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

CHEMBL5357337

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

Functional
Antiplasmodial activity against PYR-resistant Plasmodium falciparum V1/S encoding QM DHFR infected in human erythrocytes assessed as inhibition of parasite growth by [3H]-hypoxanthine incorporation assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum
Cell Type Erythrocyte
Confidence 1 — Organism
Curated By Autocuration

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Discovery of rigid biphenyl <i>Plasmodium falciparum</i> DHFR inhibitors using a fragment linking strategy.
Hoarau M, Sermmai P, Varatthan T, Thiabma R, Jantra T, Rattanajak R, Vitsupakorn D, Vanichtanankul J, Saepua S, Yuthavong Y, Thongpanchang C, Kamchonwongpaisan S.
RSC Med Chem (2023) 14 : 1755 -1766
PubMed 37731689 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.02 7.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3040038 1 7.25
CHEMBL5417784 1 4.53
CHEMBL5406769 1 4.46
CHEMBL5397904 1 4.46
CHEMBL5415214 1 4.40
CHEMBL5440218 1 -
CHEMBL5404134 1 -
CHEMBL5421199 1 -
CHEMBL5432011 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3040038 IC50 = 56.0 nM 7.25
CHEMBL5417784 IC50 = 29700.0 nM 4.53
CHEMBL5406769 IC50 = 34500.0 nM 4.46
CHEMBL5397904 IC50 = 35000.0 nM 4.46
CHEMBL5415214 IC50 = 40000.0 nM 4.40
CHEMBL5440218 IC50 > 25000.0 nM -
CHEMBL5404134 IC50 > 50000.0 nM -
CHEMBL5421199 IC50 > 50000.0 nM -
CHEMBL5432011 IC50 > 50000.0 nM -