Assay Detail
Binding
CHEMBL899399
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Inhibition of PTP1B after 10 mins
17
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Tyrosine-protein phosphatase non-receptor type 1 (CHEMBL335) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
2-O-carboxymethylpyrogallol derivatives as PTP1B inhibitors with antihyperglycemic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.02 | 5.85 |
| Ki | 1 | 5.96 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL238138 | — | — | 2 | 5.96 |
| CHEMBL184041 | ERTIPROTAFIB | 2.0 | 1 | 5.85 |
| CHEMBL236216 | — | — | 1 | 5.66 |
| CHEMBL237915 | — | — | 1 | 5.30 |
| CHEMBL236636 | — | — | 1 | 5.27 |
| CHEMBL238137 | — | — | 1 | 5.24 |
| CHEMBL393866 | — | — | 1 | 4.89 |
| CHEMBL236215 | — | — | 1 | 4.77 |
| CHEMBL236846 | — | — | 1 | 4.40 |
| CHEMBL236009 | — | — | 1 | 4.14 |
| CHEMBL396634 | — | — | 1 | 4.03 |
| CHEMBL396633 | — | — | 1 | - |
| CHEMBL236214 | — | — | 1 | - |
| CHEMBL236008 | — | — | 1 | - |
| CHEMBL236007 | — | — | 1 | - |
| CHEMBL139393 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL238138 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL184041 | ERTIPROTAFIB | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL238138 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL236216 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL237915 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL236636 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL238137 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL393866 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL236215 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL236846 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL236009 | — | IC50 | = | 73000.0 | nM | 4.14 |
| CHEMBL396634 | — | IC50 | = | 93000.0 | nM | 4.03 |
| CHEMBL236214 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL236008 | — | IC50 | = | 300000.0 | nM | - |
| CHEMBL236007 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL396633 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL139393 | — | IC50 | = | 500000.0 | nM | - |