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Assay Detail

CHEMBL3424959

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

Binding
Inhibition of Wistar rat kidney aldehyde reductase using D-glucuronate as substrate by spectrophotometry
12
Total Activities
12
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 B7 (CHEMBL3421523)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Identification of novel aldose reductase inhibitors based on carboxymethylated mercaptotriazinoindole scaffold.
Stefek M, Soltesova Prnova M, Majekova M, Rechlin C, Heine A, Klebe G.
J Med Chem (2015) 58 : 2649 -2657
PubMed 25695864 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.86 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10372 ZOPOLRESTAT 2.0 1 7.31
CHEMBL3422326 1 5.32
CHEMBL3422329 1 4.85
CHEMBL3422332 1 4.71
CHEMBL1984484 1 4.61
CHEMBL1405739 1 4.39
CHEMBL109 VALPROIC ACID 4.0 1 4.25
CHEMBL1337856 1 4.17
CHEMBL1333950 1 4.10
CHEMBL56337 EPALRESTAT 4.0 1 -
CHEMBL3422334 1 -
CHEMBL3422333 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10372 ZOPOLRESTAT IC50 = 49.0 nM 7.31
CHEMBL3422326 IC50 = 4820.0 nM 5.32
CHEMBL3422329 IC50 = 14130.0 nM 4.85
CHEMBL3422332 IC50 = 19560.0 nM 4.71
CHEMBL1984484 IC50 = 24790.0 nM 4.61
CHEMBL1405739 IC50 = 40550.0 nM 4.39
CHEMBL109 VALPROIC ACID IC50 = 56100.0 nM 4.25
CHEMBL1337856 IC50 = 68440.0 nM 4.17
CHEMBL1333950 IC50 = 80160.0 nM 4.10
CHEMBL56337 EPALRESTAT IC50 - -
CHEMBL3422334 IC50 - -
CHEMBL3422333 IC50 - -