Assay Detail
Functional
CHEMBL1073095
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Prostaglandin E2 receptor EP4 subtype (CHEMBL1836) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin E2 subtype 4 receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.42 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL601299 | — | — | 1 | 8.80 |
| CHEMBL591431 | — | — | 1 | 8.74 |
| CHEMBL598198 | — | — | 1 | 8.64 |
| CHEMBL597997 | — | — | 1 | 8.60 |
| CHEMBL599052 | — | — | 1 | 8.44 |
| CHEMBL603690 | — | — | 1 | 8.35 |
| CHEMBL605330 | — | — | 1 | 8.33 |
| CHEMBL599262 | — | — | 1 | 8.27 |
| CHEMBL604546 | — | — | 1 | 8.07 |
| CHEMBL599051 | — | — | 1 | 7.92 |
| CHEMBL603462 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL601299 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL591431 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL598198 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL597997 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL599052 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL603690 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL605330 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL599262 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL604546 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL599051 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL603462 | — | IC50 | - | — | - |