| Reaction Details |
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 | Report a problem with these data |
| Target | Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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| Ligand | BDBM50327990 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEBML_665227 |
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| IC50 | 54±n/a nM |
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| Citation |  Fletcher, S; Keaney, EP; Cummings, CG; Blaskovich, MA; Hast, MA; Glenn, MP; Chang, SY; Bucher, CJ; Floyd, RJ; Katt, WP; Gelb, MH; Van Voorhis, WC; Beese, LS; Sebti, SM; Hamilton, AD Structure-based design and synthesis of potent, ethylenediamine-based, mammalian farnesyltransferase inhibitors as anticancer agents. J Med Chem53:6867-88 (2010) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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| Name: | Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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| Synonyms: | Farnesyltransferase (FTase) | Protein Farnesyltransferase (PFT) | Protein Farnesyltransferase (PFT) Chain B | Protein farnesyltransferase |
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| Type: | Protein Complex |
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| Mol. Mass.: | n/a |
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| 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. |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | Protein farnesyltransferase subunit beta |
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| 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 |
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| Type: | Enzyme Subunit |
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| Mol. Mass.: | 48766.02 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Protein farnesyltransferase subunit beta |
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| Residue: | 437 |
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| Sequence: | MASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ
IVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQY
LYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG
GVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY
SFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDF
YHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPV
PGFEELKDETSAEPATD
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| Component 2 |
| Name: | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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| 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 |
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| Type: | Enzyme |
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| Mol. Mass.: | 44392.46 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Recombinant human FTase. |
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| Residue: | 379 |
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| Sequence: | MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDS
PSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLR
DPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQR
YFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLL
DLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHSTENDSPTNVQQ
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| BDBM50327990 |
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| n/a |
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| Name | BDBM50327990 |
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| Synonyms: | 1-methyl-1H-imidazole-4-sulfonic acid {2-[(4-cyanophenyl)-(3-methyl-3H-imidazol-4-ylmethyl)amino]ethyl}-(3-methylbenzyl)amide-m-toluene | CHEMBL214659 | N-(2-((4-cyanophenyl)((1-methyl-1H-imidazol-5-yl)methyl)amino)ethyl)-1-methyl-N-(3-methylbenzyl)-1H-imidazole-4-sulfonamide |
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| Type | Small organic molecule |
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| Emp. Form. | C26H29N7O2S |
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| Mol. Mass. | 503.619 |
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| SMILES | Cc1cccc(CN(CCN(Cc2cncn2C)c2ccc(cc2)C#N)S(=O)(=O)c2cn(C)cn2)c1 |
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| Structure | 
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