Assay Detail
Binding
CHEMBL892787
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Inhibition of human platelet cPLA2-alpha assessed as arachidonic acid release by vesicle assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
1-(5-Carboxy- and 5-carbamoylindol-1-yl)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: bioisosteric replacement of the carboxylic acid and carboxamide moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.59 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL426665 | — | — | 1 | 8.30 |
| CHEMBL30108 | — | — | 1 | 7.96 |
| CHEMBL205892 | — | — | 1 | 7.46 |
| CHEMBL204302 | — | — | 1 | 6.92 |
| CHEMBL242320 | — | — | 1 | 6.51 |
| CHEMBL242960 | — | — | 1 | 6.43 |
| CHEMBL242101 | — | — | 1 | 6.41 |
| CHEMBL397954 | — | — | 1 | 6.30 |
| CHEMBL428391 | — | — | 1 | 6.30 |
| CHEMBL242961 | — | — | 1 | 6.08 |
| CHEMBL241892 | — | — | 1 | 5.96 |
| CHEMBL281211 | ARACHIDONYL TRIFLUOROMETHYLKETONE | — | 1 | 5.64 |
| CHEMBL241891 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL426665 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL30108 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL205892 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL204302 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL242320 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL242960 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL242101 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL397954 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL428391 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL242961 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL241892 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL281211 | ARACHIDONYL TRIFLUOROMETHYLKETONE | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL241891 | — | IC50 | = | 3500.0 | nM | 5.46 |