Assay Detail
Binding
CHEMBL856877
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Binding affinity to human EP2 receptor expressed in HEK293 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Prostaglandin E2 receptor EP2 subtype (CHEMBL1881) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 6.56 | 6.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL426559 | LAROPIPRANT | 4.0 | 1 | 6.87 |
| CHEMBL383484 | — | — | 1 | 6.64 |
| CHEMBL385126 | — | — | 1 | 6.51 |
| CHEMBL207203 | — | — | 1 | 6.41 |
| CHEMBL426387 | — | — | 1 | 6.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL426559 | LAROPIPRANT | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL383484 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL385126 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL207203 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL426387 | — | Ki | = | 410.0 | nM | 6.39 |