Assay Detail
Binding
CHEMBL3761047
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 preincubated for 15 mins by HPLC analysis
11
Total Activities
11
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
Can Small Chemical Modifications of Natural Pan-inhibitors Modulate the Biological Selectivity? The Case of Curcumin Prenylated Derivatives Acting as HDAC or mPGES-1 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.84 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL140 | CURCUMIN | 3.0 | 1 | 6.66 |
| CHEMBL1087690 | — | — | 1 | 6.03 |
| CHEMBL3758791 | — | — | 1 | 5.99 |
| CHEMBL1087807 | — | — | 1 | 5.70 |
| CHEMBL3758528 | — | — | 1 | 5.70 |
| CHEMBL3758432 | — | — | 1 | 5.70 |
| CHEMBL3758253 | — | — | 1 | 5.70 |
| CHEMBL3758656 | — | — | 1 | 5.70 |
| CHEMBL3759699 | — | — | 1 | 5.70 |
| CHEMBL3759529 | — | — | 1 | 5.70 |
| CHEMBL3759749 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL140 | CURCUMIN | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1087690 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL3758791 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL1087807 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3758528 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3758432 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3758253 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3758656 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3759699 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3759529 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3759749 | — | IC50 | = | 2000.0 | nM | 5.70 |