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Assay Detail

CHEMBL5320304

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

Functional
Antimalarial activity against N-(3-Fluoropheny1)-8-methoxy-4-methy1-1,5-dioxo-2,3-dihydropyrrolo(1,2-alquinazoline-3a-carboxamide-resistant Plasmodium falciparum Dd2 B2 harboring D425E single nucleotide polymorphism in ATP4 assessed as reduction in parasitemia incubated for 72 hrs by LDH assay
5
Total Activities
5
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

Optimization of 2,3-Dihydroquinazolinone-3-carboxamides as Antimalarials Targeting PfATP4.
Ashton TD, Dans MG, Favuzza P, Ngo A, Lehane AM, Zhang X, Qiu D, Chandra Maity B, De N, Schindler KA, Yeo T, Park H, Uhlemann AC, Churchyard A, Baum J, Fidock DA, Jarman KE, Lowes KN, Baud D, Brand S, Jackson PF, Cowman AF, Sleebs BE.
J Med Chem (2023) 66 : 3540 -3565
PubMed 36812492 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.61 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5399238 1 8.68
CHEMBL5436150 1 7.52
CHEMBL5403669 1 7.40
CHEMBL5395617 1 7.37
CHEMBL5408296 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5399238 EC50 = 2.1 nM 8.68
CHEMBL5436150 EC50 = 30.1 nM 7.52
CHEMBL5403669 EC50 = 39.6 nM 7.40
CHEMBL5395617 EC50 = 42.8 nM 7.37
CHEMBL5408296 EC50 = 78.9 nM 7.10