Assay Detail
Binding
CHEMBL4431157
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Inhibition of recombinant sPLA2-10 (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins by colorimetric method
11
Total Activities
11
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 AZD2716: A Novel Secreted Phospholipase A<sub>2</sub> (sPLA<sub>2</sub>) Inhibitor for the Treatment of Coronary Artery Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.07 | 7.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL148674 | VARESPLADIB | 2.0 | 1 | 7.39 |
| CHEMBL4457557 | — | — | 1 | 6.55 |
| CHEMBL4593409 | — | — | 1 | 6.40 |
| CHEMBL4533403 | — | — | 1 | 6.37 |
| CHEMBL4453126 | — | — | 1 | 6.24 |
| CHEMBL4451830 | — | — | 1 | 6.12 |
| CHEMBL4468927 | — | — | 1 | 5.96 |
| CHEMBL4536076 | — | — | 1 | 5.66 |
| CHEMBL4469134 | — | — | 1 | 5.43 |
| CHEMBL4555962 | — | — | 1 | 5.42 |
| CHEMBL4591759 | — | — | 1 | 5.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL148674 | VARESPLADIB | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4457557 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4593409 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4533403 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4453126 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4451830 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4468927 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4536076 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4469134 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4555962 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4591759 | — | IC50 | = | 5400.0 | nM | 5.27 |