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Assay Detail

CHEMBL1781265

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

Binding
Inhibition of human recombinant aldose reductase 1 after 10 mins by spectrophotometry analysis
4
Total Activities
4
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

Aldo-keto reductase family 1 member B1 (CHEMBL1900)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acids as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications.
Van Zandt MC, Doan B, Sawicki DR, Sredy J, Podjarny AD.
Bioorg Med Chem Lett (2009) 19 : 2006 -2008
PubMed 19250825 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.57 4.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL363387 LIDORESTAT 2.0 1 4.57
CHEMBL1235556 1 -
CHEMBL1780235 1 -
CHEMBL1780236 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL363387 LIDORESTAT IC50 = 27000.0 nM 4.57
CHEMBL1235556 IC50 > 100000.0 nM -
CHEMBL1780235 IC50 > 100000.0 nM -
CHEMBL1780236 IC50 > 100000.0 nM -