Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4605504

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

Functional
Antimalarial activity against Plasmodium falciparum 3D70087/N9 infected in po dosed NOD-SCID IL2Rgamma null mouse assessed as reduction in parasitemia administered once daily for 4 days by flow cytometric analysis
8
Total Activities
3
Compounds Tested
3
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 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
fEC50 3 - -
EC50 3 7.96 8.22
ED90 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1956285 DSM-265 2.0 2 8.22
CHEMBL4557830 3 7.85
CHEMBL4633246 3 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1956285 DSM-265 EC50 = 6.0 nM 8.22
CHEMBL4557830 EC50 = 14.0 nM 7.85
CHEMBL4633246 EC50 = 16.0 nM 7.80
CHEMBL4633246 fEC50 = 0.0077 uM -
CHEMBL1956285 DSM-265 fEC50 = 0.001 uM -
CHEMBL4633246 ED90 = 50.0 mg/kg/day -
CHEMBL4557830 ED90 = 2.6 mg/kg/day -
CHEMBL4557830 fEC50 = 0.007 uM -