Assay Detail
Binding
CHEMBL4841671
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length 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
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 | 13 | 5.94 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 8.30 |
| CHEMBL3936761 | ZANUBRUTINIB | 4.0 | 1 | 7.18 |
| CHEMBL4864983 | — | — | 1 | 6.07 |
| CHEMBL4878626 | — | — | 1 | 5.72 |
| CHEMBL4863836 | — | — | 1 | 5.66 |
| CHEMBL4863913 | — | — | 1 | 5.22 |
| CHEMBL4878421 | — | — | 1 | 4.82 |
| CHEMBL4860527 | — | — | 1 | 4.53 |
| CHEMBL4874550 | — | — | 1 | - |
| CHEMBL4852748 | — | — | 1 | - |
| CHEMBL4847730 | — | — | 1 | - |
| CHEMBL4849268 | — | — | 1 | - |
| CHEMBL3707348 | ACALABRUTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3936761 | ZANUBRUTINIB | IC50 | = | 65.9 | nM | 7.18 |
| CHEMBL4864983 | — | IC50 | = | 847.0 | nM | 6.07 |
| CHEMBL4878626 | — | IC50 | = | 1915.0 | nM | 5.72 |
| CHEMBL4863836 | — | IC50 | = | 2210.0 | nM | 5.66 |
| CHEMBL4863913 | — | IC50 | = | 6057.0 | nM | 5.22 |
| CHEMBL4878421 | — | IC50 | = | 15295.0 | nM | 4.82 |
| CHEMBL4860527 | — | IC50 | = | 29485.0 | nM | 4.53 |
| CHEMBL4874550 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4852748 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4847730 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4849268 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3707348 | ACALABRUTINIB | IC50 | > | 30000.0 | nM | - |