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Assay Detail

CHEMBL1785545

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

Functional
Antimalarial activity against Plasmodium falciparum 3D7 infected in human A positive erythrocytes by [3H]hypoxanthine uptake assay in presence of serum in medium albumax
3
Total Activities
3
Compounds Tested
1
Activity Types
0
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 aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice.
Gujjar R, El Mazouni F, White KL, White J, Creason S, Shackleford DM, Deng X, Charman WN, Bathurst I, Burrows J, Floyd DM, Matthews D, Buckner FS, Charman SA, Phillips MA, Rathod PK.
J Med Chem (2011) 54 : 3935 -3949
PubMed 21517059 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.86 7.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL475813 1 7.18
CHEMBL1784567 1 6.75
CHEMBL1784577 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL475813 EC50 = 66.0 nM 7.18
CHEMBL1784567 EC50 = 180.0 nM 6.75
CHEMBL1784577 EC50 = 220.0 nM 6.66