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Assay Detail

CHEMBL968446

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Binding
Inhibition of Wistar rat lens aldose reductase 2
8
Total Activities
8
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

Carboxymethylated pyridoindole antioxidants as aldose reductase inhibitors: Synthesis, activity, partitioning, and molecular modeling.
Stefek M, Snirc V, Djoubissie PO, Majekova M, Demopoulos V, Rackova L, Bezakova Z, Karasu C, Carbone V, El-Kabbani O.
Bioorg Med Chem (2008) 16 : 4908 -4920
PubMed 18395454 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.52 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10372 ZOPOLRESTAT 2.0 1 8.30
CHEMBL476908 1 4.78
CHEMBL477942 1 4.74
CHEMBL477933 1 4.27
CHEMBL303192 DEHYDROSTOBADINE 1 -
CHEMBL479176 STOBADINE 1 -
CHEMBL479175 1 -
CHEMBL479174 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10372 ZOPOLRESTAT IC50 = 5.0 nM 8.30
CHEMBL476908 IC50 = 16700.0 nM 4.78
CHEMBL477942 IC50 = 18200.0 nM 4.74
CHEMBL477933 IC50 = 54000.0 nM 4.27
CHEMBL303192 DEHYDROSTOBADINE IC50 > 1000000.0 nM -
CHEMBL479176 STOBADINE IC50 > 1000000.0 nM -
CHEMBL479175 IC50 = 266000.0 nM -
CHEMBL479174 IC50 = 380700.0 nM -