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Assay Detail

CHEMBL1027392

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Binding
Inhibition of Mycobacterium avium dihydrofolate reductase
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dihydrofolate reductase (CHEMBL5457)
Type SINGLE PROTEIN
Organism Mycobacterium avium

Publication

N9-substituted 2,4-diaminoquinazolines: synthesis and biological evaluation of lipophilic inhibitors of pneumocystis carinii and toxoplasma gondii dihydrofolate reductase.
Gangjee A, Adair OO, Pagley M, Queener SF.
J Med Chem (2008) 51 : 6195 -6200
PubMed 18771252 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.29 9.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL521672 1 9.01
CHEMBL493717 1 8.96
CHEMBL522678 1 8.64
CHEMBL493718 1 8.54
CHEMBL492895 1 8.48
CHEMBL492896 1 7.89
CHEMBL522543 1 7.85
CHEMBL523004 1 7.80
CHEMBL455012 1 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL521672 IC50 = 0.98 nM 9.01
CHEMBL493717 IC50 = 1.1 nM 8.96
CHEMBL522678 IC50 = 2.3 nM 8.64
CHEMBL493718 IC50 = 2.9 nM 8.54
CHEMBL492895 IC50 = 3.3 nM 8.48
CHEMBL492896 IC50 = 13.0 nM 7.89
CHEMBL522543 IC50 = 14.0 nM 7.85
CHEMBL523004 IC50 = 16.0 nM 7.80
CHEMBL455012 IC50 = 34.0 nM 7.47