Assay Detail
Binding
CHEMBL960612
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Inhibition of GST-tagged pyk2 assessed as inhibition of poly-Glu-Tyr phosphorylation
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): structure-activity relationships and strategies for the elimination of reactive metabolite formation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.12 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL452341 | — | — | 1 | 8.70 |
| CHEMBL487229 | — | — | 1 | 8.30 |
| CHEMBL455680 | — | — | 1 | 8.22 |
| CHEMBL488089 | — | — | 1 | 7.82 |
| CHEMBL529889 | — | — | 1 | 7.77 |
| CHEMBL487057 | — | — | 1 | 7.60 |
| CHEMBL487228 | — | — | 1 | 7.48 |
| CHEMBL488247 | — | — | 1 | 7.46 |
| CHEMBL488446 | — | — | 1 | 7.31 |
| CHEMBL452342 | — | — | 1 | 7.30 |
| CHEMBL487227 | — | — | 1 | 7.28 |
| CHEMBL472211 | — | — | 1 | 7.17 |
| CHEMBL519418 | — | — | 1 | 7.02 |
| CHEMBL471520 | — | — | 1 | 6.92 |
| CHEMBL518905 | — | — | 1 | 6.84 |
| CHEMBL509485 | — | — | 1 | 6.81 |
| CHEMBL513744 | — | — | 1 | 6.72 |
| CHEMBL520059 | — | — | 1 | 6.68 |
| CHEMBL470316 | — | — | 1 | 6.24 |
| CHEMBL471526 | — | — | 1 | 6.22 |
| CHEMBL471357 | — | — | 1 | 6.17 |
| CHEMBL470314 | — | — | 1 | 5.92 |
| CHEMBL470317 | — | — | 1 | 5.75 |
| CHEMBL511152 | — | — | 1 | - |
| CHEMBL471698 | — | — | 1 | - |
| CHEMBL487246 | — | — | 1 | - |
| CHEMBL471697 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL452341 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL487229 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL455680 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL488089 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL529889 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL487057 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL487228 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL488247 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL488446 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL452342 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL487227 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL472211 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL519418 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL471520 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL518905 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL509485 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL513744 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL520059 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL470316 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL471526 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL471357 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL470314 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL470317 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL511152 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL471698 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL487246 | — | IC50 | > | 1100.0 | nM | - |
| CHEMBL471697 | — | IC50 | > | 10000.0 | nM | - |