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Assay Detail

CHEMBL643096

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

Binding
Inhibitory activity against aldose reductase isolated from human placenta
29
Total Activities
29
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

Orally active aldose reductase inhibitors: indazoleacetic, oxopyridazineacetic, and oxopyridopyridazineacetic acid derivatives.
Mylari BL, Zembrowski WJ, Beyer TA, Aldinger CE, Siegel TW.
J Med Chem (1992) 35 : 2155 -2162
PubMed 1613743 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.39 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69956 1 8.68
CHEMBL71966 1 8.48
CHEMBL304995 1 8.40
CHEMBL73505 1 8.34
CHEMBL10372 ZOPOLRESTAT 2.0 1 8.32
CHEMBL73560 1 8.30
CHEMBL68580 1 8.28
CHEMBL69350 1 7.80
CHEMBL303210 1 7.75
CHEMBL21091 1 7.72
CHEMBL305064 1 7.58
CHEMBL308216 1 7.52
CHEMBL66006 1 7.50
CHEMBL306244 1 7.48
CHEMBL68705 1 7.46
CHEMBL309132 1 7.39
CHEMBL69537 1 7.34
CHEMBL67591 1 7.24
CHEMBL421487 1 7.19
CHEMBL69907 1 7.00
CHEMBL419254 1 6.96
CHEMBL68586 1 6.54
CHEMBL69183 1 6.47
CHEMBL67922 1 6.38
CHEMBL70247 1 6.17
CHEMBL69371 1 6.12
CHEMBL306222 1 5.21
CHEMBL66920 1 -
CHEMBL69591 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69956 IC50 = 2.1 nM 8.68
CHEMBL71966 IC50 = 3.3 nM 8.48
CHEMBL304995 IC50 = 4.0 nM 8.40
CHEMBL73505 IC50 = 4.6 nM 8.34
CHEMBL10372 ZOPOLRESTAT IC50 = 4.8 nM 8.32
CHEMBL73560 IC50 = 5.0 nM 8.30
CHEMBL68580 IC50 = 5.2 nM 8.28
CHEMBL69350 IC50 = 16.0 nM 7.80
CHEMBL303210 IC50 = 18.0 nM 7.75
CHEMBL21091 IC50 = 19.0 nM 7.72
CHEMBL305064 IC50 = 26.0 nM 7.58
CHEMBL308216 IC50 = 30.0 nM 7.52
CHEMBL66006 IC50 = 32.0 nM 7.50
CHEMBL306244 IC50 = 33.0 nM 7.48
CHEMBL68705 IC50 = 35.0 nM 7.46
CHEMBL309132 IC50 = 41.0 nM 7.39
CHEMBL69537 IC50 = 46.0 nM 7.34
CHEMBL67591 IC50 = 58.0 nM 7.24
CHEMBL421487 IC50 = 65.0 nM 7.19
CHEMBL69907 IC50 = 100.0 nM 7.00
CHEMBL419254 IC50 = 110.0 nM 6.96
CHEMBL68586 IC50 = 290.0 nM 6.54
CHEMBL69183 IC50 = 340.0 nM 6.47
CHEMBL67922 IC50 = 420.0 nM 6.38
CHEMBL70247 IC50 = 680.0 nM 6.17
CHEMBL69371 IC50 = 760.0 nM 6.12
CHEMBL306222 IC50 = 6200.0 nM 5.21
CHEMBL66920 IC50 < 10.0 nM -
CHEMBL69591 IC50 < 10.0 nM -