Assay Detail
Binding
CHEMBL5524535
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PTPN2 using DiFMUP as substrate by fluorescence based phosphatase assay
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Tyrosine-protein phosphatase non-receptor type 2 (CHEMBL3807) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity optimization of azepane-containing derivatives as PTPN2/PTPN1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.95 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5095164 | OSUNPROTAFIB | 2.0 | 1 | 8.66 |
| CHEMBL5564604 | — | — | 1 | 8.37 |
| CHEMBL5562964 | — | — | 1 | 8.35 |
| CHEMBL5557812 | — | — | 1 | 8.35 |
| CHEMBL5561163 | — | — | 2 | 8.30 |
| CHEMBL5559694 | — | — | 1 | 8.22 |
| CHEMBL5564299 | — | — | 1 | 8.04 |
| CHEMBL5559660 | — | — | 1 | 8.03 |
| CHEMBL5560433 | — | — | 1 | 8.01 |
| CHEMBL5567463 | — | — | 1 | 7.76 |
| CHEMBL5562456 | — | — | 1 | 7.71 |
| CHEMBL5561180 | — | — | 1 | 7.55 |
| CHEMBL5561290 | — | — | 1 | 7.12 |
| CHEMBL5561962 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5095164 | OSUNPROTAFIB | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5564604 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5562964 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL5557812 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL5561163 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5559694 | — | IC50 | = | 6.04 | nM | 8.22 |
| CHEMBL5564299 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL5559660 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL5560433 | — | IC50 | = | 9.73 | nM | 8.01 |
| CHEMBL5561163 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL5567463 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL5562456 | — | IC50 | = | 19.7 | nM | 7.71 |
| CHEMBL5561180 | — | IC50 | = | 28.1 | nM | 7.55 |
| CHEMBL5561290 | — | IC50 | = | 75.5 | nM | 7.12 |
| CHEMBL5561962 | — | IC50 | = | 100.0 | nM | 7.00 |