| 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 | BDBM50127252 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEBML_70126 |
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| IC50 | 1.6±n/a nM |
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| Citation |  Angibaud, P; Bourdrez, X; Devine, A; End, DW; Freyne, E; Ligny, Y; Muller, P; Mannens, G; Pilatte, I; Poncelet, V; Skrzat, S; Smets, G; Van Dun, J; Van Remoortere, P; Venet, M; Wouters, W 5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors. Bioorg Med Chem Lett13:1543-7 (2003) [PubMed] |
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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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| BDBM50127252 |
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| n/a |
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| Name | BDBM50127252 |
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| Synonyms: | 8-[Amino-(4-chloro-phenyl)-(3-methyl-3H-imidazol-4-yl)-methyl]-6-(3-chloro-phenyl)-2,3-dihydro-1-oxa-3a-aza-phenalen-4-one | CHEMBL38080 |
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| Type | Small organic molecule |
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| Emp. Form. | C28H22Cl2N4O2 |
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| Mol. Mass. | 517.406 |
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| SMILES | Cn1cncc1C(N)(c1ccc(Cl)cc1)c1cc2OCCn3c2c(c1)c(cc3=O)-c1cccc(Cl)c1 |
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| Structure | 
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