Assay Detail
Binding
CHEMBL1036476
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Inhibition of mPGES1 in IL1-beta treated human A549 cell microsomal membrane assessed as residual enzyme activity after 1 min by measuring PGE2 level using RP-HPLC method
16
Total Activities
16
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 | Intermediate |
Publication
Arylpyrrolizines as inhibitors of microsomal prostaglandin E2 synthase-1 (mPGES-1) or as dual inhibitors of mPGES-1 and 5-lipoxygenase (5-LOX).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.62 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL182032 | — | — | 1 | 7.92 |
| CHEMBL550489 | — | — | 1 | 5.75 |
| CHEMBL551236 | — | — | 1 | 5.68 |
| CHEMBL29097 | — | — | 1 | 5.68 |
| CHEMBL564318 | — | — | 1 | 5.41 |
| CHEMBL563280 | — | — | 1 | 5.35 |
| CHEMBL550894 | — | — | 1 | 5.32 |
| CHEMBL560898 | — | — | 1 | 5.23 |
| CHEMBL561824 | — | — | 1 | 5.21 |
| CHEMBL300982 | LICOFELONE | 2.0 | 1 | 5.17 |
| CHEMBL549341 | — | — | 1 | 5.14 |
| CHEMBL294159 | — | — | 1 | - |
| CHEMBL292239 | — | — | 1 | - |
| CHEMBL565159 | — | — | 1 | - |
| CHEMBL57062 | — | — | 1 | - |
| CHEMBL560897 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL182032 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL550489 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL551236 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL29097 | — | IC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL564318 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL563280 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL550894 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL560898 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL561824 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL300982 | LICOFELONE | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL549341 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL294159 | — | IC50 | - | — | - | |
| CHEMBL292239 | — | IC50 | - | — | - | |
| CHEMBL565159 | — | IC50 | - | — | - | |
| CHEMBL57062 | — | IC50 | - | — | - | |
| CHEMBL560897 | — | IC50 | - | — | - |