Assay Detail
Functional
CHEMBL4125534
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at EP1 receptor (unknown origin) by reporter gene assay
9
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| 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 2-(1H-pyrazolo[3,4-b]pyridin-1-yl)thiazole derivative as an EP1 receptor antagonist and in vivo studies in a bone fracture model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.37 | 9.52 |
| Ki | 1 | 8.06 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4129609 | — | — | 2 | 9.52 |
| CHEMBL3127163 | — | — | 1 | 9.22 |
| CHEMBL4126319 | — | — | 1 | 9.15 |
| CHEMBL4128163 | — | — | 1 | 7.92 |
| CHEMBL4129545 | — | — | 1 | 7.92 |
| CHEMBL4129401 | — | — | 1 | 7.92 |
| CHEMBL4126167 | — | — | 1 | 7.92 |
| CHEMBL4126096 | — | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4129609 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3127163 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4126319 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4129609 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL4128163 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4129545 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4129401 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4126167 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4126096 | — | IC50 | = | 40.0 | nM | 7.40 |