Assay Detail
Binding
CHEMBL4616764
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Inhibition of recombinant human BTK using fluoresceinated peptide as substrate after 60 mins fluorescence assay
20
Total Activities
20
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 Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 8.83 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4648442 | — | — | 1 | 10.15 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 10.10 |
| CHEMBL4297674 | BRANEBRUTINIB | 2.0 | 1 | 10.00 |
| CHEMBL4634162 | — | — | 1 | 9.85 |
| CHEMBL4642827 | — | — | 1 | 9.28 |
| CHEMBL4645440 | — | — | 1 | 9.22 |
| CHEMBL4646648 | — | — | 1 | 9.07 |
| CHEMBL4641586 | — | — | 1 | 8.92 |
| CHEMBL4638741 | — | — | 1 | 8.85 |
| CHEMBL4649352 | — | — | 1 | 8.85 |
| CHEMBL4640555 | — | — | 1 | 8.80 |
| CHEMBL4649284 | — | — | 1 | 8.62 |
| CHEMBL4644786 | — | — | 1 | 8.48 |
| CHEMBL4639092 | — | — | 1 | 8.48 |
| CHEMBL4642103 | — | — | 1 | 8.46 |
| CHEMBL4646406 | — | — | 1 | 8.38 |
| CHEMBL4634526 | — | — | 1 | 8.19 |
| CHEMBL4643248 | — | — | 1 | 8.08 |
| CHEMBL4633931 | — | — | 1 | 7.54 |
| CHEMBL4640731 | — | — | 1 | 7.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4648442 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL4297674 | BRANEBRUTINIB | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4634162 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL4642827 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL4645440 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4646648 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL4641586 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4638741 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4649352 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4640555 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4649284 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4644786 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4639092 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4642103 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4646406 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4634526 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4643248 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4633931 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4640731 | — | IC50 | = | 59.0 | nM | 7.23 |