Assay Detail
Binding
CHEMBL3887533
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.
27
Total Activities
25
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 | 27 | 7.11 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 2 | 9.30 |
| CHEMBL3910496 | — | — | 1 | 8.64 |
| CHEMBL4109796 | — | — | 1 | 7.73 |
| CHEMBL3903870 | — | — | 1 | 7.72 |
| CHEMBL3647967 | — | — | 2 | 7.69 |
| CHEMBL3893004 | — | — | 1 | 7.65 |
| CHEMBL3921017 | — | — | 1 | 7.55 |
| CHEMBL3912266 | — | — | 1 | 7.35 |
| CHEMBL3647970 | — | — | 1 | 7.31 |
| CHEMBL3647973 | — | — | 1 | 7.21 |
| CHEMBL3894938 | — | — | 1 | 7.15 |
| CHEMBL3931858 | — | — | 1 | 7.13 |
| CHEMBL3889694 | — | — | 1 | 7.08 |
| CHEMBL3921655 | — | — | 1 | 6.81 |
| CHEMBL3917698 | — | — | 1 | 6.57 |
| CHEMBL3894102 | — | — | 1 | 6.56 |
| CHEMBL4107879 | — | — | 1 | 6.54 |
| CHEMBL3982014 | — | — | 1 | 6.52 |
| CHEMBL3902180 | — | — | 1 | 6.49 |
| CHEMBL4110614 | — | — | 1 | 6.42 |
| CHEMBL4106607 | — | — | 1 | 6.36 |
| CHEMBL3926657 | — | — | 1 | 6.31 |
| CHEMBL3903249 | — | — | 1 | 6.16 |
| CHEMBL3905432 | — | — | 1 | 5.55 |
| CHEMBL3915538 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3910496 | — | IC50 | = | 2.298 | nM | 8.64 |
| CHEMBL4109796 | — | IC50 | = | 18.75 | nM | 7.73 |
| CHEMBL3903870 | — | IC50 | = | 18.85 | nM | 7.72 |
| CHEMBL3647967 | — | IC50 | = | 20.6 | nM | 7.69 |
| CHEMBL3647967 | — | IC50 | = | 20.6 | nM | 7.69 |
| CHEMBL3893004 | — | IC50 | = | 22.53 | nM | 7.65 |
| CHEMBL3921017 | — | IC50 | = | 28.22 | nM | 7.55 |
| CHEMBL3912266 | — | IC50 | = | 44.5 | nM | 7.35 |
| CHEMBL3647970 | — | IC50 | = | 48.8 | nM | 7.31 |
| CHEMBL3647973 | — | IC50 | = | 60.9 | nM | 7.21 |
| CHEMBL3894938 | — | IC50 | = | 70.49 | nM | 7.15 |
| CHEMBL3931858 | — | IC50 | = | 74.5 | nM | 7.13 |
| CHEMBL3889694 | — | IC50 | = | 83.4 | nM | 7.08 |
| CHEMBL3921655 | — | IC50 | = | 156.3 | nM | 6.81 |
| CHEMBL3917698 | — | IC50 | = | 268.7 | nM | 6.57 |
| CHEMBL3894102 | — | IC50 | = | 272.9 | nM | 6.56 |
| CHEMBL4107879 | — | IC50 | = | 289.4 | nM | 6.54 |
| CHEMBL3982014 | — | IC50 | = | 303.6 | nM | 6.52 |
| CHEMBL3902180 | — | IC50 | = | 326.0 | nM | 6.49 |
| CHEMBL4110614 | — | IC50 | = | 383.7 | nM | 6.42 |
| CHEMBL4106607 | — | IC50 | = | 435.3 | nM | 6.36 |
| CHEMBL3926657 | — | IC50 | = | 487.6 | nM | 6.31 |
| CHEMBL3903249 | — | IC50 | = | 698.3 | nM | 6.16 |
| CHEMBL3905432 | — | IC50 | = | 2807.0 | nM | 5.55 |
| CHEMBL3915538 | — | IC50 | = | 6238.0 | nM | 5.21 |