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Assay Detail

CHEMBL665593

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Binding
Inhibitory concentration against Toxoplasma gondii Dihydrofolate reductase
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Toxoplasma gondii
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Bifunctional dihydrofolate reductase-thymidylate synthase (CHEMBL2425)
Type SINGLE PROTEIN
Organism Toxoplasma gondii

Publication

Synthesis and biological activities of conformationally restricted, tricyclic nonclassical antifolates as inhibitors of dihydrofolate reductases.
Gangjee A, Shi J, Queener SF.
J Med Chem (1997) 40 : 1930 -1936
PubMed 9191971 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.92 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50514 1 9.07
CHEMBL119 TRIMETREXATE 4.0 1 8.00
CHEMBL7492 PIRITREXIM 2.0 1 7.77
CHEMBL299927 1 6.54
CHEMBL57682 1 6.28
CHEMBL58597 1 6.12
CHEMBL293512 1 5.95
CHEMBL431740 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50514 IC50 = 0.85 nM 9.07
CHEMBL119 TRIMETREXATE IC50 = 10.0 nM 8.00
CHEMBL7492 PIRITREXIM IC50 = 17.0 nM 7.77
CHEMBL299927 IC50 = 290.0 nM 6.54
CHEMBL57682 IC50 = 520.0 nM 6.28
CHEMBL58597 IC50 = 760.0 nM 6.12
CHEMBL293512 IC50 = 1120.0 nM 5.95
CHEMBL431740 IC50 = 2300.0 nM 5.64