Assay Detail
Binding
CHEMBL1068501
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Inhibition of mPGES1 in IL1-beta induced human A549 cell microsomal membrane assessed as blockade of conversion of PGH2 to PGE2
17
Total Activities
17
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
Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E(2) synthase-1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.94 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL523292 | — | — | 1 | 7.00 |
| CHEMBL521164 | — | — | 1 | 6.70 |
| CHEMBL519508 | — | — | 1 | 6.30 |
| CHEMBL490461 | — | — | 1 | 6.22 |
| CHEMBL520317 | — | — | 1 | 6.22 |
| CHEMBL490460 | — | — | 1 | 5.80 |
| CHEMBL527421 | — | — | 1 | 5.77 |
| CHEMBL29097 | — | — | 1 | 5.70 |
| CHEMBL595040 | — | — | 1 | 5.55 |
| CHEMBL605093 | — | — | 1 | 5.51 |
| CHEMBL490656 | — | — | 1 | 5.47 |
| CHEMBL519337 | — | — | 1 | 5.04 |
| CHEMBL595490 | — | — | 1 | - |
| CHEMBL482849 | — | — | 1 | - |
| CHEMBL486691 | — | — | 1 | - |
| CHEMBL508183 | — | — | 1 | - |
| CHEMBL212366 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL523292 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL521164 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL519508 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL490461 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL520317 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL490460 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL527421 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL29097 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL595040 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL605093 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL490656 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL519337 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL595490 | — | IC50 | - | — | - | |
| CHEMBL482849 | — | IC50 | - | — | - | |
| CHEMBL486691 | — | IC50 | - | — | - | |
| CHEMBL508183 | — | IC50 | - | — | - | |
| CHEMBL212366 | — | IC50 | - | — | - |