Assay Detail
Binding
CHEMBL4349141
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal His6-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf21 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 | 7.47 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4464404 | — | — | 1 | 9.22 |
| CHEMBL4457018 | — | — | 1 | 8.92 |
| CHEMBL4543893 | — | — | 1 | 8.43 |
| CHEMBL4549626 | — | — | 1 | 8.38 |
| CHEMBL4458344 | — | — | 1 | 7.96 |
| CHEMBL4469900 | — | — | 1 | 7.62 |
| CHEMBL4463563 | — | — | 1 | 7.29 |
| CHEMBL4562542 | — | — | 1 | 7.21 |
| CHEMBL4593230 | — | — | 1 | 7.16 |
| CHEMBL4440621 | — | — | 1 | 7.08 |
| CHEMBL4520286 | — | — | 1 | 6.98 |
| CHEMBL4443805 | — | — | 1 | 6.91 |
| CHEMBL4562744 | — | — | 1 | 6.73 |
| CHEMBL4465231 | — | — | 1 | 6.33 |
| CHEMBL4574694 | — | — | 1 | 5.84 |
| CHEMBL4563157 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4464404 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4457018 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4543893 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4549626 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4458344 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4469900 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4463563 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4562542 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4593230 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4440621 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4520286 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL4443805 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL4562744 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL4465231 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4574694 | — | IC50 | = | 1428.0 | nM | 5.84 |
| CHEMBL4563157 | — | IC50 | - | — | - |