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Assay Detail

CHEMBL665602

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Binding
The ability to inhibit Toxoplasma gondii Dihydrofolate reductase was tested
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and antiparasitic and antitumor activity of 2, 4-diamino-6-(arylmethyl)-5,6,7,8-tetrahydroquinazoline analogues of piritrexim.
Rosowsky A, Papoulis AT, Forsch RA, Queener SF.
J Med Chem (1999) 42 : 1007 -1017
PubMed 10090784 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.11 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL266024 1 7.85
CHEMBL268870 1 7.85
CHEMBL7492 PIRITREXIM 2.0 1 7.77
CHEMBL7571 1 7.75
CHEMBL268355 1 7.68
CHEMBL7375 1 7.68
CHEMBL267616 1 7.64
CHEMBL7542 1 7.64
CHEMBL7063 1 7.62
CHEMBL6970 1 7.50
CHEMBL7779 1 7.44
CHEMBL7170 1 7.40
CHEMBL7586 1 7.31
CHEMBL7452 1 7.30
CHEMBL7488 1 7.27
CHEMBL267207 1 7.21
CHEMBL7062 1 7.14
CHEMBL267437 1 6.85
CHEMBL7263 1 6.75
CHEMBL6899 1 6.70
CHEMBL7139 1 6.52
CHEMBL6696 1 5.96
CHEMBL7535 1 5.89
CHEMBL6971 1 5.58
CHEMBL22 TRIMETHOPRIM 4.0 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL266024 IC50 = 14.0 nM 7.85
CHEMBL268870 IC50 = 14.0 nM 7.85
CHEMBL7492 PIRITREXIM IC50 = 17.0 nM 7.77
CHEMBL7571 IC50 = 18.0 nM 7.75
CHEMBL268355 IC50 = 21.0 nM 7.68
CHEMBL7375 IC50 = 21.0 nM 7.68
CHEMBL267616 IC50 = 23.0 nM 7.64
CHEMBL7542 IC50 = 23.0 nM 7.64
CHEMBL7063 IC50 = 24.0 nM 7.62
CHEMBL6970 IC50 = 32.0 nM 7.50
CHEMBL7779 IC50 = 36.0 nM 7.44
CHEMBL7170 IC50 = 40.0 nM 7.40
CHEMBL7586 IC50 = 49.0 nM 7.31
CHEMBL7452 IC50 = 50.0 nM 7.30
CHEMBL7488 IC50 = 54.0 nM 7.27
CHEMBL267207 IC50 = 62.0 nM 7.21
CHEMBL7062 IC50 = 73.0 nM 7.14
CHEMBL267437 IC50 = 140.0 nM 6.85
CHEMBL7263 IC50 = 180.0 nM 6.75
CHEMBL6899 IC50 = 200.0 nM 6.70
CHEMBL7139 IC50 = 300.0 nM 6.52
CHEMBL6696 IC50 = 1100.0 nM 5.96
CHEMBL7535 IC50 = 1300.0 nM 5.89
CHEMBL6971 IC50 = 2600.0 nM 5.58
CHEMBL22 TRIMETHOPRIM IC50 = 2700.0 nM 5.57