Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4146155

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

Binding
Inhibition of human DHFR 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 Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dihydrofolate reductase (CHEMBL202)
Type SINGLE PROTEIN
Organism Homo sapiens

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 7.57 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL526243 1 8.17
CHEMBL526013 1 8.12
CHEMBL531405 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL526243 IC50 = 6.8 nM 8.17
CHEMBL526013 IC50 = 7.6 nM 8.12
CHEMBL531405 IC50 = 382.1 nM 6.42