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 | BDBM50051824 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_71811 (CHEMBL683642) |
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IC50 | 360±n/a nM |
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Citation | Williams, TM; Ciccarone, TM; MacTough, SC; Bock, RL; Conner, MW; Davide, JP; Hamilton, K; Koblan, KS; Kohl, NE; Kral, AM; Mosser, SD; Omer, CA; Pompliano, DL; Rands, E; Schaber, MD; Shah, D; Wilson, FR; Gibbs, JB; Graham, SL; Hartman, GD; Oliff, AI; Smith, RL 2-substituted piperazines as constrained amino acids. Application to the synthesis of potent, non carboxylic acid inhibitors of farnesyltransferase. J Med Chem39:1345-8 (1996) [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 (GGTase-I) | Geranylgeranyl Transferase (GGTase-I)/Protein Farnesyltransferase (PFT) | Geranylgeranyl transferase type I |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
Name: | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
Synonyms: | CAAX farnesyltransferase alpha subunit | FNTA | FNTA_BOVIN | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Protein Farnesyltransferase (PFT) Chain A | Protein farnesyltransferase | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha | Type I protein geranyl-geranyltransferase alpha subunit |
Type: | Enzyme |
Mol. Mass.: | 43827.38 |
Organism: | Bos taurus (bovine) |
Description: | The enzyme was purified from a bovine brain homogenate by sequential ammonium sulfate fractionation and affinity chromatography. |
Residue: | 375 |
Sequence: | MAAADGVGEAAQGGDPGQPEPPPPPQPHPPPPPPQPPQEEAAAASPIDDGFLSLDSPTYV
LYRDRPEWADIDPVPQNDGPNPVVQIIYSEKFQDVYDYFRAVLQRDERSERAFKLTRDAI
ELNAANYTVWHFRRVLLKSLQKDLHEEMNYISAIIEEQPKNYQVWHHRRVLVEWLRDPSQ
ELEFIADILTQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVI
SNTTGYNDRAILEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQP
SHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQ
SKHSTESDPPTNVQQ
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Component 2 |
Name: | Geranylgeranyl transferase type-1 subunit beta |
Synonyms: | GGTase-I-beta | Geranylgeranyl transferase type I | Geranylgeranyl transferase type-1 subunit beta | PGGT1B | PGTB1_BOVIN | Type I protein geranyl-geranyltransferase subunit beta |
Type: | Enzyme |
Mol. Mass.: | 42483.88 |
Organism: | Bos taurus (bovine) |
Description: | Purified from bovine brain |
Residue: | 377 |
Sequence: | MAATEDERPTGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDM
LDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKNPGTAHPYDSG
HIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASC
ICYMLNNWSGMDMKKAINYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVF
SEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILS
TQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLRDLHQS
WKTKDSKQCSENVHIST
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BDBM50051824 |
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n/a |
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Name | BDBM50051824 |
Synonyms: | CHEMBL283208 | [(S)-4-((R)-2-Amino-3-mercapto-propyl)-3-butyl-piperazin-1-yl]-(2,3-dimethyl-phenyl)-methanone |
Type | Small organic molecule |
Emp. Form. | C20H33N3OS |
Mol. Mass. | 363.561 |
SMILES | CCCC[C@H]1CN(CCN1C[C@@H](N)CS)C(=O)c1cccc(C)c1C |
Structure |
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