Assay Detail
Binding
CHEMBL4358489
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK in human B cells assessed as reduction in anti-IgM/IL4-stimulated CD69 expression on B cells preincubated for 60 mins followed by anti-IgM antibody/IL4 stimulation and measured after 16 hrs by flow cytometry
28
Total Activities
28
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 |
|---|---|---|---|
| IC50 | 28 | 6.95 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4483575 | REMIBRUTINIB | 3.0 | 1 | 7.75 |
| CHEMBL4297674 | BRANEBRUTINIB | 2.0 | 1 | 7.75 |
| CHEMBL4439622 | — | — | 1 | 7.55 |
| CHEMBL4546324 | — | — | 1 | 7.36 |
| CHEMBL4471613 | — | — | 1 | 7.31 |
| CHEMBL4576902 | — | — | 1 | 7.30 |
| CHEMBL4463185 | — | — | 1 | 7.26 |
| CHEMBL4537231 | — | — | 1 | 7.24 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 7.18 |
| CHEMBL4567040 | — | — | 1 | 7.07 |
| CHEMBL4550284 | — | — | 1 | 7.04 |
| CHEMBL4463650 | — | — | 1 | 7.02 |
| CHEMBL4557061 | — | — | 1 | 6.98 |
| CHEMBL4559123 | — | — | 1 | 6.97 |
| CHEMBL4071161 | TIRABRUTINIB | 4.0 | 1 | 6.88 |
| CHEMBL4441128 | — | — | 1 | 6.82 |
| CHEMBL4437701 | — | — | 1 | 6.79 |
| CHEMBL4445790 | — | — | 1 | 6.70 |
| CHEMBL3707348 | ACALABRUTINIB | 4.0 | 1 | 6.69 |
| CHEMBL4450082 | — | — | 1 | 6.65 |
| CHEMBL4513614 | — | — | 1 | 6.60 |
| CHEMBL4072833 | EVOBRUTINIB | 3.0 | 1 | 6.50 |
| CHEMBL4591291 | — | — | 1 | 6.45 |
| CHEMBL4576801 | — | — | 1 | 6.01 |
| CHEMBL4461398 | — | — | 1 | 5.91 |
| CHEMBL4468719 | — | — | 1 | - |
| CHEMBL4468095 | — | — | 1 | - |
| CHEMBL4589396 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4483575 | REMIBRUTINIB | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4297674 | BRANEBRUTINIB | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4439622 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4546324 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4471613 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4576902 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4463185 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4537231 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4567040 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4550284 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4463650 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4557061 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL4559123 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL4071161 | TIRABRUTINIB | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL4441128 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL4437701 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL4445790 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL3707348 | ACALABRUTINIB | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL4450082 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL4513614 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4072833 | EVOBRUTINIB | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4591291 | — | IC50 | = | 354.0 | nM | 6.45 |
| CHEMBL4576801 | — | IC50 | = | 983.0 | nM | 6.01 |
| CHEMBL4461398 | — | IC50 | = | 1245.0 | nM | 5.91 |
| CHEMBL4468719 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4468095 | — | IC50 | - | — | - | |
| CHEMBL4589396 | — | IC50 | - | — | - |