Assay Detail
Binding
CHEMBL1009646
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]PGE2 from human EP1 receptor expressed in CHO cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP(1) receptor antagonist for the treatment of inflammatory pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.62 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2110364 | — | — | 1 | 9.89 |
| CHEMBL234940 | — | — | 1 | 8.60 |
| CHEMBL233043 | — | — | 1 | 8.00 |
| CHEMBL467720 | — | — | 1 | 8.00 |
| CHEMBL513491 | — | — | 1 | 7.90 |
| CHEMBL467114 | — | — | 1 | 7.90 |
| CHEMBL467510 | — | — | 1 | 7.80 |
| CHEMBL466101 | — | — | 1 | 7.60 |
| CHEMBL511252 | — | — | 1 | 7.50 |
| CHEMBL466103 | — | — | 1 | 7.40 |
| CHEMBL467113 | — | — | 1 | 7.40 |
| CHEMBL257998 | — | — | 1 | 7.40 |
| CHEMBL466102 | — | — | 1 | 7.10 |
| CHEMBL508276 | — | — | 1 | 7.10 |
| CHEMBL511733 | — | — | 1 | 7.00 |
| CHEMBL468723 | — | — | 1 | 7.00 |
| CHEMBL258041 | — | — | 1 | 6.80 |
| CHEMBL511919 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2110364 | — | IC50 | = | 0.1288 | nM | 9.89 |
| CHEMBL234940 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL233043 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL467720 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL513491 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL467114 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL467510 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL466101 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL511252 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL466103 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL467113 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL257998 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL466102 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL508276 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL511733 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL468723 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL258041 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL511919 | — | IC50 | = | 199.53 | nM | 6.70 |