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 | BDBM50097076 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_70196 |
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IC50 | >20000±n/a nM |
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Citation | Dinsmore, CJ; Bergman, JM; Wei, DD; Zartman, CB; Davide, JP; Greenberg, IB; Liu, D; O'Neill, TJ; Gibbs, JB; Koblan, KS; Kohl, NE; Lobell, RB; Chen, IW; McLoughlin, DA; Olah, TV; Graham, SL; Hartman, GD; Williams, TM Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase. Bioorg Med Chem Lett11:537-40 (2001) [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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BDBM50097076 |
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n/a |
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Name | BDBM50097076 |
Synonyms: | 4-[5-(2,3-Dioxo-4-phenyl-piperazin-1-ylmethyl)-imidazol-1-ylmethyl]-benzonitrile | CHEMBL356470 |
Type | Small organic molecule |
Emp. Form. | C22H19N5O2 |
Mol. Mass. | 385.4186 |
SMILES | O=C1N(Cc2cncn2Cc2ccc(cc2)C#N)CCN(C1=O)c1ccccc1 |
Structure |
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