Assay Detail
Binding
CHEMBL4843876
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Inhibition of N-terminal DYKDDDD-tagged EGFR (669 to 1210 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 | 7.34 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3647964 | — | — | 1 | 8.92 |
| CHEMBL3936761 | ZANUBRUTINIB | 4.0 | 1 | 8.22 |
| CHEMBL4869409 | — | — | 1 | 7.79 |
| CHEMBL4875332 | — | — | 1 | 7.53 |
| CHEMBL4871192 | — | — | 1 | 7.51 |
| CHEMBL4857353 | — | — | 1 | 7.48 |
| CHEMBL4863088 | — | — | 1 | 7.47 |
| CHEMBL4852264 | — | — | 1 | 7.41 |
| CHEMBL4856592 | — | — | 1 | 7.29 |
| CHEMBL4867893 | — | — | 1 | 7.05 |
| CHEMBL4873984 | — | — | 1 | 6.98 |
| CHEMBL4863078 | — | — | 1 | 6.96 |
| CHEMBL4878090 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3647964 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3936761 | ZANUBRUTINIB | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4869409 | — | IC50 | = | 16.3 | nM | 7.79 |
| CHEMBL4875332 | — | IC50 | = | 29.7 | nM | 7.53 |
| CHEMBL4871192 | — | IC50 | = | 30.8 | nM | 7.51 |
| CHEMBL4857353 | — | IC50 | = | 32.8 | nM | 7.48 |
| CHEMBL4863088 | — | IC50 | = | 33.8 | nM | 7.47 |
| CHEMBL4852264 | — | IC50 | = | 38.6 | nM | 7.41 |
| CHEMBL4856592 | — | IC50 | = | 50.8 | nM | 7.29 |
| CHEMBL4867893 | — | IC50 | = | 88.3 | nM | 7.05 |
| CHEMBL4873984 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL4863078 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4878090 | — | IC50 | = | 14010.0 | nM | 4.85 |