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Target
Dimer of Protein farnesyltransferase subunit beta
Ligand
BDBM50103356
Substrate
n/a
Meas. Tech.
ChEMBL_69996 (CHEMBL681469)
IC50
65±n/a nM
Citation
Bell, IM; Gallicchio, SN; Abrams, M; Beshore, DC; Buser, CA; Culberson, JC; Davide, J; Ellis-Hutchings, M; Fernandes, C; Gibbs, JB; Graham, SL; Hartman, GD; Heimbrook, DC; Homnick, CF; Huff, JR; Kassahun, K; Koblan, KS; Kohl, NE; Lobell, RB; Lynch, JJ; Miller, PA; Omer, CA; Rodrigues, AD; Walsh, ES; Williams, TM Design and biological activity of (S)-4-(5-([1-(3-chlorobenzyl)-2-oxopyrrolidin-3-ylamino]methyl)imidazol-1-ylmethyl)benzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency. J Med Chem 44:2933-49 (2001) [PubMed] Article
More Info.:
Target
Name:
Dimer of Protein farnesyltransferase subunit beta
Synonyms:
Protein Farnesyltransferase (PFT) Chain B
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of EBI is 51428
Components:
This complex has 3 components.
Component 1
Name:
Protein farnesyltransferase subunit beta
Synonyms:
CAAX farnesyltransferase subunit alpha | CAAX farnesyltransferase subunit beta | FNTB | FNTB_HUMAN | FTase-alpha | FTase-beta | GGTase-I-alpha | Protein Farnesyltransferase (PFT) Chain B | Protein farnesyl/geranylgeranyl transferase | Protein farnesyltransferase beta subunit | Protein farnesyltransferase subunit beta | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Ras proteins prenyltransferase subunit alpha | Ras proteins prenyltransferase subunit beta | Type I protein geranyl-geranyltransferase subunit alpha
Type:
Enzyme Subunit
Mol. Mass.:
48766.02
Organism:
Homo sapiens (Human)
Description:
Protein farnesyltransferase subunit beta
Residue:
437
Sequence:
MASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFSSYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQIVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQYLYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIGGVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCYSFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDFYHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPVPGFEELKDETSAEPATD
Component 2
Name:
Protein farnesyltransferase subunit beta
Synonyms:
CAAX farnesyltransferase subunit alpha | CAAX farnesyltransferase subunit beta | FNTB | FNTB_HUMAN | FTase-alpha | FTase-beta | GGTase-I-alpha | Protein Farnesyltransferase (PFT) Chain B | Protein farnesyl/geranylgeranyl transferase | Protein farnesyltransferase beta subunit | Protein farnesyltransferase subunit beta | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Ras proteins prenyltransferase subunit alpha | Ras proteins prenyltransferase subunit beta | Type I protein geranyl-geranyltransferase subunit alpha
Type:
Enzyme Subunit
Mol. Mass.:
48766.02
Organism:
Homo sapiens (Human)
Description:
Protein farnesyltransferase subunit beta
Residue:
437
Sequence:
MASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFSSYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQIVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQYLYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIGGVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCYSFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDFYHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPVPGFEELKDETSAEPATD
Inhibitor
Name:
BDBM50103356
Synonyms:
(3-{(1-Benzyl-2-oxo-pyrrolidin-3-yl)-[3-(4-cyano-benzyl)-3H-imidazol-4-ylmethyl]-amino}-propyl)-carbamic acid tert-butyl ester | (S)-tert-butyl 3-((1-benzyl-2-oxopyrrolidin-3-yl)((1-(4-cyanobenzyl)-1H-imidazol-5-yl)methyl)amino)propylcarbamate | CHEMBL98553
Type:
Small organic molecule
Emp. Form.:
C31H38N6O3
Mol. Mass.:
542.6718
SMILES:
CC(C)(C)OC(=O)NCCCN(Cc1cncn1Cc1ccc(cc1)C#N)[C@H]1CCN(Cc2ccccc2)C1=O |r|