Assay Detail
Binding
CHEMBL4236252
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Inhibition of human full length BTK using FITC-AHA-EEPLYWSFPAKKK-NH2 as substrate after 90 mins by microfluid mobility shift assay
11
Total Activities
11
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 potent, highly selective covalent irreversible BTK inhibitors from a fragment hit.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.77 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 9.70 |
| CHEMBL4242598 | — | — | 1 | 9.15 |
| CHEMBL4250200 | — | — | 1 | 8.39 |
| CHEMBL4246399 | — | — | 1 | 8.36 |
| CHEMBL4246409 | — | — | 1 | 7.92 |
| CHEMBL4243203 | — | — | 1 | 7.89 |
| CHEMBL4241920 | — | — | 1 | 7.60 |
| CHEMBL4240087 | — | — | 1 | 7.50 |
| CHEMBL4238999 | — | — | 1 | 7.40 |
| CHEMBL4239634 | — | — | 1 | 6.37 |
| CHEMBL4243865 | — | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4242598 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4250200 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4246399 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4246409 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4243203 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4241920 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4240087 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4238999 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4239634 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4243865 | — | IC50 | = | 5900.0 | nM | 5.23 |