Assay Detail
Binding
CHEMBL3761674
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Inhibition of mPGES1 in rhIL-1beta-stimulated human A549 cells assessed as PGE2 level treated for 18 hrs after 30 mins pre-incubation with rhIL-1beta by EIA method
19
Total Activities
19
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
Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.26 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3342693 | — | — | 1 | 7.92 |
| CHEMBL3758953 | — | — | 1 | 7.72 |
| CHEMBL3758924 | — | — | 1 | 7.43 |
| CHEMBL3759288 | — | — | 1 | 7.41 |
| CHEMBL412099 | — | — | 1 | 7.12 |
| CHEMBL3758222 | — | — | 1 | 7.01 |
| CHEMBL2152710 | — | — | 1 | 6.55 |
| CHEMBL3758879 | — | — | 1 | 6.14 |
| CHEMBL2152712 | LY-3031207 | 1.0 | 1 | 6.06 |
| CHEMBL3758663 | — | — | 1 | 5.91 |
| CHEMBL3758186 | — | — | 1 | 5.91 |
| CHEMBL2152711 | — | — | 1 | 5.56 |
| CHEMBL3760103 | — | — | 1 | 5.50 |
| CHEMBL3759737 | — | — | 1 | 5.49 |
| CHEMBL3758743 | — | — | 1 | 5.49 |
| CHEMBL3759709 | — | — | 1 | 5.33 |
| CHEMBL3760032 | — | — | 1 | 5.05 |
| CHEMBL3759119 | — | — | 1 | 5.05 |
| CHEMBL3758980 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3342693 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3758953 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3758924 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3759288 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL412099 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3758222 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL2152710 | — | IC50 | = | 284.0 | nM | 6.55 |
| CHEMBL3758879 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL2152712 | LY-3031207 | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL3758663 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL3758186 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL2152711 | — | IC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL3760103 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL3759737 | — | IC50 | = | 3230.0 | nM | 5.49 |
| CHEMBL3758743 | — | IC50 | = | 3250.0 | nM | 5.49 |
| CHEMBL3759709 | — | IC50 | = | 4620.0 | nM | 5.33 |
| CHEMBL3760032 | — | IC50 | = | 8860.0 | nM | 5.05 |
| CHEMBL3759119 | — | IC50 | = | 8850.0 | nM | 5.05 |
| CHEMBL3758980 | — | IC50 | > | 10000.0 | nM | - |