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Assay Detail

CHEMBL642970

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Binding
Compound was tested for inhibitory concentration against rat lens aldose reductase (uncompetitive inhibition type)
11
Total Activities
11
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 (CHEMBL2622)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and rat lens aldose reductase inhibitory activity of some benzopyran-2-ones.
Brubaker AN, DeRuiter J, Whitmer WL.
J Med Chem (1986) 29 : 1094 -1099
PubMed 3086557 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.01 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL266497 SORBINIL 3.0 1 7.77
CHEMBL12655 1 7.70
CHEMBL268279 1 6.85
CHEMBL12281 1 6.62
CHEMBL268492 1 6.25
CHEMBL274190 1 6.22
CHEMBL12580 1 5.36
CHEMBL276618 4-METHYLDAPHNETIN 1 5.00
CHEMBL12241 1 5.00
CHEMBL12567 1 4.96
CHEMBL275000 1 4.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL266497 SORBINIL IC50 = 17.0 nM 7.77
CHEMBL12655 IC50 = 20.0 nM 7.70
CHEMBL268279 IC50 = 140.0 nM 6.85
CHEMBL12281 IC50 = 240.0 nM 6.62
CHEMBL268492 IC50 = 560.0 nM 6.25
CHEMBL274190 IC50 = 600.0 nM 6.22
CHEMBL12580 IC50 = 4400.0 nM 5.36
CHEMBL276618 4-METHYLDAPHNETIN IC50 = 10000.0 nM 5.00
CHEMBL12241 IC50 = 10000.0 nM 5.00
CHEMBL12567 IC50 = 11000.0 nM 4.96
CHEMBL275000 IC50 = 38000.0 nM 4.42