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Assay Detail

CHEMBL667225

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

Binding
Inhibitory activity against Dihydrofolate reductase in rat liver
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dihydrofolate reductase (CHEMBL2363)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 12. 1,2-Dihydroquinolylmethyl analogues with high activity and specificity for bacterial dihydrofolate reductase.
Johnson JV, Rauchman BS, Baccanari DP, Roth B.
J Med Chem (1989) 32 : 1942 -1949
PubMed 2666668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 4.40 4.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL294638 1 4.70
CHEMBL58038 1 4.48
CHEMBL60827 1 4.46
CHEMBL292827 1 4.25
CHEMBL294678 1 4.12
CHEMBL22 TRIMETHOPRIM 4.0 1 -
CHEMBL58138 1 -
CHEMBL418293 1 -
CHEMBL60931 1 -
CHEMBL58149 1 -
CHEMBL58079 1 -
CHEMBL300371 1 -
CHEMBL300385 1 -
CHEMBL300545 1 -
CHEMBL418492 1 -
CHEMBL61305 1 -
CHEMBL300370 1 -
CHEMBL60647 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL294638 IC50 = 20000.0 nM 4.70
CHEMBL58038 IC50 = 33000.0 nM 4.48
CHEMBL60827 IC50 = 35000.0 nM 4.46
CHEMBL292827 IC50 = 56000.0 nM 4.25
CHEMBL294678 IC50 = 76000.0 nM 4.12
CHEMBL22 TRIMETHOPRIM IC50 = 0.0026 nM -
CHEMBL58138 IC50 = 250000.0 nM -
CHEMBL418293 IC50 = 233000.0 nM -
CHEMBL60931 IC50 = 300000.0 nM -
CHEMBL58149 IC50 = 230000.0 nM -
CHEMBL58079 IC50 = 240000.0 nM -
CHEMBL300371 IC50 = 174000.0 nM -
CHEMBL300385 IC50 = 340000.0 nM -
CHEMBL300545 IC50 = 118000.0 nM -
CHEMBL418492 IC50 = 300000.0 nM -
CHEMBL61305 IC50 = 164000.0 nM -
CHEMBL300370 IC50 = 500000.0 nM -
CHEMBL60647 IC50 = 430000.0 nM -