Assay Detail
Binding
CHEMBL3887530
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 | 5.87 | 7.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 2 | 7.93 |
| CHEMBL4110614 | — | — | 1 | 6.32 |
| CHEMBL3921017 | — | — | 1 | 6.27 |
| CHEMBL3910496 | — | — | 1 | 6.23 |
| CHEMBL3894938 | — | — | 1 | 6.08 |
| CHEMBL3647967 | — | — | 2 | 6.04 |
| CHEMBL3912266 | — | — | 1 | 5.71 |
| CHEMBL4106607 | — | — | 1 | 5.63 |
| CHEMBL3893004 | — | — | 1 | 5.60 |
| CHEMBL4109796 | — | — | 1 | 5.52 |
| CHEMBL3921655 | — | — | 1 | 5.43 |
| CHEMBL3917698 | — | — | 1 | 5.21 |
| CHEMBL3903870 | — | — | 1 | 5.16 |
| CHEMBL3982014 | — | — | 1 | 5.10 |
| CHEMBL3903249 | — | — | 1 | 4.84 |
| CHEMBL4107879 | — | — | 1 | 4.68 |
| CHEMBL3894102 | — | — | 1 | - |
| CHEMBL3915538 | — | — | 1 | - |
| CHEMBL3905432 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL4110614 | — | IC50 | = | 476.0 | nM | 6.32 |
| CHEMBL3921017 | — | IC50 | = | 534.6 | nM | 6.27 |
| CHEMBL3910496 | — | IC50 | = | 592.3 | nM | 6.23 |
| CHEMBL3894938 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL3647967 | — | IC50 | = | 909.9 | nM | 6.04 |
| CHEMBL3647967 | — | IC50 | = | 909.9 | nM | 6.04 |
| CHEMBL3912266 | — | IC50 | = | 1954.0 | nM | 5.71 |
| CHEMBL4106607 | — | IC50 | = | 2333.0 | nM | 5.63 |
| CHEMBL3893004 | — | IC50 | = | 2536.0 | nM | 5.60 |
| CHEMBL4109796 | — | IC50 | = | 3013.0 | nM | 5.52 |
| CHEMBL3921655 | — | IC50 | = | 3691.0 | nM | 5.43 |
| CHEMBL3917698 | — | IC50 | = | 6123.0 | nM | 5.21 |
| CHEMBL3903870 | — | IC50 | = | 6891.0 | nM | 5.16 |
| CHEMBL3982014 | — | IC50 | = | 7993.0 | nM | 5.10 |
| CHEMBL3903249 | — | IC50 | = | 14290.0 | nM | 4.84 |
| CHEMBL4107879 | — | IC50 | = | 21100.0 | nM | 4.68 |
| CHEMBL3915538 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3905432 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3894102 | — | IC50 | > | 10000.0 | nM | - |