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Assay Detail

CHEMBL649695

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

Binding
Inhibition of bovine lens aldose reductase with DL-glyceraldehyde as substrate
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

N-[5-(trifluoromethyl)-6-methoxy-1-naphthalenyl]thioxomethyl]- N-methylglycine (Tolrestat), a potent, orally active aldose reductase inhibitor.
Sestanj K, Bellini F, Fung S, Abraham N, Treasurywala A, Humber L, Simard-Duquesne N, Dvornik D.
J Med Chem (1984) 27 : 255 -256
PubMed 6422042 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.28 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL436 TOLRESTAT 4.0 1 7.46
CHEMBL266497 SORBINIL 3.0 1 5.82
CHEMBL63055 ALRESTATIN 2.0 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL436 TOLRESTAT IC50 = 35.0 nM 7.46
CHEMBL266497 SORBINIL IC50 = 1500.0 nM 5.82
CHEMBL63055 ALRESTATIN IC50 = 2700.0 nM 5.57