Assay Detail
Binding
CHEMBL992544
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Inhibition of human ITK expressed in chicken DT40 cells assessed as B cell receptor-stimulated calcium influx by FLIPR assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | DT40 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Itk kinase inhibitors: initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.24 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL462301 | — | — | 1 | 6.80 |
| CHEMBL484766 | — | — | 1 | 6.58 |
| CHEMBL485556 | — | — | 1 | 6.52 |
| CHEMBL483581 | — | — | 1 | 6.48 |
| CHEMBL460824 | — | — | 1 | 6.47 |
| CHEMBL485203 | — | — | 1 | 6.47 |
| CHEMBL484945 | — | — | 1 | 6.43 |
| CHEMBL490269 | — | — | 1 | 6.30 |
| CHEMBL485030 | — | — | 1 | 6.14 |
| CHEMBL485626 | — | — | 1 | 5.96 |
| CHEMBL519033 | — | — | 1 | 5.64 |
| CHEMBL485201 | — | — | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL462301 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL484766 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL485556 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL483581 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL460824 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL485203 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL484945 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL490269 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL485030 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL485626 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL519033 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL485201 | — | IC50 | = | 7200.0 | nM | 5.14 |