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Assay Detail

CHEMBL668093

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

Binding
Compound was evaluated for Dihydrofolate Reductase (DHFR) inhibition
6
Total Activities
6
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

Synthesis and biological activity of the 2-desamino and 2-desamino-2-methyl analogues of aminopterin and methotrexate.
Rosowsky A, Forsch RA, Moran RG, Freisheim JH.
J Med Chem (1991) 34 : 227 -234
PubMed 1992122 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.29 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34259 METHOTREXATE 4.0 1 7.62
CHEMBL376180 AMINOPTERIN 2.0 1 7.60
CHEMBL74422 1 5.22
CHEMBL430797 1 4.72
CHEMBL307137 1 -
CHEMBL419087 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34259 METHOTREXATE IC50 = 24.0 nM 7.62
CHEMBL376180 AMINOPTERIN IC50 = 25.0 nM 7.60
CHEMBL74422 IC50 = 6000.0 nM 5.22
CHEMBL430797 IC50 = 19000.0 nM 4.72
CHEMBL307137 IC50 > 50000.0 nM -
CHEMBL419087 IC50 > 20000.0 nM -