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Assay Detail

CHEMBL651283

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

Functional
Cytotoxicity against human breast cancer cells.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type BC
Confidence 1 — Organism
Curated By Expert

Target

BC (CHEMBL613535)
Type CELL-LINE

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 16 4.52 5.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL22403 1 5.21
CHEMBL416373 1 4.80
CHEMBL278847 1 4.60
CHEMBL22327 1 4.50
CHEMBL22139 1 4.25
CHEMBL21885 1 4.25
CHEMBL21395 1 4.00
CHEMBL416376 1 -
CHEMBL36 PYRIMETHAMINE 4.0 1 -
CHEMBL22693 1 -
CHEMBL278813 1 -
CHEMBL25112 1 -
CHEMBL22148 1 -
CHEMBL416552 1 -
CHEMBL22 TRIMETHOPRIM 4.0 1 -
CHEMBL22901 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL22403 IC50 = 6100.0 nM 5.21
CHEMBL416373 IC50 = 16000.0 nM 4.80
CHEMBL278847 IC50 = 25000.0 nM 4.60
CHEMBL22327 IC50 = 32000.0 nM 4.50
CHEMBL22139 IC50 = 56000.0 nM 4.25
CHEMBL21885 IC50 = 56000.0 nM 4.25
CHEMBL21395 IC50 = 100000.0 nM 4.00
CHEMBL416376 IC50 > 250000.0 nM -
CHEMBL36 PYRIMETHAMINE IC50 > 250000.0 nM -
CHEMBL22693 IC50 > 500000.0 nM -
CHEMBL278813 IC50 > 500000.0 nM -
CHEMBL25112 IC50 > 50000.0 nM -
CHEMBL22148 IC50 > 500000.0 nM -
CHEMBL416552 IC50 = 268000.0 nM -
CHEMBL22 TRIMETHOPRIM IC50 > 250000.0 nM -
CHEMBL22901 IC50 = 139000.0 nM -