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Assay Detail

CHEMBL666696

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

Binding
Inhibition of rat liver dihydrofolate reductase assayed spectrophotometrically at 340 nM
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dihydrofolate reductase (CHEMBL2363)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Chemistry and antitumor evaluation of selected classical 2,4-diaminoquinazoline analogues of folic acid.
Hynes JB, Harmon SJ, Floyd GG, Farrington M, Hart LD, Gale GR, Washtien WL, Susten SS, Freisheim JH.
J Med Chem (1985) 28 : 209 -215
PubMed 3968685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.32 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL305253 1 8.48
CHEMBL34259 METHOTREXATE 4.0 1 8.34
CHEMBL69713 1 8.33
CHEMBL305177 1 8.32
CHEMBL423123 1 8.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL305253 IC50 = 3.3 nM 8.48
CHEMBL34259 METHOTREXATE IC50 = 4.6 nM 8.34
CHEMBL69713 IC50 = 4.7 nM 8.33
CHEMBL305177 IC50 = 4.8 nM 8.32
CHEMBL423123 IC50 = 7.2 nM 8.14