Assay Detail
Binding
CHEMBL3887548
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 | 5.84 | 7.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 2 | 7.98 |
| CHEMBL3910496 | — | — | 1 | 5.84 |
| CHEMBL3894938 | — | — | 1 | 5.48 |
| CHEMBL3921017 | — | — | 1 | 5.22 |
| CHEMBL3647967 | — | — | 2 | 5.08 |
| CHEMBL4110614 | — | — | 1 | 5.04 |
| CHEMBL4109796 | — | — | 1 | 4.89 |
| CHEMBL3917698 | — | — | 1 | - |
| CHEMBL3912266 | — | — | 1 | - |
| CHEMBL3903870 | — | — | 1 | - |
| CHEMBL3903249 | — | — | 1 | - |
| CHEMBL4107879 | — | — | 1 | - |
| CHEMBL3905432 | — | — | 1 | - |
| CHEMBL4106607 | — | — | 1 | - |
| CHEMBL3893004 | — | — | 1 | - |
| CHEMBL3982014 | — | — | 1 | - |
| CHEMBL3915538 | — | — | 1 | - |
| CHEMBL3921655 | — | — | 1 | - |
| CHEMBL3894102 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL3910496 | — | IC50 | = | 1456.0 | nM | 5.84 |
| CHEMBL3894938 | — | IC50 | = | 3306.0 | nM | 5.48 |
| CHEMBL3921017 | — | IC50 | = | 5997.0 | nM | 5.22 |
| CHEMBL3647967 | — | IC50 | = | 8278.0 | nM | 5.08 |
| CHEMBL3647967 | — | IC50 | = | 8278.0 | nM | 5.08 |
| CHEMBL4110614 | — | IC50 | = | 9077.0 | nM | 5.04 |
| CHEMBL4109796 | — | IC50 | = | 12980.0 | nM | 4.89 |
| CHEMBL3917698 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3912266 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3903870 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3903249 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4107879 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3905432 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4106607 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3893004 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3982014 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3915538 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3921655 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3894102 | — | IC50 | > | 10000.0 | nM | - |