Assay Detail
Binding
CHEMBL3361803
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of cPLA2alpha isolated from human U937 cell cytoplasm assessed as suppression of [14C]arachidonic acid release from L-alpha-1-palmitoyl-2-[14C]arachidonyl-phosphatidylcholine liposomes substrate by scintillation counting
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U-937 |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and biological evaluation of 3-(1-Aryl-1H-indol-5-yl)propanoic acids as new indole-based cytosolic phospholipase A2α inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 6.62 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL272342 | EFIPLADIB | 2.0 | 1 | 9.27 |
| CHEMBL3327088 | — | — | 1 | 8.15 |
| CHEMBL3326971 | — | — | 1 | 8.15 |
| CHEMBL3326966 | — | — | 1 | 7.96 |
| CHEMBL3327089 | — | — | 1 | 7.85 |
| CHEMBL3326970 | — | — | 1 | 7.82 |
| CHEMBL3327092 | — | — | 1 | 7.70 |
| CHEMBL3326969 | — | — | 1 | 7.58 |
| CHEMBL3327090 | — | — | 1 | 7.55 |
| CHEMBL3327094 | — | — | 1 | 7.44 |
| CHEMBL3327095 | — | — | 1 | 7.24 |
| CHEMBL3326948 | — | — | 1 | 7.12 |
| CHEMBL3327093 | — | — | 1 | 7.11 |
| CHEMBL3326949 | — | — | 1 | 6.89 |
| CHEMBL3327091 | — | — | 1 | 6.85 |
| CHEMBL3326947 | — | — | 1 | 6.75 |
| CHEMBL3326967 | — | — | 1 | 6.72 |
| CHEMBL3326960 | — | — | 1 | 6.50 |
| CHEMBL3326964 | — | — | 1 | 6.40 |
| CHEMBL3326950 | — | — | 1 | 6.24 |
| CHEMBL3326952 | — | — | 1 | 6.14 |
| CHEMBL3326968 | — | — | 1 | 6.11 |
| CHEMBL3326956 | — | — | 1 | 6.01 |
| CHEMBL3327096 | — | — | 1 | 6.00 |
| CHEMBL3326953 | — | — | 1 | 6.00 |
| CHEMBL3326959 | — | — | 1 | 5.92 |
| CHEMBL3326951 | — | — | 1 | 5.92 |
| CHEMBL3326954 | — | — | 1 | 5.85 |
| CHEMBL3326965 | — | — | 1 | 5.80 |
| CHEMBL3326963 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL272342 | EFIPLADIB | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL3327088 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3326971 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3326966 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3327089 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3326970 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3327092 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3326969 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3327090 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3327094 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3327095 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3326948 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL3327093 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL3326949 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3327091 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3326947 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3326967 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3326960 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3326964 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3326950 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL3326952 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL3326968 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL3326956 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL3327096 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3326953 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3326959 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3326951 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3326954 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3326965 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3326963 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3326961 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL3327097 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3326957 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL3326962 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL3326955 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL3326958 | — | IC50 | > | 100000.0 | nM | - |