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Assay Detail

CHEMBL5155787

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

Binding
Inhibition of Escherichia coli C-terminal hexahistidine tagged DHFR incubated for 5 mins in presence of NADPH by measuring oxidation of NADPH to NADP+
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

The discovery of 1, 3-diamino-7H-pyrrol[3, 2-f]quinazoline compounds as potent antimicrobial antifolates.
Li Y, Ouyang Y, Wu H, Wang P, Huang Y, Li X, Chen H, Sun Y, Hu X, Wang X, Li G, Lu Y, Li C, Lu X, Pang J, Nie T, Sang X, Dong L, Dong W, Jiang J, Paterson IC, Yang X, Hong W, Wang H, You X.
Eur J Med Chem (2022) 228 : 113979 -113979
PubMed 34802838 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.66 8.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5194771 1 8.63
CHEMBL5201889 1 7.80
CHEMBL22 TRIMETHOPRIM 4.0 1 7.21
CHEMBL525149 1 7.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5194771 IC50 = 2.36 nM 8.63
CHEMBL5201889 IC50 = 15.93 nM 7.80
CHEMBL22 TRIMETHOPRIM IC50 = 61.6 nM 7.21
CHEMBL525149 IC50 = 98.36 nM 7.01