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Assay Detail

CHEMBL666733

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

Binding
Inhibition of Escherichia coli dihydrofolate reductase (DHFR)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Dihydrofolate reductase (CHEMBL1809)
Type SINGLE PROTEIN
Organism Escherichia coli

Publication

Synthesis of N-[4-[1-ethyl-2-(2,4-diaminofuro[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid as an antifolate.
Gangjee A, Zeng Y, McGuire JJ, Kisliuk RL.
J Med Chem (2002) 45 : 1942 -1948
PubMed 11960504 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.79 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34259 METHOTREXATE 4.0 1 8.05
CHEMBL56977 1 6.36
CHEMBL60639 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34259 METHOTREXATE IC50 = 9.0 nM 8.05
CHEMBL56977 IC50 = 440.0 nM 6.36
CHEMBL60639 IC50 = 1100.0 nM 5.96