-3-(morpholin-4-ylmethyl)-1H-indole
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1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-3-(piperidin-1-ylmethyl)-1H-indole
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1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-3-[(morpholin-4-yl)methyl]-1H-indole
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1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-3-[(piperidin-1-yl)methyl]-1H-indole
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1-(3-chlorophenyl)-3-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)thiourea
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1-(3-chlorophenyl)-3-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)urea
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1-(3-methylbut-2-enyl)-5-m-tolyl-1H-indole
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1-octyl-5-(3-methylphenyl)-1H-indole
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a cysmethynil analogue
1-octyl-5-m-tolyl-1H-indole
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1-octyl-5-m-tolyl-1H-indole-3-carboxamide
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1-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methanamine
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2'-methoxy-3',3''-diprenyl-licodione
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isolated from Hovea parvicalyx, collected in Australia, structure determination, overview
2'-methoxy-3'-prenyllicodione
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isolated from Hovea parvicalyx, collected in Australia, structure determination, overview
2-(1-octyl-1H-indol-3-yl)acetamide
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2-(1-octyl-5-phenyl-1H-indol-3-yl)acetamide
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2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-N-(3-methoxyphenyl)acetamide
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2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-N-phenylacetamide
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2-(5-(3-ethoxyphenyl)-1-octyl-1H-indol-3-yl)-N,N-diethylacetamide
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2-(5-fluoro-1-(3-methylbut-2-enyl)-1H-indol-3-yl)acetamide
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2-(5-fluoro-1-octyl-1H-indol-3-yl)acetamide
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2-phenoxy-phenylfarnesylcysteine
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low micromolar inhibitor
2-[1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-1H-indol-3-yl]acetamide
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2-[1-[(2E,6E)-2,6-dimethylocta-2,6-dien-1-yl]-5-(3-methylphenyl)-1H-indol-3-yl]acetamide
-
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2-[5-(2-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
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2-[5-(3-ethoxyphenyl)-1-octyl-1H-indol-3-yl]-N,N-diethylacetamide
-
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2-[5-(3-ethoxyphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
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2-[5-(3-ethylphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
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2-[5-(3-fluorophenyl)-1-(2-methylidenebut-3-en-1-yl)-1H-indol-3-yl]acetamide
-
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2-[5-(3-fluorophenyl)-1-octyl-1H-indol-3-yl]acetamide
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2-[5-(3-methoxyphenyl)-1-octyl-1H-indol-3-yl]acetamide
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2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(4-methylpiperazin-1-yl)ethan-1-one
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2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(4-methylpiperazin-1-yl)ethanone
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2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(piperidin-1-yl)ethan-1-one
-
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2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(piperidin-1-yl)ethanone
-
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2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(pyrrolidin-1-yl)ethan-1-one
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2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(pyrrolidin-1-yl)ethanone
-
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2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
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2-[5-(3-methylphenyl)-1-[3-(trifluoromethyl)benzyl]-1H-indol-3-yl]acetamide
-
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2-[5-(3-methylphenyl)-1-[[3-(trifluoromethyl)phenyl]methyl]-1H-indol-3-yl]acetamide
-
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2-[5-(3-methylphenyl)-1H-indol-3-yl]acetamide
-
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2-[5-(4-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
-
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2-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]sulfanyl]ethanol
-
-
2-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl](phenyl)amino]-1-(furan-2-yl)ethanone
-
-
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-(2,2-dimethyloxan-4-yl)-N-[(4-methoxyphenyl)methyl]-3-phenylpropan-1-amine
-
-
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-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]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-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]propanamide
-
-
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-tert-butyl-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
-
-
4-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]-N-methylbenzene-1-sulfonamide
-
-
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-1H-indole-3-carboxamide
-
-
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)-1-octyl-3-[(piperidin-1-yl)methyl]-1H-indole
-
-
5-(3-methylphenyl)-1-octyl-3-[(pyrrolidin-1-yl)methyl]-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-(3-methylphenyl)-3-[(morpholin-4-yl)methyl]-1-octyl-1H-indole
-
-
5-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]-N,N-dimethylpyridin-2-amine
-
-
5-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]pyrimidin-2-amine
-
-
5-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]pyrimidine-2-carbonitrile
-
-
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
aplysamine 6
-
-
cysmethynil
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
-
-
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 3-[[(2E)-5-[4-[2-([1,1'-biphenyl]-4-yl)ethyl]-1H-1,2,3-triazol-1-yl]-3-methylpent-2-en-1-yl]sulfanyl]propanoate
-
-
methyl [5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetate
-
-
Mg2+
-
inhibition of 23000 Da protein methylation
N'-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N,N-dimethylbenzene-1,3-diamine
-
-
N,N-diethyl-2-(5-(3-methoxyphenyl)-1-octyl-1H-indol-3-yl)acetamide
-
-
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-(2-phenoxybenzoyl)-S-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-L-cysteine
-
-
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-farnesyl-L-cysteine
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-[(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-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-([1-octyl-5-[3-(trifluoromethyl)phenyl]-1H-indol-3-yl]methyl)ethanamine
-
-
N-ethyl-N-([5-[4-(methanesulfonyl)phenyl]-1-octyl-1H-indol-3-yl]methyl)ethanamine
-
-
N-ethyl-N-[(4-fluoro-1-octyl-1H-indol-3-yl)methyl]ethanamine
-
-
N-ethyl-N-[(5-fluoro-1-octyl-1H-indol-3-yl)methyl]-ethanamine
-
-
N-ethyl-N-[(5-fluoro-1-octyl-1H-indol-3-yl)methyl]ethanamine
-
-
N-ethyl-N-[(6-fluoro-1-octyl-1H-indol-3-yl)methyl]ethanamine
-
-
N-ethyl-N-[(7-fluoro-1-octyl-1H-indol-3-yl)methyl]ethanamine
-
-
N-ethyl-N-[[1-(2-methylidenebut-3-en-1-yl)-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-[[1-octyl-5-(pyridin-3-yl)-1H-indol-3-yl]methyl]ethanamine
-
-
N-ethyl-N-[[1-octyl-5-(pyrimidin-5-yl)-1H-indol-3-yl]methyl]ethanamine
-
-
N-ethyl-N-[[5-(2-fluorophenyl)-1-octyl-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-fluorophenyl)-1-(2-methylidenebut-3-en-1-yl)-1H-indol-3-yl]methyl]ethanamine
-
-
N-ethyl-N-[[5-(3-fluorophenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
-
-
N-ethyl-N-[[5-(3-fluoropyridin-4-yl)-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-methyl-N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]propan-2-amine
-
-
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
-
-
N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]acetamide
-
-
N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]methanesulfonamide
-
-
retinoic acid
-
20% decrease of N-acetyl-S-(E,E)-farnesyl-L-cysteine methylation in cells treated with 0.01 mM retinoic acid
S-adenosyl-L-homocysteine
S-Farnesylthioacetic acid
S-[(2E)-3-[2-([1,1'-biphenyl]-4-yl)ethyl]-6-methylhepta-2,5-dien-1-yl]-N-(2-phenoxybenzoyl)-L-cysteine
-
-
S-[(2E,6E)-8-(3-benzoylphenoxy)-3,7-dimethylocta-2,6-dien-1-yl]-N-([2-[2-([5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl]amino)ethoxy]ethoxy]acetyl)-D-cysteine
-
-
S-{(2E)-3-[2-(biphenyl-4-yl)ethyl]-6-methylhepta-2,5-dien-1-yl}-N-(2-phenoxybenzoyl)-L-homocysteine
-
low micromolar inhibitor
sinefungin
-
-
spermatinamine
-
-
[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
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
formyl-methionine-leucine-phenylalanine
-
stimulation of carboxyl methylation of GTP-binding proteins through a substrate-dependent mechanism
guanosine 5'-[gamma-thio]-triphosphate
-
stimulation of 23000 Da protein methylation
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0059
4-benzoyl-N-([2-[2-([5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl]amino)ethoxy]ethoxy]acetyl)-L-phenylalanyl-S-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-L-cysteine
-
at pH 7.5 and 25°C
0.015
biotin-Peg4-YIIKGVFWDPAC(C10-meta-Bp)
-
at pH 7.5 and 25°C
0.0051
biotin-Peg4-YIIKGVFWDPAC(C10-para-Bp)
-
at pH 7.5 and 25°C
0.0146
biotin-Peg4-YIIKGVFWDPAC(C5-meta-Bp)
-
IC50 above 0.1 mM, at pH 7.5 and 25°C
0.0061
biotin-Peg4-YIIKGVFWDPAC(C5-para-Bp)
-
IC50 above 0.1 mM, at pH 7.5 and 25°C
0.0021
biotin-S-farnesyl-L-cysteine
-
-
0.0105
N-((benzoylglycyl)glycyl)-S-farnesyl-L-cysteine
-
-
0.00255
N-(benzoylglycyl)-S-farnesyl-L-cysteine
-
-
0.0116 - 0.02
N-acetyl-S-(E,E)-farnesyl-L-cysteine
0.0159
N-acetyl-S-farnesyl-L-cysteine
-
at pH 7.5 and 25°C
0.0014
N-acetyl-S-geranylgeranyl-L-cysteine
-
-
0.00295
N-isobutyryl-S-farnesyl-L-cysteine
-
-
0.00255
N-isovaleryl-S-farnesyl-L-cysteine
-
-
0.0013 - 0.0084
S-adenosyl-L-methionine
0.0034
S-[(2E,6E)-8-(3-benzoylphenoxy)-3,7-dimethylocta-2,6-dien-1-yl]-N-([2-[2-([5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl]amino)ethoxy]ethoxy]acetyl)-D-cysteine
-
at pH 7.5 and 25°C
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1.25
S-adenosyl-L-methionine
-
wild type enzyme, at pH 7.4 and 25°C
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0011 - 0.0029
4-[(naphthalen-2-yl)(thiophen-2-yl)methylidene]oxane
3.95
5'-deoxymethylthioadenosine
-
-
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
0.1193 - 0.3772
N-Acetyl-S-(3-(3-methylbut-2-enyl)-5-(4-phenyl)phenylpent-2Z-en-1-yl)-L-cysteine
0.00207 - 0.005
N-acetyl-S-farnesyl-L-cysteine methyl ester
0.00157 - 0.0044
S-adenosyl-L-homocysteine
0.00117 - 0.0137
S-Farnesylthioacetic acid
0.00007
sinefungin
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0015
4-[(naphthalen-2-yl)(thiophen-2-yl)methylidene]oxane
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0007
(1-octyl-5-m-tolyl-1H-indol-3-yl)methanamine
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.000031
(3,5-difluoro-4-methoxyphenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000025
(3-chloro-4-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.0000038
(3-chlorophenyl)-[2-(2,2-dimethyl-4-thiophen-2-yltetrahydropyran-4-yl)ethyl]amine
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00047
(4-chloro-3-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000032
(5-chloro-2-fluorophenyl)-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]amine
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.049
(R)-2-(2-((benzyloxy)methyl)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)-thio)propanoic acid
Homo sapiens
-
in 100 mM Tris-HCl, pH 7.5, at 30°C
0.075
(R)-2-(2-(phenoxymethyl)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
Homo sapiens
-
in 100 mM Tris-HCl, pH 7.5, at 30°C
0.0147
(R)-2-(2-(phenylthio)benzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
Homo sapiens
-
in 100 mM Tris-HCl, pH 7.5, at 30°C
0.038
(R)-2-(2-benzylbenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
Homo sapiens
-
in 100 mM Tris-HCl, pH 7.5, at 30°C
0.038
(R)-2-(2-phenoxybenzamido)-3-(((2E,6E,10E)-3,7,11,15-tetramethylhexadeca-2,6,10,14-tetraen-1-yl)thio)propanoic acid
Homo sapiens
-
in 100 mM Tris-HCl, pH 7.5, at 30°C
0.21
(R)-2-(2-phenoxybenzamido)-3-(undecylthio)propanoic acid
Homo sapiens
-
in 100 mM Tris-HCl, pH 7.5, at 30°C
0.0226
(R)-2-(3-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
Homo sapiens
-
in 100 mM Tris-HCl, pH 7.5, at 30°C
0.063
(R)-2-(4-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
Homo sapiens
-
in 100 mM Tris-HCl, pH 7.5, at 30°C
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
Homo sapiens
-
in 100 mM Tris-HCl, pH 7.5, at 30°C
0.0067
(R)-2-(N-methyl-2-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
Homo sapiens
-
in 100 mM Tris-HCl, pH 7.5, at 30°C
0.149
(R,E)-3-((3,7-dimethylocta-2,6-dien-1-yl)thio)-2-(2-phenoxybenzamido)propanoic acid
Homo sapiens
-
in 100 mM Tris-HCl, pH 7.5, at 30°C
0.0078
(S)-2-(2-phenoxybenzamido)-3-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)propanoic acid
Homo sapiens
-
in 100 mM Tris-HCl, pH 7.5, at 30°C
0.025
(S)-glabrol
Homo sapiens
-
-
0.001
1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-fluorophenyl)thiourea
Homo sapiens
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.001
1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-methoxphenyl)urea
Homo sapiens
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
1
1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-(3-methoxyphenyl)thiourea
Homo sapiens
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.001
1-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-3-phenylthiourea
Homo sapiens
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.002
1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-3-(morpholin-4-ylmethyl)-1H-indole
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.0021
1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-3-(piperidin-1-ylmethyl)-1H-indole
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.002
1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-3-[(morpholin-4-yl)methyl]-1H-indole
Homo sapiens
-
pH and temperature not specified in the publication
0.0021
1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-3-[(piperidin-1-yl)methyl]-1H-indole
Homo sapiens
-
pH and temperature not specified in the publication
1
1-(3-chlorophenyl)-3-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)thiourea
Homo sapiens
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
1
1-(3-chlorophenyl)-3-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)urea
Homo sapiens
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.1
1-(3-methylbut-2-enyl)-5-m-tolyl-1H-indole
Homo sapiens
-
IC50 above 0.1 mM, in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.1
1-octyl-5-m-tolyl-1H-indole
Homo sapiens
-
IC50 above 0.1 mM, in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.03
1-octyl-5-m-tolyl-1H-indole-3-carboxamide
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.0007
1-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methanamine
Homo sapiens
-
pH and temperature not specified in the publication
0.017
2'-methoxy-3',3''-diprenyl-licodione
Homo sapiens
-
-
0.03
2'-methoxy-3'-prenyllicodione
Homo sapiens
-
-
0.0065
2-(1-octyl-1H-indol-3-yl)acetamide
0.0018
2-(1-octyl-5-phenyl-1H-indol-3-yl)acetamide
0.005
2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-N-(3-methoxyphenyl)acetamide
Homo sapiens
-
IC50 above 0.005 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.005
2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)-N-phenylacetamide
Homo sapiens
-
IC50 above 0.005 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.001
2-(5-(3-ethoxyphenyl)-1-octyl-1H-indol-3-yl)-N,N-diethylacetamide
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.069
2-(5-fluoro-1-(3-methylbut-2-enyl)-1H-indol-3-yl)acetamide
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.007
2-(5-fluoro-1-octyl-1H-indol-3-yl)acetamide
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.0062
2-phenoxy-phenylfarnesylcysteine
Homo sapiens
-
in 100 mM Tris-HCl, pH 7.5, at 30°C
0.0077
2-[1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-1H-indol-3-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0011
2-[1-[(2E,6E)-2,6-dimethylocta-2,6-dien-1-yl]-5-(3-methylphenyl)-1H-indol-3-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.001
2-[5-(2-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
0.001
2-[5-(3-ethoxyphenyl)-1-octyl-1H-indol-3-yl]-N,N-diethylacetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0013
2-[5-(3-ethoxyphenyl)-1-octyl-1H-indol-3-yl]acetamide
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.0013
2-[5-(3-ethylphenyl)-1-octyl-1H-indol-3-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.069
2-[5-(3-fluorophenyl)-1-(2-methylidenebut-3-en-1-yl)-1H-indol-3-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.007
2-[5-(3-fluorophenyl)-1-octyl-1H-indol-3-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0019
2-[5-(3-methoxyphenyl)-1-octyl-1H-indol-3-yl]acetamide
0.0017
2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(4-methylpiperazin-1-yl)ethan-1-one
Homo sapiens
-
pH and temperature not specified in the publication
0.0017
2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(4-methylpiperazin-1-yl)ethanone
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.0018
2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(piperidin-1-yl)ethan-1-one
Homo sapiens
-
pH and temperature not specified in the publication
0.0018
2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(piperidin-1-yl)ethanone
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.0012
2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(pyrrolidin-1-yl)ethan-1-one
Homo sapiens
-
pH and temperature not specified in the publication
0.0012
2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.0015
2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0025
2-[5-(3-methylphenyl)-1-[3-(trifluoromethyl)benzyl]-1H-indol-3-yl]acetamide
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.0025
2-[5-(3-methylphenyl)-1-[[3-(trifluoromethyl)phenyl]methyl]-1H-indol-3-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.033
2-[5-(3-methylphenyl)-1H-indol-3-yl]acetamide
0.001
2-[5-(4-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
0.00031
2-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl](phenyl)amino]-1-(furan-2-yl)ethanone
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000181
3,4-dichloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2Hpyran-4-yl)ethyl]aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00017
3,5-dichloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.0012
3-(1-octyl-5-m-tolyl-1H-indol-3-yl)propanamide
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.001
3-chloro-4-methyl-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)ethyl]aniline
Homo sapiens
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00046
3-chloro-4-methyl-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.005
3-chloro-N-(3-chlorophenyl)-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydropyran-4-yl)ethyl]aniline
Homo sapiens
-
IC50 above 0.005 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.001
3-chloro-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)-ethyl]aniline
Homo sapiens
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00249
3-chloro-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydrothiopyran-4-yl)ethyl]aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000049
3-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-4-methylaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000025
3-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00383
3-chloro-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.001
3-fluoro-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)-ethyl]aniline
Homo sapiens
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00325
3-fluoro-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.001
3-methoxy-N-[2-(2,2,6,6-tetramethyl-4-phenyl-4-piperidyl)-ethyl]aniline
Homo sapiens
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.0000013
3-methoxy-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydropyran-4-yl)ethyl]aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00042
3-methoxy-N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydrothiopyran-4-yl)ethyl]aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000777
3-methoxy-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.0125
3-methoxy-N-[2-[4-(4-methoxyphenyl)-2,2-dimethyltetrahydro-2H-pyran-4-yl]ethyl]aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00325
3-methyl-N-[2-(4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000556
3-tert-butyl-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.005
3-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethylamino]benzoic acid
Homo sapiens
-
IC50 above 0.005 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.005
3-[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethylamino]phenol
Homo sapiens
-
IC50 above 0.005 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00245
3-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]phenol
Homo sapiens
-
at pH 7.4 and 37°C
0.0012
3-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]propanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00383
3-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]-N,N-dimethylbenzenesulfonamide
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000066
3-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]benzonitrile
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000308
4-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-3-methylaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00036
4-chloro-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00076
4-tert-butyl-N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00171
4-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]-N-methylbenzene-1-sulfonamide
Homo sapiens
-
at pH 7.4 and 37°C
0.0131
4-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]benzenesulfonamide
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000123
4-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]benzonitrile
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.03
5-(3-methylphenyl)-1-octyl-1H-indole-3-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0007
5-(3-methylphenyl)-1-octyl-3-(piperidin-1-ylmethyl)-1H-indole
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.0005
5-(3-methylphenyl)-1-octyl-3-(pyrrolidin-1-ylmethyl)-1H-indole
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.0007
5-(3-methylphenyl)-1-octyl-3-[(piperidin-1-yl)methyl]-1H-indole
Homo sapiens
-
pH and temperature not specified in the publication
0.0005
5-(3-methylphenyl)-1-octyl-3-[(pyrrolidin-1-yl)methyl]-1H-indole
Homo sapiens
-
pH and temperature not specified in the publication
0.0027
5-(3-methylphenyl)-3-(morpholin-4-ylmethyl)-1-octyl-1H-indole
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.0009
5-(3-methylphenyl)-3-[(4-methylpiperazin-1-yl)methyl]-1-octyl-1H-indole
0.0027
5-(3-methylphenyl)-3-[(morpholin-4-yl)methyl]-1-octyl-1H-indole
Homo sapiens
-
pH and temperature not specified in the publication
0.00163
5-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]-N,N-dimethylpyridin-2-amine
Homo sapiens
-
at pH 7.4 and 37°C
0.00086
5-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]pyrimidin-2-amine
Homo sapiens
-
at pH 7.4 and 37°C
0.00226
5-[3-[(diethylamino)methyl]-1-octyl-1H-indol-5-yl]pyrimidine-2-carbonitrile
Homo sapiens
-
at pH 7.4 and 37°C
0.0015 - 0.0019
cysmethynil
0.00288
ethyl 4-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]amino]benzoate
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.1
ethyl [5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetate
Homo sapiens
-
IC50 above 0.1 mM, in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.076
methyl [5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetate
0.000131
N'-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N,N-dimethylbenzene-1,3-diamine
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.0008
N,N-diethyl-2-(5-(3-methoxyphenyl)-1-octyl-1H-indol-3-yl)acetamide
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.0008
N,N-diethyl-2-[5-(3-methoxyphenyl)-1-octyl-1H-indol-3-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0014
N,N-diethyl-2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
0.0013
N,N-dimethyl-1-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methanamine
0.0015
N,N-dimethyl-2-[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]acetamide
0.0012
N-((1-octyl-5-m-tolyl-1H-indol-3-yl)methyl)methanesulfonamide
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.0077
N-(2-methylidenebut-3-en-1-yl)-2-[5-(3-methylphenyl)-1-[3-(trifluoromethyl)benzyl]-1H-indol-3-yl]acetamide
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
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
Homo sapiens
-
pH and temperature not specified in the publication
0.005
N-(3-chlorophenyl)-2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)acetamide
Homo sapiens
-
IC50 above 0.005 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00135
N-(3-[[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]amino]phenyl)acetamide
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.0346
N-acetyl-S-[(2E)-3-methyl-5-(4-octylphenyl)pent-2-en-1-yl]-L-cysteine
Homo sapiens
-
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
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.067
N-ethyl-N-((1-(3-methylbut-2-enyl)-1H-indol-3-yl)methyl) ethanamine
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.035
N-ethyl-N-((5-fluoro-1-(3-methylbut-2-enyl)-1H-indol-3-yl)methyl)ethanamine
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.00261
N-ethyl-N-([1-octyl-5-[3-(trifluoromethyl)phenyl]-1H-indol-3-yl]methyl)ethanamine
Homo sapiens
-
at pH 7.4 and 37°C
0.00172
N-ethyl-N-([5-[4-(methanesulfonyl)phenyl]-1-octyl-1H-indol-3-yl]methyl)ethanamine
Homo sapiens
-
at pH 7.4 and 37°C
0.00442
N-ethyl-N-[(4-fluoro-1-octyl-1H-indol-3-yl)methyl]ethanamine
Homo sapiens
-
at pH 7.4 and 37°C
0.0041
N-ethyl-N-[(5-fluoro-1-octyl-1H-indol-3-yl)methyl]-ethanamine
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.00483
N-ethyl-N-[(5-fluoro-1-octyl-1H-indol-3-yl)methyl]ethanamine
Homo sapiens
-
at pH 7.4 and 37°C
0.00222
N-ethyl-N-[(6-fluoro-1-octyl-1H-indol-3-yl)methyl]ethanamine
Homo sapiens
-
at pH 7.4 and 37°C
0.00227
N-ethyl-N-[(7-fluoro-1-octyl-1H-indol-3-yl)methyl]ethanamine
Homo sapiens
-
at pH 7.4 and 37°C
0.067
N-ethyl-N-[[1-(2-methylidenebut-3-en-1-yl)-1H-indol-3-yl]methyl]ethanamine
Homo sapiens
-
pH and temperature not specified in the publication
0.0024
N-ethyl-N-[[1-(2-methylidenebut-3-en-1-yl)-5-(3-methylphenyl)-1H-indol-3-yl]methyl]ethanamine
0.00175
N-ethyl-N-[[1-octyl-5-(pyridin-3-yl)-1H-indol-3-yl]methyl]ethanamine
Homo sapiens
-
at pH 7.4 and 37°C
0.00158
N-ethyl-N-[[1-octyl-5-(pyrimidin-5-yl)-1H-indol-3-yl]methyl]ethanamine
Homo sapiens
-
at pH 7.4 and 37°C
0.00256
N-ethyl-N-[[5-(2-fluorophenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
Homo sapiens
-
at pH 7.4 and 37°C
0.0006
N-ethyl-N-[[5-(2-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
0.035
N-ethyl-N-[[5-(3-fluorophenyl)-1-(2-methylidenebut-3-en-1-yl)-1H-indol-3-yl]methyl]ethanamine
Homo sapiens
-
pH and temperature not specified in the publication
0.00161 - 0.0041
N-ethyl-N-[[5-(3-fluorophenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
0.00096
N-ethyl-N-[[5-(3-fluoropyridin-4-yl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
Homo sapiens
-
at pH 7.4 and 37°C
0.0007 - 0.00218
N-ethyl-N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
0.0006
N-ethyl-N-[[5-(4-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]ethanamine
0.0009
N-methyl-N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]propan-2-amine
0.0018
N-[(1-octyl-5-m-tolyl-1H-indol-3-yl)methyl]acetamide
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
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
Homo sapiens
-
in 100 mM HEPES buffer pH 7.4, 5 mM MgCl2, and 0.1 mM EDTA, at 37°C
0.000015
N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydropyran-4-yl)-ethyl]aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.001
N-[2-(2,2,6,6-tetramethyl-4-phenyltetrahydrothiopyran-4-yl)ethyl]aniline
Homo sapiens
-
IC50 above 0.001 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.0036
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-2-methylaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000652
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3,4-dimethoxyaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000054
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3,5-dimethylaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00009
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-(trifluoromethoxy)aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00038
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-(trifluoromethyl)aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00004
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-ethylaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000052
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-fluoroaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000167
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-isopropylaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00009
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-methoxy-4-methylaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000015
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-methoxyaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000031
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-3-methylaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000184
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-(trifluoromethoxy)aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000168
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-fluoroaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000132
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-isopropylaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00027
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-methoxyaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000031
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-4-methylaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00985
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N,3-dimethylaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.01
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N-methylaniline
Homo sapiens
-
IC50 above 0.01 mM, in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00234
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]-N-phenylacetamide
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.0027
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)-ethyl]aniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000069
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-3,4-dimethylaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000026
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-3-nitroaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000682
N-[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-4-nitroaniline
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.0134
N-[2-(benzyloxy)benzoyl]-S-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-L-cysteine
Homo sapiens
-
in 100 mM Tris-HCl, pH 7.5, at 30°C
0.0035
N-[3-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-3-(2-methoxyphenyl)propyl]-N-(4-methoxybenzyl)furan-2-carboxamide
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.0017
N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]-N-(propan-2-yl)propan-2-amine
0.0008
N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]-N-propylpropan-1-amine
0.0018
N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0012
N-[[5-(3-methylphenyl)-1-octyl-1H-indol-3-yl]methyl]methanesulfonamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00543
S-[(2E,6E)-8-(3-benzoylphenoxy)-3,7-dimethylocta-2,6-dien-1-yl]-N-([2-[2-([5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl]amino)ethoxy]ethoxy]acetyl)-D-cysteine
Homo sapiens
-
at pH 7.4 and 37°C
0.0025
S-{(2E)-3-[2-(biphenyl-4-yl)ethyl]-6-methylhepta-2,5-dien-1-yl}-N-(2-phenoxybenzoyl)-L-homocysteine
Homo sapiens
-
in 100 mM Tris-HCl, pH 7.5, at 30°C
0.00419
[2-(2,2-dimethyl-4-p-tolyltetrahydropyran-4-yl)ethyl]-(3-methoxyphenyl)amine
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00055
[2-(2,2-dimethyl-4-phenyltetrahydro-2H-pyran-4-yl)ethyl]-(2-fluorophenyl)amine
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.0003
[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]-(2-fluoro-4-methylphenyl)amine
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00016
[2-(2,2-dimethyl-4-phenyltetrahydropyran-4-yl)ethyl]-(3-fluoro-4-methoxyphenyl)amine
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000019
[2-(2,2-dimethyl-4-thiophen-2-yltetrahydropyran-4-yl)-ethyl]-(3-methoxyphenyl)amine
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00027
[2-(2,2-dimethyl-4-thiophen-2-yltetrahydropyran-4-yl)-ethyl]phenylamine
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00019
[2-[4-(3-chlorophenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.000008
[2-[4-(3-fluoro-phenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.00063
[2-[4-(4-chlorophenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
0.0001
[2-[4-(4-fluorophenyl)-2,2-dimethyltetrahydropyran-4-yl]-ethyl]-(3-methoxyphenyl)amine
Homo sapiens
-
in 100 mM HEPES, pH 7.5, 5 mM MgCl2, at 22°C
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
activities of wild-type and mutant enzymes expressed in HEK-293 cells
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.4
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22
-
assay at room temperature
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
UniProt
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
physiological function
ICMT loss-of-function isogenic cell lines for both RAS-transformed human mammary epithelial cells (HME1) and human cancer cell lines MiaPaca-2 and MDA-MB-231 containing naturally occurring mutant KRAS. In both in vitro and in vivo tumorigenesis studies, ICMT loss-of-function abolishes the tumor initiation ability of all major isoforms of mutant RAS in HME1 cells, and the tumor maintenance capacity of MiaPaca-2 and MDA-MB-231 cells
malfunction
metabolism
physiological function
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
ICMT_HUMAN
284
4
31938
Swiss-Prot
Secretory Pathway (Reliability: 3)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
33000
-
x * 33000, SDS-PAGE
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
?
-
x * 33000, SDS-PAGE
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
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
F72A
-
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
additional information
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
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expressed in Sf9 insect cells
-
expressed in Spodoptera frugiperda ovarian membranes
-
Icmt, expression in HEK-293 cells and Cos-1 cells
-
into the pCHH10m3N vector, overexpressed in Saccharomyces cerevisiae
-
overepression in tissue culture cells
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
wild-type p53 represses ICMT transcription. The repressive effect of wild-type p53 is localized to the -209 and -14 region on the ICMT promoter, and p53 is recruited to this region. p53 mutants show a positive effect on ICMT expression
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine
analysis
-
approaches to establish the quantitative structure–activity relationship of indoloacetamides as inhibitors of ICMT
drug development
-
the enzyme is a target for anticancer drug design
medicine
pharmacology
-
the enzyme is a target in anticancer therapy
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Park, S.H.; Lee, H.W.
Inhibition of C-terminal O-methyltransferase by a rat liver cytosolic peptide
Arch. Pharm. Res.
17
354-359
1994
Homo sapiens, Rattus norvegicus
-
Manually annotated by BRENDA team
Klein, Z.; Ben-Baruch, G.; Marciano, D.; Solomon, R.; Altaras, M.; Kloog, Y.
Characterization of the prenylated protein methyltransferase in human endometrial carcinoma
Biochim. Biophys. Acta
1226
330-336
1994
Homo sapiens
Manually annotated by BRENDA team
Pillinger, M.H.; Volker, C.; Stock, J.B.; Weissmann, G.; Philips, M.R.
Characterization of a plasma membrane-associated prenylcysteine-directed a carboxyl methyltransferase in human neutrophils
J. Biol. Chem.
269
1486-1492
1994
Homo sapiens
Manually annotated by BRENDA team
Ma, Y.T.; Shi, Y.Q.; Lim, Y.H.; McGrail, S.H.; Ware, J.A.; Rando, R.R.
Mechanistic studies on human platelet isoprenylated protein methyltransferase: farnesylcysteine analogs block platelet aggregation without inhibiting the methyltransferase
Biochemistry
33
5414-5420
1994
Homo sapiens
Manually annotated by BRENDA team
Hong, K.M.; Choi, Y.B.; Hong, J.H.; Chang, H.S.; Rhee, K.I.; Park, H.; Paik, M.K.
Cysteine carboxyl O-methylation of human placental 23 kDa protein
Exp. Mol. Med.
31
30-35
1999
Homo sapiens
Manually annotated by BRENDA team
Van Dessel, G.A.F.; De Busser, H.M.; Lagrou, A.R.
Prenylcysteine carboxymethyltransferase type III activity is decreased in retinoic acid-treated SH-SY5Y neuroblastoma cells
Int. J. Biochem. Cell Biol.
34
477-486
2002
Homo sapiens
Manually annotated by BRENDA team
Choy, E.; Philips, M.
Expression and activity of human prenylcysteine-directed carboxyl methyltransferase
Methods Enzymol.
325
101-114
2000
Homo sapiens
Manually annotated by BRENDA team
Baron, R.A.; Casey, P.J.
Analysis of the kinetic mechanism of recombinant human isoprenylcysteine carboxylmethyltransferase (Icmt)
BMC Biochem.
5
19
2004
Homo sapiens
Manually annotated by BRENDA team
Papaharalambus, C.; Sajjad, W.; Syed, A.; Zhang, C.; Bergo, M.O.; Alexander, R.W.; Ahmad, M.
Tumor necrosis factor alpha stimulation of Rac1 activity. Role of isoprenylcysteine carboxylmethyltransferase
J. Biol. Chem.
280
18790-18796
2005
Homo sapiens
Manually annotated by BRENDA team
Donelson, J.L.; Hodges, H.B.; Macdougall, D.D.; Henriksen, B.S.; Hrycyna, C.A.; Gibbs, R.A.
Amide-substituted farnesylcysteine analogs as inhibitors of human isoprenylcysteine carboxyl methyltransferase
Bioorg. Med. Chem. Lett.
16
4420-4423
2006
Homo sapiens
Manually annotated by BRENDA team
Leow, J.L.; Baron, R.; Casey, P.J.; Go, M.L.
Quantitative structure-activity relationship (QSAR) of indoloacetamides as inhibitors of human isoprenylcysteine carboxyl methyltransferase
Bioorg. Med. Chem. Lett.
17
1025-1032
2007
Homo sapiens
Manually annotated by BRENDA team
Anderson, J.L.; Henriksen, B.S.; Gibbs, R.A.; Hrycyna, C.A.
The isoprenoid substrate specificity of isoprenylcysteine carboxylmethyltransferase: development of novel inhibitors
J. Biol. Chem.
280
29454-29461
2005
Homo sapiens, Saccharomyces cerevisiae
Manually annotated by BRENDA team
Winter-Vann, A.M.; Baron, R.A.; Wong, W.; dela Cruz, J.; York, J.D.; Gooden, D.M.; Bergo, M.O.; Young, S.G.; Toone, E.J.; Casey, P.J.
A small-molecule inhibitor of isoprenylcysteine carboxyl methyltransferase with antitumor activity in cancer cells
Proc. Natl. Acad. Sci. USA
102
4336-4341
2005
Homo sapiens
Manually annotated by BRENDA team
Cushman, I.; Casey, P.J.
Role of isoprenylcysteine carboxylmethyltransferase-catalyzed methylation in Rho function and migration
J. Biol. Chem.
284
27964-27973
2009
Homo sapiens
Manually annotated by BRENDA team
Wright, L.P.; Court, H.; Mor, A.; Ahearn, I.M.; Casey, P.J.; Philips, M.R.
Topology of mammalian isoprenylcysteine carboxyl methyltransferase determined in live cells with a fluorescent probe
Mol. Cell. Biol.
29
1826-1833
2009
Homo sapiens
Manually annotated by BRENDA team
Buchanan, M.S.; Carroll, A.R.; Fechner, G.A.; Boyle, A.; Simpson, M.; Addepalli, R.; Avery, V.M.; Forster, P.I.; Guymer, G.P.; Cheung, T.; Chen, H.; Quinn, R.J.
Small-molecule inhibitors of the cancer target, isoprenylcysteine carboxyl methyltransferase, from Hovea parvicalyx
Phytochemistry
69
1886-1889
2008
Homo sapiens
Manually annotated by BRENDA team
Bergman, J.A.; Hahne, K.; Song, J.; Hrycyna, C.A.; Gibbs, R.A.
S-farnesyl-thiopropionic acid (FTPA) triazoles as potent inhibitors of isoprenylcysteine carboxyl methyltransferase
ACS Med. Chem. Lett.
3
15-19
2012
Homo sapiens
Manually annotated by BRENDA team
Bergman, J.A.; Hahne, K.; Hrycyna, C.A.; Gibbs, R.A.
Lipid and sulfur substituted prenylcysteine analogs as human Icmt inhibitors
Bioorg. Med. Chem. Lett.
21
5616-5619
2011
Homo sapiens
Manually annotated by BRENDA team
Majmudar, J.D.; Hodges-Loaiza, H.B.; Hahne, K.; Donelson, J.L.; Song, J.; Shrestha, L.; Harrison, M.L.; Hrycyna, C.A.; Gibbs, R.A.
Amide-modified prenylcysteine based Icmt inhibitors: Structure-activity relationships, kinetic analysis and cellular characterization
Bioorg. Med. Chem.
20
283-295
2012
Homo sapiens
Manually annotated by BRENDA team
Cushman, I.; Casey, P.J.
RHO methylation matters: a role for isoprenylcysteine carboxylmethyltransferase in cell migration and adhesion
Cell Adh. Migr.
5
11-15
2011
Homo sapiens
Manually annotated by BRENDA team
Go, M.L.; Leow, J.L.; Gorla, S.K.; Schueller, A.P.; Wang, M.; Casey, P.J.
Amino derivatives of indole as potent inhibitors of isoprenylcysteine carboxyl methyltransferase
J. Med. Chem.
53
6838-6850
2010
Homo sapiens
Manually annotated by BRENDA team
Judd, W.R.; Slattum, P.M.; Hoang, K.C.; Bhoite, L.; Valppu, L.; Alberts, G.; Brown, B.; Roth, B.; Ostanin, K.; Huang, L.; Wettstein, D.; Richards, B.; Willardsen, J.A.
Discovery and SAR of methylated tetrahydropyranyl derivatives as inhibitors of isoprenylcysteine carboxyl methyltransferase (ICMT)
J. Med. Chem.
54
5031-5047
2011
Homo sapiens
Manually annotated by BRENDA team
Hahne, K.; Vervacke, J.S.; Shrestha, L.; Donelson, J.L.; Gibbs, R.A.; Distefano, M.D.; Hrycyna, C.A.
Evaluation of substrate and inhibitor binding to yeast and human isoprenylcysteine carboxyl methyltransferases (Icmts) using biotinylated benzophenone-containing photoaffinity probes
Biochem. Biophys. Res. Commun.
423
98-103
2012
Homo sapiens, Saccharomyces cerevisiae
Manually annotated by BRENDA team
Ramanujulu, P.M.; Yang, T.; Yap, S.Q.; Wong, F.C.; Casey, P.J.; Wang, M.; Go, M.L.
Functionalized indoleamines as potent, drug-like inhibitors of isoprenylcysteine carboxyl methyltransferase (Icmt)
Eur. J. Med. Chem.
63
378-386
2013
Homo sapiens
Manually annotated by BRENDA team
Diver, M.M.; Long, S.B.
Mutational analysis of the integral membrane methyltransferase isoprenylcysteine carboxyl methyltransferase (ICMT) reveals potential substrate binding sites
J. Biol. Chem.
289
26007-26020
2014
Anopheles gambiae (Q7PXA7), Anopheles gambiae, Homo sapiens
Manually annotated by BRENDA team
Bhadoriya, K.; Sharma, M.; Jain, S.
Pharmacophore modeling and atom-based 3D-QSAR studies on amino derivatives of indole as potent isoprenylcysteine carboxyl methyltransferase (Icmt) inhibitors
J. Mol. Struct.
1081
466-476
2015
Homo sapiens
-
Manually annotated by BRENDA team
Teh, J.T.; Zhu, W.L.; Ilkayeva, O.R.; Li, Y.; Gooding, J.; Casey, P.J.; Summers, S.A.; Newgard, C.B.; Wang, M.
Isoprenylcysteine carboxylmethyltransferase regulates mitochondrial respiration and cancer cell metabolism
Oncogene
34
3296-3304
2015
Homo sapiens
Manually annotated by BRENDA team
Liu, Q.; Chen, J.; Fu, B.; Dai, J.; Zhao, Y.; Lai, L.
Isoprenylcysteine carboxylmethyltransferase regulates ovarian cancer cell response to chemotherapy and Ras activation
Biochem. Biophys. Res. Commun.
501
556-562
2018
Homo sapiens (A0A024R4F6), Homo sapiens
Manually annotated by BRENDA team
Zhu, Y.; Hu, Q.; Li, H.
Isoprenylcysteine carboxylmethyltransferase is associated with nasopharyngeal carcinoma chemoresistance and Ras activation
Biochem. Biophys. Res. Commun.
516
784-789
2019
Homo sapiens (A0A024R4F6)
Manually annotated by BRENDA team
Borini Etichetti, C.; Di Benedetto, C.; Rossi, C.; Baglioni, M.V.; Bicciato, S.; Del Sal, G.; Menacho-Marquez, M.; Girardini, J.
Isoprenylcysteine carboxy methyltransferase (ICMT) is associated with tumor aggressiveness and its expression is controlled by the p53 tumor suppressor
J. Biol. Chem.
294
5060-5073
2019
Homo sapiens
Manually annotated by BRENDA team
Butler, K.V.; Bohn, K.; Hrycyna, C.A.; Jin, J.
Non-substrate based, small molecule inhibitors of the human isoprenylcysteine carboxyl methyltransferase
MedChemComm
7
1016-1021
2016
Homo sapiens (O60725), Homo sapiens
Manually annotated by BRENDA team
Lau, H.Y.; Tang, J.; Casey, P.J.; Wang, M.
Isoprenylcysteine carboxylmethyltransferase is critical for malignant transformation and tumor maintenance by all RAS isoforms
Oncogene
36
3934-3942
2017
Homo sapiens (O60725), Homo sapiens
Manually annotated by BRENDA team
Do, M.T.; Chai, T.F.; Casey, P.J.; Wang, M.
Isoprenylcysteine carboxylmethyltransferase function is essential for RAB4A-mediated integrin beta3 recycling, cell migration and cancer metastasis
Oncogene
36
5757-5767
2017
Homo sapiens (O60725)
Manually annotated by BRENDA team