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Assay Detail

CHEMBL4329976

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

Functional
Antiplasmodial activity against Plasmodium falciparum K1CB1 harboring DHFR NRNI haplotype C59R/S108N double mutant infected in human erythrocytes by microdilution radioisotope method
4
Total Activities
4
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

Hybrid Inhibitors of Malarial Dihydrofolate Reductase with Dual Binding Modes That Can Forestall Resistance.
Tarnchompoo B, Chitnumsub P, Jaruwat A, Shaw PJ, Vanichtanankul J, Poen S, Rattanajak R, Wongsombat C, Tonsomboon A, Decharuangsilp S, Anukunwithaya T, Arwon U, Kamchonwongpaisan S, Yuthavong Y.
ACS Med Chem Lett (2018) 9 : 1235 -1240
PubMed 30613332 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.15 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4442735 1 6.66
CHEMBL4460601 1 6.48
CHEMBL4454693 1 5.74
CHEMBL3819601 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4442735 IC50 = 220.0 nM 6.66
CHEMBL4460601 IC50 = 330.0 nM 6.48
CHEMBL4454693 IC50 = 1840.0 nM 5.74
CHEMBL3819601 IC50 = 1920.0 nM 5.72