Assay Detail
Binding
CHEMBL4349142
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-tagged EGFR kinase domain (696 to end residues) expressed in baculovirus infected Sf21 insect cells using STK as substrate by HTRF assay
16
Total Activities
16
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 | 16 | 6.66 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4464404 | — | — | 1 | 8.64 |
| CHEMBL4457018 | — | — | 1 | 8.06 |
| CHEMBL4549626 | — | — | 1 | 7.42 |
| CHEMBL4458344 | — | — | 1 | 6.86 |
| CHEMBL4593230 | — | — | 1 | 6.82 |
| CHEMBL4469900 | — | — | 1 | 6.30 |
| CHEMBL4520286 | — | — | 1 | 6.18 |
| CHEMBL4463563 | — | — | 1 | 6.04 |
| CHEMBL4562744 | — | — | 1 | 6.03 |
| CHEMBL4465231 | — | — | 1 | 5.98 |
| CHEMBL4443805 | — | — | 1 | 5.90 |
| CHEMBL4543893 | — | — | 1 | 5.70 |
| CHEMBL4563157 | — | — | 1 | - |
| CHEMBL4440621 | — | — | 1 | - |
| CHEMBL4574694 | — | — | 1 | - |
| CHEMBL4562542 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4464404 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4457018 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4549626 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4458344 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL4593230 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4469900 | — | IC50 | = | 499.0 | nM | 6.30 |
| CHEMBL4520286 | — | IC50 | = | 654.0 | nM | 6.18 |
| CHEMBL4463563 | — | IC50 | = | 903.0 | nM | 6.04 |
| CHEMBL4562744 | — | IC50 | = | 937.0 | nM | 6.03 |
| CHEMBL4465231 | — | IC50 | = | 1048.0 | nM | 5.98 |
| CHEMBL4443805 | — | IC50 | = | 1257.0 | nM | 5.90 |
| CHEMBL4543893 | — | IC50 | = | 1975.0 | nM | 5.70 |
| CHEMBL4563157 | — | IC50 | - | — | - | |
| CHEMBL4440621 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4574694 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4562542 | — | IC50 | > | 3000.0 | nM | - |