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Target
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM13374
Substrate
K-ras(B) decapeptide
Meas. Tech.
Enzyme Inhibition Assay
pH
7±n/a
Temperature
310.15±n/a K
IC50
8.9±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 
Target
Name:
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
CAAX farnesyltransferase alpha subunit | FNTA | FNTA_HUMAN | FTase-1-alpha | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Geranylgeranyl transferase type I | Protein Farnesyltransferase (PFT) Chain A | Protein farnesyl/geranylgeranyl transferase | Protein farnesyltransferase | Protein farnesyltransferase subunit alpha | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha
Type:
Enzyme
Mol. Mass.:
44392.46
Organism:
Homo sapiens (Human)
Description:
Recombinant human FTase.
Residue:
379
Sequence:
MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDSPSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLRDPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHSTENDSPTNVQQ
  
Inhibitor
Name:
BDBM13374
Synonyms:
4-({[4-chloro-2-(2-chlorophenyl)phenyl]methoxy}(1-methyl-1H-imidazol-5-yl)methyl)benzonitrile | A313326 Analogue 7
Type:
Small organic molecule
Emp. Form.:
C25H19Cl2N3O
Mol. Mass.:
448.344
SMILES:
Cn1cncc1C(OCc1ccc(Cl)cc1-c1ccccc1Cl)c1ccc(cc1)C#N
Structure:
Search PDB for entries with ligand similarity:
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