Assay Detail
Functional
CHEMBL5322835
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Antiproliferative activity against mouse BaF3 cells expressing BTK C481S mutant assessed as inhibition of cell growth measured after 3 days by CCK-8 assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | BaF3 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of novel BTK PROTACs with improved metabolic stability via linker rigidification strategy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.22 | 7.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5403933 | — | — | 1 | 7.07 |
| CHEMBL4756476 | NEMTABRUTINIB | 3.0 | 1 | 6.26 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 5.81 |
| CHEMBL5071105 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5403933 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4756476 | NEMTABRUTINIB | IC50 | = | 547.9 | nM | 6.26 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 1546.0 | nM | 5.81 |
| CHEMBL5071105 | — | IC50 | = | 1760.0 | nM | 5.75 |