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Target
Chloroquine resistance transporter
Ligand
BDBM50353743
Substrate
n/a
Meas. Tech.
ChEMBL_769822 (CHEMBL1831816)
IC50
58000±n/a nM
Citation
 Zishiri, VK; Joshi, MC; Hunter, R; Chibale, K; Smith, PJ; Summers, RL; Martin, RE; Egan, TJ Quinoline antimalarials containing a dibemethin group are active against chloroquinone-resistant Plasmodium falciparum and inhibit chloroquine transport via the P. falciparum chloroquine-resistance transporter (PfCRT). J Med Chem 54:6956-68 (2011) [PubMed]  Article 
Target
Name:
Chloroquine resistance transporter
Synonyms:
CRT | CRT_PLAFA | PfCRT
Type:
PROTEIN
Mol. Mass.:
48687.29
Organism:
Plasmodium falciparum
Description:
ChEMBL_1364181
Residue:
424
Sequence:
MKFASKKNNQKNSSKNDERYRELDNLVQEGNGSRLGGGSCLGKCAHVFKLIFKEIKDNIFIYILSIIYLSVCVMNKIFAKRTLNKIGNYSFVTSETHNFICMIMFFIVYSLFGNKKGNSKERHRSFNLQFFAISMLDACSVILAFIGLTRTTGNIQSFVLQLSIPINMFFCFLILRYRYHLYNYLGAVIIVVTIALVEMKLSFETQEENSIIFNLVLISALIPVCFSNMTREIVFKKYKIDILRLNAMVSFFQLFTSCLILPVYTLPFLKQLHLPYNEIWTNIKNGFACLFLGRNTVVENCGLGMAKLCDDCDGAWKTFALFSFFNICDNLITSYIIDKFSTMTYTIVSCIQGPAIAIAYYFKFLAGDVVREPRLLDFVTLFGYLFGSIIYRVGNIILERKKMRNEENEDSEGELTNVDSIITQ
  
Inhibitor
Name:
BDBM50353743
Synonyms:
CHEMBL1830985
Type:
Small organic molecule
Emp. Form.:
C25H24ClN3
Mol. Mass.:
401.931
SMILES:
CN(Cc1ccccc1)Cc1ccccc1CNc1ccnc2cc(Cl)ccc12
Structure:
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