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Assay Detail

CHEMBL644305

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

Binding
In vitro inhibition of Aldose reductase (AR) from rat lens (RL)
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

Spiro[fluoreneisothiazolidin]one dioxides: new aldose reductase and L-hexonate dehydrogenase inhibitors.
DuPriest MT, Griffin BW, Kuzmich D, McNatt LG.
J Med Chem (1991) 34 : 3229 -3234
PubMed 1956041 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.40 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL436 TOLRESTAT 4.0 1 8.70
CHEMBL418832 1 8.30
CHEMBL269455 IMIRESTAT 2.0 1 8.05
CHEMBL327139 1 7.75
CHEMBL7679 PONALRESTAT 2.0 1 7.70
CHEMBL266497 SORBINIL 3.0 1 7.00
CHEMBL324907 1 6.77
CHEMBL326920 1 6.63
CHEMBL325136 1 5.72
CHEMBL109865 1 -
CHEMBL322815 1 -
CHEMBL110661 1 -
CHEMBL325596 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL436 TOLRESTAT IC50 = 2.0 nM 8.70
CHEMBL418832 IC50 = 5.0 nM 8.30
CHEMBL269455 IMIRESTAT IC50 = 9.0 nM 8.05
CHEMBL327139 IC50 = 18.0 nM 7.75
CHEMBL7679 PONALRESTAT IC50 = 20.0 nM 7.70
CHEMBL266497 SORBINIL IC50 = 100.0 nM 7.00
CHEMBL324907 IC50 = 169.0 nM 6.77
CHEMBL326920 IC50 = 233.0 nM 6.63
CHEMBL325136 IC50 = 1900.0 nM 5.72
CHEMBL109865 IC50 = 6150000.0 nM -
CHEMBL322815 IC50 > 10000000.0 nM -
CHEMBL110661 IC50 > 10000000.0 nM -
CHEMBL325596 IC50 = 2370000.0 nM -