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Assay Detail

CHEMBL4380036

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

Binding
Inhibition of rat lens ALR2 using methylglyoxal as substrate incubated for 1 min and measured up to 4 mins by spectrophotometric analysis
2
Total Activities
2
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

Development of Novel Oxotriazinoindole Inhibitors of Aldose Reductase: Isosteric Sulfur/Oxygen Replacement in the Thioxotriazinoindole Cemtirestat Markedly Improved Inhibition Selectivity.
Hlaváč M, Kováčiková L, Prnová MŠ, Šramel P, Addová G, Májeková M, Hanquet G, Boháč A, Štefek M.
J Med Chem (2020) 63 : 369 -381
PubMed 31820975 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.12 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4582264 1 7.40
CHEMBL1405739 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4582264 IC50 = 40.0 nM 7.40
CHEMBL1405739 IC50 = 146.0 nM 6.84