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Assay Detail

CHEMBL1072267

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

Binding
Inhibition of rat kidney aldehyde reductase at 0.1 mM after 20 mins by spectrometric analysis
9
Total Activities
9
Compounds Tested
2
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 A1 (CHEMBL3871)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design and synthesis of novel series of pyrrole based chemotypes and their evaluation as selective aldose reductase inhibitors. A case of bioisosterism between a carboxylic acid moiety and that of a tetrazole.
Pegklidou K, Koukoulitsa C, Nicolaou I, Demopoulos VJ.
Bioorg Med Chem (2010) 18 : 2107 -2114
PubMed 20189816 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 8 - -
IC50 1 4.30 4.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL109 VALPROIC ACID 4.0 1 4.30
CHEMBL602309 1 -
CHEMBL590016 1 -
CHEMBL592208 1 -
CHEMBL589792 1 -
CHEMBL590017 1 -
CHEMBL590230 1 -
CHEMBL602310 1 -
CHEMBL93723 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL109 VALPROIC ACID IC50 = 50100.0 nM 4.30
CHEMBL602309 Inhibition = 20.0 % -
CHEMBL590016 Inhibition = 22.0 % -
CHEMBL592208 Inhibition = 23.0 % -
CHEMBL589792 Inhibition = 41.0 % -
CHEMBL590017 Inhibition = 35.0 % -
CHEMBL590230 Inhibition = 18.0 % -
CHEMBL602310 Inhibition = 18.0 % -
CHEMBL93723 Inhibition = 34.0 % -