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Assay Detail

CHEMBL4428530

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of CRT CVIET haplotype mutant in chloroquine-resistant Plasmodium falciparum K1 isolate MRA-159 assessed as reversal of chloroquine resistance by measuring reduction in chloroquine IC50 relative to chloroquine alone
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum K1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
Boudhar A, Ng XW, Loh CY, Chia WN, Tan ZM, Nosten F, Dymock BW, Tan KS.
Eur J Med Chem (2016) 119 : 231 -249
PubMed 27173385 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.56 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4472492 1 6.77
CHEMBL10780 1 6.70
CHEMBL2205324 1 6.53
CHEMBL4574174 1 6.46
CHEMBL4449669 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4472492 EC50 = 170.0 nM 6.77
CHEMBL10780 EC50 = 200.0 nM 6.70
CHEMBL2205324 EC50 = 295.0 nM 6.53
CHEMBL4574174 EC50 = 343.0 nM 6.46
CHEMBL4449669 EC50 = 482.0 nM 6.32