Reaction Details |
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Target | Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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Ligand | BDBM13320 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_305032 (CHEMBL831671) |
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IC50 | 0.3±n/a nM |
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Citation | Lombardo, LJ; Camuso, A; Clark, J; Fager, K; Gullo-Brown, J; Hunt, JT; Inigo, I; Kan, D; Koplowitz, B; Lee, F; McGlinchey, K; Qian, L; Ricca, C; Rovnyak, G; Traeger, S; Tokarski, J; Williams, DK; Wu, LI; Zhao, Y; Manne, V; Bhide, RS Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors. Bioorg Med Chem Lett15:1895-9 (2005) [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 |
Synonyms: | Farnesyltransferase (FTase) | Protein Farnesyltransferase (PFT) | Protein Farnesyltransferase (PFT) Chain B | Protein farnesyltransferase |
Type: | Protein Complex |
Mol. Mass.: | n/a |
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. |
Components: | This complex has 2 components. |
Component 1 |
Name: | Protein farnesyltransferase subunit beta |
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 |
Type: | Enzyme Subunit |
Mol. Mass.: | 48766.02 |
Organism: | Homo sapiens (Human) |
Description: | Protein farnesyltransferase subunit beta |
Residue: | 437 |
Sequence: | MASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ
IVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQY
LYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG
GVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY
SFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDF
YHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPV
PGFEELKDETSAEPATD
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Component 2 |
Name: | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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 |
Type: | Enzyme |
Mol. Mass.: | 44392.46 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant human FTase. |
Residue: | 379 |
Sequence: | MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDS
PSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLR
DPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQR
YFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLL
DLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHSTENDSPTNVQQ
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BDBM13320 |
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n/a |
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Name | BDBM13320 |
Synonyms: | 1-Methyl-1H-imidazole-4-sulfonic Acid [6-Cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]-(2-methylallyl)amide | BMS-388891 | CHEMBL181102 | N-{6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl}-1-methyl-N-(2-methylprop-2-en-1-yl)-1H-imidazole-4-sulfonamide | tetrahydroquinoline (THQ)-based inhibitor 4b |
Type | Small organic molecule |
Emp. Form. | C23H27N7O2S |
Mol. Mass. | 465.571 |
SMILES | CC(=C)CN(C1CN(Cc2cncn2C)c2ccc(cc2C1)C#N)S(=O)(=O)c1cn(C)cn1 |
Structure |
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