Assay Detail
Binding
CHEMBL3389824
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mPGES-1 in human A549 cells assessed as inhibition of IL-1beta-induced PGE2 production incubated for 30 mins prior to IL-1beta challenge measured after 18 to 24 hrs
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of 2-aryl substituted quinazolin-4(3H)-one, pyrido[4,3-d]pyrimidin-4(3H)-one and pyrido[2,3-d]pyrimidin-4(3H)-one derivatives as microsomal prostaglandin E(2) synthase-1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.72 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3342849 | — | — | 1 | 8.30 |
| CHEMBL3342712 | — | — | 1 | 8.00 |
| CHEMBL3342850 | — | — | 1 | 7.96 |
| CHEMBL3342847 | — | — | 1 | 7.64 |
| CHEMBL3342848 | — | — | 1 | 7.48 |
| CHEMBL3342851 | — | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3342849 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3342712 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3342850 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3342847 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3342848 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3342851 | — | IC50 | = | 111.0 | nM | 6.96 |