Assay Detail
Binding
CHEMBL2149157
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mPGES1 in IL-1beta treated human A549 cell microsomal membrane assessed as inhibition of PGE2 formation incubated for 15 mins before addition of PGH2 by RP-HPLC method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 4.92 | 5.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL29097 | — | — | 1 | 5.68 |
| CHEMBL2147422 | — | — | 1 | 5.28 |
| CHEMBL2147420 | — | — | 1 | 5.13 |
| CHEMBL463574 | RATANIAPHENOL II | — | 1 | 4.96 |
| CHEMBL2147424 | RATANIAPHENOL I | — | 1 | 4.89 |
| CHEMBL2147423 | RATANIAPHENOL III | — | 1 | 4.87 |
| CHEMBL2147421 | — | — | 1 | 4.71 |
| CHEMBL2147418 | — | — | 1 | 4.40 |
| CHEMBL2147419 | — | — | 1 | 4.38 |
| CHEMBL2147415 | — | — | 1 | - |
| CHEMBL2147416 | — | — | 1 | - |
| CHEMBL2147417 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL29097 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2147422 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL2147420 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL463574 | RATANIAPHENOL II | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2147424 | RATANIAPHENOL I | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL2147423 | RATANIAPHENOL III | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL2147421 | — | IC50 | = | 19500.0 | nM | 4.71 |
| CHEMBL2147418 | — | IC50 | = | 39500.0 | nM | 4.40 |
| CHEMBL2147419 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL2147415 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2147416 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2147417 | — | IC50 | > | 50000.0 | nM | - |