Assay Detail
Binding
CHEMBL3888236
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). 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 for the treatment of solid tumors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 8.74 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3894938 | — | — | 1 | 9.49 |
| CHEMBL3910496 | — | — | 1 | 9.41 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 2 | 9.30 |
| CHEMBL4109796 | — | — | 1 | 9.17 |
| CHEMBL4110614 | — | — | 1 | 9.05 |
| CHEMBL4107818 | — | — | 1 | 9.04 |
| CHEMBL3647967 | — | — | 2 | 9.00 |
| CHEMBL3647970 | — | — | 1 | 8.96 |
| CHEMBL3912266 | — | — | 1 | 8.88 |
| CHEMBL3903249 | — | — | 1 | 8.88 |
| CHEMBL3980550 | — | — | 1 | 8.86 |
| CHEMBL3889694 | — | — | 1 | 8.85 |
| CHEMBL3921655 | — | — | 1 | 8.80 |
| CHEMBL3921017 | — | — | 1 | 8.80 |
| CHEMBL4106607 | — | — | 1 | 8.70 |
| CHEMBL3647973 | — | — | 1 | 8.51 |
| CHEMBL3905432 | — | — | 1 | 8.50 |
| CHEMBL3894102 | — | — | 1 | 8.46 |
| CHEMBL3982014 | — | — | 1 | 8.39 |
| CHEMBL4107879 | — | — | 1 | 8.38 |
| CHEMBL3915538 | — | — | 1 | 8.38 |
| CHEMBL3902180 | — | — | 1 | 8.25 |
| CHEMBL3917698 | — | — | 1 | 8.20 |
| CHEMBL3931858 | — | — | 1 | 7.68 |
| CHEMBL3926657 | — | — | 1 | 7.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3894938 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL3910496 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4109796 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL4110614 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL4107818 | — | IC50 | = | 0.92 | nM | 9.04 |
| CHEMBL3647967 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3647967 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3647970 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3903249 | — | IC50 | = | 1.33 | nM | 8.88 |
| CHEMBL3912266 | — | IC50 | = | 1.31 | nM | 8.88 |
| CHEMBL3980550 | — | IC50 | = | 1.38 | nM | 8.86 |
| CHEMBL3889694 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3921017 | — | IC50 | = | 1.58 | nM | 8.80 |
| CHEMBL3921655 | — | IC50 | = | 1.57 | nM | 8.80 |
| CHEMBL4106607 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3647973 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3905432 | — | IC50 | = | 3.14 | nM | 8.50 |
| CHEMBL3894102 | — | IC50 | = | 3.48 | nM | 8.46 |
| CHEMBL3982014 | — | IC50 | = | 4.07 | nM | 8.39 |
| CHEMBL4107879 | — | IC50 | = | 4.16 | nM | 8.38 |
| CHEMBL3915538 | — | IC50 | = | 4.15 | nM | 8.38 |
| CHEMBL3902180 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3917698 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3931858 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3926657 | — | IC50 | = | 22.2 | nM | 7.65 |