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Target
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM238359
Substrate
n/a
Meas. Tech.
Yeast FTase Assay
pH
7.5±n/a
IC50
580±130 nM
Comments
extracted
Citation
 Lethu, S; Bosc, D; Mouray, E; Grellier, P; Dubois, J New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis. J Enzyme Inhib Med Chem 28:163-71 (2013) [PubMed]  Article 
Target
Name:
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
Farnesyltransferase | Farnesyltransferase (FTase) | Protein farnesyltransferase beta/geranylgeranyltransferase type I alpha subunit
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of EBI is 70753
Components:
This complex has 2 components.
Component 1
Name:
Protein farnesyltransferase subunit beta
Synonyms:
CAAX farnesyltransferase subunit beta | DPR1 | FNTB_YEAST | FTase-beta | Farnesyltransferase | RAM1 | Ras proteins prenyltransferase subunit beta | SCG2 | STE16
Type:
Protein
Mol. Mass.:
48188.41
Organism:
Saccharomyces cerevisiae (Baker's yeast)
Description:
P22007
Residue:
431
Sequence:
MRQRVGRSIARAKFINTALLGRKRPVMERVVDIAHVDSSKAIQPLMKELETDTTEARYKVLQSVLEIYDDEKNIEPALTKEFHKMYLDVAFEISLPPQMTALDASQPWMLYWIANSLKVMDRDWLSDDTKRKIVDKLFTISPSGGPFGGGPGQLSHLASTYAAINALSLCDNIDGCWDRIDRKGIYQWLISLKEPNGGFKTCLEVGEVDTRGIYCALSIATLLNILTEELTEGVLNYLKNCQNYEGGFGSCPHVDEAHGGYTFCATASLAILRSMDQINVEKLLEWSSARQLQEERGFCGRSNKLVDGCYSFWVGGSAAILEAFGYGQCFNKHALRDYILYCCQEKEQPGLRDKPGAHSDFYHTNYCLLGLAVAESSYSCTPNDSPHNIKCTPDRLIGSSKLTDVNPVYGLPIENVRKIIHYFKSNLSSPS
  
Component 2
Name:
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
CAAX farnesyltransferase subunit alpha | FNTA_YEAST | FTase-alpha | Farnesyltransferase | GGTase-I-alpha | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | RAM2 | Ras proteins prenyltransferase subunit alpha | Type I protein geranyl-geranyltransferase subunit alpha
Type:
PROTEIN
Mol. Mass.:
37495.69
Organism:
Saccharomyces cerevisiae
Description:
ChEMBL_588425
Residue:
316
Sequence:
MEEYDYSDVKPLPIETDLQDELCRIMYTEDYKRLMGLARALISLNELSPRALQLTAEIIDVAPAFYTIWNYRFNIVRHMMSESEDTVLYLNKELDWLDEVTLNNPKNYQIWSYRQSLLKLHPSPSFKRELPILKLMIDDDSKNYHVWSYRKWCCLFFSDFQHELAYASDLIETDIYNNSAWTHRMFYWVNAKDVISKVELADELQFIMDKIQLVPQNISPWTYLRGFQELFHDRLQWDSKVVDFATTFIGDVLSLPIGSPEDLPEIESSYALEFLAYHWGADPCTRDNAVKAYSLLAIKYDPIRKNLWHHKINNLN
  
Inhibitor
Name:
BDBM238359
Synonyms:
3-(4-(Trifluoromethyl)phenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid (1g)
Type:
Small organic molecule
Emp. Form.:
C16H12F3NO2S2
Mol. Mass.:
371.397
SMILES:
CC(C)Sc1sc(C(O)=O)c(c1C#N)-c1ccc(cc1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: