Assay Detail
Binding
CHEMBL5508745
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of USP2 (267 to 599 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells using ubiquitin-rhodamine-110 as substrate preincubated with compound for 30 mins followed by substrate addition measured after 30 mins by fluorometric assay
24
Total Activities
24
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
Ubiquitin carboxyl-terminal hydrolase 2 (CHEMBL1293227) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The discovery of potent USP2/USP8 dual-target inhibitors for the treatment of breast cancer via structure guided optimization of ML364.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.35 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5561761 | — | — | 1 | 6.10 |
| CHEMBL5523555 | — | — | 1 | 6.05 |
| CHEMBL5523445 | — | — | 1 | 5.89 |
| CHEMBL5560776 | — | — | 1 | 5.85 |
| CHEMBL5562321 | — | — | 1 | 5.82 |
| CHEMBL5542690 | — | — | 1 | 5.80 |
| CHEMBL5562765 | — | — | 1 | 5.50 |
| CHEMBL5532378 | — | — | 1 | 5.48 |
| CHEMBL5560773 | — | — | 1 | 5.47 |
| CHEMBL3392741 | — | — | 1 | 5.44 |
| CHEMBL5557100 | — | — | 1 | 5.42 |
| CHEMBL5557814 | — | — | 1 | 5.36 |
| CHEMBL5562196 | — | — | 1 | 5.34 |
| CHEMBL5566850 | — | — | 1 | 5.26 |
| CHEMBL5559526 | — | — | 1 | 5.26 |
| CHEMBL5565871 | — | — | 1 | 5.23 |
| CHEMBL5559268 | — | — | 1 | 5.19 |
| CHEMBL5562787 | — | — | 1 | 4.98 |
| CHEMBL5523454 | — | — | 1 | 4.88 |
| CHEMBL5560170 | — | — | 1 | 4.84 |
| CHEMBL5558678 | — | — | 1 | 4.81 |
| CHEMBL5523517 | — | — | 1 | 4.65 |
| CHEMBL5568379 | — | — | 1 | 4.54 |
| CHEMBL5562286 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5561761 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL5523555 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL5523445 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5560776 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL5562321 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL5542690 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL5562765 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5532378 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL5560773 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3392741 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL5557100 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL5557814 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL5562196 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL5566850 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL5559526 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL5565871 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL5559268 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL5562787 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL5523454 | — | IC50 | = | 13300.0 | nM | 4.88 |
| CHEMBL5560170 | — | IC50 | = | 14500.0 | nM | 4.84 |
| CHEMBL5558678 | — | IC50 | = | 15400.0 | nM | 4.81 |
| CHEMBL5523517 | — | IC50 | = | 22300.0 | nM | 4.65 |
| CHEMBL5568379 | — | IC50 | = | 29100.0 | nM | 4.54 |
| CHEMBL5562286 | — | IC50 | > | 100000.0 | nM | - |