Assay Detail
Binding
CHEMBL829926
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory activity against recombinant p56 lck tyrosine kinase expressed as a His-tagged protein in insect cells
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 8.13 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL186480 | — | — | 1 | 9.40 |
| CHEMBL186568 | — | — | 1 | 9.30 |
| CHEMBL186177 | — | — | 1 | 9.22 |
| CHEMBL361065 | — | — | 1 | 8.96 |
| CHEMBL364623 | — | — | 1 | 8.92 |
| CHEMBL189776 | — | — | 1 | 8.92 |
| CHEMBL189771 | — | — | 1 | 8.70 |
| CHEMBL188478 | — | — | 1 | 8.40 |
| CHEMBL187697 | — | — | 1 | 8.40 |
| CHEMBL186363 | — | — | 1 | 8.40 |
| CHEMBL189675 | — | — | 1 | 8.17 |
| CHEMBL188675 | — | — | 1 | 8.14 |
| CHEMBL360810 | — | — | 1 | 8.00 |
| CHEMBL131577 | — | — | 1 | 7.46 |
| CHEMBL186564 | — | — | 1 | 7.30 |
| CHEMBL364868 | — | — | 1 | 6.56 |
| CHEMBL187198 | — | — | 1 | 6.43 |
| CHEMBL364152 | — | — | 1 | 5.63 |
| CHEMBL365505 | — | — | 1 | - |
| CHEMBL189649 | — | — | 1 | - |
| CHEMBL185851 | — | — | 1 | - |
| CHEMBL186498 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL186480 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL186568 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL186177 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL361065 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL364623 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL189776 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL189771 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL188478 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL187697 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL186363 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL189675 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL188675 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL360810 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL131577 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL186564 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL364868 | — | IC50 | = | 277.0 | nM | 6.56 |
| CHEMBL187198 | — | IC50 | = | 374.0 | nM | 6.43 |
| CHEMBL364152 | — | IC50 | = | 2345.0 | nM | 5.63 |
| CHEMBL365505 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL189649 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL185851 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL186498 | — | IC50 | < | 1.0 | nM | - |