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Target
Chloroquine resistance transporter
Ligand
BDBM50017696
Substrate
n/a
Meas. Tech.
ChEMBL_1364181 (CHEMBL3292896)
IC50
85000±n/a nM
Citation
 Deane, KJ; Summers, RL; Lehane, AM; Martin, RE; Barrow, RA Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT. ACS Med Chem Lett 5:576-81 (2014) [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:
BDBM50017696
Synonyms:
(2-dimethylamino-2-methyl)ethyl-N-dibenzoparathiazine | 10-(2-Dimethylaminopropyl)phenothiazine | 10-[2-(dimethylamino)propyl]phenothiazine | CHEMBL643 | N,N,alpha-trimethyl-10H-phenothiazine-10-ethanamine | N,N-dimethyl-1-(10H-phenothiazin-10-yl)propan-2-amine | PROMETHAZINE | med.21724, Compound 16 | proazamine
Type:
Small organic molecule
Emp. Form.:
C17H20N2S
Mol. Mass.:
284.419
SMILES:
CC(CN1c2ccccc2Sc2ccccc12)N(C)C
Structure:
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