Assay Detail
Binding
CHEMBL4843877
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged BMX (1 to 675 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Cytoplasmic tyrosine-protein kinase BMX (CHEMBL3834) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-activity relationship investigation for imidazopyrazole-3-carboxamide derivatives as novel selective inhibitors of Bruton's tyrosine kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.54 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3647964 | — | — | 1 | 9.40 |
| CHEMBL3936761 | ZANUBRUTINIB | 4.0 | 1 | 7.94 |
| CHEMBL4871192 | — | — | 1 | 7.85 |
| CHEMBL4869409 | — | — | 1 | 7.84 |
| CHEMBL4863088 | — | — | 1 | 7.67 |
| CHEMBL4875332 | — | — | 1 | 7.56 |
| CHEMBL4857353 | — | — | 1 | 7.46 |
| CHEMBL4856592 | — | — | 1 | 7.46 |
| CHEMBL4867893 | — | — | 1 | 7.13 |
| CHEMBL4873984 | — | — | 1 | 7.03 |
| CHEMBL4878090 | — | — | 1 | 7.01 |
| CHEMBL4852264 | — | — | 1 | 6.92 |
| CHEMBL4863078 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3647964 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3936761 | ZANUBRUTINIB | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL4871192 | — | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL4869409 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL4863088 | — | IC50 | = | 21.4 | nM | 7.67 |
| CHEMBL4875332 | — | IC50 | = | 27.5 | nM | 7.56 |
| CHEMBL4857353 | — | IC50 | = | 34.4 | nM | 7.46 |
| CHEMBL4856592 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4867893 | — | IC50 | = | 73.4 | nM | 7.13 |
| CHEMBL4873984 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4878090 | — | IC50 | = | 97.2 | nM | 7.01 |
| CHEMBL4852264 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL4863078 | — | IC50 | = | 179.0 | nM | 6.75 |