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Target
Geranylgeranyl transferase type-1 subunit beta
Ligand
BDBM13377
Substrate
K-ras(B) decapeptide
Meas. Tech.
Enzyme Inhibition Assay
IC50
2000±n/a nM
Citation
Wang, L; Wang, GT; Wang, X; Tong, Y; Sullivan, G; Park, D; Leonard, NM; Li, Q; Cohen, J; Gu, WZ; Zhang, H; Bauch, JL; Jakob, CG; Hutchins, CW; Stoll, VS; Marsh, K; Rosenberg, SH; Sham, HL; Lin, NH Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors. J Med Chem 47:612-26 (2004) [PubMed] Article
More Info.:
Target
Name:
Geranylgeranyl transferase type-1 subunit beta
Synonyms:
GGTase-I-beta | Geranylgeranyl transferase type I | Geranylgeranyl transferase type-1 subunit beta | PGGT1B | PGTB1_BOVIN | Type I protein geranyl-geranyltransferase subunit beta
Type:
Enzyme
Mol. Mass.:
42483.88
Organism:
Bovine
Description:
Purified from bovine brain
Residue:
377
Sequence:
MAATEDERPTGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDMLDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKNPGTAHPYDSGHIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASCICYMLNNWSGMDMKKAINYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVFSEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILSTQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLRDLHQSWKTKDSKQCSENVHIST
Inhibitor
Name:
BDBM13377
Synonyms:
4-({[4-chloro-2-(3-methoxyphenyl)phenyl]methoxy}(1-methyl-1H-imidazol-5-yl)methyl)benzonitrile | A313326 Analogue 10
Type:
Small organic molecule
Emp. Form.:
C26H22ClN3O2
Mol. Mass.:
443.925
SMILES:
COc1cccc(c1)-c1cc(Cl)ccc1COC(c1cncn1C)c1ccc(cc1)C#N
Substrate
Name:
K-ras(B) decapeptide
Synonyms:
biotin conjugated K-ras decapeptide
Type:
Peptide
Mol. Mass.:
1611.07
Organism:
n/a
Description:
n/a
Residue:
14
Sequence:
ITINKKSKTKCVIM