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Assay Detail

CHEMBL4380030

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

Binding
Inhibition of rat kidney ALR1 using sodium D-glucuronate as substrate incubated for 1 min and measured up to 4 mins using H2O-dissolved compound by spectrophotometric analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 5 4.58 4.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4566195 1 4.70
CHEMBL1405739 1 4.46
CHEMBL4582264 1 -
CHEMBL4541343 1 -
CHEMBL4462469 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4566195 IC50 = 20200.0 nM 4.70
CHEMBL1405739 IC50 = 35000.0 nM 4.46
CHEMBL4582264 IC50 > 100000.0 nM -
CHEMBL4541343 IC50 > 100000.0 nM -
CHEMBL4462469 IC50 > 100000.0 nM -