Assay Detail
Binding
CHEMBL4151115
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human sPLA2-2A expressed in Escherichia coli BL21(DE3) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins
9
Total Activities
9
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 |
Target
Phospholipase A2, membrane associated (CHEMBL3474) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A2 Type X (sPLA2-X) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.95 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL148674 | VARESPLADIB | 2.0 | 1 | 7.92 |
| CHEMBL4171084 | — | — | 1 | 6.51 |
| CHEMBL4176544 | — | — | 1 | 6.05 |
| CHEMBL4173359 | — | — | 1 | 5.64 |
| CHEMBL4160483 | — | — | 1 | 5.44 |
| CHEMBL4174522 | — | — | 1 | 5.41 |
| CHEMBL4175643 | — | — | 1 | 5.36 |
| CHEMBL4172222 | — | — | 1 | 5.24 |
| CHEMBL4175583 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL148674 | VARESPLADIB | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4171084 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4176544 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL4173359 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4160483 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4174522 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4175643 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4172222 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4175583 | — | IC50 | > | 10000.0 | nM | - |