| 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 | BDBM50128792 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_70274 (CHEMBL681413) |
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| IC50 | >3700±n/a nM |
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| Citation |  Nara, S; Tanaka, R; Eishima, J; Hara, M; Takahashi, Y; Otaki, S; Foglesong, RJ; Hughes, PF; Turkington, S; Kanda, Y Discovery and structure-activity relationships of novel piperidine inhibitors of farnesyltransferase. J Med Chem46:2467-73 (2003) [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: | Protein Farnesyltransferase (PFT) | Protein farnesyltransferase |
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| Type: | Protein Complex |
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| Mol. Mass.: | n/a |
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| Description: | Purified bovine brain FTase. |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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| Synonyms: | CAAX farnesyltransferase alpha subunit | FNTA | FNTA_BOVIN | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Protein Farnesyltransferase (PFT) Chain A | Protein farnesyltransferase | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha | Type I protein geranyl-geranyltransferase alpha subunit |
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| Type: | Enzyme |
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| Mol. Mass.: | 43827.38 |
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| Organism: | Bos taurus (bovine) |
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| Description: | The enzyme was purified from a bovine brain homogenate by sequential ammonium sulfate fractionation and affinity chromatography. |
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| Residue: | 375 |
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| Sequence: | MAAADGVGEAAQGGDPGQPEPPPPPQPHPPPPPPQPPQEEAAAASPIDDGFLSLDSPTYV
LYRDRPEWADIDPVPQNDGPNPVVQIIYSEKFQDVYDYFRAVLQRDERSERAFKLTRDAI
ELNAANYTVWHFRRVLLKSLQKDLHEEMNYISAIIEEQPKNYQVWHHRRVLVEWLRDPSQ
ELEFIADILTQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVI
SNTTGYNDRAILEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQP
SHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQ
SKHSTESDPPTNVQQ
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| Component 2 |
| Name: | Protein farnesyltransferase subunit beta |
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| Synonyms: | CAAX farnesyltransferase subunit beta | FNTB | FNTB_BOVIN | FTase-beta | Protein farnesyltransferase | Protein farnesyltransferase beta subunit | Protein farnesyltransferase subunit beta | RAS proteins prenyltransferase beta | Ras proteins prenyltransferase subunit beta |
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| Type: | Enzyme Subunit |
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| Mol. Mass.: | 48758.49 |
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| Organism: | Bos taurus (bovine) |
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| Description: | Protein farnesyltransferase subunit beta |
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| Residue: | 437 |
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| Sequence: | MASPSSFTYCCPPSSSPIWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ
MVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDVINREKLLQY
LYSLKQPDGSFLMHDGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG
GVPGMEAHGGYTFCGLAALVILKKERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY
SFWQAGLLPLLHRALHAQGDPALSMSRWMFHQQALQEYILMCCQCPTGGLLDKPGKSRDF
YHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATMHFLQKPV
PGFEEHEDEASAEPATD
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| BDBM50128792 |
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| n/a |
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| Name | BDBM50128792 |
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| Synonyms: | 5-Amino-4-(3-bromo-phenyl)-6-(4-hydroxy-phenyl)-1-pyridin-3-ylmethyl-piperidin-2-one | CHEMBL433139 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H22BrN3O2 |
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| Mol. Mass. | 452.344 |
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| SMILES | N[C@H]1C(CC(=O)N(Cc2cccnc2)[C@@H]1c1ccc(O)cc1)c1cccc(Br)c1 |
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| Structure | 
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