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Assay Detail

CHEMBL665605

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Binding
Inhibitory activity against purified Dihydrofolate reductase from Toxoplasma gondii.
12
Total Activities
12
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

Nonclassical 2,4-diamino-6-(aminomethyl)-5,6,7,8-tetrahydroquinazoline antifolates: synthesis and biological activities.
Gangjee A, Zaveri N, Kothare M, Queener SF.
J Med Chem (1995) 38 : 3660 -3668
PubMed 7658454 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.64 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL123122 1 8.15
CHEMBL119 TRIMETREXATE 4.0 1 8.00
CHEMBL120821 1 7.92
CHEMBL121868 1 7.82
CHEMBL264548 1 7.77
CHEMBL121683 1 7.77
CHEMBL121433 1 7.68
CHEMBL123043 1 7.66
CHEMBL121348 1 7.64
CHEMBL123276 1 7.52
CHEMBL120994 1 6.96
CHEMBL7263 1 6.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL123122 IC50 = 7.0 nM 8.15
CHEMBL119 TRIMETREXATE IC50 = 10.0 nM 8.00
CHEMBL120821 IC50 = 12.0 nM 7.92
CHEMBL121868 IC50 = 15.0 nM 7.82
CHEMBL264548 IC50 = 17.0 nM 7.77
CHEMBL121683 IC50 = 17.0 nM 7.77
CHEMBL121433 IC50 = 21.0 nM 7.68
CHEMBL123043 IC50 = 22.0 nM 7.66
CHEMBL121348 IC50 = 23.0 nM 7.64
CHEMBL123276 IC50 = 30.0 nM 7.52
CHEMBL120994 IC50 = 110.0 nM 6.96
CHEMBL7263 IC50 = 181.0 nM 6.74