Assay Detail
Binding
CHEMBL5127265
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK C481S mutant (unknown origin)
5
Total Activities
5
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 | 4 | 8.60 | 9.41 |
| Ki | 1 | 8.80 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4756476 | NEMTABRUTINIB | 3.0 | 1 | 9.41 |
| CHEMBL4065122 | FENEBRUTINIB | 3.0 | 1 | 8.80 |
| CHEMBL5169992 | — | — | 1 | 8.60 |
| CHEMBL1230541 | — | — | 1 | 7.80 |
| CHEMBL4650485 | PIRTOBRUTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4756476 | NEMTABRUTINIB | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL4065122 | FENEBRUTINIB | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL5169992 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL1230541 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4650485 | PIRTOBRUTINIB | IC50 | < | 1.0 | nM | - |