Assay Detail
Binding
CHEMBL1049477
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Inhibition of GST-tagged human LCK by scintillation counting
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 8.86 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL607366 | — | — | 1 | 9.52 |
| CHEMBL591324 | — | — | 1 | 9.39 |
| CHEMBL595398 | — | — | 1 | 9.36 |
| CHEMBL592260 | — | — | 1 | 9.29 |
| CHEMBL592262 | — | — | 1 | 9.26 |
| CHEMBL596079 | — | — | 1 | 9.25 |
| CHEMBL591325 | — | — | 1 | 9.14 |
| CHEMBL601096 | — | — | 1 | 9.12 |
| CHEMBL591793 | — | — | 1 | 9.11 |
| CHEMBL595624 | — | — | 1 | 9.10 |
| CHEMBL582959 | — | — | 1 | 9.03 |
| CHEMBL591326 | — | — | 1 | 9.00 |
| CHEMBL595401 | — | — | 1 | 9.00 |
| CHEMBL605724 | — | — | 1 | 9.00 |
| CHEMBL603859 | — | — | 1 | 8.96 |
| CHEMBL603737 | — | — | 1 | 8.92 |
| CHEMBL591322 | — | — | 1 | 8.92 |
| CHEMBL592261 | — | — | 1 | 8.82 |
| CHEMBL591559 | — | — | 1 | 8.82 |
| CHEMBL595625 | — | — | 1 | 8.70 |
| CHEMBL592259 | — | — | 1 | 8.64 |
| CHEMBL592267 | — | — | 1 | 8.64 |
| CHEMBL600873 | — | — | 1 | 8.55 |
| CHEMBL604694 | — | — | 1 | 8.41 |
| CHEMBL592507 | — | — | 1 | 8.41 |
| CHEMBL592026 | — | — | 1 | 8.32 |
| CHEMBL591091 | — | — | 1 | 8.27 |
| CHEMBL606459 | — | — | 1 | 8.09 |
| CHEMBL596078 | — | — | 1 | 8.00 |
| CHEMBL592505 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL607366 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL591324 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL595398 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL592260 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL592262 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL596079 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL591325 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL601096 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL591793 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL595624 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL582959 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL591326 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL595401 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL605724 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL603859 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL603737 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL591322 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL592261 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL591559 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL595625 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL592259 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL592267 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL600873 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL604694 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL592507 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL592026 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL591091 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL606459 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL596078 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL592505 | — | IC50 | > | 100.0 | nM | - |