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Assay Detail

CHEMBL645594

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Binding
Inhibitory activity against aldose reductase enzyme
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Substituted pyrrol-1-ylacetic acids that combine aldose reductase enzyme inhibitory activity and ability to prevent the nonenzymatic irreversible modification of proteins from monosaccharides.
Nicolaou I, Demopoulos VJ.
J Med Chem (2003) 46 : 417 -426
PubMed 12540241 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.86 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10372 ZOPOLRESTAT 2.0 1 8.51
CHEMBL56337 EPALRESTAT 4.0 1 8.00
CHEMBL84446 FIDARESTAT 2.0 1 7.46
CHEMBL436 TOLRESTAT 4.0 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10372 ZOPOLRESTAT IC50 = 3.1 nM 8.51
CHEMBL56337 EPALRESTAT IC50 = 10.0 nM 8.00
CHEMBL84446 FIDARESTAT IC50 = 35.0 nM 7.46
CHEMBL436 TOLRESTAT IC50 = 35.0 nM 7.46