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Assay Detail

CHEMBL664916

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Binding
Inhibitory activity against Dihydrofolate reductase from Toxoplasma gondii
20
Total Activities
20
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

6-substituted 2,4-diamino-5-methylpyrido[2,3-d]pyrimidines as inhibitors of dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii and as antitumor agents.
Gangjee A, Vasudevan A, Queener SF, Kisliuk RL.
J Med Chem (1995) 38 : 1778 -1785
PubMed 7752201 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.75 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50514 1 9.07
CHEMBL52433 1 8.57
CHEMBL23569 1 8.32
CHEMBL53693 1 8.17
CHEMBL23532 1 8.13
CHEMBL49454 1 8.11
CHEMBL283518 1 8.06
CHEMBL119 TRIMETREXATE 4.0 1 8.00
CHEMBL7492 PIRITREXIM 2.0 1 7.96
CHEMBL23867 1 7.84
CHEMBL23021 1 7.80
CHEMBL279679 1 7.77
CHEMBL53903 1 7.64
CHEMBL279680 1 7.54
CHEMBL281803 1 7.52
CHEMBL23705 1 7.42
CHEMBL279983 1 7.25
CHEMBL22623 1 7.24
CHEMBL23844 1 7.00
CHEMBL22 TRIMETHOPRIM 4.0 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50514 IC50 = 0.85 nM 9.07
CHEMBL52433 IC50 = 2.7 nM 8.57
CHEMBL23569 IC50 = 4.8 nM 8.32
CHEMBL53693 IC50 = 6.7 nM 8.17
CHEMBL23532 IC50 = 7.4 nM 8.13
CHEMBL49454 IC50 = 7.7 nM 8.11
CHEMBL283518 IC50 = 8.8 nM 8.06
CHEMBL119 TRIMETREXATE IC50 = 10.0 nM 8.00
CHEMBL7492 PIRITREXIM IC50 = 11.0 nM 7.96
CHEMBL23867 IC50 = 14.5 nM 7.84
CHEMBL23021 IC50 = 16.0 nM 7.80
CHEMBL279679 IC50 = 17.0 nM 7.77
CHEMBL53903 IC50 = 23.0 nM 7.64
CHEMBL279680 IC50 = 29.0 nM 7.54
CHEMBL281803 IC50 = 30.1 nM 7.52
CHEMBL23705 IC50 = 38.0 nM 7.42
CHEMBL279983 IC50 = 56.5 nM 7.25
CHEMBL22623 IC50 = 58.0 nM 7.24
CHEMBL23844 IC50 = 100.0 nM 7.00
CHEMBL22 TRIMETHOPRIM IC50 = 2700.0 nM 5.57