Assay Detail
Binding
CHEMBL1787944
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Inhibition of PYK2 assessed as reduction in peptide substrate phosphorylation by fluorimetric method
13
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Sulfoximine-substituted trifluoromethylpyrimidine analogs as inhibitors of proline-rich tyrosine kinase 2 (PYK2) show reduced hERG activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.31 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2029181 | — | — | 3 | 7.80 |
| CHEMBL2448536 | — | — | 1 | 7.68 |
| CHEMBL2029182 | — | — | 1 | 7.66 |
| CHEMBL472212 | — | — | 1 | 7.51 |
| CHEMBL2029180 | — | — | 3 | 7.37 |
| CHEMBL2029183 | — | — | 1 | 7.19 |
| CHEMBL519418 | — | — | 1 | 7.02 |
| CHEMBL509485 | — | — | 1 | 6.85 |
| CHEMBL1783837 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2029181 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2448536 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2029182 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL472212 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL2029181 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2029180 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL2029181 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL2029183 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL2029180 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL2029180 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL519418 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL509485 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1783837 | — | IC50 | = | 140.0 | nM | 6.85 |