Assay Detail
Binding
CHEMBL4036699
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full length His-tagged BTK expressed in baculovirus expression system by Z-LYTE assay
21
Total Activities
20
Compounds Tested
2
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 | 20 | 7.93 | 9.00 |
| Ki | 1 | 8.89 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3670081 | — | — | 1 | 9.00 |
| CHEMBL3670082 | — | — | 2 | 8.89 |
| CHEMBL3670094 | — | — | 1 | 8.70 |
| CHEMBL4090189 | — | — | 1 | 8.70 |
| CHEMBL4067714 | — | — | 1 | 8.52 |
| CHEMBL4077625 | — | — | 1 | 8.52 |
| CHEMBL4080943 | — | — | 1 | 8.52 |
| CHEMBL4069030 | — | — | 1 | 8.40 |
| CHEMBL3670139 | — | — | 1 | 8.40 |
| CHEMBL3670088 | — | — | 1 | 8.40 |
| CHEMBL3670095 | — | — | 1 | 8.40 |
| CHEMBL4096404 | — | — | 1 | 8.30 |
| CHEMBL3670086 | — | — | 1 | 8.22 |
| CHEMBL4060453 | — | — | 1 | 8.10 |
| CHEMBL4102294 | — | — | 1 | 7.96 |
| CHEMBL4084331 | — | — | 1 | 7.38 |
| CHEMBL4071845 | — | — | 1 | 7.09 |
| CHEMBL4095477 | — | — | 1 | 6.86 |
| CHEMBL4100365 | — | — | 1 | 5.58 |
| CHEMBL4082346 | — | — | 1 | 4.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3670081 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3670082 | — | Ki | = | 1.28 | nM | 8.89 |
| CHEMBL3670094 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3670082 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4090189 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4067714 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4077625 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4080943 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3670139 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4069030 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3670088 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3670095 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4096404 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3670086 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4060453 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4102294 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4084331 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4071845 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4095477 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL4100365 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4082346 | — | IC50 | = | 16700.0 | nM | 4.78 |