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Assay Detail

CHEMBL669355

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

Binding
Compound was tested for the inhibition of dihydrofolate reductase in Bovine liver
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dihydrofolate reductase (CHEMBL2902)
Type SINGLE PROTEIN
Organism Lactobacillus casei

Publication

Synthesis and antitumor activities of novel 6-5 fused ring heterocycle antifolates: N-[4-[omega-(2-amino-4-substituted-6,7-dihydrocyclopenta [d]pyrimidin-5-yl)alkyl]benzoyl]-L-glutamic acids.
Kotake Y, Iijima A, Yoshimatsu K, Tamai N, Ozawa Y, Koyanagi N, Kitoh K, Nomura H.
J Med Chem (1994) 37 : 1616 -1624
PubMed 8201595 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.39 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34259 METHOTREXATE 4.0 1 8.89
CHEMBL41056 1 8.60
CHEMBL296373 EDATREXATE 2.0 1 8.42
CHEMBL42159 1 7.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34259 METHOTREXATE IC50 = 1.3 nM 8.89
CHEMBL41056 IC50 = 2.5 nM 8.60
CHEMBL296373 EDATREXATE IC50 = 3.8 nM 8.42
CHEMBL42159 IC50 = 22.0 nM 7.66