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Assay Detail

CHEMBL669254

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Binding
Tested for 50% inhibition of WI-L2 Dihydrofolate reductase
9
Total Activities
9
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 (CHEMBL202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent inhibition of thymidylate synthase by two series of nonclassical quinazolines.
McNamara DJ, Berman EM, Fry DW, Werbel LM.
J Med Chem (1990) 33 : 2045 -2051
PubMed 2362285 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.49 5.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL422395 1 5.14
CHEMBL304407 1 4.99
CHEMBL302669 1 4.69
CHEMBL62769 1 4.65
CHEMBL62599 1 4.43
CHEMBL433059 1 4.18
CHEMBL62675 1 4.18
CHEMBL417562 1 4.14
CHEMBL64215 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL422395 IC50 = 7200.0 nM 5.14
CHEMBL304407 IC50 = 10200.0 nM 4.99
CHEMBL302669 IC50 = 20300.0 nM 4.69
CHEMBL62769 IC50 = 22600.0 nM 4.65
CHEMBL62599 IC50 = 37300.0 nM 4.43
CHEMBL433059 IC50 = 66600.0 nM 4.18
CHEMBL62675 IC50 = 66600.0 nM 4.18
CHEMBL417562 IC50 = 72600.0 nM 4.14
CHEMBL64215 IC50 = 100000.0 nM 4.00