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Assay Detail

CHEMBL643204

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

Binding
Inhibitory concentration against porcine lens aldose reductase (AR) with DL-glyceraldehyde as the substrate
22
Total Activities
22
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 (CHEMBL4559)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Benzothiazol-2-ylcarboxylic acids with diverse spacers: A novel class of potent, orally active aldose reductase inhibitors
Aotsuka T, Abe N, Fukushima K, Ashizawa N, Yoshida M
Bioorg Med Chem Lett (1997) 7 : 1677 -1682
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.91 8.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL44717 1 8.18
CHEMBL288748 1 8.15
CHEMBL44780 1 8.08
CHEMBL44743 1 8.08
CHEMBL47614 1 8.06
CHEMBL45074 1 8.06
CHEMBL45751 1 8.03
CHEMBL46074 1 8.03
CHEMBL47646 1 8.02
CHEMBL46170 1 8.02
CHEMBL43995 1 8.01
CHEMBL442690 1 7.96
CHEMBL45290 1 7.96
CHEMBL542104 1 7.92
CHEMBL10413 ZENARESTAT 2.0 1 7.92
CHEMBL296769 1 7.89
CHEMBL436 TOLRESTAT 4.0 1 7.80
CHEMBL297861 1 7.72
CHEMBL45352 1 7.68
CHEMBL44941 1 7.64
CHEMBL296780 1 7.42
CHEMBL431145 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL44717 IC50 = 6.6 nM 8.18
CHEMBL288748 IC50 = 7.0 nM 8.15
CHEMBL44780 IC50 = 8.4 nM 8.08
CHEMBL44743 IC50 = 8.3 nM 8.08
CHEMBL47614 IC50 = 8.8 nM 8.06
CHEMBL45074 IC50 = 8.7 nM 8.06
CHEMBL45751 IC50 = 9.3 nM 8.03
CHEMBL46074 IC50 = 9.4 nM 8.03
CHEMBL47646 IC50 = 9.5 nM 8.02
CHEMBL46170 IC50 = 9.6 nM 8.02
CHEMBL43995 IC50 = 9.7 nM 8.01
CHEMBL442690 IC50 = 11.0 nM 7.96
CHEMBL45290 IC50 = 11.0 nM 7.96
CHEMBL542104 IC50 = 12.0 nM 7.92
CHEMBL10413 ZENARESTAT IC50 = 12.0 nM 7.92
CHEMBL296769 IC50 = 13.0 nM 7.89
CHEMBL436 TOLRESTAT IC50 = 16.0 nM 7.80
CHEMBL297861 IC50 = 19.0 nM 7.72
CHEMBL45352 IC50 = 21.0 nM 7.68
CHEMBL44941 IC50 = 23.0 nM 7.64
CHEMBL296780 IC50 = 38.0 nM 7.42
CHEMBL431145 IC50 = 50.0 nM 7.30