Assay Detail
Binding
CHEMBL4726192
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Inhibition of His-tagged recombinant human His-tagged full length BTK expressed in baculovirus expression system using Tyr01 peptide as substrate preincubated for 1 hr by Z'lyte assay
5
Total Activities
5
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
Discovery of quinoline-based irreversible BTK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 8.64 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 9.37 |
| CHEMBL4755977 | — | — | 1 | 8.82 |
| CHEMBL3707348 | ACALABRUTINIB | 4.0 | 1 | 8.51 |
| CHEMBL4752700 | — | — | 1 | 8.40 |
| CHEMBL4782725 | — | — | 1 | 8.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL4755977 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3707348 | ACALABRUTINIB | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4752700 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4782725 | — | IC50 | = | 8.3 | nM | 8.08 |