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Assay Detail

CHEMBL821471

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

Binding
Inhibition of human recombinant Aldose reductase in streptozotocin diabetic rat
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one.
Mylari BL, Armento SJ, Beebe DA, Conn EL, Coutcher JB, Dina MS, O'Gorman MT, Linhares MC, Martin WH, Oates PJ, Tess DA, Withbroe GJ, Zembrowski WJ.
J Med Chem (2003) 46 : 2283 -2286
PubMed 12773033 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.69 9.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL240725 1 9.08
CHEMBL10372 ZOPOLRESTAT 2.0 1 8.40
CHEMBL241777 1 7.60
CHEMBL307279 1 6.85
CHEMBL73415 1 6.82
CHEMBL72699 1 6.77
CHEMBL74183 1 6.72
CHEMBL74579 1 6.68
CHEMBL73491 1 6.55
CHEMBL73330 1 6.35
CHEMBL74814 1 6.22
CHEMBL72368 1 5.72
CHEMBL74785 1 5.70
CHEMBL72752 1 5.66
CHEMBL72278 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL240725 IC50 = 0.84 nM 9.08
CHEMBL10372 ZOPOLRESTAT IC50 = 4.0 nM 8.40
CHEMBL241777 IC50 = 25.0 nM 7.60
CHEMBL307279 IC50 = 140.0 nM 6.85
CHEMBL73415 IC50 = 150.0 nM 6.82
CHEMBL72699 IC50 = 170.0 nM 6.77
CHEMBL74183 IC50 = 190.0 nM 6.72
CHEMBL74579 IC50 = 210.0 nM 6.68
CHEMBL73491 IC50 = 280.0 nM 6.55
CHEMBL73330 IC50 = 450.0 nM 6.35
CHEMBL74814 IC50 = 600.0 nM 6.22
CHEMBL72368 IC50 = 1900.0 nM 5.72
CHEMBL74785 IC50 = 2000.0 nM 5.70
CHEMBL72752 IC50 = 2200.0 nM 5.66
CHEMBL72278 IC50 = 5000.0 nM 5.30