Assay Detail
Functional
CHEMBL1009645
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant EP1 receptor expressed in CHO cells assessed as inhibition of PGE2-mediated intracellular calcium mobilization by FLIPR method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Prostaglandin E2 receptor EP1 subtype (CHEMBL1811) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP(1) receptor antagonist for the treatment of inflammatory pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 7.57 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL467114 | — | — | 1 | 8.10 |
| CHEMBL467720 | — | — | 1 | 7.60 |
| CHEMBL513491 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL467114 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL467720 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL513491 | — | Ki | = | 100.0 | nM | 7.00 |