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TargetProtein Farnesyltransferase (PFT)
LigandBDBM50127321
Substrate/Competitorn/a
Meas. Tech.ChEMBL_69852
IC50 0.180000±n/a nM
Citation Tong YLin NHWang LHasvold LWang WLeonard NLi TLi QCohen JGu WZZhang HStoll VBauch JMarsh KRosenberg SHSham HL Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability. Bioorg Med Chem Lett 13:1571-4 (2003) [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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BDBM50127321
n/a
NameBDBM50127321
Synonyms:5-[(4-Cyano-phenyl)-(3-methyl-3H-imidazol-4-yl)-methoxymethyl]-6-(2,2-difluoro-benzo[1,3]dioxol-5-yl)-pyridine-2-carbonitrile | CHEMBL41951
TypeSmall organic molecule
Emp. Form.C26H17F2N5O3
Mol. Mass.485.4417
SMILESCn1cncc1C(OCc1ccc(nc1-c1ccc2OC(F)(F)Oc2c1)C#N)c1ccc(cc1)C#N
Structure
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