Assay Detail
Binding
CHEMBL643203
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory activity against aldose reductase in porcine lens.
47
Total Activities
47
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
Novel, highly potent aldose reductase inhibitors: (R)-(-)-2-(4-bromo-2-fluorobenzyl)-1,2,3,4- tetrahydropyrrolo[1,2-a]pyrazine -4-spiro-3'-pyrrolidine-1,2',3,5'-tetrone (AS-3201) and its congeners.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 47 | 7.00 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL334830 | RANIRESTAT | 3.0 | 1 | 7.82 |
| CHEMBL436 | TOLRESTAT | 4.0 | 1 | 7.82 |
| CHEMBL7679 | PONALRESTAT | 2.0 | 1 | 7.68 |
| CHEMBL133731 | — | — | 1 | 7.64 |
| CHEMBL443545 | — | — | 1 | 7.46 |
| CHEMBL133475 | — | — | 1 | 7.46 |
| CHEMBL132749 | — | — | 1 | 7.43 |
| CHEMBL335004 | — | — | 1 | 7.43 |
| CHEMBL334863 | — | — | 1 | 7.42 |
| CHEMBL335972 | — | — | 1 | 7.40 |
| CHEMBL134018 | — | — | 1 | 7.39 |
| CHEMBL132846 | — | — | 1 | 7.35 |
| CHEMBL337165 | — | — | 1 | 7.34 |
| CHEMBL334518 | — | — | 1 | 7.33 |
| CHEMBL341433 | — | — | 1 | 7.30 |
| CHEMBL335991 | — | — | 1 | 7.28 |
| CHEMBL130174 | — | — | 1 | 7.28 |
| CHEMBL409108 | — | — | 1 | 7.28 |
| CHEMBL422439 | — | — | 1 | 7.21 |
| CHEMBL435190 | — | — | 1 | 7.14 |
| CHEMBL130516 | — | — | 1 | 7.10 |
| CHEMBL336653 | — | — | 1 | 7.00 |
| CHEMBL335990 | — | — | 1 | 7.00 |
| CHEMBL337903 | — | — | 1 | 6.96 |
| CHEMBL133791 | — | — | 1 | 6.96 |
| CHEMBL134188 | — | — | 1 | 6.92 |
| CHEMBL135624 | — | — | 1 | 6.88 |
| CHEMBL133662 | — | — | 1 | 6.88 |
| CHEMBL131906 | — | — | 1 | 6.85 |
| CHEMBL134089 | — | — | 1 | 6.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL334830 | RANIRESTAT | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL436 | TOLRESTAT | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL7679 | PONALRESTAT | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL133731 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL443545 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL133475 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL132749 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL335004 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL334863 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL335972 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL134018 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL132846 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL337165 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL334518 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL341433 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL335991 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL409108 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL130174 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL422439 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL435190 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL130516 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL336653 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL335990 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL337903 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL133791 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL134188 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL135624 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL133662 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL131906 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL134089 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL335776 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL131730 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL130145 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL132245 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL131150 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL133721 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL337084 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL335447 | — | IC50 | = | 803.0 | nM | 6.09 |
| CHEMBL133737 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL335386 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL132069 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL337706 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL337464 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL337469 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL133123 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL132299 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL335079 | — | IC50 | > | 10000.0 | nM | - |