Assay Detail

CHEMBL4812778

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Functional

Antiplasmodial activity against Plasmodium falciparum Dd2 Brazilian infected in human erythrocytes assessed as parasite killing using albumax media measured after 72 hrs by schizont maturation 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

Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series.

Palmer MJ, Deng X, Watts S, Krilov G, Gerasyuto A, Kokkonda S, El Mazouni F, White J, White KL, Striepen J, Bath J, Schindler KA, Yeo T, Shackleford DM, Mok S, Deni I, Lawong A, Huang A, Chen G, Wang W, Jayaseelan J, Katneni K, Patil R, Saunders J, Shahi SP, Chittimalla R, Angulo-Barturen I, Jiménez-Díaz MB, Wittlin S, Tumwebaze PK, Rosenthal PJ, Cooper RA, Aguiar ACC, Guido RVC, Pereira DB, Mittal N, Winzeler EA, Tomchick DR, Laleu B, Burrows JN, Rathod PK, Fidock DA, Charman SA, Phillips MA.
J Med Chem (2021) 64 : 6085 -6136
PubMed 33876936 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	2	7.39	7.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4876457	—	—	1	7.70
CHEMBL4848632	—	—	1	7.07

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4876457	—	EC50	=	20.0	nM	7.70
CHEMBL4848632	—	EC50	=	86.0	nM	7.07