Assay Detail
Binding
CHEMBL4843875
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length N-terminal GST tagged BTK (1 to 659 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
69
Total Activities
69
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 | 69 | 7.00 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3647964 | — | — | 1 | 9.40 |
| CHEMBL4869409 | — | — | 1 | 8.82 |
| CHEMBL4849585 | — | — | 1 | 8.72 |
| CHEMBL3936761 | ZANUBRUTINIB | 4.0 | 1 | 8.66 |
| CHEMBL4875332 | — | — | 1 | 8.54 |
| CHEMBL4863088 | — | — | 1 | 8.49 |
| CHEMBL4853615 | — | — | 1 | 8.32 |
| CHEMBL4878090 | — | — | 1 | 8.31 |
| CHEMBL4867893 | — | — | 1 | 8.27 |
| CHEMBL4870320 | — | — | 1 | 8.21 |
| CHEMBL4857353 | — | — | 1 | 8.20 |
| CHEMBL4856592 | — | — | 1 | 8.19 |
| CHEMBL4867850 | — | — | 1 | 8.14 |
| CHEMBL4873984 | — | — | 1 | 8.13 |
| CHEMBL4871192 | — | — | 1 | 8.12 |
| CHEMBL4857322 | — | — | 1 | 7.92 |
| CHEMBL4863138 | — | — | 1 | 7.87 |
| CHEMBL4876450 | — | — | 1 | 7.84 |
| CHEMBL4857245 | — | — | 1 | 7.83 |
| CHEMBL4861647 | — | — | 1 | 7.72 |
| CHEMBL4868355 | — | — | 1 | 7.55 |
| CHEMBL4856208 | — | — | 1 | 7.46 |
| CHEMBL4874730 | — | — | 1 | 7.38 |
| CHEMBL4863078 | — | — | 1 | 7.28 |
| CHEMBL4870576 | — | — | 1 | 7.26 |
| CHEMBL4871465 | — | — | 1 | 7.22 |
| CHEMBL4846339 | — | — | 1 | 7.21 |
| CHEMBL4866284 | — | — | 1 | 7.20 |
| CHEMBL4874306 | — | — | 1 | 7.10 |
| CHEMBL4878064 | — | — | 1 | 7.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3647964 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4869409 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4849585 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3936761 | ZANUBRUTINIB | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4875332 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4863088 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4853615 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4878090 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4867893 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4870320 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4857353 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4856592 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4867850 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4873984 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4871192 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4857322 | — | IC50 | = | 11.9 | nM | 7.92 |
| CHEMBL4863138 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL4876450 | — | IC50 | = | 14.6 | nM | 7.84 |
| CHEMBL4857245 | — | IC50 | = | 14.7 | nM | 7.83 |
| CHEMBL4861647 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL4868355 | — | IC50 | = | 27.9 | nM | 7.55 |
| CHEMBL4856208 | — | IC50 | = | 34.7 | nM | 7.46 |
| CHEMBL4874730 | — | IC50 | = | 41.8 | nM | 7.38 |
| CHEMBL4863078 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4870576 | — | IC50 | = | 54.8 | nM | 7.26 |
| CHEMBL4871465 | — | IC50 | = | 60.2 | nM | 7.22 |
| CHEMBL4846339 | — | IC50 | = | 61.9 | nM | 7.21 |
| CHEMBL4866284 | — | IC50 | = | 62.5 | nM | 7.20 |
| CHEMBL4874306 | — | IC50 | = | 78.7 | nM | 7.10 |
| CHEMBL4878064 | — | IC50 | = | 82.6 | nM | 7.08 |
| CHEMBL4868372 | — | IC50 | = | 84.8 | nM | 7.07 |
| CHEMBL4856336 | — | IC50 | = | 99.9 | nM | 7.00 |
| CHEMBL4849212 | — | IC50 | = | 99.6 | nM | 7.00 |
| CHEMBL4852264 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL4870651 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL4846509 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL4870437 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4865458 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL4871640 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL4861061 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4866177 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL4873420 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL4848746 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL4877720 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL4878459 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL4871737 | — | IC50 | = | 349.0 | nM | 6.46 |
| CHEMBL4876114 | — | IC50 | = | 408.0 | nM | 6.39 |
| CHEMBL4859613 | — | IC50 | = | 433.0 | nM | 6.36 |
| CHEMBL4873676 | — | IC50 | = | 494.0 | nM | 6.31 |
| CHEMBL4869123 | — | IC50 | = | 505.0 | nM | 6.30 |