Assay Detail
Binding
CHEMBL889917
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human EP1 receptor
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
The discovery of 6-[2-(5-chloro-2-{[(2,4-difluorophenyl)methyl]oxy}phenyl)-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid, GW848687X, a potent and selective prostaglandin EP1 receptor antagonist for the treatment of inflammatory pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.60 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL389796 | — | — | 1 | 8.80 |
| CHEMBL389996 | — | — | 1 | 8.70 |
| CHEMBL234940 | — | — | 1 | 8.60 |
| CHEMBL390188 | — | — | 1 | 8.60 |
| CHEMBL395542 | — | — | 1 | 8.50 |
| CHEMBL207577 | — | — | 1 | 8.30 |
| CHEMBL387605 | — | — | 1 | 8.30 |
| CHEMBL395582 | — | — | 1 | 8.20 |
| CHEMBL233245 | — | — | 1 | 8.20 |
| CHEMBL233043 | — | — | 1 | 8.00 |
| CHEMBL397687 | — | — | 1 | 7.90 |
| CHEMBL428370 | — | — | 1 | 7.90 |
| CHEMBL234709 | — | — | 1 | 7.80 |
| CHEMBL234710 | — | — | 1 | 7.80 |
| CHEMBL395284 | — | — | 1 | 7.70 |
| CHEMBL233230 | — | — | 1 | 7.60 |
| CHEMBL389596 | — | — | 1 | 7.50 |
| CHEMBL234280 | — | — | 1 | 7.40 |
| CHEMBL397957 | — | — | 1 | 7.40 |
| CHEMBL233044 | — | — | 1 | 7.40 |
| CHEMBL234290 | — | — | 1 | 7.40 |
| CHEMBL388655 | — | — | 1 | 7.30 |
| CHEMBL234281 | — | — | 1 | 7.20 |
| CHEMBL265086 | — | — | 1 | 7.10 |
| CHEMBL395311 | — | — | 1 | 7.10 |
| CHEMBL234069 | — | — | 1 | 7.00 |
| CHEMBL233858 | — | — | 1 | 7.00 |
| CHEMBL234924 | — | — | 1 | 7.00 |
| CHEMBL234939 | — | — | 1 | 6.80 |
| CHEMBL234289 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL389796 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL389996 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL234940 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL390188 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL395542 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL207577 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL387605 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL395582 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL233245 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL233043 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL397687 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL428370 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL234709 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL234710 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL395284 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL233230 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL389596 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL234280 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL397957 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL233044 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL234290 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL388655 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL234281 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL265086 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL395311 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL234069 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL233858 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL234924 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL234939 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL234289 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL389994 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL234082 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL233231 | — | IC50 | = | 398.11 | nM | 6.40 |