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Assay Detail

CHEMBL664909

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Binding
Concentration inhibiting Toxoplasma gondii dihydrofolate reductase
14
Total Activities
14
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-Diaminopyrido[3,2-d]pyrimidine inhibitors of dihydrofolate reductase from Pneumocystis carinii and Toxoplasma gondii.
Rosowsky A, Forsch RA, Queener SF.
J Med Chem (1995) 38 : 2615 -2620
PubMed 7629801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.82 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50514 1 9.07
CHEMBL52688 1 8.33
CHEMBL88555 1 8.28
CHEMBL328897 1 8.19
CHEMBL23532 1 8.13
CHEMBL119 TRIMETREXATE 4.0 1 8.00
CHEMBL89528 1 7.82
CHEMBL7492 PIRITREXIM 2.0 1 7.77
CHEMBL54399 1 7.70
CHEMBL82975 1 7.57
CHEMBL88430 1 7.52
CHEMBL55179 1 7.09
CHEMBL300603 1 7.01
CHEMBL52947 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50514 IC50 = 0.85 nM 9.07
CHEMBL52688 IC50 = 4.7 nM 8.33
CHEMBL88555 IC50 = 5.2 nM 8.28
CHEMBL328897 IC50 = 6.4 nM 8.19
CHEMBL23532 IC50 = 7.4 nM 8.13
CHEMBL119 TRIMETREXATE IC50 = 10.0 nM 8.00
CHEMBL89528 IC50 = 15.0 nM 7.82
CHEMBL7492 PIRITREXIM IC50 = 17.0 nM 7.77
CHEMBL54399 IC50 = 20.0 nM 7.70
CHEMBL82975 IC50 = 27.0 nM 7.57
CHEMBL88430 IC50 = 30.0 nM 7.52
CHEMBL55179 IC50 = 82.0 nM 7.09
CHEMBL300603 IC50 = 98.0 nM 7.01
CHEMBL52947 IC50 = 100.0 nM 7.00