Assay Detail
Functional
CHEMBL1073247
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Prostaglandin E2 receptor EP3 subtype (CHEMBL4336) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.27 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL605833 | — | — | 1 | 7.66 |
| CHEMBL596515 | — | — | 1 | 7.30 |
| CHEMBL595632 | — | — | 1 | 7.14 |
| CHEMBL593041 | — | — | 1 | 6.85 |
| CHEMBL594365 | — | — | 1 | 6.82 |
| CHEMBL594210 | — | — | 1 | 6.48 |
| CHEMBL603653 | — | — | 1 | 6.40 |
| CHEMBL595157 | — | — | 1 | 6.34 |
| CHEMBL595830 | — | — | 1 | 6.27 |
| CHEMBL604897 | — | — | 1 | 6.24 |
| CHEMBL593526 | — | — | 1 | 6.22 |
| CHEMBL595159 | — | — | 1 | 5.92 |
| CHEMBL603625 | — | — | 1 | 5.82 |
| CHEMBL603633 | — | — | 1 | 5.58 |
| CHEMBL596499 | — | — | 1 | 5.52 |
| CHEMBL594423 | — | — | 1 | 5.51 |
| CHEMBL603227 | — | — | 1 | 5.46 |
| CHEMBL593764 | — | — | 1 | 5.32 |
| CHEMBL593260 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL605833 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL596515 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL595632 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL593041 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL594365 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL594210 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL603653 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL595157 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL595830 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL604897 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL593526 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL595159 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL603625 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL603633 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL596499 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL594423 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL603227 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL593764 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL593260 | — | IC50 | > | 10000.0 | nM | - |