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Assay Detail

CHEMBL4146154

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

Binding
Inhibition of Mycobacterium tuberculosis H37Rv DHFR expressed in Escherichia coli assessed as reduction in consumption of NADPH using DHF as substrate by fluorescence method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycobacterium tuberculosis H37Rv
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Dihydrofolate reductase (CHEMBL6065)
Type SINGLE PROTEIN
Organism Mycobacterium tuberculosis

Publication

1,3,5-triazaspiro[5.5]undeca-2,4-dienes as selective Mycobacterium tuberculosis dihydrofolate reductase inhibitors with potent whole cell activity.
Yang X, Wedajo W, Yamada Y, Dahlroth SL, Neo JJ, Dick T, Chui WK.
Eur J Med Chem (2018) 144 : 262 -276
PubMed 29274493 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.78 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL526013 1 8.09
CHEMBL526243 1 8.00
CHEMBL531405 1 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL526013 IC50 = 8.2 nM 8.09
CHEMBL526243 IC50 = 10.1 nM 8.00
CHEMBL531405 IC50 = 54.5 nM 7.26