Reaction Details |
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Target | Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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Ligand | BDBM50083589 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_70275 (CHEMBL681414) |
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IC50 | 0.400000±n/a nM |
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Citation | Dinsmore, CJ; Williams, TM; O'Neill, TJ; Liu, D; Rands, E; Culberson, JC; Lobell, RB; Koblan, KS; Kohl, NE; Gibbs, JB; Oliff, AI; Graham, SL; Hartman, GD Imidazole-containing diarylether and diarylsulfone inhibitors of farnesyl-protein transferase. Bioorg Med Chem Lett9:3301-6 (2000) [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 |
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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BDBM50083589 |
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n/a |
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Name | BDBM50083589 |
Synonyms: | 3-[4-((S)-2-Amino-3-mercapto-propylamino)-phenoxy]-benzoic acid | CHEMBL113226 |
Type | Small organic molecule |
Emp. Form. | C16H18N2O3S |
Mol. Mass. | 318.391 |
SMILES | N[C@H](CS)CNc1ccc(Oc2cccc(c2)C(O)=O)cc1 |
Structure |
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