Assay Detail
Binding
CHEMBL4701077
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Inhibition of BTK in human whole blood assessed as reduction in BTK phosphorylation measured after 30 mins by phosphotyrosine detection method
14
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.03 | 6.92 |
| fIC50 | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4744041 | — | — | 2 | 6.92 |
| CHEMBL4782313 | — | — | 2 | 6.46 |
| CHEMBL4754065 | — | — | 2 | 6.37 |
| CHEMBL4796367 | — | — | 2 | 6.19 |
| CHEMBL4749757 | — | — | 2 | 5.85 |
| CHEMBL4746275 | — | — | 1 | 5.28 |
| CHEMBL4756023 | — | — | 1 | 5.11 |
| CHEMBL4760128 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4744041 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4782313 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4754065 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4796367 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4749757 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4746275 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4756023 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL4760128 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4754065 | — | fIC50 | = | 1.3 | nM | - |
| CHEMBL4749757 | — | fIC50 | = | 9.8 | nM | - |
| CHEMBL4760128 | — | fIC50 | = | 7.0 | nM | - |
| CHEMBL4782313 | — | fIC50 | = | 0.7 | nM | - |
| CHEMBL4796367 | — | fIC50 | = | 5.9 | nM | - |
| CHEMBL4744041 | — | fIC50 | = | 7.1 | nM | - |