Reaction Details |
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Target | Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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Ligand | BDBM50062249 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_70740 (CHEMBL681452) |
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IC50 | 5.6±n/a nM |
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Citation | Aoyama, T; Satoh, T; Yonemoto, M; Shibata, J; Nonoshita, K; Arai, S; Kawakami, K; Iwasawa, Y; Sano, H; Tanaka, K; Monden, Y; Kodera, T; Arakawa, H; Suzuki-Takahashi, I; Kamei, T; Tomimoto, K A new class of highly potent farnesyl diphosphate-competitive inhibitors of farnesyltransferase. J Med Chem41:143-7 (1998) [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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BDBM50062249 |
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n/a |
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Name | BDBM50062249 |
Synonyms: | CHEMBL285434 | trisodium 5-[2-benzo[d][1,3]dioxol-5-yl-5-benzo[d][1,3]oxazol-2-yl-1-methyl-(1S,2R,4E)-4-pentenyl(2-naphthylmethyl)carbamoyl]-(4S,5R)-1,3-dioxolane-2,2,4-tricarboxylate |
Type | Small organic molecule |
Emp. Form. | C38H29N2O12 |
Mol. Mass. | 705.6447 |
SMILES | C[C@@H]([C@H](C\C=C\c1nc2ccccc2o1)c1ccc2OCOc2c1)N(Cc1ccc2ccccc2c1)C(=O)[C@@H]1OC(O[C@@H]1C([O-])=O)(C([O-])=O)C([O-])=O |
Structure |
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