Assay Detail
Binding
CHEMBL4358488
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK in vitamin D3 differentiated human THP1 cells assessed as inhibition of FCgammaR-induced IL8 production measured after 24 hrs by HTRF assay
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 | 7.53 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4483575 | REMIBRUTINIB | 3.0 | 1 | 8.60 |
| CHEMBL4439622 | — | — | 1 | 8.30 |
| CHEMBL4576902 | — | — | 1 | 8.30 |
| CHEMBL4297674 | BRANEBRUTINIB | 2.0 | 1 | 8.22 |
| CHEMBL4471613 | — | — | 1 | 8.19 |
| CHEMBL4537231 | — | — | 1 | 8.05 |
| CHEMBL4559123 | — | — | 1 | 7.96 |
| CHEMBL4546324 | — | — | 1 | 7.96 |
| CHEMBL4445790 | — | — | 1 | 7.92 |
| CHEMBL4450082 | — | — | 1 | 7.82 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 7.80 |
| CHEMBL4550284 | — | — | 1 | 7.77 |
| CHEMBL4463650 | — | — | 1 | 7.77 |
| CHEMBL4557061 | — | — | 1 | 7.75 |
| CHEMBL4567040 | — | — | 1 | 7.70 |
| CHEMBL4463185 | — | — | 1 | 7.62 |
| CHEMBL3707348 | ACALABRUTINIB | 4.0 | 1 | 7.62 |
| CHEMBL4071161 | TIRABRUTINIB | 4.0 | 1 | 7.58 |
| CHEMBL4437701 | — | — | 1 | 7.50 |
| CHEMBL4591291 | — | — | 1 | 7.22 |
| CHEMBL4072833 | EVOBRUTINIB | 3.0 | 1 | 7.21 |
| CHEMBL4441128 | — | — | 1 | 7.12 |
| CHEMBL4513614 | — | — | 1 | 6.97 |
| CHEMBL4576801 | — | — | 1 | 6.58 |
| CHEMBL4461398 | — | — | 1 | 6.17 |
| CHEMBL4589396 | — | — | 1 | 5.84 |
| CHEMBL4468095 | — | — | 1 | 5.73 |
| CHEMBL4468719 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4483575 | REMIBRUTINIB | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4439622 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4576902 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4297674 | BRANEBRUTINIB | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4471613 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4537231 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4559123 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4546324 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4445790 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4450082 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4550284 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4463650 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4557061 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4567040 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4463185 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3707348 | ACALABRUTINIB | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4071161 | TIRABRUTINIB | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4437701 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4591291 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4072833 | EVOBRUTINIB | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4441128 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4513614 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL4576801 | — | IC50 | = | 263.0 | nM | 6.58 |
| CHEMBL4461398 | — | IC50 | = | 671.0 | nM | 6.17 |
| CHEMBL4589396 | — | IC50 | = | 1437.0 | nM | 5.84 |
| CHEMBL4468095 | — | IC50 | = | 1869.0 | nM | 5.73 |
| CHEMBL4468719 | — | IC50 | > | 10000.0 | nM | - |