Assay Detail
Binding
CHEMBL4358487
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Inhibition of full-length human recombinant BTK using FITC-Ahx-TSELKKVVALYDYMPMNAND-NH2 as substrate measured after 60 mins by caliper assay
30
Total Activities
30
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 | 30 | 7.92 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4439622 | — | — | 1 | 9.05 |
| CHEMBL4593663 | — | — | 1 | 9.05 |
| CHEMBL4483575 | REMIBRUTINIB | 3.0 | 1 | 8.89 |
| CHEMBL4537231 | — | — | 1 | 8.85 |
| CHEMBL4450082 | — | — | 1 | 8.74 |
| CHEMBL4471613 | — | — | 1 | 8.74 |
| CHEMBL4546324 | — | — | 1 | 8.72 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 8.64 |
| CHEMBL4463185 | — | — | 1 | 8.64 |
| CHEMBL4576902 | — | — | 1 | 8.51 |
| CHEMBL4550284 | — | — | 1 | 8.44 |
| CHEMBL4463650 | — | — | 1 | 8.44 |
| CHEMBL4445790 | — | — | 1 | 8.43 |
| CHEMBL4559123 | — | — | 1 | 8.42 |
| CHEMBL4567040 | — | — | 1 | 8.35 |
| CHEMBL4437701 | — | — | 1 | 8.28 |
| CHEMBL4071161 | TIRABRUTINIB | 4.0 | 1 | 8.28 |
| CHEMBL4591291 | — | — | 1 | 8.12 |
| CHEMBL4557061 | — | — | 1 | 8.06 |
| CHEMBL4441128 | — | — | 1 | 7.96 |
| CHEMBL4566818 | — | — | 1 | 7.89 |
| CHEMBL3707348 | ACALABRUTINIB | 4.0 | 1 | 7.72 |
| CHEMBL4513614 | — | — | 1 | 7.64 |
| CHEMBL4461398 | — | — | 1 | 7.29 |
| CHEMBL4072833 | EVOBRUTINIB | 3.0 | 1 | 7.21 |
| CHEMBL4576801 | — | — | 1 | 6.98 |
| CHEMBL4468719 | — | — | 1 | 5.89 |
| CHEMBL4468095 | — | — | 1 | 5.89 |
| CHEMBL4589396 | — | — | 1 | 5.44 |
| CHEMBL4446119 | — | — | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4439622 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4593663 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4483575 | REMIBRUTINIB | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4537231 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4450082 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4471613 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4546324 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4463185 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4576902 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4550284 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4463650 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4445790 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4559123 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4567040 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4437701 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4071161 | TIRABRUTINIB | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4591291 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL4557061 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4441128 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4566818 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3707348 | ACALABRUTINIB | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4513614 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4461398 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4072833 | EVOBRUTINIB | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4576801 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL4468719 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4468095 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL4589396 | — | IC50 | = | 3651.0 | nM | 5.44 |
| CHEMBL4446119 | — | IC50 | = | 7300.0 | nM | 5.14 |