Assay Detail

CHEMBL4812781

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Functional

Antiplasmodial activity against Plasmodium vivax Brazilian field isolated from patients 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 vivax (CHEMBL613013) ↗

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Plasmodium vivax (CHEMBL613013) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Plasmodium vivax

CHEMBL613013

Anchored from Assay target.

Protein identity Plasmodium vivax

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 vivax
Confidence	1 — Organism
Curated By	Autocuration

Target

Plasmodium vivax (CHEMBL613013) ↗

Type	ORGANISM
Organism	Plasmodium vivax

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	7.14	7.36

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4876457	—	—	1	7.36
CHEMBL4848632	—	—	1	6.92

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4876457	—	EC50	=	44.0	nM	7.36
CHEMBL4848632	—	EC50	=	120.0	nM	6.92