Assay Detail
Binding
CHEMBL923246
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Inhibition of cPLA2-alpha in TPA-stimulated intact human platelets assessed as liberation of arachidonic acid after 60 mins
5
Total Activities
5
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
1-(2-Carboxyindol-5-yloxy)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: synthesis, biological activity, metabolic stability, and solubility.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.54 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL205892 | — | — | 1 | 7.75 |
| CHEMBL260248 | — | — | 1 | 6.52 |
| CHEMBL260708 | — | — | 1 | 6.30 |
| CHEMBL260365 | — | — | 1 | 6.22 |
| CHEMBL260247 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL205892 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL260248 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL260708 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL260365 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL260247 | — | IC50 | = | 1300.0 | nM | 5.89 |