Reaction Details Report a problem with these data
Target
ATP-dependent RNA helicase RhlE
Ligand
BDBM16180
Substrate
biotinylated lamin B peptide substrate
Meas. Tech.
PfPFT and Rat PFT IC50 Determination
IC50
5±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:
BDBM16180
Synonyms:
(2S)-2-{[4-({[(2S)-1-cyclohexyl-3-(ethylsulfanyl)propan-2-yl]amino}methyl)-2-(2-methylphenyl)phenyl]formamido}-4-(methylsulfanyl)butanoic acid | A197574 | CHEMBL344100 | N-({5-[({(1S)-2-cyclohexyl-1-[(ethylsulfanyl)methyl]ethyl}amino)methyl]-2 -methylbiphenyl-2-yl}carbonyl)-L-methionine
Type:
Small organic molecule
Emp. Form.:
C31H44N2O3S2
Mol. Mass.:
556.823
SMILES:
CCSC[C@H](CC1CCCCC1)NCc1ccc(C(=O)N[C@@H](CCSC)C(O)=O)c(c1)-c1ccccc1C |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