Assay Detail
Binding
CHEMBL4036701
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK in goat anti-human IgM F(ab')2-stimulated human whole blood assessed as suppression of BCR-induced CD69 expression on B cells preincubated for 1 hr followed by blood stimulation measured after 18 hrs by FACS analysis
6
Total Activities
6
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 and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.27 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3670094 | — | — | 1 | 7.54 |
| CHEMBL3670095 | — | — | 1 | 7.46 |
| CHEMBL3670088 | — | — | 1 | 7.35 |
| CHEMBL4060453 | — | — | 1 | 7.16 |
| CHEMBL3670082 | — | — | 1 | 7.06 |
| CHEMBL3670139 | — | — | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3670094 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3670095 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3670088 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4060453 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3670082 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3670139 | — | IC50 | = | 89.0 | nM | 7.05 |