Reaction Details |
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Target | Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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Ligand | BDBM50055614 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_70746 (CHEMBL681606) |
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IC50 | 49±n/a nM |
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Citation | Leonard, DM; Shuler, KR; Poulter, CJ; Eaton, SR; Sawyer, TK; Hodges, JC; Su, TZ; Scholten, JD; Gowan, RC; Sebolt-Leopold, JS; Doherty, AM Structure-activity relationships of cysteine-lacking pentapeptide derivatives that inhibit ras farnesyltransferase. J Med Chem40:192-200 (1997) [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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BDBM50055614 |
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n/a |
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Name | BDBM50055614 |
Synonyms: | (4-{2-{(R)-2-Benzyloxy-1-[(R)-1-((S)-1-carbamoyl-ethylcarbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-ethylcarbamoyl}-2-[(R)-2-benzyloxycarbonylamino-3-(1H-imidazol-4-yl)-propionylamino]-ethyl}-benzyl)-phosphonic acid diethyl ester | CHEMBL385848 |
Type | Small organic molecule |
Emp. Form. | C52H62N9O11P |
Mol. Mass. | 1020.0761 |
SMILES | CCOP(=O)(Cc1ccc(CC(NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)OCc2ccccc2)C(=O)N[C@H](COCc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C)C(N)=O)cc1)OCC |
Structure |
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