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Assay Detail

CHEMBL783705

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

Functional
Inhibition of galactitol accumulation in rat RBC incubated in presence of 50 mM glucose
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Syntheses of tolrestat analogues containing additional substituents in the ring and their evaluation as aldose reductase inhibitors. Identification of potent, orally active 2-fluoro derivatives.
Wrobel J, Millen J, Sredy J, Dietrich A, Gorham BJ, Malamas M, Kelly JM, Bauman JG, Harrison MC, Jones LR.
J Med Chem (1991) 34 : 2504 -2520
PubMed 1908522 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.82 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL436 TOLRESTAT 4.0 1 7.82
CHEMBL84152 1 7.72
CHEMBL84767 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL436 TOLRESTAT IC50 = 15.0 nM 7.82
CHEMBL84152 IC50 = 19.0 nM 7.72
CHEMBL84767 IC50 = 12000.0 nM 4.92