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Assay Detail

CHEMBL764859

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

Binding
Inhibition of human placental aldose reductase (HPAR) activity with glyceraldehyde as substrate
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Aldo-keto reductase family 1 member B1 (CHEMBL1900)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rotationally restricted mimics of rigid molecules: nonspirocyclic hydantoin aldose reductase inhibitors.
Rizzi JP, Schnur RC, Hutson NJ, Kraus KG, Kelbaugh PR.
J Med Chem (1989) 32 : 1208 -1213
PubMed 2498517 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.39 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19187 1 7.52
CHEMBL19427 1 7.30
CHEMBL19711 1 7.00
CHEMBL266497 SORBINIL 3.0 1 6.92
CHEMBL19744 1 6.89
CHEMBL279878 1 6.82
CHEMBL19495 1 6.75
CHEMBL19532 1 6.72
CHEMBL19316 1 6.66
CHEMBL274727 1 6.64
CHEMBL18854 1 6.64
CHEMBL443492 1 6.60
CHEMBL19502 1 6.57
CHEMBL19649 1 6.57
CHEMBL18865 1 6.42
CHEMBL19781 1 6.33
CHEMBL440790 1 6.24
CHEMBL429059 1 6.24
CHEMBL278584 1 6.21
CHEMBL19885 1 6.21
CHEMBL277427 1 6.21
CHEMBL19789 1 5.92
CHEMBL275868 1 5.90
CHEMBL278565 1 5.41
CHEMBL280357 1 5.35
CHEMBL19392 1 5.25
CHEMBL19746 1 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19187 IC50 = 30.0 nM 7.52
CHEMBL19427 IC50 = 50.0 nM 7.30
CHEMBL19711 IC50 = 100.0 nM 7.00
CHEMBL266497 SORBINIL IC50 = 120.0 nM 6.92
CHEMBL19744 IC50 = 130.0 nM 6.89
CHEMBL279878 IC50 = 150.0 nM 6.82
CHEMBL19495 IC50 = 180.0 nM 6.75
CHEMBL19532 IC50 = 190.0 nM 6.72
CHEMBL19316 IC50 = 220.0 nM 6.66
CHEMBL274727 IC50 = 230.0 nM 6.64
CHEMBL18854 IC50 = 230.0 nM 6.64
CHEMBL443492 IC50 = 250.0 nM 6.60
CHEMBL19502 IC50 = 270.0 nM 6.57
CHEMBL19649 IC50 = 270.0 nM 6.57
CHEMBL18865 IC50 = 380.0 nM 6.42
CHEMBL19781 IC50 = 470.0 nM 6.33
CHEMBL440790 IC50 = 580.0 nM 6.24
CHEMBL429059 IC50 = 580.0 nM 6.24
CHEMBL278584 IC50 = 620.0 nM 6.21
CHEMBL19885 IC50 = 610.0 nM 6.21
CHEMBL277427 IC50 = 610.0 nM 6.21
CHEMBL19789 IC50 = 1200.0 nM 5.92
CHEMBL275868 IC50 = 1260.0 nM 5.90
CHEMBL278565 IC50 = 3870.0 nM 5.41
CHEMBL280357 IC50 = 4470.0 nM 5.35
CHEMBL19392 IC50 = 5630.0 nM 5.25
CHEMBL19746 IC50 = 7470.0 nM 5.13