Reaction Details Report a problem with these data
Target
Geranylgeranyl transferase type-1 subunit beta
Ligand
BDBM13376
Substrate
K-ras(B) decapeptide
Meas. Tech.
Enzyme Inhibition Assay
IC50
>1000±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:
Bos taurus (bovine)
Description:
Purified from bovine brain
Residue:
377
Sequence:
MAATEDERPTGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDMLDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKNPGTAHPYDSGHIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASCICYMLNNWSGMDMKKAINYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVFSEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILSTQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLRDLHQSWKTKDSKQCSENVHIST
Inhibitor
Name:
BDBM13376
Synonyms:
4-({[4-chloro-2-(4-chlorophenyl)phenyl]methoxy}(1-methyl-1H-imidazol-5-yl)methyl)benzonitrile | A313326 Analogue 9
Type:
Small organic molecule
Emp. Form.:
C25H19Cl2N3O
Mol. Mass.:
448.344
SMILES:
Cn1cncc1C(OCc1ccc(Cl)cc1-c1ccc(Cl)cc1)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