Assay Detail
Binding
CHEMBL4349140
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full-length N-terminal His6-tagged BTK expressed in baculovirus infected Sf21 insect cells using STK substrate by HTRF assay
17
Total Activities
17
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 7H-pyrrolo[2,3-d]pyrimidine derivatives as selective covalent irreversible inhibitors of interleukin-2-inducible T-cell kinase (Itk).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.70 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4464404 | — | — | 1 | 8.41 |
| CHEMBL4438914 | — | — | 1 | 8.10 |
| CHEMBL4457018 | — | — | 1 | 7.58 |
| CHEMBL4458344 | — | — | 1 | 7.46 |
| CHEMBL4549626 | — | — | 1 | 7.44 |
| CHEMBL4469900 | — | — | 1 | 6.57 |
| CHEMBL4593230 | — | — | 1 | 6.54 |
| CHEMBL4543893 | — | — | 1 | 6.36 |
| CHEMBL4440621 | — | — | 1 | 6.03 |
| CHEMBL4443805 | — | — | 1 | 6.00 |
| CHEMBL4465231 | — | — | 1 | 5.84 |
| CHEMBL4463563 | — | — | 1 | 5.83 |
| CHEMBL4520286 | — | — | 1 | 5.83 |
| CHEMBL4562744 | — | — | 1 | 5.79 |
| CHEMBL4563157 | — | — | 1 | - |
| CHEMBL4574694 | — | — | 1 | - |
| CHEMBL4562542 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4464404 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4438914 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4457018 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4458344 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4549626 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4469900 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4593230 | — | IC50 | = | 286.0 | nM | 6.54 |
| CHEMBL4543893 | — | IC50 | = | 434.0 | nM | 6.36 |
| CHEMBL4440621 | — | IC50 | = | 942.0 | nM | 6.03 |
| CHEMBL4443805 | — | IC50 | = | 996.0 | nM | 6.00 |
| CHEMBL4465231 | — | IC50 | = | 1456.0 | nM | 5.84 |
| CHEMBL4463563 | — | IC50 | = | 1481.0 | nM | 5.83 |
| CHEMBL4520286 | — | IC50 | = | 1469.0 | nM | 5.83 |
| CHEMBL4562744 | — | IC50 | = | 1607.0 | nM | 5.79 |
| CHEMBL4563157 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4574694 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4562542 | — | IC50 | > | 3000.0 | nM | - |