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Assay Detail

CHEMBL968427

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

Binding
Inhibition of aldose reductase in rat lenses
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aldo-keto reductase family 1 member B1 (CHEMBL2622)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design and synthesis of N-(3,5-difluoro-4-hydroxyphenyl)benzenesulfonamides as aldose reductase inhibitors.
Alexiou P, Nicolaou I, Stefek M, Kristl A, Demopoulos VJ.
Bioorg Med Chem (2008) 16 : 3926 -3932
PubMed 18267362 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.81 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL266497 SORBINIL 3.0 1 6.60
CHEMBL507525 1 4.85
CHEMBL458588 1 4.81
CHEMBL285053 1 4.80
CHEMBL444802 1 4.51
CHEMBL458568 1 4.48
CHEMBL457486 1 4.35
CHEMBL288404 1 4.10
CHEMBL37054 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL266497 SORBINIL IC50 = 249.0 nM 6.60
CHEMBL507525 IC50 = 14100.0 nM 4.85
CHEMBL458588 IC50 = 15500.0 nM 4.81
CHEMBL285053 IC50 = 16000.0 nM 4.80
CHEMBL444802 IC50 = 31000.0 nM 4.51
CHEMBL458568 IC50 = 32900.0 nM 4.48
CHEMBL457486 IC50 = 44400.0 nM 4.35
CHEMBL288404 IC50 = 79000.0 nM 4.10
CHEMBL37054 IC50 = 134000.0 nM -