Assay Detail
Binding
CHEMBL931249
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Displacement of [3H]PGE2 from human EP1 receptor expressed in CHOK1 cells
38
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| IC50 | 38 | 7.45 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL257134 | — | — | 1 | 8.40 |
| CHEMBL258184 | — | — | 1 | 8.20 |
| CHEMBL257997 | — | — | 2 | 8.20 |
| CHEMBL255675 | — | — | 1 | 8.20 |
| CHEMBL255652 | — | — | 1 | 8.20 |
| CHEMBL403892 | — | — | 1 | 8.20 |
| CHEMBL255009 | — | — | 1 | 8.10 |
| CHEMBL402338 | — | — | 1 | 8.10 |
| CHEMBL402656 | — | — | 1 | 8.00 |
| CHEMBL402392 | — | — | 1 | 7.90 |
| CHEMBL401768 | — | — | 1 | 7.60 |
| CHEMBL403407 | — | — | 1 | 7.60 |
| CHEMBL254764 | — | — | 1 | 7.50 |
| CHEMBL255880 | — | — | 1 | 7.50 |
| CHEMBL256334 | — | — | 1 | 7.40 |
| CHEMBL257135 | — | — | 1 | 7.40 |
| CHEMBL403082 | — | — | 1 | 7.40 |
| CHEMBL403890 | — | — | 1 | 7.40 |
| CHEMBL257998 | — | — | 1 | 7.40 |
| CHEMBL402608 | — | — | 1 | 7.30 |
| CHEMBL254763 | — | — | 1 | 7.20 |
| CHEMBL401698 | — | — | 1 | 7.00 |
| CHEMBL404309 | — | — | 1 | 7.00 |
| CHEMBL404176 | — | — | 1 | 6.90 |
| CHEMBL257413 | — | — | 1 | 6.80 |
| CHEMBL436656 | — | — | 1 | 6.80 |
| CHEMBL401785 | — | — | 1 | 6.80 |
| CHEMBL258041 | — | — | 1 | 6.80 |
| CHEMBL256336 | — | — | 1 | 6.60 |
| CHEMBL255928 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL257134 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL257997 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL258184 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL257997 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL255675 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL255652 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL403892 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL402338 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL255009 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL402656 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL402392 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL401768 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL403407 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL254764 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL255880 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL256334 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL403082 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL257135 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL257998 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL403890 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL402608 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL254763 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL401698 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL404309 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL404176 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL401785 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL258041 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL436656 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL257413 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL256336 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL255928 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL255319 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL255669 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL255929 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL255909 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL257144 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL258374 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL257792 | — | IC50 | < | 1000.0 | nM | - |