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Assay Detail

CHEMBL665261

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

Binding
Inhibitory activity against purified DHFR (Dihydrofolate reductase) from Pneumocystis carinii.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Pneumocystis carinii
Confidence 9 — Direct single protein target
Curated By Expert

Target

Dihydrofolate reductase (CHEMBL1926)
Type SINGLE PROTEIN
Organism Pneumocystis carinii

Publication

Nonclassical 2,4-diamino-6-(aminomethyl)-5,6,7,8-tetrahydroquinazoline antifolates: synthesis and biological activities.
Gangjee A, Zaveri N, Kothare M, Queener SF.
J Med Chem (1995) 38 : 3660 -3668
PubMed 7658454 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.92 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL120826 1 6.68
CHEMBL121319 1 6.39
CHEMBL333791 1 6.30
CHEMBL121264 1 6.29
CHEMBL121947 1 6.03
CHEMBL120939 1 5.80
CHEMBL122704 1 5.51
CHEMBL7488 1 5.34
CHEMBL22 TRIMETHOPRIM 4.0 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL120826 IC50 = 210.0 nM 6.68
CHEMBL121319 IC50 = 410.0 nM 6.39
CHEMBL333791 IC50 = 502.0 nM 6.30
CHEMBL121264 IC50 = 517.0 nM 6.29
CHEMBL121947 IC50 = 940.0 nM 6.03
CHEMBL120939 IC50 = 1570.0 nM 5.80
CHEMBL122704 IC50 = 3100.0 nM 5.51
CHEMBL7488 IC50 = 4600.0 nM 5.34
CHEMBL22 TRIMETHOPRIM IC50 = 12000.0 nM 4.92