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TargetProtein Farnesyltransferase (PFT)
LigandBDBM50112379
Substrate/Competitorn/a
Meas. Tech.ChEMBL_70268
IC50 0.170000±n/a nM
Citation Nguyen DNStump CAWalsh ESFernandes CDavide JPEllis-Hutchings MRobinson RGWilliams TMLobell RBHuber HEBuser CA Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I. Bioorg Med Chem Lett 12:1269-73 (2002) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
Protein Farnesyltransferase (PFT)
Name:Protein Farnesyltransferase (PFT)
Synonyms:Protein farnesyltransferase
Type:Protein Complex
Mol. Mass.:n/a
Description:Purified bovine brain FTase.
Components:This complex has 2 components.
Component 1
Name:Protein farnesyltransferase
Synonyms:CAAX farnesyltransferase alpha subunit | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Protein Farnesyltransferase (PFT) Chain A | 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:
MAAADGVGEAAQGGDPGQPEPPPPPQPHPPPPPPQPPQEEAAAASPIDDGFLSLDSPTYV
LYRDRPEWADIDPVPQNDGPNPVVQIIYSEKFQDVYDYFRAVLQRDERSERAFKLTRDAI
ELNAANYTVWHFRRVLLKSLQKDLHEEMNYISAIIEEQPKNYQVWHHRRVLVEWLRDPSQ
ELEFIADILTQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVI
SNTTGYNDRAILEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQP
SHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQ
SKHSTESDPPTNVQQ
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Component 2
Name:Protein farnesyltransferase
Synonyms:CAAX farnesyltransferase subunit beta | FTase-beta | Protein farnesyltransferase beta subunit | Protein farnesyltransferase subunit beta | RAS proteins prenyltransferase beta | Ras proteins prenyltransferase subunit beta
Type:Enzyme Subunit
Mol. Mass.:48758.49
Organism:Bos taurus (bovine)
Description:Protein farnesyltransferase subunit beta
Residue:437
Sequence:
MASPSSFTYCCPPSSSPIWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ
MVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDVINREKLLQY
LYSLKQPDGSFLMHDGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG
GVPGMEAHGGYTFCGLAALVILKKERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY
SFWQAGLLPLLHRALHAQGDPALSMSRWMFHQQALQEYILMCCQCPTGGLLDKPGKSRDF
YHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATMHFLQKPV
PGFEEHEDEASAEPATD
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BDBM50112379
n/a
NameBDBM50112379
Synonyms:1-(3-Chloro-phenyl)-4-{2-[3-(2-methoxy-4'-trifluoromethyl-biphenyl-4-ylmethyl)-3H-imidazol-4-yl]-ethyl}-piperazin-2-one | CHEMBL23460
TypeSmall organic molecule
Emp. Form.C30H28ClF3N4O2
Mol. Mass.569.017
SMILESCOc1cc(Cn2cncc2CCN2CCN(C(=O)C2)c2cccc(Cl)c2)ccc1-c1ccc(cc1)C(F)(F)F
Structure
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