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Assay Detail

CHEMBL665204

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

Binding
Inhibitory activity against Dihydrofolate reductase in rat liver
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dihydrofolate reductase (CHEMBL2363)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Quinazoline antifolate thymidylate synthase inhibitors: alkyl, substituted alkyl, and aryl substituents in the C2 position.
Hughes LR, Jackman AL, Oldfield J, Smith RC, Burrows KD, Marsham PR, Bishop JA, Jones TR, O'Connor BM, Calvert AH.
J Med Chem (1990) 33 : 3060 -3067
PubMed 2231606 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.39 7.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL389051 1 7.12
CHEMBL103059 1 5.65
CHEMBL434209 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL389051 Ki = 75.0 nM 7.12
CHEMBL103059 Ki = 2250.0 nM 5.65
CHEMBL434209 Ki > 2660.0 nM -