Assay Detail
Binding
CHEMBL4413446
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 reduction in 16:0 LPC 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 | 6.42 | 7.20 |
| XI50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL89506 | — | — | 2 | 7.20 |
| CHEMBL148674 | VARESPLADIB | 2.0 | 2 | 6.23 |
| CHEMBL4438490 | — | — | 2 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL89506 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL148674 | VARESPLADIB | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4438490 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL148674 | VARESPLADIB | XI50 | = | 0.0009 | uM | - |
| CHEMBL89506 | — | XI50 | = | 9e-05 | uM | - |
| CHEMBL4438490 | — | XI50 | = | 0.0022 | uM | - |