Assay Detail
Binding
CHEMBL4358514
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Binding affinity to DNA-tagged recombinant BTK (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR 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
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 6 | 8.42 | 9.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297674 | BRANEBRUTINIB | 2.0 | 1 | 9.25 |
| CHEMBL4483575 | REMIBRUTINIB | 3.0 | 1 | 9.20 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 8.72 |
| CHEMBL4071161 | TIRABRUTINIB | 4.0 | 1 | 7.85 |
| CHEMBL4072833 | EVOBRUTINIB | 3.0 | 1 | 7.80 |
| CHEMBL3707348 | ACALABRUTINIB | 4.0 | 1 | 7.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297674 | BRANEBRUTINIB | Kd | = | 0.56 | nM | 9.25 |
| CHEMBL4483575 | REMIBRUTINIB | Kd | = | 0.63 | nM | 9.20 |
| CHEMBL1873475 | IBRUTINIB | Kd | = | 1.9 | nM | 8.72 |
| CHEMBL4071161 | TIRABRUTINIB | Kd | = | 14.0 | nM | 7.85 |
| CHEMBL4072833 | EVOBRUTINIB | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL3707348 | ACALABRUTINIB | Kd | = | 21.0 | nM | 7.68 |