Cloned (Comment) | Organism |
---|---|
recombinant mammalian enzyme expressed in Sf9 cells | Mammalia |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3-chloro-N-[2-oxo-2-[2-[[1-phenyl-3-(4-propoxyphenyl)pyrazol-4-yl]methylidene]hydrazinyl]ethyl]benzamide | GGTI-DU.Sig1, PubChem CID 3311883, inhibitor of protein geranylgeranyltransferase type I | Mammalia | |
4-[[([5-[(4-ethylphenoxy)methyl]-4-(1-phenylethyl)-4H-pyrazol-3-yl]sulfanyl)acetyl]amino]benzamide | inhibitor identified using quantitative structure-activity realtionship models and virtual screening of chemicals. confirmation of predicted data by experiment | Rattus norvegicus | |
4-[[2-[[5-(2-methoxyphenyl)-4-phenethyl-1,2,4-triazol-3-yl]sulfanyl]acetyl]amino]benzamide | GGTI-DU.En1, PubChem CID 2118978, inhibitor of protein geranylgeranyltransferase type I | Mammalia | |
4-[[2-[[5-[(4-ethylphenoxy)methyl]-4-(1-phenylethyl)-1,2,4-triazol-3-yl]sulfanyl]acetyl]amino]benzamide | GGTI-DU.En2, PubChem CID 3455185, inhibitor of protein geranylgeranyltransferase type I, no or little activity against protein farnesyltransferase | Mammalia | |
additional information | inhibitors pose a potential treatment for inflammation, multiple sclerosis, atherosclerosis, and other diseases, 47 potential inhibitors with a predicted IC50 greater than 5.50 microM are identified by the use of quantitative structure-activity relationship models and in vitro tests with 7 of them | Mammalia | |
N-(2,5-dichlorophenyl)-N'-[[3-(4-methylphenyl)-1-phenylpyrazol-4-yl]methylideneamino]oxamide | GGTI-DU.Sig2, PubChem CID 4277701, inhibitor of protein geranylgeranyltransferase type I | Mammalia | |
N-benzyl-2-[(2-chlorobenzyl)[[5-(4-methylphenyl)-2H-tetrazol-2-yl]acetyl]amino]butanamide | inhibitor identified using quantitative structure-activity realtionship models and virtual screening of chemicals. confirmation of predicted data by experiment | Rattus norvegicus | |
N-benzyl-2-[(2-chlorophenyl)methyl-[2-[5-(4-methylphenyl)tetrazol-2-yl]acetyl]amino]butanamide | GGTI-DU.As2, PubChem CID 3180738, inhibitor of protein geranylgeranyltransferase type I, no or little activity against protein farnesyltransferase | Mammalia | |
N-[(E)-1-(benzylcarbamoyl)-2-[5-(3,4-dichlorophenyl)furan-2-yl]ethenyl]-4-methylbenzamide | inhibitor identified using quantitative structure-activity realtionship models and virtual screening of chemicals. confirmation of predicted data by experiment | Rattus norvegicus | |
N-[2-(benzylamino)-2-oxoethyl]-2-[5-(4-chlorophenyl)tetrazol-2-yl]-N-(4-propan-2-ylphenyl)acetamide | GGTI-DU.As1, PubChem CID 3180720, inhibitor of protein geranylgeranyltransferase type I | Mammalia | |
N-[3-(benzylamino)-1-[5-(3,4-dichlorophenyl)furan-2-yl]-3-oxoprop-1-en-2-yl]-4-methylbenzamide | GGTI-DU.Sig3, PubChem CID 5143450, inhibitor of protein geranylgeranyltransferase type I, no or little activity against protein farnesyltransferase | Mammalia |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
geranylgeranyl diphosphate + Ras-CVLL | Mammalia | tritium labelled geranylgeranyl diphosphate for enzyme assay, His-tagged geranylgeranyl diphosphate | S-geranylgeranyl-Ras-CVLL + diphosphate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Mammalia | - |
- |
- |
Rattus norvegicus | - |
- |
- |
Purification (Comment) | Organism |
---|---|
- |
Mammalia |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
geranylgeranyl diphosphate + Ras-CVLL | tritium labelled geranylgeranyl diphosphate for enzyme assay, His-tagged geranylgeranyl diphosphate | Mammalia | S-geranylgeranyl-Ras-CVLL + diphosphate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
mammalian GGTase-I | - |
Mammalia |
protein geranylgeranyltransferase type I | - |
Mammalia |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.008 | - |
30°C | Rattus norvegicus | 4-[[([5-[(4-ethylphenoxy)methyl]-4-(1-phenylethyl)-4H-pyrazol-3-yl]sulfanyl)acetyl]amino]benzamide | |
0.035 | - |
30°C | Rattus norvegicus | N-benzyl-2-[(2-chlorobenzyl)[[5-(4-methylphenyl)-2H-tetrazol-2-yl]acetyl]amino]butanamide | |
0.043 | - |
30°C | Rattus norvegicus | N-[(E)-1-(benzylcarbamoyl)-2-[5-(3,4-dichlorophenyl)furan-2-yl]ethenyl]-4-methylbenzamide |