Assay Detail
Binding
CHEMBL4036700
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK in goat F(ab')2anti-mouse IgM-stimulated Balb/c mouse splenocyte B cells assessed as suppression of BCR-mediated CD86 induction preincubated for 60 mins followed by cell stimulation measured after 24 hrs by 7AAD staining-based FACS analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| 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 | 19 | 6.87 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3670139 | — | — | 1 | 8.22 |
| CHEMBL3670095 | — | — | 1 | 8.00 |
| CHEMBL3670094 | — | — | 1 | 7.66 |
| CHEMBL4080943 | — | — | 1 | 7.60 |
| CHEMBL4085292 | — | — | 1 | 7.29 |
| CHEMBL4090189 | — | — | 1 | 7.24 |
| CHEMBL3670082 | — | — | 1 | 7.19 |
| CHEMBL3670081 | — | — | 1 | 7.06 |
| CHEMBL3670088 | — | — | 1 | 6.97 |
| CHEMBL4060453 | — | — | 1 | 6.86 |
| CHEMBL4069030 | — | — | 1 | 6.77 |
| CHEMBL4067714 | — | — | 1 | 6.71 |
| CHEMBL3670086 | — | — | 1 | 6.70 |
| CHEMBL4096404 | — | — | 1 | 6.64 |
| CHEMBL4071845 | — | — | 1 | 6.32 |
| CHEMBL4084331 | — | — | 1 | 6.13 |
| CHEMBL4077625 | — | — | 1 | 5.92 |
| CHEMBL4100365 | — | — | 1 | 4.31 |
| CHEMBL4082346 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3670139 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3670095 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3670094 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4080943 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4085292 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4090189 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3670082 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL3670081 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3670088 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4060453 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4069030 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL4067714 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL3670086 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4096404 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4071845 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4084331 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4077625 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4100365 | — | IC50 | = | 48600.0 | nM | 4.31 |
| CHEMBL4082346 | — | IC50 | > | 50000.0 | nM | - |