Assay Detail
Binding
CHEMBL4413445
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant calcium-independent PLA2 using PAPE as substrate assessed as assessed as reduction in free AA formation after 30 mins in presence of equal molar mixture of PAPA/PAPC/PAPE/PAPG/PAPS/PLPC by HPLC-MS analysis
6
Total Activities
3
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 |
Target
85/88 kDa calcium-independent phospholipase A2 (CHEMBL3213) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Substrate-Specific Inhibition Constants for Phospholipase A<sub>2</sub> Acting on Unique Phospholipid Substrates in Mixed Micelles and Membranes Using Lipidomics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.47 | 7.30 |
| XI50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL89506 | — | — | 2 | 7.30 |
| CHEMBL148674 | VARESPLADIB | 2.0 | 2 | 6.22 |
| CHEMBL4438490 | — | — | 2 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL89506 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL148674 | VARESPLADIB | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4438490 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL148674 | VARESPLADIB | XI50 | = | 0.0008 | uM | - |
| CHEMBL89506 | — | XI50 | = | 7e-05 | uM | - |
| CHEMBL4438490 | — | XI50 | = | 0.0018 | uM | - |