Assay Detail

CHEMBL4605409

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

Functional

Antimalarial activity against Plasmodium falciparum R1AC1B harboring DHODH C276F mutant measured after 72 hrs by SYBR Green dye based fluorescence assay

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

Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.

Kokkonda S, Deng X, White KL, El Mazouni F, White J, Shackleford DM, Katneni K, Chiu FCK, Barker H, McLaren J, Crighton E, Chen G, Angulo-Barturen I, Jimenez-Diaz MB, Ferrer S, Huertas-Valentin L, Martinez-Martinez MS, Lafuente-Monasterio MJ, Chittimalla R, Shahi SP, Wittlin S, Waterson D, Burrows JN, Matthews D, Tomchick D, Rathod PK, Palmer MJ, Charman SA, Phillips MA.
J Med Chem (2020) 63 : 4929 -4956
PubMed 32248693 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	2	6.91	7.05

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4633246	—	—	1	7.05
CHEMBL1956285	DSM-265	2.0	1	6.77

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4633246	—	EC50	=	89.0	nM	7.05
CHEMBL1956285	DSM-265	EC50	=	170.0	nM	6.77