| 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 | BDBM13313 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_665226 (CHEMBL1260645) |
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| IC50 | 310±n/a nM |
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| Citation |  Fletcher, S; Keaney, EP; Cummings, CG; Blaskovich, MA; Hast, MA; Glenn, MP; Chang, SY; Bucher, CJ; Floyd, RJ; Katt, WP; Gelb, MH; Van Voorhis, WC; Beese, LS; Sebti, SM; Hamilton, AD Structure-based design and synthesis of potent, ethylenediamine-based, mammalian farnesyltransferase inhibitors as anticancer agents. J Med Chem53:6867-88 (2010) [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 type I | Geranylgeranyl transferase type I beta subunit/Protein Farnesyltransferase (PFT) | Geranylgeranyl transferase type I beta/Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit |
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| Type: | n/a |
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| Mol. Mass.: | n/a |
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| Description: | ASSAY_ID of EBI is 70196 |
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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_HUMAN | FTase-1-alpha | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Geranylgeranyl transferase type I | Protein Farnesyltransferase (PFT) Chain A | Protein farnesyl/geranylgeranyl transferase | Protein farnesyltransferase | Protein farnesyltransferase subunit alpha | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha |
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| Type: | Enzyme |
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| Mol. Mass.: | 44392.46 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Recombinant human FTase. |
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| Residue: | 379 |
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| Sequence: | MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDS
PSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLR
DPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQR
YFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLL
DLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHSTENDSPTNVQQ
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| Component 2 |
| Name: | Geranylgeranyl transferase type-1 subunit beta |
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| Synonyms: | 2.5.1.59 | GGTase-I-beta | Geranylgeranyl transferase type I | Geranylgeranyl transferase type I beta subunit | Geranylgeranyl transferase type I subunit beta | Geranylgeranyl transferase type-1 subunit beta | PGGT1B | PGTB1_HUMAN | Protein farnesyl/geranylgeranyl transferase | Type I protein geranyl-geranyltransferase subunit beta |
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| Type: | n/a |
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| Mol. Mass.: | 42369.84 |
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| Organism: | Homo sapiens (Human) |
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| Description: | n/a |
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| Residue: | 377 |
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| Sequence: | MAATEDERLAGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDM
LDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKAPGTAHPYDSG
HIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASC
ICYMLNNWSGMDMKKAITYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVF
SEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILS
TQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLLDLHQS
WKTKDSKQCSENVHIST
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| BDBM13313 |
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| n/a |
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| Name | BDBM13313 |
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| Synonyms: | N-Benzyl-N-{2-[(4-cyanophenyl)-(3-methyl-3H-imidazol-4-ylmethyl)amino]ethyl}benzenesulfonamide | N-benzyl-N-{2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl}benzenesulfonamide | Sulfonamide 12e |
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| Type | Small organic molecule |
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| Emp. Form. | C27H27N5O2S |
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| Mol. Mass. | 485.601 |
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| SMILES | Cn1cncc1CN(CCN(Cc1ccccc1)S(=O)(=O)c1ccccc1)c1ccc(cc1)C#N |
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| Structure | 
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