Assay Detail
Binding
CHEMBL4151117
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Inhibition of recombinant human sPLA2-5 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
4
Total Activities
4
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
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 | 4 | 6.00 | 6.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL148674 | VARESPLADIB | 2.0 | 1 | 6.91 |
| CHEMBL4171084 | — | — | 1 | 5.65 |
| CHEMBL4176544 | — | — | 1 | 5.43 |
| CHEMBL4173359 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL148674 | VARESPLADIB | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL4171084 | — | IC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL4176544 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4173359 | — | IC50 | > | 10000.0 | nM | - |