| Reaction Details |
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 | Report a problem with these data |
| Target | Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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| Ligand | BDBM50051826 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_71811 (CHEMBL683642) |
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| IC50 | 160±n/a nM |
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| Citation |  Williams, TM; Ciccarone, TM; MacTough, SC; Bock, RL; Conner, MW; Davide, JP; Hamilton, K; Koblan, KS; Kohl, NE; Kral, AM; Mosser, SD; Omer, CA; Pompliano, DL; Rands, E; Schaber, MD; Shah, D; Wilson, FR; Gibbs, JB; Graham, SL; Hartman, GD; Oliff, AI; Smith, RL 2-substituted piperazines as constrained amino acids. Application to the synthesis of potent, non carboxylic acid inhibitors of farnesyltransferase. J Med Chem39:1345-8 (1996) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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| Name: | Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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| Synonyms: | Geranylgeranyl Transferase (GGTase-I) | Geranylgeranyl Transferase (GGTase-I)/Protein Farnesyltransferase (PFT) | Geranylgeranyl transferase type I |
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| Type: | Protein Complex |
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| Mol. Mass.: | n/a |
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| Description: | n/a |
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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: | Geranylgeranyl transferase type-1 subunit beta |
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| Synonyms: | GGTase-I-beta | Geranylgeranyl transferase type I | Geranylgeranyl transferase type-1 subunit beta | PGGT1B | PGTB1_BOVIN | Type I protein geranyl-geranyltransferase subunit beta |
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| Type: | Enzyme |
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| Mol. Mass.: | 42483.88 |
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| Organism: | Bos taurus (bovine) |
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| Description: | Purified from bovine brain |
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| Residue: | 377 |
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| Sequence: | MAATEDERPTGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDM
LDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKNPGTAHPYDSG
HIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASC
ICYMLNNWSGMDMKKAINYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVF
SEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILS
TQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLRDLHQS
WKTKDSKQCSENVHIST
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| BDBM50051826 |
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| n/a |
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| Name | BDBM50051826 |
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| Synonyms: | CHEMBL27486 | [(S)-4-((R)-2-Amino-3-mercapto-propyl)-3-butyl-piperazin-1-yl]-naphthalen-1-yl-methanone | [4-((R)-2-Amino-3-mercapto-propyl)-3-butyl-piperazin-1-yl]-naphthalen-1-yl-methanone |
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| Type | Small organic molecule |
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| Emp. Form. | C22H31N3OS |
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| Mol. Mass. | 385.566 |
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| SMILES | CCCC[C@H]1CN(CCN1C[C@@H](N)CS)C(=O)c1cccc2ccccc12 |
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| Structure | 
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