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Assay Detail

CHEMBL1286654

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

Binding
Inhibition of Fischer-344 rat lens ALR2 by least-square analysis
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Lens of camera-type eye
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

A diverse series of substituted benzenesulfonamides as aldose reductase inhibitors with antioxidant activity: design, synthesis, and in vitro activity.
Alexiou P, Demopoulos VJ.
J Med Chem (2010) 53 : 7756 -7766
PubMed 20936791 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 4.71 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1277476 1 6.40
CHEMBL1277386 1 5.24
CHEMBL1277203 1 5.10
CHEMBL1277387 1 5.05
CHEMBL1277297 1 4.92
CHEMBL507525 1 4.85
CHEMBL458588 1 4.81
CHEMBL1277477 1 4.55
CHEMBL458568 1 4.48
CHEMBL1277298 1 4.42
CHEMBL457486 1 4.35
CHEMBL1277202 1 4.24
CHEMBL1275967 1 4.15
CHEMBL37054 1 4.06
CHEMBL1277113 1 4.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1277476 IC50 = 397.0 nM 6.40
CHEMBL1277386 IC50 = 5700.0 nM 5.24
CHEMBL1277203 IC50 = 7900.0 nM 5.10
CHEMBL1277387 IC50 = 9000.0 nM 5.05
CHEMBL1277297 IC50 = 12000.0 nM 4.92
CHEMBL507525 IC50 = 14100.0 nM 4.85
CHEMBL458588 IC50 = 15500.0 nM 4.81
CHEMBL1277477 IC50 = 28100.0 nM 4.55
CHEMBL458568 IC50 = 32900.0 nM 4.48
CHEMBL1277298 IC50 = 37800.0 nM 4.42
CHEMBL457486 IC50 = 44400.0 nM 4.35
CHEMBL1277202 IC50 = 57100.0 nM 4.24
CHEMBL1275967 IC50 = 71200.0 nM 4.15
CHEMBL37054 IC50 = 86700.0 nM 4.06
CHEMBL1277113 IC50 = 91500.0 nM 4.04