Assay Detail
Binding
CHEMBL4349139
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal His6-tagged ITK (352 to 617 residues) expressed in baculovirus infected Sf21 insect cells using STK substrate by HTRF assay
20
Total Activities
17
Compounds Tested
2
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 | 8.18 | 9.30 |
| Ki | 3 | 7.97 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4464404 | — | — | 1 | 9.30 |
| CHEMBL4457018 | — | — | 1 | 8.89 |
| CHEMBL4593230 | — | — | 1 | 8.66 |
| CHEMBL4463563 | — | — | 1 | 8.64 |
| CHEMBL4440621 | — | — | 1 | 8.44 |
| CHEMBL4443805 | — | — | 2 | 8.43 |
| CHEMBL4469900 | — | — | 2 | 8.43 |
| CHEMBL4520286 | — | — | 1 | 8.29 |
| CHEMBL4438914 | — | — | 1 | 8.27 |
| CHEMBL4465231 | — | — | 1 | 8.27 |
| CHEMBL4458344 | — | — | 2 | 8.24 |
| CHEMBL4562744 | — | — | 1 | 8.15 |
| CHEMBL4543893 | — | — | 1 | 8.11 |
| CHEMBL4562542 | — | — | 1 | 7.26 |
| CHEMBL4574694 | — | — | 1 | 7.13 |
| CHEMBL4563157 | — | — | 1 | 6.43 |
| CHEMBL4549626 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4464404 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4457018 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4593230 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4463563 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4440621 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4443805 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4469900 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4520286 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4465231 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4438914 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4458344 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL4443805 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL4562744 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL4543893 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4469900 | — | Ki | = | 33.7 | nM | 7.47 |
| CHEMBL4562542 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4574694 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4563157 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL4458344 | — | IC50 | < | 1.26 | nM | - |
| CHEMBL4549626 | — | IC50 | < | 1.26 | nM | - |