Assay Detail
Binding
CHEMBL4841669
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length N-terminal GST tagged BTK (2 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
55
Total Activities
55
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
Discovery of 1-Amino-1<i>H</i>-imidazole-5-carboxamide Derivatives as Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 55 | 7.53 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 9.05 |
| CHEMBL4878626 | — | — | 1 | 8.72 |
| CHEMBL3936761 | ZANUBRUTINIB | 4.0 | 1 | 8.66 |
| CHEMBL4864983 | — | — | 1 | 8.57 |
| CHEMBL4878421 | — | — | 1 | 8.36 |
| CHEMBL4863913 | — | — | 1 | 8.30 |
| CHEMBL4863836 | — | — | 1 | 8.29 |
| CHEMBL4873581 | — | — | 1 | 8.21 |
| CHEMBL4847730 | — | — | 1 | 8.14 |
| CHEMBL4874550 | — | — | 1 | 8.04 |
| CHEMBL4875714 | — | — | 1 | 8.00 |
| CHEMBL4852838 | — | — | 1 | 7.97 |
| CHEMBL4855886 | — | — | 1 | 7.97 |
| CHEMBL4856243 | — | — | 1 | 7.95 |
| CHEMBL4860527 | — | — | 1 | 7.95 |
| CHEMBL4871950 | — | — | 1 | 7.88 |
| CHEMBL4865483 | — | — | 1 | 7.83 |
| CHEMBL4847824 | — | — | 1 | 7.83 |
| CHEMBL4849268 | — | — | 1 | 7.79 |
| CHEMBL4854001 | — | — | 1 | 7.77 |
| CHEMBL4868899 | — | — | 1 | 7.75 |
| CHEMBL4850186 | — | — | 1 | 7.74 |
| CHEMBL4846437 | — | — | 1 | 7.74 |
| CHEMBL4855655 | — | — | 1 | 7.73 |
| CHEMBL4867982 | — | — | 1 | 7.72 |
| CHEMBL4852748 | — | — | 1 | 7.71 |
| CHEMBL4878506 | — | — | 1 | 7.65 |
| CHEMBL4854853 | — | — | 1 | 7.65 |
| CHEMBL4861285 | — | — | 1 | 7.64 |
| CHEMBL3707348 | ACALABRUTINIB | 4.0 | 1 | 7.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4878626 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3936761 | ZANUBRUTINIB | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4864983 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4878421 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4863913 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4863836 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4873581 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4847730 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4874550 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4875714 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4852838 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL4855886 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL4860527 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL4856243 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL4871950 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL4865483 | — | IC50 | = | 14.7 | nM | 7.83 |
| CHEMBL4847824 | — | IC50 | = | 14.8 | nM | 7.83 |
| CHEMBL4849268 | — | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL4854001 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL4868899 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL4850186 | — | IC50 | = | 18.1 | nM | 7.74 |
| CHEMBL4846437 | — | IC50 | = | 18.4 | nM | 7.74 |
| CHEMBL4855655 | — | IC50 | = | 18.7 | nM | 7.73 |
| CHEMBL4867982 | — | IC50 | = | 18.9 | nM | 7.72 |
| CHEMBL4852748 | — | IC50 | = | 19.4 | nM | 7.71 |
| CHEMBL4854853 | — | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL4878506 | — | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL4861285 | — | IC50 | = | 22.8 | nM | 7.64 |
| CHEMBL3707348 | ACALABRUTINIB | IC50 | = | 23.5 | nM | 7.63 |
| CHEMBL4868393 | — | IC50 | = | 29.2 | nM | 7.54 |
| CHEMBL4853848 | — | IC50 | = | 39.3 | nM | 7.41 |
| CHEMBL4873198 | — | IC50 | = | 44.5 | nM | 7.35 |
| CHEMBL4871608 | — | IC50 | = | 45.6 | nM | 7.34 |
| CHEMBL4874339 | — | IC50 | = | 58.1 | nM | 7.24 |
| CHEMBL4855894 | — | IC50 | = | 79.6 | nM | 7.10 |
| CHEMBL4868212 | — | IC50 | = | 85.7 | nM | 7.07 |
| CHEMBL4873239 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4877159 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4868737 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4856467 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL4855796 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL4862197 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL4875984 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL4875477 | — | IC50 | = | 571.0 | nM | 6.24 |
| CHEMBL4875092 | — | IC50 | = | 2283.0 | nM | 5.64 |
| CHEMBL4847802 | — | IC50 | = | 4755.0 | nM | 5.32 |
| CHEMBL4875125 | — | IC50 | = | 5157.0 | nM | 5.29 |
| CHEMBL4875877 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4847285 | — | IC50 | > | 10000.0 | nM | - |