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Assay Detail

CHEMBL845118

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

Functional
Cytotoxicity by the selective inhibition against African green monkey kidney fibroblast (vero cells).
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Chlorocebus sabaeus
Cell Type Vero
Confidence 1 — Organism
Curated By Intermediate

Target

Vero (CHEMBL391)
Type CELL-LINE
Organism Chlorocebus sabaeus

Publication

Development of 2,4-diaminopyrimidines as antimalarials based on inhibition of the S108N and C59R+S108N mutants of dihydrofolate reductase from pyrimethamine-resistant Plasmodium falciparum.
Tarnchompoo B, Sirichaiwat C, Phupong W, Intaraudom C, Sirawaraporn W, Kamchonwongpaisan S, Vanichtanankul J, Thebtaranonth Y, Yuthavong Y.
J Med Chem (2002) 45 : 1244 -1252
PubMed 11881993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.74 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278813 1 5.52
CHEMBL278847 1 5.16
CHEMBL22139 1 4.89
CHEMBL22403 1 4.82
CHEMBL22901 1 4.47
CHEMBL25112 1 4.35
CHEMBL21885 1 4.00
CHEMBL22327 1 -
CHEMBL416373 1 -
CHEMBL22693 1 -
CHEMBL21395 1 -
CHEMBL22148 1 -
CHEMBL22 TRIMETHOPRIM 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278813 IC50 = 3000.0 nM 5.52
CHEMBL278847 IC50 = 7000.0 nM 5.16
CHEMBL22139 IC50 = 13000.0 nM 4.89
CHEMBL22403 IC50 = 15000.0 nM 4.82
CHEMBL22901 IC50 = 34000.0 nM 4.47
CHEMBL25112 IC50 = 45000.0 nM 4.35
CHEMBL21885 IC50 = 100000.0 nM 4.00
CHEMBL22327 IC50 = 200000.0 nM -
CHEMBL416373 IC50 > 50000.0 nM -
CHEMBL22693 IC50 > 50000.0 nM -
CHEMBL21395 IC50 > 250000.0 nM -
CHEMBL22148 IC50 = 320000.0 nM -
CHEMBL22 TRIMETHOPRIM IC50 > 50000.0 nM -