Reaction Details Report a problem with these data
Target
ATP-dependent RNA helicase RhlE
Ligand
BDBM13333
Substrate
biotinylated lamin B peptide substrate
Meas. Tech.
PfPFT and Rat PFT IC50 Determination
pH
7.5±n/a
Temperature
310.15±n/a K
IC50
1000±n/a nM
Citation
 Nallan, L; Bauer, KD; Bendale, P; Rivas, K; Yokoyama, K; Horney, CP; Pendyala, PR; Floyd, D; Lombardo, LJ; Williams, DK; Hamilton, A; Sebti, S; Windsor, WT; Weber, PC; Buckner, FS; Chakrabarti, D; Gelb, MH; Van Voorhis, WC Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. J Med Chem 48:3704-13 (2005) [PubMed]  Article 
Target
Name:
ATP-dependent RNA helicase RhlE
Synonyms:
Protein Farnesyltransferase (PFT) | Protein prenyltransferase, alpha subunit
Type:
Enzyme
Mol. Mass.:
54781.31
Organism:
Plasmodium falciparum (malaria parasite P. falciparum)
Description:
Q5E175
Residue:
500
Sequence:
MGFTSLGLSAPILKAVEEQGYSTPSPIQLQAIPAVIEGKDVMAAAQTGTGKTAGFTLPLLERLSNGPKRKFNQVRALVLTPTRELAAQVHESVEKYSKNLPLTSDVVFGGVKVNPQMQRLRRGVDVLVATPGRLLDLANQNAIKFDQLEILVLDEADRMLDMGFIHDIKKILAKLPKNRQNLLFSATFSDEIRQLAKGLVKDPVEISVAKRNTTAETVEQSVYVMDKGRKPKVLTKLIKDNDWKQVLVFSKTKHGANRLAKTLEEKGVSAAAIHGNKSQGARTKALANFKSGQVRVLVATDIAARGLDIEQLPQVINVDLPKVPEDYVHRIGRTGRAGATGKAISFVSEDEAKELFAIERLIQKVLPRHVLEGFEPVNKVPESKLDTRPIKPKKPKKPKAPRVEHKDGQRSGENRNGNKQGAKQGQKPATKRTPTNNPSGKKEGTDSDKKKRPFSGKPKTKGTGENRGNGSNFGKSKSTPKSDVKPRRQGPRPARKPKAN
  
Inhibitor
Name:
BDBM13333
Synonyms:
N-tert-Butyl-2-[[6-isocyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]-(pyridine-4-sulfonyl)amino]acetamide | N-tert-butyl-2-({6-isocyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl}(pyridine-4-)sulfonamido)acetamide | tetrahydroquinoline (THQ)-based inhibitor 4o
Type:
Small organic molecule
Emp. Form.:
C26H31N7O3S
Mol. Mass.:
521.634
SMILES:
Cn1cncc1CN1CC(Cc2cc(ccc12)[N+]#[C-])N(CC(=O)NC(C)(C)C)S(=O)(=O)c1ccncc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated lamin B peptide substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1715.01
Organism:
n/a
Description:
A human lamin-B carboxy-terminus sequence peptide (biotin-YRASNRSCAIM) is 3H-farnesylated at the cysteine residue when processed by farnesyltransferase.
Residue:
15
Sequence:
ITINYRASNRSCAIM