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Assay Detail

CHEMBL879985

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of dihydrofolate reductase (DHFR) in WIL2 cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type WIL2
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Dihydrofolate reductase (CHEMBL202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 5-deazaisofolic acid, 5-deaza-5,6,7,8-tetrahydroisofolic acid, and their N9-substituted analogues.
Singh SK, Dev IK, Duch DS, Ferone R, Smith GK, Freisheim JH, Hynes JB.
J Med Chem (1991) 34 : 606 -610
PubMed 1995883 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.33 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157857 1 6.68
CHEMBL156551 1 6.60
CHEMBL157775 1 5.71
CHEMBL13659 1 -
CHEMBL157230 1 -
CHEMBL170101 1 -
CHEMBL156308 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157857 IC50 = 210.0 nM 6.68
CHEMBL156551 IC50 = 250.0 nM 6.60
CHEMBL157775 IC50 = 1950.0 nM 5.71
CHEMBL13659 IC50 > 100000.0 nM -
CHEMBL157230 IC50 > 1000000.0 nM -
CHEMBL170101 IC50 > 100000.0 nM -
CHEMBL156308 IC50 > 1000000.0 nM -