Assay Detail
Binding
CHEMBL4358519
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to DNA-tagged recombinant ERBB2 (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 |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 7.75 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 8.92 |
| CHEMBL3707348 | ACALABRUTINIB | 4.0 | 1 | 8.13 |
| CHEMBL4071161 | TIRABRUTINIB | 4.0 | 1 | 6.21 |
| CHEMBL4483575 | REMIBRUTINIB | 3.0 | 1 | - |
| CHEMBL4072833 | EVOBRUTINIB | 3.0 | 1 | - |
| CHEMBL4297674 | BRANEBRUTINIB | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | Kd | = | 1.2 | nM | 8.92 |
| CHEMBL3707348 | ACALABRUTINIB | Kd | = | 7.4 | nM | 8.13 |
| CHEMBL4071161 | TIRABRUTINIB | Kd | = | 610.0 | nM | 6.21 |
| CHEMBL4483575 | REMIBRUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL4072833 | EVOBRUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL4297674 | BRANEBRUTINIB | Kd | > | 10000.0 | nM | - |