Reaction Details |
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Target | Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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Ligand | BDBM50128788 |
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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 |
Synonyms: | Protein Farnesyltransferase (PFT) | Protein farnesyltransferase |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | Purified bovine brain FTase. |
Components: | This complex has 2 components. |
Component 1 |
Name: | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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 |
Type: | Enzyme |
Mol. Mass.: | 43827.38 |
Organism: | Bos taurus (bovine) |
Description: | The enzyme was purified from a bovine brain homogenate by sequential ammonium sulfate fractionation and affinity chromatography. |
Residue: | 375 |
Sequence: | MAAADGVGEAAQGGDPGQPEPPPPPQPHPPPPPPQPPQEEAAAASPIDDGFLSLDSPTYV
LYRDRPEWADIDPVPQNDGPNPVVQIIYSEKFQDVYDYFRAVLQRDERSERAFKLTRDAI
ELNAANYTVWHFRRVLLKSLQKDLHEEMNYISAIIEEQPKNYQVWHHRRVLVEWLRDPSQ
ELEFIADILTQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVI
SNTTGYNDRAILEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQP
SHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQ
SKHSTESDPPTNVQQ
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Component 2 |
Name: | Protein farnesyltransferase subunit beta |
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 |
Type: | Enzyme Subunit |
Mol. Mass.: | 48758.49 |
Organism: | Bos taurus (bovine) |
Description: | Protein farnesyltransferase subunit beta |
Residue: | 437 |
Sequence: | MASPSSFTYCCPPSSSPIWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ
MVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDVINREKLLQY
LYSLKQPDGSFLMHDGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG
GVPGMEAHGGYTFCGLAALVILKKERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY
SFWQAGLLPLLHRALHAQGDPALSMSRWMFHQQALQEYILMCCQCPTGGLLDKPGKSRDF
YHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATMHFLQKPV
PGFEEHEDEASAEPATD
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BDBM50128788 |
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n/a |
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Name | BDBM50128788 |
Synonyms: | 4-(3-Bromo-phenyl)-6-(4-hydroxy-phenyl)-5-nitro-1-(1-oxy-pyridin-3-ylmethyl)-piperidin-2-one | CHEMBL82466 |
Type | Small organic molecule |
Emp. Form. | C23H20BrN3O5 |
Mol. Mass. | 498.326 |
SMILES | Oc1ccc(cc1)[C@@H]1[C@H](C(CC(=O)N1Cc1ccc[n+]([O-])c1)c1cccc(Br)c1)[N+]([O-])=O |
Structure |
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