Reaction Details |
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Target | Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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Ligand | BDBM50327989 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_665230 |
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IC50 | >10000±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 |
Synonyms: | Geranylgeranyl transferase type 1 |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 665230 |
Components: | This complex has 2 components. |
Component 1 |
Name: | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
Synonyms: | CAAX farnesyltransferase subunit alpha | FNTA_MOUSE | FTase-alpha | Fnta | GGTase-I-alpha | Geranylgeranyl transferase type 1 | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Ras proteins prenyltransferase subunit alpha | Type I protein geranyl-geranyltransferase subunit alpha |
Type: | PROTEIN |
Mol. Mass.: | 43994.09 |
Organism: | Mus musculus |
Description: | EBI_10570 |
Residue: | 377 |
Sequence: | MAATEGVGESAAGGEPGQPEQPPPPPPPPPAQQPQEEEMAAEAGEAAASPMDDGFLSLDS
PTYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSEKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLRSLQKDLQEEMNYITAIIEEQPKNYQVWHHRRVLVEWLK
DPSQELEFIADILSQDAKNYHAWQHRQWVIQEFRLWDNELQYVDQLLKEDVRNNSVWNQR
HFVISNTTGYSDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSRYPNLLNQLL
DLQPSHSSPYLIAFLVDVYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHCRESDIPASV
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Component 2 |
Name: | Geranylgeranyl transferase type-1 subunit beta |
Synonyms: | GGTase-I-beta | Geranylgeranyl transferase type 1 | Geranylgeranyl transferase type I subunit beta | Geranylgeranyl transferase type-1 subunit beta | PGTB1_MOUSE | Pggt1b | Type I protein geranyl-geranyltransferase subunit beta |
Type: | PROTEIN |
Mol. Mass.: | 42355.77 |
Organism: | Mus musculus |
Description: | ChEMBL_108428 |
Residue: | 377 |
Sequence: | MATTEDDRLAGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDM
LDSLDVVNKDDIIEWIYSLQVLPTEDRSNLSRCGFRGSSYLGIPFNPSKNPGAAHPYDSG
HIAMTYTGLSCLIILGDDLGRVDKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASC
ICYMLNNWSGMDMKKAISYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVF
SEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILS
TQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLRDLHQS
WKTKDSKQCSDNVHIAT
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BDBM50327989 |
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n/a |
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Name | BDBM50327989 |
Synonyms: | CHEMBL1257999 | N-(2-((4-cyanophenyl)((1-methyl-1H-imidazol-5-yl)methyl)amino)ethyl)-N-((2,4-dimethylthiazol-5-yl)methyl)-1-methyl-1H-imidazole-4-sulfonamide |
Type | Small organic molecule |
Emp. Form. | C24H28N8O2S2 |
Mol. Mass. | 524.662 |
SMILES | Cc1nc(C)c(CN(CCN(Cc2cncn2C)c2ccc(cc2)C#N)S(=O)(=O)c2cn(C)cn2)s1 |
Structure |
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