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Assay Detail

CHEMBL665613

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Binding
Inhibitory activity against Toxoplasma gondii dihydrofolate reductase (in 50 uM dihydrofolic acid)
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 Autocuration

Target

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

Publication

2,4-diamino-5-deaza-6-substituted pyrido[2,3-d]pyrimidine antifolates as potent and selective nonclassical inhibitors of dihydrofolate reductases.
Gangjee A, Vasudevan A, Queener SF, Kisliuk RL.
J Med Chem (1996) 39 : 1438 -1446
PubMed 8691474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.14 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34259 METHOTREXATE 4.0 1 7.66
CHEMBL35222 1 7.58
CHEMBL32113 1 7.55
CHEMBL36245 1 7.54
CHEMBL33038 1 7.46
CHEMBL32708 1 6.30
CHEMBL33208 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34259 METHOTREXATE IC50 = 22.0 nM 7.66
CHEMBL35222 IC50 = 26.0 nM 7.58
CHEMBL32113 IC50 = 28.0 nM 7.55
CHEMBL36245 IC50 = 29.0 nM 7.54
CHEMBL33038 IC50 = 35.0 nM 7.46
CHEMBL32708 IC50 = 500.0 nM 6.30
CHEMBL33208 IC50 = 1300.0 nM 5.89