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Assay Detail

CHEMBL669252

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

Binding
Tested in vitro for inhibitory concentration against CCRF-CEM human Leukemic lymphoblast by using DHFR as primary target
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CCRF-CEM
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 N omega-hemiphthaloyl-alpha,omega- diaminoalkanoic acid analogues of aminopterin and 3',5-dichloroaminopterin.
Rosowsky A, Bader H, Wright JE, Keyomarsi K, Matherly LH.
J Med Chem (1994) 37 : 2167 -2174
PubMed 8035423 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.69 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18155 1 8.96
CHEMBL296373 EDATREXATE 2.0 1 8.59
CHEMBL376180 AMINOPTERIN 2.0 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18155 IC50 = 1.1 nM 8.96
CHEMBL296373 EDATREXATE IC50 = 2.6 nM 8.59
CHEMBL376180 AMINOPTERIN IC50 = 3.0 nM 8.52