Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
LigandBDBM50126029
Substrate/Competitorn/a
Meas. Tech.ChEBML_69994
IC50 3.3±n/a nM
Citation Lin, NHWang, LCohen, JGu, WZFrost, DZhang, HRosenberg, SSham, H Synthesis and biological evaluation of 4-[3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile as novel farnesyltransferase inhibitor. Bioorg Med Chem Lett13:1293-6 (2003) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Name:Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Synonyms:Farnesyltransferase (FTase) | Protein Farnesyltransferase (PFT) | Protein Farnesyltransferase (PFT) Chain B | Protein farnesyltransferase
Type:Protein Complex
Mol. Mass.:n/a
Description:To express recombinant enzyme in E. coli, the cloned human alpha and beta subunits were co-expressed from a plasmid, in which their expression was translationally coupled.
Components:This complex has 2 components.
Component 1
Name:Protein farnesyltransferase subunit beta
Synonyms:CAAX farnesyltransferase subunit alpha | CAAX farnesyltransferase subunit beta | FNTB | FNTB_HUMAN | FTase-alpha | FTase-beta | GGTase-I-alpha | Protein Farnesyltransferase (PFT) Chain B | Protein farnesyl/geranylgeranyl transferase | Protein farnesyltransferase beta subunit | Protein farnesyltransferase subunit beta | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Ras proteins prenyltransferase subunit alpha | Ras proteins prenyltransferase subunit beta | Type I protein geranyl-geranyltransferase subunit alpha
Type:Enzyme Subunit
Mol. Mass.:48766.02
Organism:Homo sapiens (Human)
Description:Protein farnesyltransferase subunit beta
Residue:437
Sequence:
MASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ
IVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQY
LYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG
GVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY
SFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDF
YHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPV
PGFEELKDETSAEPATD
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
Component 2
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:
MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDS
PSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLR
DPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQR
YFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLL
DLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHSTENDSPTNVQQ
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50126029
n/a
NameBDBM50126029
Synonyms:5-[1-Hydroxy-1-(3-methyl-3H-imidazol-4-yl)-3-phenyl-prop-2-ynyl]-2'-methyl-biphenyl-2-carbonitrile | CHEMBL24822
TypeSmall organic molecule
Emp. Form.C27H21N3O
Mol. Mass.403.4751
SMILESCc1ccccc1-c1cc(ccc1C#N)C(O)(C#Cc1ccccc1)c1cncn1C
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: