Assay Detail
Binding
CHEMBL3887536
Review assay metadata, readout intent, target linkage, and publication context from the same page.
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
21
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Inhibitors of bruton's tyrosine kinase
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 8.13 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3893004 | — | — | 1 | 9.12 |
| CHEMBL3912266 | — | — | 1 | 9.06 |
| CHEMBL3647967 | — | — | 2 | 9.00 |
| CHEMBL4109796 | — | — | 1 | 8.81 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 2 | 8.70 |
| CHEMBL4106607 | — | — | 1 | 8.68 |
| CHEMBL3903870 | — | — | 1 | 8.61 |
| CHEMBL3917698 | — | — | 1 | 8.59 |
| CHEMBL3905432 | — | — | 1 | 8.42 |
| CHEMBL4107879 | — | — | 1 | 8.23 |
| CHEMBL3903249 | — | — | 1 | 8.22 |
| CHEMBL3921017 | — | — | 1 | 8.18 |
| CHEMBL3910496 | — | — | 1 | 8.03 |
| CHEMBL3921655 | — | — | 1 | 7.66 |
| CHEMBL3894102 | — | — | 1 | 7.59 |
| CHEMBL3982014 | — | — | 1 | 7.01 |
| CHEMBL3894938 | — | — | 1 | 6.68 |
| CHEMBL4110614 | — | — | 1 | 6.63 |
| CHEMBL3915538 | — | — | 1 | 5.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3893004 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL3912266 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL3647967 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3647967 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4109796 | — | IC50 | = | 1.56 | nM | 8.81 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4106607 | — | IC50 | = | 2.07 | nM | 8.68 |
| CHEMBL3903870 | — | IC50 | = | 2.43 | nM | 8.61 |
| CHEMBL3917698 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3905432 | — | IC50 | = | 3.82 | nM | 8.42 |
| CHEMBL4107879 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL3903249 | — | IC50 | = | 5.97 | nM | 8.22 |
| CHEMBL3921017 | — | IC50 | = | 6.62 | nM | 8.18 |
| CHEMBL3910496 | — | IC50 | = | 9.24 | nM | 8.03 |
| CHEMBL3921655 | — | IC50 | = | 22.12 | nM | 7.66 |
| CHEMBL3894102 | — | IC50 | = | 25.81 | nM | 7.59 |
| CHEMBL3982014 | — | IC50 | = | 98.59 | nM | 7.01 |
| CHEMBL3894938 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL4110614 | — | IC50 | = | 235.4 | nM | 6.63 |
| CHEMBL3915538 | — | IC50 | = | 1346.0 | nM | 5.87 |