Reaction Details |
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Target | Protein farnesyltransferase subunit beta/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_163505 (CHEMBL772416) |
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IC50 | 500±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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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)/farnesyltransferase beta subunit | Protein farnesyltransferase |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of EBI is 69815 |
Components: | This complex has 2 components. |
Component 1 |
Name: | Protein farnesyltransferase subunit beta |
Synonyms: | CAAX farnesyltransferase subunit beta | FNTB_RAT | FTase-beta | Fntb | Protein farnesyltransferase | Protein farnesyltransferase subunit beta | Ras proteins prenyltransferase subunit beta |
Type: | PROTEIN |
Mol. Mass.: | 48666.41 |
Organism: | Rattus norvegicus |
Description: | EBI_10573 |
Residue: | 437 |
Sequence: | MASSSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ
IVATDVCQFLELCQSPDGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYNVINREKLLQY
LYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG
GVPGMEAHGGYTFCGLAALVILKKERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY
SFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDF
YHTCYCLSGLSIAQHFGSGAMLHDVVMGVPENVLQPTHPVYNIGPDKVIQATTHFLQKPV
PGFEECEDAVTSDPATD
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Component 2 |
Name: | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
Synonyms: | CAAX farnesyltransferase alpha subunit | FNTA_RAT | FTase-alpha | Fnta | GGTase-I-alpha | Protein farnesyltransferase | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha | Type I protein geranyl-geranyltransferase alpha subunit | geranylgeranyltransferase type-I |
Type: | Enzyme |
Mol. Mass.: | 44030.14 |
Organism: | Rattus norvegicus (rat) |
Description: | Recombinant rat enzyme. |
Residue: | 377 |
Sequence: | MAATEGVGESAPGGEPGQPEQPPPPPPPPPAQQPQEEEMAAEAGEAAASPMDDGFLSLDS
PTYVLYRDRAEWADIDPVPQNDGPSPVVQIIYSEKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLRSLQKDLQEEMNYIIAIIEEQPKNYQVWHHRRVLVEWLK
DPSQELEFIADILNQDAKNYHAWQHRQWVIQEFRLWDNELQYVDQLLKEDVRNNSVWNQR
HFVISNTTGYSDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSRYPNLLNQLL
DLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHSRESDIPASV
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BDBM50051826 |
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n/a |
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Name | BDBM50051826 |
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 |
Type | Small organic molecule |
Emp. Form. | C22H31N3OS |
Mol. Mass. | 385.566 |
SMILES | CCCC[C@H]1CN(CCN1C[C@@H](N)CS)C(=O)c1cccc2ccccc12 |
Structure |
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