Assay Detail
Binding
CHEMBL5626709
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PROTAC activity at CRBN/BTK in human Ramos cells assessed as induction of BTK degradation incubated for 24 hrs by Western blot analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Ramos |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Protein cereblon/Tyrosine-protein kinase BTK (CHEMBL4523704) ↗| Type | PROTEIN-PROTEIN INTERACTION |
| Organism | Homo sapiens |
Publication
Discovery of Ibrutinib-based BTK PROTACs with in vivo anti-inflammatory efficacy by inhibiting NF-κB activation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 7.79 | 8.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5583871 | — | — | 1 | 8.50 |
| CHEMBL5631313 | — | — | 1 | 8.21 |
| CHEMBL5632777 | — | — | 1 | 8.14 |
| CHEMBL5631802 | — | — | 1 | 8.03 |
| CHEMBL5633727 | — | — | 1 | 7.57 |
| CHEMBL5633732 | — | — | 1 | 7.34 |
| CHEMBL5631854 | — | — | 1 | 7.29 |
| CHEMBL4441907 | — | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5583871 | — | EC50 | = | 3.18 | nM | 8.50 |
| CHEMBL5631313 | — | EC50 | = | 6.11 | nM | 8.21 |
| CHEMBL5632777 | — | EC50 | = | 7.27 | nM | 8.14 |
| CHEMBL5631802 | — | EC50 | = | 9.37 | nM | 8.03 |
| CHEMBL5633727 | — | EC50 | = | 26.87 | nM | 7.57 |
| CHEMBL5633732 | — | EC50 | = | 46.1 | nM | 7.34 |
| CHEMBL5631854 | — | EC50 | = | 51.1 | nM | 7.29 |
| CHEMBL4441907 | — | EC50 | = | 63.31 | nM | 7.20 |