Reaction Details Report a problem with these data
Target
ATP-dependent RNA helicase RhlE
Ligand
BDBM13312
Substrate
biotinylated lamin B peptide substrate
Meas. Tech.
PFT IC50 Determination
pH
7.5±n/a
Temperature
310.15±n/a K
IC50
8.0±n/a nM
Citation
 Glenn, MP; Chang, SY; Horney, C; Rivas, K; Yokoyama, K; Pusateri, EE; Fletcher, S; Cummings, CG; Buckner, FS; Pendyala, PR; Chakrabarti, D; Sebti, SM; Gelb, M; Van Voorhis, WC; Hamilton, AD Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites. J Med Chem 49:5710-27 (2006) [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:
BDBM13312
Synonyms:
1-Methyl-1H-imidazole-4-sulfonic Acid {2-[Biphenyl-4-yl-(3-methyl-3H-imidazol-4-ylmethyl)amino]ethyl}-(2-methylbenzyl)amide | 1-methyl-N-(2-{[(1-methyl-1H-imidazol-5-yl)methyl](4-phenylphenyl)amino}ethyl)-N-[(2-methylphenyl)methyl]-1H-imidazole-4-sulfonamide | Sulfonamide 12c
Type:
Small organic molecule
Emp. Form.:
C31H34N6O2S
Mol. Mass.:
554.706
SMILES:
Cc1ccccc1CN(CCN(Cc1cncn1C)c1ccc(cc1)-c1ccccc1)S(=O)(=O)c1cn(C)cn1
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