Assay Detail
Binding
CHEMBL4843878
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Inhibition of N-terminal GST-tagged ITK (2 to 620 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 |
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 | 6.03 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3647964 | — | — | 1 | 8.05 |
| CHEMBL3936761 | ZANUBRUTINIB | 4.0 | 1 | 6.69 |
| CHEMBL4852264 | — | — | 1 | 6.42 |
| CHEMBL4863088 | — | — | 1 | 6.33 |
| CHEMBL4878090 | — | — | 1 | 6.26 |
| CHEMBL4875332 | — | — | 1 | 6.13 |
| CHEMBL4863078 | — | — | 1 | 5.96 |
| CHEMBL4856592 | — | — | 1 | 5.85 |
| CHEMBL4867893 | — | — | 1 | 5.79 |
| CHEMBL4873984 | — | — | 1 | 5.72 |
| CHEMBL4871192 | — | — | 1 | 5.69 |
| CHEMBL4869409 | — | — | 1 | 5.05 |
| CHEMBL4857353 | — | — | 1 | 4.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3647964 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL3936761 | ZANUBRUTINIB | IC50 | = | 202.9 | nM | 6.69 |
| CHEMBL4852264 | — | IC50 | = | 385.0 | nM | 6.42 |
| CHEMBL4863088 | — | IC50 | = | 465.0 | nM | 6.33 |
| CHEMBL4878090 | — | IC50 | = | 549.0 | nM | 6.26 |
| CHEMBL4875332 | — | IC50 | = | 734.0 | nM | 6.13 |
| CHEMBL4863078 | — | IC50 | = | 1109.0 | nM | 5.96 |
| CHEMBL4856592 | — | IC50 | = | 1415.0 | nM | 5.85 |
| CHEMBL4867893 | — | IC50 | = | 1619.0 | nM | 5.79 |
| CHEMBL4873984 | — | IC50 | = | 1916.0 | nM | 5.72 |
| CHEMBL4871192 | — | IC50 | = | 2033.0 | nM | 5.69 |
| CHEMBL4869409 | — | IC50 | = | 8940.0 | nM | 5.05 |
| CHEMBL4857353 | — | IC50 | = | 37225.0 | nM | 4.43 |