Assay Detail

CHEMBL1960909

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Functional

Antimalarial activity against atovoquone-resistant Plasmodium falciparum TM90C2A by [3H]hypoxanthine incorporation assay in presence of human serum

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

Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential.

Coteron JM, Marco M, Esquivias J, Deng X, White KL, White J, Koltun M, El Mazouni F, Kokkonda S, Katneni K, Bhamidipati R, Shackleford DM, Angulo-Barturen I, Ferrer SB, Jiménez-Díaz MB, Gamo FJ, Goldsmith EJ, Charman WN, Bathurst I, Floyd D, Matthews D, Burrows JN, Rathod PK, Charman SA, Phillips MA.
J Med Chem (2011) 54 : 5540 -5561
PubMed 21696174 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	2	7.81	8.10

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1738786	—	—	1	8.10
CHEMBL1956285	DSM-265	2.0	1	7.51

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1738786	—	EC50	=	7.9	nM	8.10
CHEMBL1956285	DSM-265	EC50	=	31.0	nM	7.51