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 | BDBM50112379 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_71822 (CHEMBL683653) |
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IC50 | 151±n/a nM |
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Citation | Nguyen, DN; Stump, CA; Walsh, ES; Fernandes, C; Davide, JP; Ellis-Hutchings, M; Robinson, RG; Williams, TM; Lobell, RB; Huber, HE; Buser, CA Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I. Bioorg Med Chem Lett12:1269-73 (2002) [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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BDBM50112379 |
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n/a |
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Name | BDBM50112379 |
Synonyms: | 1-(3-Chloro-phenyl)-4-{2-[3-(2-methoxy-4'-trifluoromethyl-biphenyl-4-ylmethyl)-3H-imidazol-4-yl]-ethyl}-piperazin-2-one | CHEMBL23460 |
Type | Small organic molecule |
Emp. Form. | C30H28ClF3N4O2 |
Mol. Mass. | 569.017 |
SMILES | COc1cc(Cn2cncc2CCN2CCN(C(=O)C2)c2cccc(Cl)c2)ccc1-c1ccc(cc1)C(F)(F)F |
Structure |
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