2.5.1.59: protein geranylgeranyltransferase type I

This is an abbreviated version!
For detailed information about protein geranylgeranyltransferase type I, go to the full flat file.

Word Map on EC 2.5.1.59

2.5.1.59

geranylgeranylation

prenylation

farnesyltransferase

farnesylation

ftase

isoprenoids

prenyltransferases

gtpases

rhoa

peptidomimetic

rab

mevalonate

isoprenylation

ggtis

h-ras

geranylgeraniol

farnesylpyrophosphate

rap1a

lovastatin

geranylgeranylpyrophosphate

20-carbon

escort

medicine

molecular biology

k-ras4b

pharmacology

Reaction

Synonyms

CAAX geranylgeranyltransferase, CaaX prenyltransferase, CaGGTase-I, CDC43, geranylgeranyl protein transferase type I, geranylgeranyltransferase I, geranylgeranyltransferase type I, geranylgeranyltransferase type-I, geranylgeranyltransferase-1, geranylgeranyltransferase-I, geranylgeranyltransferaseI, GGT, GGT I, GGTalpha, GGTase, GGTase I, Ggtase-1, GGTase-I, GGTaseI, GGTbeta, GGTI, mammalian GGTase-I, PGGT, PGGT beta, PGGT I, PGGT-I, PGGTase-I, PGGTaseI, Ppggb, protein geranylgeranyltransferase, protein geranylgeranyltransferase I, protein geranylgeranyltransferase type I, protein geranylgeranyltransferase type-I, protein geranylgeranyltransferase-I, type I protein geranylgeranyltransferase

ECTree

2 Transferases

2.5 Transferring alkyl or aryl groups, other than methyl groups

2.5.1 Transferring alkyl or aryl groups, other than methyl groups (only sub-subclass identified to date)

2.5.1.59 protein geranylgeranyltransferase type I

Advanced search results

Do not include text mining results

Include

results (more...)

Include

results (more...)

Results	in table
2	Activating Compound
1401	AA Sequence
7	Application
1	CAS Registry Number
19	Cloned(Commentary)
5	Crystallization (Commentary)
346	Disease/ Diagnostics
32	General Information
41	IC50 Value
117	Inhibitors
4	kcat/KM [mM/s]
14	Ki Value [mM]
28	KM Value [mM]
12	Localization
30	Metals/Ions
14	Molecular Weight [Da]
57	Natural Substrates/ Products (Substrates)
1	Organic Solvent Stability
73	Organism
150	PDB ID
3	pH Optimum
1	pH Range
1	pH Stability
1	Posttranslational Modification
15	Protein Variants
15	Purification (Commentary)
17	Reaction
73	Reference
58	Source Tissue
3	Specific Activity [micromol/min/mg]
162	Substrates and Products (Substrate)
18	Subunits
105	Synonyms
1	Systematic Name
32	Turnover Number [1/s]

IC50 Value

print visible entries

print all entries

Go back to the abbreviated version
of the Enzyme Summary Page.

IC50 Value on EC 2.5.1.59 - protein geranylgeranyltransferase type I

Please wait a moment until all data is loaded. This message will disappear when all data is loaded.

top print hide

Go to IC50 Value Search

0.25 - 4

(2S,5R)-5-ethyl-2-(4-fluorophenyl)-1-tosyl-2,5-dihydro-1H-pyrrole-3-carboxylic acid

Homo sapiens

IC50: 0.2 mM using RhoA as a substrate, IC50: 0.25 mM using Ki-Ras4B as a substrate

674210

0.0009 - 4

(2S,5S)-5-tert-butyl-2-(4-chlorophenyl)-1-[(2-methylphenyl)sulfonyl]-2,5-dihydro-1H-pyrrole-3-carboxylic acid

Homo sapiens

IC50: 0.0005 mM using RhoA as a substrate, IC50: 0.0009 mM using Ki-Ras4B as a substrate

674210

0.002 - 4

(2S,6S)-2,6-bis(4-chlorophenyl)-1-[(2-methylphenyl)sulfonyl]-1,2,5,6-tetrahydropyridine-3-carboxylic acid

Homo sapiens

IC50: 0.0003 mM using RhoA as a substrate, IC50: 0.002 mM using Ki-Ras4B as a substrate

674210

0.08 - 4

(2S,6S)-6-(4-fluorophenyl)-1-[(4-methylphenyl)sulfonyl]-2-phenyl-1,2,5,6-tetrahydropyridine-3-carboxylic acid

Homo sapiens

IC50: 0.12 mM using RhoA as a substrate, IC50: 0.08 mM using Ki-Ras4B as a substrate

674210

0.0024

(S)-N-(1-amino-3-(4-fluorophenyl)-1-oxopropan-2-yl)-4-((1-(3,4-dichlorophenyl)-4-(2-(methylthio)ethyl)-3-(pyridin-3-yl)-1H-pyrazol-5-yl)oxy)butanamide

Homo sapiens

P49354; P49356

pH 7.4, 30°C

759142

0.0031

(S)-N-(1-amino-3-(4-methoxyphenyl)-1-oxopropan-2-yl)-4-((1-(3,4-dichlorophenyl)-4-(2-(methylthio)ethyl)-3-(pyridin-3-yl)-1H-pyrazol-5-yl)oxy)butanamide

Homo sapiens

P49354; P49356

pH 7.4, 30°C

759142

0.021

(S)-N-(4-(3,4-dichlorophenoxy)benzyl)-6-(1H-indol-3-yl)piperazine-2,5-dione

Rattus norvegicus

pH 7.4, 30°C

722188

0.0323

(S)-N-(4-(3-chlorophenoxy)benzyl)-6-(1H-indol-3-yl)piperazine-2,5-dione

Rattus norvegicus

pH 7.4, 30°C

722188

0.006525

1-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-cyclohexanecarboxylic acid

Homo sapiens

IC50: 6525 nM

672535

0.01

1-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-cyclohexanecarboxylic acid methyl ester

Homo sapiens

IC50: above 0.01 mM

672535

0.0014

11-aminoundecylcarbonyl-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine

Rattus norvegicus

686092

0.000021

2-aryl-4-aminobenzoic acid

Homo sapiens

IC50: 21 nM

672535

0.01

2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-N-(3-methyl-butyl)-acetamide

Homo sapiens

IC50: above 0.01 mM

672535

0.01

2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl] acetylamino}-4-methyl-pentanoic acid methyl ester

Homo sapiens

IC50: above 0.01 mM

672535

0.00017 - 0.0063

2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-3-phenyl-propionic acid

2 entries

0.0045 - 0.01

2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-3-phenyl-propionic acid methyl ester

2 entries

0.00058 - 0.0027

2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-4-methyl-pentanoic acid

2 entries

0.01

2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-4-methyl-pentanoic acid methyl ester

Homo sapiens

IC50: above 0.01 mM

672535

0.00335

2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-4-methylsulfanyl-butyric acid

Homo sapiens

IC50: 3350 nM

672535

0.01

2-{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-4-methylsulfanyl-butyric acid methyl ester

Homo sapiens

IC50: above 0.01 mM

672535

0.008

4-[[([5-[(4-ethylphenoxy)methyl]-4-(1-phenylethyl)-4H-pyrazol-3-yl]sulfanyl)acetyl]amino]benzamide

Rattus norvegicus

30°C

705040

0.00007

GGTI-DU40

Sus scrofa

complete inhibition at 5 microM, tritium-labelled geranylgeranyl diphosphate for activity assay with lysate of trabecular mesh cells, 30°C

708819

0.0048

L-cysteinyl-L-valyl-L-isoleucyl-L-leucine

Homo sapiens

686092

0.0014

N-(12-ammoniododecanoyl)-D-cysteinyl-L-valyl-L-isoleucyl-L-leucine trifluoroacetate

Homo sapiens

686092

0.00098

N-(12-[[(3-[[(3R)-3-ammonio-4-phenylbutyl]oxy]-4,5-bis[[(3S)-3-ammonio-4-phenylbutyl]oxy]phenyl)carbonyl]amino]dodecanoyl)-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine tris(trifluoroacetate)

Homo sapiens

686092

0.00066

N-(4-[[(3-[[(3R)-3-ammonio-4-phenylbutyl]oxy]-4,5-bis[[(3S)-3-ammonio-4-phenylbutyl]oxy]phenyl)carbonyl]amino]butanoyl)-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine tris(trifluoroacetate)

Homo sapiens

686092

0.000466

N-([(2S)-2-benzyl-4-[(4-methyl-1H-imidazol-5-yl)methyl]-3-oxopiperazin-1-yl]carbonyl)-L-leucine

Homo sapiens

P49354, P53609

pH and temperature not specified in the publication

738097

0.035

N-benzyl-2-[(2-chlorobenzyl)[[5-(4-methylphenyl)-2H-tetrazol-2-yl]acetyl]amino]butanamide

Rattus norvegicus

30°C

705040

0.043

N-[(E)-1-(benzylcarbamoyl)-2-[5-(3,4-dichlorophenyl)furan-2-yl]ethenyl]-4-methylbenzamide

Rattus norvegicus

30°C

705040

0.0006

N-[12-([[3,4,5-tris(3-ammoniopropoxy)phenyl]carbonyl]amino)dodecanoyl]-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine tris(trifluoroacetate)

Homo sapiens

686092

0.0006

N-[6-(3,4,5-tris(3-amino-1-propoxy)benzoylamino)-undecylcarbonyl]-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine

Rattus norvegicus

686092

0.00066

N-[6-(3,4,5-tris(3-amino-4-phenyl-1-butoxy)benzoylamino)-propylcarbonyl]-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine

Rattus norvegicus

686092

0.00064 - 0.00098

N-[6-(3,4,5-tris(3-amino-4-phenyl-1-butoxy)benzoylamino)-undecylcarbonyl]-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine

2 entries

0.000313

Na-(4-[[1-(3,4-dichlorophenyl)-4-[2-(methylsulfanyl)ethyl]-3-(pyridin-3-yl)-1H-pyrazol-5-yl]oxy]butanoyl)-L-phenylalaninamide

Homo sapiens

P49354, P53609

pH and temperature not specified in the publication

738097

0.01

[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetic acid benzyl ester

Homo sapiens

IC50: above 0.01 mM

672535

0.01

{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-acetic acid

Homo sapiens

IC50: above 0.01 mM

672535

0.01

{2-[3-(1H-imidazol-4-ylmethyl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-acetylamino}-acetic acid methyl ester

Homo sapiens

IC50: above 0.01 mM

672535