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Assay Detail

CHEMBL2033123

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

Functional
Antimalarial activity against atoquinone-resistant Plasmodium falciparum TM90C2B containing cytochrome-b Y268S mutant
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum
Confidence 1 — Organism
Curated By Autocuration

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Identification, design and biological evaluation of heterocyclic quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).
Leung SC, Gibbons P, Amewu R, Nixon GL, Pidathala C, Hong WD, Pacorel B, Berry NG, Sharma R, Stocks PA, Srivastava A, Shone AE, Charoensutthivarakul S, Taylor L, Berger O, Mbekeani A, Hill A, Fisher NE, Warman AJ, Biagini GA, Ward SA, O'Neill PM.
J Med Chem (2012) 55 : 1844 -1857
PubMed 22364417 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.23 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2030313 1 6.50
CHEMBL2030291 1 6.49
CHEMBL2030322 1 6.49
CHEMBL2030298 1 6.46
CHEMBL2030297 1 6.44
CHEMBL2030321 1 6.42
CHEMBL2030300 1 6.39
CHEMBL2030296 1 5.94
CHEMBL1450 ATOVAQUONE 4.0 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2030313 IC50 = 314.0 nM 6.50
CHEMBL2030291 IC50 = 326.0 nM 6.49
CHEMBL2030322 IC50 = 324.0 nM 6.49
CHEMBL2030298 IC50 = 344.0 nM 6.46
CHEMBL2030297 IC50 = 361.0 nM 6.44
CHEMBL2030321 IC50 = 381.0 nM 6.42
CHEMBL2030300 IC50 = 410.0 nM 6.39
CHEMBL2030296 IC50 = 1150.0 nM 5.94
CHEMBL1450 ATOVAQUONE IC50 = 12000.0 nM 4.92