Reaction Details Report a problem with these data
Target
ATP-dependent RNA helicase RhlE
Ligand
BDBM16183
Substrate
biotinylated lamin B peptide substrate
Meas. Tech.
PfPFT and Rat PFT IC50 Determination
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:
BDBM16183
Synonyms:
Hamilton/Sebti Compound 10b | benzyl (2S)-2-[(4-{[(1H-imidazol-4-ylmethyl)amino]methyl}-2-(2-methylphenyl)phenyl)formamido]-4-(methylsulfanyl)butanoate | benzyl N-[(5-{[(1H-imidazol-4-ylmethyl)amino]methyl}-2 -methylbiphenyl-2-yl)carbonyl]-L-methioninate
Type:
Small organic molecule
Emp. Form.:
C31H34N4O3S
Mol. Mass.:
542.692
SMILES:
CSCC[C@H](NC(=O)c1ccc(CNCc2cnc[nH]2)cc1-c1ccccc1C)C(=O)OCc1ccccc1 |r|
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