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Assay Detail

CHEMBL665596

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Binding
Inhibitory concentration against Toxoplasma gondii dihydrofolate reductase
7
Total Activities
7
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

Preliminary in vitro studies on two potent, water-soluble trimethoprim analogues with exceptional species selectivity against dihydrofolate reductase from Pneumocystis carinii and Mycobacterium avium.
Forsch RA, Queener SF, Rosowsky A.
Bioorg Med Chem Lett (2004) 14 : 1811 -1815
PubMed 15026078 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.08 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7492 PIRITREXIM 2.0 1 8.37
CHEMBL119 TRIMETREXATE 4.0 1 7.80
CHEMBL37334 1 7.50
CHEMBL300419 1 7.47
CHEMBL34293 1 6.47
CHEMBL52415 1 6.38
CHEMBL53193 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7492 PIRITREXIM IC50 = 4.3 nM 8.37
CHEMBL119 TRIMETREXATE IC50 = 16.0 nM 7.80
CHEMBL37334 IC50 = 32.0 nM 7.50
CHEMBL300419 IC50 = 34.0 nM 7.47
CHEMBL34293 IC50 = 340.0 nM 6.47
CHEMBL52415 IC50 = 420.0 nM 6.38
CHEMBL53193 IC50 = 2800.0 nM 5.55