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Target
Protein farnesyltransferase alpha subunit/subunit beta
Ligand
BDBM238354
Substrate
n/a
Meas. Tech.
T. brucei FTase Assay
IC50
14500±1500 nM
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 alpha subunit/subunit beta
Synonyms:
Farnesyltransferase (FTase)
Type:
Enzyme
Mol. Mass.:
n/a
Description:
T. brucei FTase
Components:
This complex has 2 components.
Component 1
Name:
Protein farnesyltransferase alpha subunit
Synonyms:
Protein farnesyltransferase subunit alpha
Type:
Protein
Mol. Mass.:
70116.60
Organism:
Trypanosoma brucei brucei
Description:
Q9NC77
Residue:
612
Sequence:
MNKSAVRSEESRQSSSLPSTYSSSSLNSEDERLALLSDINALQALFPGVTPKEETPLIKHPNMTPAVFSKKFDYVMGIYRAVGVTFKGTRVGPSTPQWLLLTSFVIQQNASHYSAWKDRRDVFLQPSRLVTSTRDAFMAENGQQCCGDKTDSLAKVSQEWLPAQCDVQGPTGECSVWRAIRWELKAMERFALMNPKNFQVWHHRREMLREALMHANPVVTGSRSAFDGYLLTCHNMQFSDIDERVFCDAALDDDGKNYHAWLYRSWFVHSFPFLLHPPSWDSLLGGDQGTEDKHSELRAAPFRSFTVEEDWLHKCLQPIIPECPLSDELTSTAKRILHDCMNNSAWCHRFYVFEHDLIVPLIRVIPPQQTEEAKLILKRLCECEMFYALQWCAYEPCNESAFVHARCVAVLHQAVAIHLCLSSHGDAPHVFLRGDETIQVAGSSSLRHINLRDKLRWGAFLETFRLLLCQVNVLSDVITPRAEEFRSGGEGRDNATISVIHKRRSQFLLDNTHQVYTARYRCLFTILEYMWRCYFTVSDRANVAAALPPEVYAGGDAEAAALAQQQSDDCVKFFLEAELQALRLARRLVVEDDIRRKYWKHEMNIVMNRDYV
  
Component 2
Name:
Protein farnesyltransferase subunit beta
Synonyms:
n/a
Type:
Protein
Mol. Mass.:
65426.56
Organism:
Trypanosoma brucei brucei
Description:
Q9NC76
Residue:
585
Sequence:
MSFVPPPASSTTHAQREVELTLLRFLEKYRPEVCDLWGTHSDIHLHADSNEKEEEMCTIDNEEGIVHSLNRESHEKYLKSRLVKLPEYAQRLYNAQPWMVYWTLQAAEMLGITEKLYEQISQDALGEFILSCLQEQPVEDEQKGCWGSEEGGKHGKGSMPQQCGNVYDFLRRCDADHTCAIGFSGGNYGQIPHLATSYAGVCSLCILGCPEYLQALPRSAIKRWLLSLRCADGSFRMHIGGEADIRASYCVAVITTLLQLQDVDVRSGDILREQEAQFVASCQTHEGGFACGRFASEAHGAYTQCGLAALILMKRPELCNYTALRGWLAARQLRFEGGFNGRTNKLVDSCYAHWVGASHVLLRVGESLAKITTCGETKRSLTSREMLLLDHAQLVDISNLHPESFEAWSQHEEEKQERASRVEAYLSATPLAASWSSSGVPNVLDDDAGDFYFNQRRLQLYILACCQNREEGGLMDKPNYPNDFYHTCYSLSGMSSAQNLQGMQVNRDGRDLSGNSFYAAALSRGYIPGRRDSYGIVLPSDERSGVSSELHLSKNCLRPTNPIFNINQSKVLFALRTWGAKTFMC
  
Inhibitor
Name:
BDBM238354
Synonyms:
3-(3-Chlorophenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid (1b)
Type:
Small organic molecule
Emp. Form.:
C15H12ClNO2S2
Mol. Mass.:
337.844
SMILES:
CC(C)Sc1sc(C(O)=O)c(c1C#N)-c1cccc(Cl)c1
Structure:
Search PDB for entries with ligand similarity: