Assay Detail

CHEMBL1260955

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Functional

Antimalarial activity against pyrimethamine-resistant Plasmodium falciparum clinical isolate harboring S108N, N51I mutation in DHFR assessed as decrease in parasitaemia

ChEMBL ↗

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Target

Plasmodium falciparum (CHEMBL364) ↗

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Primary target Plasmodium falciparum

CHEMBL364

Anchored from Assay target.

Protein identity Plasmodium falciparum

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

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

Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.

Nzila A, Rottmann M, Chitnumsub P, Kiara SM, Kamchonwongpaisan S, Maneeruttanarungroj C, Taweechai S, Yeung BK, Goh A, Lakshminarayana SB, Zou B, Wong J, Ma NL, Weaver M, Keller TH, Dartois V, Wittlin S, Brun R, Yuthavong Y, Diagana TT.
Antimicrob Agents Chemother (2010) 54 : 2603 -2610
PubMed 20350951 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	7.39	8.35

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL138060	—	—	1	8.35
CHEMBL36	PYRIMETHAMINE	4.0	1	6.43

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL138060	—	IC50	=	4.48	nM	8.35
CHEMBL36	PYRIMETHAMINE	IC50	=	371.0	nM	6.43