Assay Detail
Binding
CHEMBL4151113
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Inhibition of recombinant human sPLA2-10 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
32
Total Activities
32
Compounds Tested
2
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 | 27 | 6.06 | 7.58 |
| Inhibition | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4171084 | — | — | 1 | 7.58 |
| CHEMBL148674 | VARESPLADIB | 2.0 | 1 | 7.39 |
| CHEMBL4176544 | — | — | 1 | 7.37 |
| CHEMBL4160483 | — | — | 1 | 7.17 |
| CHEMBL4172222 | — | — | 1 | 7.05 |
| CHEMBL4175583 | — | — | 1 | 7.03 |
| CHEMBL4174522 | — | — | 1 | 6.96 |
| CHEMBL4173359 | — | — | 1 | 6.80 |
| CHEMBL4175643 | — | — | 1 | 6.77 |
| CHEMBL4171797 | — | — | 1 | 6.64 |
| CHEMBL4161605 | — | — | 1 | 6.58 |
| CHEMBL4160502 | — | — | 1 | 6.21 |
| CHEMBL4159939 | — | — | 1 | 6.08 |
| CHEMBL4176269 | — | — | 1 | 6.00 |
| CHEMBL4170085 | — | — | 1 | 5.72 |
| CHEMBL4168202 | — | — | 1 | 5.57 |
| CHEMBL4163859 | — | — | 1 | 5.55 |
| CHEMBL4172025 | — | — | 1 | 5.32 |
| CHEMBL4169491 | — | — | 1 | 5.16 |
| CHEMBL4168275 | — | — | 1 | 5.14 |
| CHEMBL4176688 | — | — | 1 | 4.99 |
| CHEMBL4175476 | — | — | 1 | 4.68 |
| CHEMBL4168405 | — | — | 1 | 4.63 |
| CHEMBL4160366 | — | — | 1 | 4.57 |
| CHEMBL4166071 | — | — | 1 | 4.54 |
| CHEMBL4164836 | — | — | 1 | - |
| CHEMBL4161571 | — | — | 1 | - |
| CHEMBL4176533 | — | — | 1 | - |
| CHEMBL4161426 | — | — | 1 | - |
| CHEMBL4168676 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4171084 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL148674 | VARESPLADIB | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4176544 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4160483 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4172222 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4175583 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4174522 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4173359 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4175643 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4171797 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4161605 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4160502 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL4159939 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4176269 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL4170085 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4168202 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4163859 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4172025 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4169491 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL4168275 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4176688 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL4175476 | — | IC50 | = | 20700.0 | nM | 4.68 |
| CHEMBL4168405 | — | IC50 | = | 23600.0 | nM | 4.63 |
| CHEMBL4160366 | — | IC50 | = | 26900.0 | nM | 4.57 |
| CHEMBL4166071 | — | IC50 | = | 29100.0 | nM | 4.54 |
| CHEMBL4164836 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4161571 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4176533 | — | Inhibition | - | % | - | |
| CHEMBL4161426 | — | Inhibition | - | % | - | |
| CHEMBL4168676 | — | Inhibition | - | % | - | |
| CHEMBL4173162 | — | Inhibition | - | % | - | |
| CHEMBL4165255 | — | Inhibition | - | % | - |