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Assay Detail

CHEMBL665695

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Binding
Inhibition of Toxoplasma gondii Dihydrofolate Reductase
9
Total Activities
9
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

2,4-Diaminothieno[2,3-d]pyrimidine lipophilic antifolates as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.
Rosowsky A, Papoulis AT, Queener SF.
J Med Chem (1997) 40 : 3694 -3699
PubMed 9357537 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.13 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL280378 EPIROPRIM 2.0 1 8.00
CHEMBL31891 BRODIMOPRIM 2.0 1 7.77
CHEMBL36 PYRIMETHAMINE 4.0 1 6.41
CHEMBL22 TRIMETHOPRIM 4.0 1 5.57
CHEMBL331351 1 4.58
CHEMBL331682 1 4.47
CHEMBL122259 1 -
CHEMBL433021 1 -
CHEMBL122214 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL280378 EPIROPRIM IC50 = 10.0 nM 8.00
CHEMBL31891 BRODIMOPRIM IC50 = 17.0 nM 7.77
CHEMBL36 PYRIMETHAMINE IC50 = 390.0 nM 6.41
CHEMBL22 TRIMETHOPRIM IC50 = 2700.0 nM 5.57
CHEMBL331351 IC50 = 26000.0 nM 4.58
CHEMBL331682 IC50 = 34000.0 nM 4.47
CHEMBL122259 IC50 > 100000.0 nM -
CHEMBL433021 IC50 > 10000.0 nM -
CHEMBL122214 IC50 = 127000.0 nM -