Assay Detail
Binding
CHEMBL832655
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of recombinant human aldose reductase expressed in Escherichia coli
41
Total Activities
41
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
Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 7.57 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL363387 | LIDORESTAT | 2.0 | 1 | 8.30 |
| CHEMBL190931 | — | — | 1 | 8.30 |
| CHEMBL192886 | — | — | 1 | 8.22 |
| CHEMBL371991 | — | — | 1 | 8.15 |
| CHEMBL192167 | — | — | 1 | 8.15 |
| CHEMBL371162 | — | — | 1 | 8.10 |
| CHEMBL192255 | — | — | 1 | 8.10 |
| CHEMBL191508 | — | — | 1 | 8.10 |
| CHEMBL370478 | — | — | 1 | 8.10 |
| CHEMBL364235 | — | — | 1 | 8.10 |
| CHEMBL193155 | — | — | 1 | 8.10 |
| CHEMBL10413 | ZENARESTAT | 2.0 | 1 | 8.10 |
| CHEMBL193569 | — | — | 1 | 8.05 |
| CHEMBL189801 | — | — | 1 | 8.05 |
| CHEMBL10372 | ZOPOLRESTAT | 2.0 | 1 | 8.05 |
| CHEMBL192927 | — | — | 1 | 8.00 |
| CHEMBL192263 | — | — | 1 | 8.00 |
| CHEMBL193277 | — | — | 1 | 7.96 |
| CHEMBL193254 | — | — | 1 | 7.96 |
| CHEMBL192399 | — | — | 1 | 7.92 |
| CHEMBL192434 | — | — | 1 | 7.89 |
| CHEMBL436 | TOLRESTAT | 4.0 | 1 | 7.89 |
| CHEMBL193030 | — | — | 1 | 7.85 |
| CHEMBL192762 | — | — | 1 | 7.82 |
| CHEMBL193839 | — | — | 1 | 7.77 |
| CHEMBL195065 | — | — | 1 | 7.60 |
| CHEMBL363850 | — | — | 1 | 7.52 |
| CHEMBL372902 | — | — | 1 | 7.47 |
| CHEMBL192182 | — | — | 1 | 7.28 |
| CHEMBL191570 | — | — | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL363387 | LIDORESTAT | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL190931 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL192886 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL371991 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL192167 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL10413 | ZENARESTAT | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL193155 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL364235 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL370478 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL191508 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL192255 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL371162 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL193569 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL189801 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL10372 | ZOPOLRESTAT | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL192927 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL192263 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL193277 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL193254 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL192399 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL192434 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL436 | TOLRESTAT | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL193030 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL192762 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL193839 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL195065 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL363850 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL372902 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL192182 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL191570 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL364313 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL192453 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL364699 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL410917 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL371122 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL193307 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL191951 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL192213 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL192534 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL193570 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL193566 | — | IC50 | = | 1600.0 | nM | 5.80 |