Assay Detail
Binding
CHEMBL4616765
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Inhibition of BTK in human Ramos B cells assessed as reduction in BCR-stimulated calcium flux after 1 hr in dark condition measured for 180 sec
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Ramos |
| 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 | 7.66 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4648442 | — | — | 1 | 8.80 |
| CHEMBL4640555 | — | — | 1 | 8.16 |
| CHEMBL4634526 | — | — | 1 | 8.14 |
| CHEMBL4297674 | BRANEBRUTINIB | 2.0 | 1 | 8.14 |
| CHEMBL4649284 | — | — | 1 | 8.03 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 7.85 |
| CHEMBL4645440 | — | — | 1 | 7.82 |
| CHEMBL4646648 | — | — | 1 | 7.80 |
| CHEMBL4634162 | — | — | 1 | 7.75 |
| CHEMBL4649352 | — | — | 1 | 7.58 |
| CHEMBL4641586 | — | — | 1 | 7.55 |
| CHEMBL4638741 | — | — | 1 | 7.52 |
| CHEMBL4642827 | — | — | 1 | 7.40 |
| CHEMBL4639092 | — | — | 1 | 7.37 |
| CHEMBL4644786 | — | — | 1 | 7.00 |
| CHEMBL4642103 | — | — | 1 | 6.77 |
| CHEMBL4646406 | — | — | 1 | 6.57 |
| CHEMBL4643248 | — | — | 1 | - |
| CHEMBL4640731 | — | — | 1 | - |
| CHEMBL4633931 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4648442 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4640555 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL4634526 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4297674 | BRANEBRUTINIB | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4649284 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4645440 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4646648 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4634162 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4649352 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4641586 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4638741 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4642827 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4639092 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4644786 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4642103 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4646406 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4643248 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL4640731 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL4633931 | — | IC50 | > | 300.0 | nM | - |