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Assay Detail

CHEMBL1799477

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

Binding
Inhibition of bovine lens ALR2
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Tissue Lens of camera-type eye
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aldo-keto reductase family 1 member B1 (CHEMBL3081)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Identification of 5-arylidene-4-thiazolidinone derivatives endowed with dual activity as aldose reductase inhibitors and antioxidant agents for the treatment of diabetic complications.
Ottanà R, Maccari R, Giglio M, Del Corso A, Cappiello M, Mura U, Cosconati S, Marinelli L, Novellino E, Sartini S, La Motta C, Da Settimo F.
Eur J Med Chem (2011) 46 : 2797 -2806
PubMed 21531055 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.13 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1645381 1 7.16
CHEMBL56337 EPALRESTAT 4.0 1 6.77
CHEMBL1796882 1 6.60
CHEMBL1796755 1 6.57
CHEMBL1796887 1 6.52
CHEMBL1796881 1 6.46
CHEMBL1796886 1 6.07
CHEMBL1796885 1 5.98
CHEMBL1796883 1 5.90
CHEMBL1796884 1 5.88
CHEMBL266497 SORBINIL 3.0 1 5.70
CHEMBL1796890 1 5.57
CHEMBL1796888 1 5.36
CHEMBL1796889 1 5.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1645381 IC50 = 70.0 nM 7.16
CHEMBL56337 EPALRESTAT IC50 = 170.0 nM 6.77
CHEMBL1796882 IC50 = 250.0 nM 6.60
CHEMBL1796755 IC50 = 270.0 nM 6.57
CHEMBL1796887 IC50 = 300.0 nM 6.52
CHEMBL1796881 IC50 = 350.0 nM 6.46
CHEMBL1796886 IC50 = 850.0 nM 6.07
CHEMBL1796885 IC50 = 1050.0 nM 5.98
CHEMBL1796883 IC50 = 1250.0 nM 5.90
CHEMBL1796884 IC50 = 1320.0 nM 5.88
CHEMBL266497 SORBINIL IC50 = 2000.0 nM 5.70
CHEMBL1796890 IC50 = 2700.0 nM 5.57
CHEMBL1796888 IC50 = 4400.0 nM 5.36
CHEMBL1796889 IC50 = 4900.0 nM 5.31