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Assay Detail

CHEMBL668914

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

Binding
Compound was tested for its inhibitory concentration to inhibit the enzyme Dihydro Folate Reductase (DHFR) from murine L1210 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. 28. Synthesis and biological evaluation of new gamma-monoamides of aminopterin and methotrexate.
Rosowsky A, Bader H, Radike-Smith M, Cucchi CA, Wick MM, Freisheim JH.
J Med Chem (1986) 29 : 1703 -1709
PubMed 3462394 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.28 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34259 METHOTREXATE 4.0 1 7.70
CHEMBL376180 AMINOPTERIN 2.0 1 7.70
CHEMBL44693 1 7.38
CHEMBL44697 1 7.36
CHEMBL47316 1 7.35
CHEMBL45735 1 7.22
CHEMBL48044 1 7.10
CHEMBL46140 1 7.06
CHEMBL45572 1 7.00
CHEMBL416261 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34259 METHOTREXATE IC50 = 20.0 nM 7.70
CHEMBL376180 AMINOPTERIN IC50 = 20.0 nM 7.70
CHEMBL44693 IC50 = 42.0 nM 7.38
CHEMBL44697 IC50 = 44.0 nM 7.36
CHEMBL47316 IC50 = 45.0 nM 7.35
CHEMBL45735 IC50 = 60.0 nM 7.22
CHEMBL48044 IC50 = 80.0 nM 7.10
CHEMBL46140 IC50 = 87.0 nM 7.06
CHEMBL45572 IC50 = 100.0 nM 7.00
CHEMBL416261 IC50 = 130.0 nM 6.89