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Assay Detail

CHEMBL668878

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

Binding
Inhibitory activity against Dihydrofolate reductase enzyme purified from rat liver.
3
Total Activities
3
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

2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 2. C-Alkylation of pyrimidines with Mannich bases and application to the synthesis of trimethoprim and analogues.
Roth B, Strelitz JZ, Rauckman BS.
J Med Chem (1980) 23 : 379 -384
PubMed 6991692 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.04 4.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1181 4-HYDROXYTRIMETHOPRIM 1 4.04
CHEMBL325533 1 -
CHEMBL22 TRIMETHOPRIM 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1181 4-HYDROXYTRIMETHOPRIM IC50 = 92000.0 nM 4.04
CHEMBL325533 IC50 > 400000.0 nM -
CHEMBL22 TRIMETHOPRIM IC50 = 260000.0 nM -