Assay Detail
Binding
CHEMBL1768451
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Inhibition of Src after 10 mins by radiometric phosphate incorporation assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Proto-oncogene tyrosine-protein kinase Src (CHEMBL267) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.36 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1738829 | — | — | 1 | 7.40 |
| CHEMBL1765781 | — | — | 1 | 6.92 |
| CHEMBL1765774 | — | — | 1 | 6.85 |
| CHEMBL1765776 | — | — | 1 | 6.66 |
| CHEMBL1765782 | — | — | 1 | 6.55 |
| CHEMBL1765783 | — | — | 1 | 6.52 |
| CHEMBL1765777 | — | — | 1 | 6.32 |
| CHEMBL1765784 | — | — | 1 | 6.32 |
| CHEMBL1765779 | — | — | 1 | 6.23 |
| CHEMBL1765780 | — | — | 1 | 6.23 |
| CHEMBL1765775 | — | — | 1 | 5.92 |
| CHEMBL1765770 | — | — | 1 | 5.88 |
| CHEMBL1765097 | — | — | 1 | 5.75 |
| CHEMBL1765772 | — | — | 1 | 5.55 |
| CHEMBL1765778 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1738829 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL1765781 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL1765774 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL1765776 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL1765782 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL1765783 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL1765777 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL1765784 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL1765779 | — | Ki | = | 590.0 | nM | 6.23 |
| CHEMBL1765780 | — | Ki | = | 590.0 | nM | 6.23 |
| CHEMBL1765775 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL1765770 | — | Ki | = | 1320.0 | nM | 5.88 |
| CHEMBL1765097 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL1765772 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL1765778 | — | Ki | > | 4000.0 | nM | - |