Assay Detail
Binding
CHEMBL5127254
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK (unknown origin)
8
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.53 | 9.30 |
| Ki | 1 | 9.05 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5193128 | — | — | 1 | 9.30 |
| CHEMBL4065122 | FENEBRUTINIB | 3.0 | 1 | 9.05 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 8.82 |
| CHEMBL5169992 | — | — | 1 | 8.49 |
| CHEMBL5187554 | — | — | 1 | 8.29 |
| CHEMBL4071161 | TIRABRUTINIB | 4.0 | 1 | 8.25 |
| CHEMBL1230541 | — | — | 1 | 8.05 |
| CHEMBL4650485 | PIRTOBRUTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5193128 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4065122 | FENEBRUTINIB | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5169992 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5187554 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4071161 | TIRABRUTINIB | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL1230541 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL4650485 | PIRTOBRUTINIB | IC50 | < | 1.0 | nM | - |