Assay Detail
Binding
CHEMBL962347
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Inhibition of GST-tagged FAK assessed as inhibition of poly-Glu-Tyr phosphorylation
32
Total Activities
32
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 | 32 | 7.00 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL487229 | — | — | 1 | 9.30 |
| CHEMBL488247 | — | — | 1 | 9.03 |
| CHEMBL452341 | — | — | 1 | 9.00 |
| CHEMBL472212 | — | — | 1 | 8.82 |
| CHEMBL513744 | — | — | 1 | 8.72 |
| CHEMBL487246 | — | — | 1 | 8.05 |
| CHEMBL471526 | — | — | 1 | 7.80 |
| CHEMBL471357 | — | — | 1 | 7.72 |
| CHEMBL471520 | — | — | 1 | 7.47 |
| CHEMBL520059 | — | — | 1 | 7.42 |
| CHEMBL470316 | — | — | 1 | 7.34 |
| CHEMBL488089 | — | — | 1 | 7.23 |
| CHEMBL455680 | — | — | 1 | 7.14 |
| CHEMBL511152 | — | — | 1 | 7.11 |
| CHEMBL470314 | — | — | 1 | 6.80 |
| CHEMBL529889 | — | — | 1 | 6.77 |
| CHEMBL470317 | — | — | 1 | 6.72 |
| CHEMBL488446 | — | — | 1 | 6.52 |
| CHEMBL472211 | — | — | 1 | 6.21 |
| CHEMBL487227 | — | — | 1 | 6.09 |
| CHEMBL518905 | — | — | 1 | 6.06 |
| CHEMBL519418 | — | — | 1 | 5.89 |
| CHEMBL471698 | — | — | 1 | 5.66 |
| CHEMBL487057 | — | — | 1 | 5.50 |
| CHEMBL455677 | — | — | 1 | 5.48 |
| CHEMBL509485 | — | — | 1 | 5.42 |
| CHEMBL453649 | — | — | 1 | 5.41 |
| CHEMBL452340 | — | — | 1 | 5.39 |
| CHEMBL487228 | — | — | 1 | - |
| CHEMBL507488 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL487229 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL488247 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL452341 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL472212 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL513744 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL487246 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL471526 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL471357 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL471520 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL520059 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL470316 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL488089 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL455680 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL511152 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL470314 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL529889 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL470317 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL488446 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL472211 | — | IC50 | = | 623.0 | nM | 6.21 |
| CHEMBL487227 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL518905 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL519418 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL471698 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL487057 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL455677 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL509485 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL453649 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL452340 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL487228 | — | IC50 | - | — | - | |
| CHEMBL507488 | — | IC50 | - | — | - | |
| CHEMBL471697 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL452342 | — | IC50 | > | 650.0 | nM | - |