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Assay Detail

CHEMBL669306

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

Binding
Tested for inhibition against purified Dihydrofolate reductase from L1210 murine leukemia cells
10
Total Activities
10
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. 34. Replacement of the glutamate moiety in methotrexate and aminopterin by long-chain 2-aminoalkanedioic acids.
Rosowsky A, Bader H, Kohler W, Freisheim JH, Moran RG.
J Med Chem (1988) 31 : 1338 -1344
PubMed 2898531 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.35 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL283062 1 7.64
CHEMBL376180 AMINOPTERIN 2.0 1 7.60
CHEMBL34259 METHOTREXATE 4.0 1 7.60
CHEMBL26326 1 7.58
CHEMBL28112 1 7.54
CHEMBL25923 1 7.50
CHEMBL27306 1 7.47
CHEMBL275229 1 7.17
CHEMBL26148 1 7.09
CHEMBL434004 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL283062 IC50 = 23.0 nM 7.64
CHEMBL376180 AMINOPTERIN IC50 = 25.0 nM 7.60
CHEMBL34259 METHOTREXATE IC50 = 25.0 nM 7.60
CHEMBL26326 IC50 = 26.0 nM 7.58
CHEMBL28112 IC50 = 29.0 nM 7.54
CHEMBL25923 IC50 = 32.0 nM 7.50
CHEMBL27306 IC50 = 34.0 nM 7.47
CHEMBL275229 IC50 = 67.0 nM 7.17
CHEMBL26148 IC50 = 81.0 nM 7.09
CHEMBL434004 IC50 = 540.0 nM 6.27