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Assay Detail

CHEMBL669305

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

Binding
Inhibitory activity towards dihydrofolate reductase in L1210 murine leukemia cell lines
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type L1210
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Dihydrofolate reductase (CHEMBL4564)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Methotrexate analogues. 23. Synthesis, dihydrofolate reductase affinity, cytotoxicity, and in vivo antitumor activity of some putative degradation products of methotrexate-poly(L-lysine) conjugates.
Rosowsky A, Forsch RA, Freisheim JH, Galivan J, Wick M.
J Med Chem (1984) 27 : 888 -893
PubMed 6737432 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.07 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34259 METHOTREXATE 4.0 1 7.30
CHEMBL344876 1 7.07
CHEMBL171937 1 7.06
CHEMBL3143620 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34259 METHOTREXATE IC50 = 50.0 nM 7.30
CHEMBL344876 IC50 = 86.0 nM 7.07
CHEMBL171937 IC50 = 87.0 nM 7.06
CHEMBL3143620 IC50 = 140.0 nM 6.85