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TargetProtein Farnesyltransferase (PFT)/farnesyltransferase beta subunit
LigandBDBM50060141
Substrate/Competitorn/a
Meas. Tech.ChEMBL_70733
IC50 4±n/a nM
Citation McNamara DJDobrusin ELeonard DMShuler KRKaltenbronn JSQuin JBur SThomas CEDoherty AMScholten JDZimmerman KKGibbs BSGowan RCLatash MPLeopold WRPrzybranowski SASebolt-Leopold JS C-terminal modifications of histidyl-N-benzylglycinamides to give improved inhibition of Ras farnesyltransferase, cellular activity, and anticancer activity in mice. J Med Chem 40:3319-22 (1997) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Protein Farnesyltransferase (PFT)/farnesyltransferase beta subunit
Name:Protein Farnesyltransferase (PFT)/farnesyltransferase beta subunit
Synonyms:Protein farnesyltransferase
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of EBI is 69815
Components:This complex has 2 components.
Component 1
Name:Protein farnesyltransferase
Synonyms:CAAX farnesyltransferase subunit beta | FTase-beta | Protein farnesyltransferase subunit beta | Ras proteins prenyltransferase subunit beta
Type:PROTEIN
Mol. Mass.:48666.41
Organism:Rattus norvegicus
Description:EBI_10573
Residue:437
Sequence:
MASSSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ
IVATDVCQFLELCQSPDGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYNVINREKLLQY
LYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG
GVPGMEAHGGYTFCGLAALVILKKERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY
SFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDF
YHTCYCLSGLSIAQHFGSGAMLHDVVMGVPENVLQPTHPVYNIGPDKVIQATTHFLQKPV
PGFEECEDAVTSDPATD
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Component 2
Name:geranylgeranyltransferase type-I
Synonyms:CAAX farnesyltransferase alpha subunit | FTase-alpha | GGTase-I-alpha | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha | Type I protein geranyl-geranyltransferase alpha subunit
Type:Enzyme
Mol. Mass.:44030.14
Organism:Rattus norvegicus (rat)
Description:Recombinant rat enzyme.
Residue:377
Sequence:
MAATEGVGESAPGGEPGQPEQPPPPPPPPPAQQPQEEEMAAEAGEAAASPMDDGFLSLDS
PTYVLYRDRAEWADIDPVPQNDGPSPVVQIIYSEKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLRSLQKDLQEEMNYIIAIIEEQPKNYQVWHHRRVLVEWLK
DPSQELEFIADILNQDAKNYHAWQHRQWVIQEFRLWDNELQYVDQLLKEDVRNNSVWNQR
HFVISNTTGYSDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSRYPNLLNQLL
DLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHSRESDIPASV
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BDBM50060141
n/a
NameBDBM50060141
Synonyms:CHEMBL431440 | [(S)-1-{(4-Benzyloxy-benzyl)-[(2-methyl-2-phenyl-propylcarbamoyl)-methyl]-carbamoyl}-2-(3H-imidazol-4-yl)-ethyl]-carbamic acid benzyl ester
TypeSmall organic molecule
Emp. Form.C40H43N5O5
Mol. Mass.673.7999
SMILESCC(C)(CNC(=O)CN(Cc1ccc(OCc2ccccc2)cc1)C(=O)[C@H](Cc1cnc[nH]1)NC(=O)OCc1ccccc1)c1ccccc1
Structure
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