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Assay Detail

CHEMBL669645

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Binding
Compound was tested for the inhibition of dihydrofolate reductase in P388 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type P388
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Dihydrofolate reductase (CHEMBL4564)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and antitumor activities of novel 6-5 fused ring heterocycle antifolates: N-[4-[omega-(2-amino-4-substituted-6,7-dihydrocyclopenta [d]pyrimidin-5-yl)alkyl]benzoyl]-L-glutamic acids.
Kotake Y, Iijima A, Yoshimatsu K, Tamai N, Ozawa Y, Koyanagi N, Kitoh K, Nomura H.
J Med Chem (1994) 37 : 1616 -1624
PubMed 8201595 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.89 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296190 1 8.68
CHEMBL34259 METHOTREXATE 4.0 1 8.18
CHEMBL41056 1 8.15
CHEMBL296373 EDATREXATE 2.0 1 7.96
CHEMBL42301 1 7.22
CHEMBL42159 1 7.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296190 IC50 = 2.1 nM 8.68
CHEMBL34259 METHOTREXATE IC50 = 6.6 nM 8.18
CHEMBL41056 IC50 = 7.1 nM 8.15
CHEMBL296373 EDATREXATE IC50 = 11.0 nM 7.96
CHEMBL42301 IC50 = 60.0 nM 7.22
CHEMBL42159 IC50 = 72.0 nM 7.14