Assay Detail
Binding
CHEMBL893459
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Inhibition of PTP1B after 10 mins
14
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Tyrosine-protein phosphatase non-receptor type 1 (CHEMBL335) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Methylenedisalicylic acid derivatives: new PTP1B inhibitors that confer resistance to diet-induced obesity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 4.78 | 5.85 |
| Ki | 4 | 5.25 | 5.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL184041 | ERTIPROTAFIB | 2.0 | 2 | 5.85 |
| CHEMBL3706920 | — | — | 2 | 5.20 |
| CHEMBL228397 | — | — | 2 | 5.03 |
| CHEMBL139393 | — | — | 2 | 4.94 |
| CHEMBL3706921 | — | — | 1 | 4.41 |
| CHEMBL114043 | — | — | 1 | 4.11 |
| CHEMBL115145 | — | — | 1 | - |
| CHEMBL234734 | — | — | 1 | - |
| CHEMBL113835 | — | — | 1 | - |
| CHEMBL116347 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL184041 | ERTIPROTAFIB | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL184041 | ERTIPROTAFIB | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL3706920 | — | Ki | = | 6300.0 | nM | 5.20 |
| CHEMBL228397 | — | Ki | = | 9400.0 | nM | 5.03 |
| CHEMBL139393 | — | Ki | = | 11500.0 | nM | 4.94 |
| CHEMBL3706920 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL228397 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL3706921 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL114043 | — | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL139393 | — | IC50 | = | 500000.0 | nM | - |
| CHEMBL115145 | — | IC50 | = | 3600000.0 | nM | - |
| CHEMBL234734 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL113835 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL116347 | — | IC50 | = | 242000.0 | nM | - |