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Assay Detail

CHEMBL668094

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

Binding
Compound was tested for its inhibitory activity on Recombinant Human Dihydrofolate Reductase.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dihydrofolate reductase (CHEMBL202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Folate analogues. 34. Synthesis and antitumor activity of non-polyglutamylatable inhibitors of dihydrofolate reductase.
Abraham A, McGuire JJ, Galivan J, Nimec Z, Kisliuk RL, Gaumont Y, Nair MG.
J Med Chem (1991) 34 : 222 -227
PubMed 1992121 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.27 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34259 METHOTREXATE 4.0 1 8.41
CHEMBL293263 1 8.39
CHEMBL296373 EDATREXATE 2.0 1 8.36
CHEMBL307820 1 8.28
CHEMBL308279 1 8.24
CHEMBL73267 1 8.23
CHEMBL65616 1 8.19
CHEMBL307486 1 8.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34259 METHOTREXATE IC50 = 3.9 nM 8.41
CHEMBL293263 IC50 = 4.1 nM 8.39
CHEMBL296373 EDATREXATE IC50 = 4.4 nM 8.36
CHEMBL307820 IC50 = 5.3 nM 8.28
CHEMBL308279 IC50 = 5.8 nM 8.24
CHEMBL73267 IC50 = 5.9 nM 8.23
CHEMBL65616 IC50 = 6.4 nM 8.19
CHEMBL307486 IC50 = 8.8 nM 8.06