Assay Detail
Functional
CHEMBL931250
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human EP1 receptor expressed in CHOK1 cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 a novel indole series of EP1 receptor antagonists by scaffold hopping.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.76 | 10.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL402392 | — | — | 1 | 10.20 |
| CHEMBL257134 | — | — | 1 | 9.70 |
| CHEMBL257997 | — | — | 2 | 9.30 |
| CHEMBL402338 | — | — | 1 | 9.00 |
| CHEMBL403407 | — | — | 1 | 8.90 |
| CHEMBL255675 | — | — | 1 | 8.40 |
| CHEMBL401785 | — | — | 1 | 7.90 |
| CHEMBL254763 | — | — | 1 | 7.70 |
| CHEMBL436656 | — | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL402392 | — | Ki | = | 0.0631 | nM | 10.20 |
| CHEMBL257134 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL257997 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL257997 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL402338 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL403407 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL255675 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL401785 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL254763 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL436656 | — | Ki | = | 63.1 | nM | 7.20 |