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Assay Detail

CHEMBL665365

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Binding
Inhibitory activity against DHFR (Dihydrofolate reductase) from Mycobacterium avium
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycobacterium avium
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Dihydrofolate reductase (CHEMBL5457)
Type SINGLE PROTEIN
Organism Mycobacterium avium

Publication

Structure-based design of selective inhibitors of dihydrofolate reductase: synthesis and antiparasitic activity of 2, 4-diaminopteridine analogues with a bridged diarylamine side chain.
Rosowsky A, Cody V, Galitsky N, Fu H, Papoulis AT, Queener SF.
J Med Chem (1999) 42 : 4853 -4860
PubMed 10579848 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.85 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301769 1 7.92
CHEMBL144839 1 7.77
CHEMBL144200 1 7.54
CHEMBL423381 1 5.60
CHEMBL424113 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301769 IC50 = 12.0 nM 7.92
CHEMBL144839 IC50 = 17.0 nM 7.77
CHEMBL144200 IC50 = 29.0 nM 7.54
CHEMBL423381 IC50 = 2500.0 nM 5.60
CHEMBL424113 IC50 = 3700.0 nM 5.43