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 | BDBM50081217 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_71824 (CHEMBL683655) |
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IC50 | 10000±n/a nM |
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Citation | Williams, TM; Bergman, JM; Brashear, K; Breslin, MJ; Dinsmore, CJ; Hutchinson, JH; MacTough, SC; Stump, CA; Wei, DD; Zartman, CB; Bogusky, MJ; Culberson, JC; Buser-Doepner, C; Davide, J; Greenberg, IB; Hamilton, KA; Koblan, KS; Kohl, NE; Liu, D; Lobell, RB; Mosser, SD; O'Neill, TJ; Rands, E; Schaber, MD; Huff, JR N-arylpiperazinone inhibitors of farnesyltransferase: discovery and biological activity. J Med Chem42:3779-84 (1999) [PubMed] |
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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 I | Geranylgeranyl transferase type I beta subunit/Protein Farnesyltransferase (PFT) | Geranylgeranyl transferase type I beta/Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of EBI is 70196 |
Components: | This complex has 2 components. |
Component 1 |
Name: | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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 |
Type: | Enzyme |
Mol. Mass.: | 44392.46 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant human FTase. |
Residue: | 379 |
Sequence: | MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDS
PSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLR
DPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQR
YFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLL
DLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHSTENDSPTNVQQ
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Component 2 |
Name: | Geranylgeranyl transferase type-1 subunit beta |
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 |
Type: | n/a |
Mol. Mass.: | 42369.84 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 377 |
Sequence: | MAATEDERLAGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDM
LDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKAPGTAHPYDSG
HIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASC
ICYMLNNWSGMDMKKAITYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVF
SEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILS
TQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLLDLHQS
WKTKDSKQCSENVHIST
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BDBM50081217 |
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n/a |
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Name | BDBM50081217 |
Synonyms: | 4-{5-[(S)-2-Butyl-4-(2,3-dimethyl-phenyl)-5-oxo-piperazin-1-ylmethyl]-imidazol-1-ylmethyl}-benzonitrile | CHEMBL125648 |
Type | Small organic molecule |
Emp. Form. | C28H33N5O |
Mol. Mass. | 455.5945 |
SMILES | CCCC[C@H]1CN(C(=O)CN1Cc1cncn1Cc1ccc(cc1)C#N)c1cccc(C)c1C |
Structure |
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