Target
Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM50157252
Substrate
n/a
Meas. Tech.
ChEMBL_305821 (CHEMBL829564)
IC50
160±n/a nM
Citation
 Wang, GTWang, XWang, WHasvold, LASullivan, GHutchins, CWO'Conner, SGentiles, RSowin, TCohen, JGu, WZZhang, HRosenberg, SHSham, HL Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase. Bioorg Med Chem Lett 15:153-8 (2004) [PubMed]  Article 
Target
Name:
Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
Geranylgeranyl Transferase (GGTase-I) | Geranylgeranyl Transferase (GGTase-I)/Protein Farnesyltransferase (PFT) | Geranylgeranyl transferase type I
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
CAAX farnesyltransferase alpha subunit | FNTA | FNTA_BOVIN | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Protein Farnesyltransferase (PFT) Chain A | Protein farnesyltransferase | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha | Type I protein geranyl-geranyltransferase alpha subunit
Type:
Enzyme
Mol. Mass.:
43827.38
Organism:
Bos taurus (bovine)
Description:
The enzyme was purified from a bovine brain homogenate by sequential ammonium sulfate fractionation and affinity chromatography.
Residue:
375
Sequence:
MAAADGVGEAAQGGDPGQPEPPPPPQPHPPPPPPQPPQEEAAAASPIDDGFLSLDSPTYVLYRDRPEWADIDPVPQNDGPNPVVQIIYSEKFQDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYISAIIEEQPKNYQVWHHRRVLVEWLRDPSQELEFIADILTQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVISNTTGYNDRAILEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHSTESDPPTNVQQ
  
Component 2
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:
BDBM50157252
Synonyms:
5-[(3-Fluoro-4-trifluoromethyl-benzyloxy)-(3-methyl-3H-imidazol-4-yl)-methyl]-2''-trifluoromethyl-biphenyl-2-carbonitrile | CHEMBL182812
Type:
Small organic molecule
Emp. Form.:
C27H18F7N3O
Mol. Mass.:
533.4401
SMILES:
Cn1cncc1C(OCc1ccc(c(F)c1)C(F)(F)F)c1ccc(C#N)c(c1)-c1ccccc1C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: