Assay Detail
Functional
CHEMBL870037
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against PGE2 activated EP1 receptor assessed as ability to inhibit intracellular calcium mobilisation by FLIPR
21
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Prostaglandin E2 receptor EP1 subtype (CHEMBL1811) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel biaryl heterocyclic EP1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 8.29 | 9.52 |
| Log Ki | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL362543 | — | — | 2 | 9.52 |
| CHEMBL383090 | — | — | 1 | 9.23 |
| CHEMBL377852 | — | — | 1 | 9.15 |
| CHEMBL207293 | — | — | 1 | 8.45 |
| CHEMBL207577 | — | — | 1 | 8.37 |
| CHEMBL206096 | — | — | 1 | 8.18 |
| CHEMBL207688 | — | — | 1 | 7.81 |
| CHEMBL210268 | — | — | 1 | 7.55 |
| CHEMBL207174 | — | — | 1 | 7.54 |
| CHEMBL207395 | — | — | 1 | 7.28 |
| CHEMBL209244 | — | — | 1 | 6.86 |
| CHEMBL207460 | — | — | 1 | - |
| CHEMBL380667 | — | — | 1 | - |
| CHEMBL377649 | — | — | 1 | - |
| CHEMBL377932 | — | — | 1 | - |
| CHEMBL207849 | — | — | 1 | - |
| CHEMBL381908 | — | — | 1 | - |
| CHEMBL207576 | — | — | 1 | - |
| CHEMBL208030 | — | — | 1 | - |
| CHEMBL207175 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL362543 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL362543 | — | Ki | = | 0.309 | nM | 9.51 |
| CHEMBL383090 | — | Ki | = | 0.5888 | nM | 9.23 |
| CHEMBL377852 | — | Ki | = | 0.7079 | nM | 9.15 |
| CHEMBL207293 | — | Ki | = | 3.548 | nM | 8.45 |
| CHEMBL207577 | — | Ki | = | 4.266 | nM | 8.37 |
| CHEMBL206096 | — | Ki | = | 6.607 | nM | 8.18 |
| CHEMBL207688 | — | Ki | = | 15.49 | nM | 7.81 |
| CHEMBL210268 | — | Ki | = | 28.18 | nM | 7.55 |
| CHEMBL207174 | — | Ki | = | 28.84 | nM | 7.54 |
| CHEMBL207395 | — | Ki | = | 52.48 | nM | 7.28 |
| CHEMBL209244 | — | Ki | = | 138.04 | nM | 6.86 |
| CHEMBL207460 | — | Ki | < | 1000.0 | nM | - |
| CHEMBL380667 | — | Log Ki | - | — | - | |
| CHEMBL377649 | — | Log Ki | - | — | - | |
| CHEMBL377932 | — | Log Ki | - | — | - | |
| CHEMBL207849 | — | Log Ki | - | — | - | |
| CHEMBL381908 | — | Ki | < | 1000.0 | nM | - |
| CHEMBL207576 | — | Ki | < | 1000.0 | nM | - |
| CHEMBL208030 | — | Log Ki | - | — | - | |
| CHEMBL207175 | — | Log Ki | - | — | - |