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Assay Detail

CHEMBL643668

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Binding
Inhibitory activity against rat lens aldose reductase(AR).
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Aldo-keto reductase family 1 member B1 (CHEMBL2622)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Highly selective aldose reductase inhibitors. 3. Structural diversity of 3-(arylmethyl)-2,4,5-trioxoimidazolidine-1-acetic acids.
Kotani T, Nagaki Y, Ishii A, Konishi Y, Yago H, Suehiro S, Okukado N, Okamoto K.
J Med Chem (1997) 40 : 684 -694
PubMed 9057855 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.66 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL159820 1 8.24
CHEMBL162697 1 7.96
CHEMBL161043 1 7.92
CHEMBL159413 1 7.82
CHEMBL355148 1 7.80
CHEMBL56337 EPALRESTAT 4.0 1 7.68
CHEMBL349508 1 7.62
CHEMBL434076 1 7.60
CHEMBL161556 1 7.60
CHEMBL433898 1 7.50
CHEMBL160032 1 7.47
CHEMBL292887 1 7.21
CHEMBL159384 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL159820 IC50 = 5.7 nM 8.24
CHEMBL162697 IC50 = 11.0 nM 7.96
CHEMBL161043 IC50 = 12.0 nM 7.92
CHEMBL159413 IC50 = 15.0 nM 7.82
CHEMBL355148 IC50 = 16.0 nM 7.80
CHEMBL56337 EPALRESTAT IC50 = 21.0 nM 7.68
CHEMBL349508 IC50 = 24.0 nM 7.62
CHEMBL434076 IC50 = 25.0 nM 7.60
CHEMBL161556 IC50 = 25.0 nM 7.60
CHEMBL433898 IC50 = 32.0 nM 7.50
CHEMBL160032 IC50 = 34.0 nM 7.47
CHEMBL292887 IC50 = 62.0 nM 7.21
CHEMBL159384 IC50 = 62.0 nM 7.21