Assay Detail
Binding
CHEMBL821471
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Inhibition of human recombinant Aldose reductase in streptozotocin diabetic rat
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Aldo-keto reductase family 1 member B1 (CHEMBL1900) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.69 | 9.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL240725 | — | — | 1 | 9.08 |
| CHEMBL10372 | ZOPOLRESTAT | 2.0 | 1 | 8.40 |
| CHEMBL241777 | — | — | 1 | 7.60 |
| CHEMBL307279 | — | — | 1 | 6.85 |
| CHEMBL73415 | — | — | 1 | 6.82 |
| CHEMBL72699 | — | — | 1 | 6.77 |
| CHEMBL74183 | — | — | 1 | 6.72 |
| CHEMBL74579 | — | — | 1 | 6.68 |
| CHEMBL73491 | — | — | 1 | 6.55 |
| CHEMBL73330 | — | — | 1 | 6.35 |
| CHEMBL74814 | — | — | 1 | 6.22 |
| CHEMBL72368 | — | — | 1 | 5.72 |
| CHEMBL74785 | — | — | 1 | 5.70 |
| CHEMBL72752 | — | — | 1 | 5.66 |
| CHEMBL72278 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL240725 | — | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL10372 | ZOPOLRESTAT | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL241777 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL307279 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL73415 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL72699 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL74183 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL74579 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL73491 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL73330 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL74814 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL72368 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL74785 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL72752 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL72278 | — | IC50 | = | 5000.0 | nM | 5.30 |