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Assay Detail

CHEMBL644880

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

Binding
In vitro inhibitory activity against aldehyde reductase 1 (ALR1) from rat kidney.
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Aldo-keto reductase family 1 member A1 (CHEMBL3871)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel, highly potent aldose reductase inhibitors: cyano(2-oxo-2,3-dihydroindol-3-yl)acetic acid derivatives.
Da Settimo F, Primofiore G, Da Settimo A, La Motta C, Simorini F, Novellino E, Greco G, Lavecchia A, Boldrini E.
J Med Chem (2003) 46 : 1419 -1428
PubMed 12672241 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.04 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL266497 SORBINIL 3.0 1 7.54
CHEMBL33835 1 6.31
CHEMBL30993 1 6.16
CHEMBL50 QUERCETIN 3.0 1 5.63
CHEMBL281442 1 5.45
CHEMBL284593 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL266497 SORBINIL IC50 = 29.0 nM 7.54
CHEMBL33835 IC50 = 490.0 nM 6.31
CHEMBL30993 IC50 = 690.0 nM 6.16
CHEMBL50 QUERCETIN IC50 = 2320.0 nM 5.63
CHEMBL281442 IC50 = 3570.0 nM 5.45
CHEMBL284593 IC50 = 6790.0 nM 5.17