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Assay Detail

CHEMBL669017

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Binding
Concentration inhibiting rat liver dihydrofolate reductase.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Dihydrofolate reductase (CHEMBL2363)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 15 7.70 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7492 PIRITREXIM 2.0 1 8.82
CHEMBL23532 1 8.68
CHEMBL119 TRIMETREXATE 4.0 1 8.52
CHEMBL88555 1 8.23
CHEMBL50514 1 8.12
CHEMBL328897 1 7.92
CHEMBL89528 1 7.66
CHEMBL52688 1 7.58
CHEMBL300603 1 7.50
CHEMBL82975 1 7.38
CHEMBL88430 1 7.36
CHEMBL54399 1 7.17
CHEMBL55179 1 6.52
CHEMBL52947 1 6.37
CHEMBL22 TRIMETHOPRIM 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7492 PIRITREXIM IC50 = 1.5 nM 8.82
CHEMBL23532 IC50 = 2.1 nM 8.68
CHEMBL119 TRIMETREXATE IC50 = 3.0 nM 8.52
CHEMBL88555 IC50 = 5.9 nM 8.23
CHEMBL50514 IC50 = 7.6 nM 8.12
CHEMBL328897 IC50 = 12.0 nM 7.92
CHEMBL89528 IC50 = 22.0 nM 7.66
CHEMBL52688 IC50 = 26.0 nM 7.58
CHEMBL300603 IC50 = 32.0 nM 7.50
CHEMBL82975 IC50 = 42.0 nM 7.38
CHEMBL88430 IC50 = 44.0 nM 7.36
CHEMBL54399 IC50 = 67.0 nM 7.17
CHEMBL55179 IC50 = 300.0 nM 6.52
CHEMBL52947 IC50 = 430.0 nM 6.37
CHEMBL22 TRIMETHOPRIM IC50 = 130000.0 nM -