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Assay Detail

CHEMBL4672512

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

Binding
Inhibition of rat lens ALR2 using D,L-glyceraldehyde as substrate preincubated for 5 mins at 30 degC followed by substrate addition and measured after 4 mins in presence of NADPH
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Lens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Dihydrobenzoxazinone derivatives as aldose reductase inhibitors with antioxidant activity.
Chen H,Zhang X,Zhang X,Fan Z,Liu W,Lei Y,Zhu C,Ma B
Bioorg Med Chem (2020) 28 : 115699 -115699
PubMed 33069078 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.52 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56337 EPALRESTAT 4.0 1 7.35
CHEMBL4764862 1 7.09
CHEMBL4744605 1 6.86
CHEMBL4762576 1 6.78
CHEMBL4755765 1 6.77
CHEMBL4759527 1 6.73
CHEMBL4761601 1 6.68
CHEMBL4758298 1 6.66
CHEMBL4789112 1 6.58
CHEMBL4747536 1 6.55
CHEMBL4796974 1 6.51
CHEMBL4740716 1 6.11
CHEMBL4761076 1 5.98
CHEMBL4758428 1 5.71
CHEMBL4745147 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56337 EPALRESTAT IC50 = 45.0 nM 7.35
CHEMBL4764862 IC50 = 82.0 nM 7.09
CHEMBL4744605 IC50 = 138.0 nM 6.86
CHEMBL4762576 IC50 = 167.0 nM 6.78
CHEMBL4755765 IC50 = 170.0 nM 6.77
CHEMBL4759527 IC50 = 188.0 nM 6.73
CHEMBL4761601 IC50 = 208.0 nM 6.68
CHEMBL4758298 IC50 = 220.0 nM 6.66
CHEMBL4789112 IC50 = 262.0 nM 6.58
CHEMBL4747536 IC50 = 281.0 nM 6.55
CHEMBL4796974 IC50 = 308.0 nM 6.51
CHEMBL4740716 IC50 = 774.0 nM 6.11
CHEMBL4761076 IC50 = 1050.0 nM 5.98
CHEMBL4758428 IC50 = 1932.0 nM 5.71
CHEMBL4745147 IC50 = 3340.0 nM 5.48