Assay Detail
Binding
CHEMBL880577
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitroy concentration against Aldose reductase incubated at 24 degree C for 15 minutes in pH 7.0
63
Total Activities
63
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 novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 63 | 6.83 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL240725 | — | — | 1 | 9.00 |
| CHEMBL198096 | — | — | 1 | 8.52 |
| CHEMBL10372 | ZOPOLRESTAT | 2.0 | 1 | 8.40 |
| CHEMBL370123 | — | — | 1 | 8.30 |
| CHEMBL440567 | — | — | 1 | 8.22 |
| CHEMBL198148 | — | — | 1 | 7.89 |
| CHEMBL197878 | — | — | 1 | 7.64 |
| CHEMBL240722 | — | — | 1 | 7.60 |
| CHEMBL371307 | — | — | 1 | 7.58 |
| CHEMBL425920 | — | — | 1 | 7.47 |
| CHEMBL197805 | — | — | 1 | 7.46 |
| CHEMBL446704 | — | — | 1 | 7.36 |
| CHEMBL372136 | — | — | 1 | 7.31 |
| CHEMBL197712 | — | — | 1 | 7.30 |
| CHEMBL372641 | — | — | 1 | 7.28 |
| CHEMBL198250 | — | — | 1 | 7.27 |
| CHEMBL371914 | — | — | 1 | 7.26 |
| CHEMBL198764 | — | — | 1 | 7.26 |
| CHEMBL371901 | — | — | 1 | 7.14 |
| CHEMBL433987 | — | — | 1 | 7.14 |
| CHEMBL239440 | — | — | 1 | 7.06 |
| CHEMBL372193 | — | — | 1 | 7.04 |
| CHEMBL373040 | — | — | 1 | 6.93 |
| CHEMBL307279 | — | — | 1 | 6.85 |
| CHEMBL266497 | SORBINIL | 3.0 | 1 | 6.85 |
| CHEMBL198331 | — | — | 1 | 6.85 |
| CHEMBL241777 | — | — | 1 | 6.82 |
| CHEMBL194582 | — | — | 1 | 6.82 |
| CHEMBL197841 | — | — | 1 | 6.80 |
| CHEMBL72699 | — | — | 1 | 6.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL240725 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL198096 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL10372 | ZOPOLRESTAT | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL370123 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL440567 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL198148 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL197878 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL240722 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL371307 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL425920 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL197805 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL446704 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL372136 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL197712 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL372641 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL198250 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL371914 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL198764 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL371901 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL433987 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL239440 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL372193 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL373040 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL198331 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL307279 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL266497 | SORBINIL | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL241777 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL194582 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL197841 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL72699 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL194905 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL73415 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL74183 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL199100 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL370444 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL74579 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL241570 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL197924 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL197806 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL73491 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL413566 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL372861 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL369911 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL425745 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL198004 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL199069 | — | IC50 | = | 422.0 | nM | 6.38 |
| CHEMBL73330 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL197678 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL425922 | — | IC50 | = | 474.0 | nM | 6.32 |
| CHEMBL197544 | — | IC50 | = | 500.0 | nM | 6.30 |