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Assay Detail

CHEMBL667228

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

Binding
Inhibitory activity against dihydrofolate reductase (DHFR) enzyme from rat liver
9
Total Activities
9
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 as antibacterial agents. 8. The 3,4,5-triethyl isostere of trimethoprim. A study of specificity.
Roth B, Aig E.
J Med Chem (1987) 30 : 1998 -2004
PubMed 3312605 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.33 4.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL60883 1 4.54
CHEMBL57582 1 4.42
CHEMBL293013 1 4.23
CHEMBL19633 DIAVERIDINE 2.0 1 4.11
CHEMBL19023 1 -
CHEMBL22 TRIMETHOPRIM 4.0 1 -
CHEMBL61287 1 -
CHEMBL59703 1 -
CHEMBL60029 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL60883 IC50 = 29000.0 nM 4.54
CHEMBL57582 IC50 = 38000.0 nM 4.42
CHEMBL293013 IC50 = 59000.0 nM 4.23
CHEMBL19633 DIAVERIDINE IC50 = 78000.0 nM 4.11
CHEMBL19023 IC50 = 170000.0 nM -
CHEMBL22 TRIMETHOPRIM IC50 = 260000.0 nM -
CHEMBL61287 IC50 = 210000.0 nM -
CHEMBL59703 IC50 = 230000.0 nM -
CHEMBL60029 IC50 > 40000.0 nM -