Assay Detail
Binding
CHEMBL5133817
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Binding affinity to TEC (unknown origin) assessed as dissociation constant by KINOMEscan analysis
6
Total Activities
6
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 |
Publication
Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 6 | 7.57 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 9.00 |
| CHEMBL3707348 | ACALABRUTINIB | 4.0 | 1 | 8.26 |
| CHEMBL3936761 | ZANUBRUTINIB | 4.0 | 1 | 7.75 |
| CHEMBL4483575 | REMIBRUTINIB | 3.0 | 1 | 7.11 |
| CHEMBL4066176 | — | — | 1 | 6.68 |
| CHEMBL5188786 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL3707348 | ACALABRUTINIB | Kd | = | 5.5 | nM | 8.26 |
| CHEMBL3936761 | ZANUBRUTINIB | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL4483575 | REMIBRUTINIB | Kd | = | 77.0 | nM | 7.11 |
| CHEMBL4066176 | — | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL5188786 | — | Kd | = | 240.0 | nM | 6.62 |