Assay Detail
Binding
CHEMBL963082
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Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Prostaglandin E2 receptor EP3 subtype (CHEMBL3710) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
3,4-Disubstituted indole acylsulfonamides: a novel series of potent and selective human EP3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 8.04 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL465122 | — | — | 1 | 9.70 |
| CHEMBL464032 | — | — | 1 | 9.52 |
| CHEMBL466184 | — | — | 1 | 9.15 |
| CHEMBL519598 | — | — | 1 | 8.96 |
| CHEMBL520741 | — | — | 1 | 8.80 |
| CHEMBL464271 | — | — | 1 | 8.72 |
| CHEMBL464031 | — | — | 1 | 8.66 |
| CHEMBL481589 | — | — | 1 | 8.64 |
| CHEMBL480011 | — | — | 1 | 8.59 |
| CHEMBL480809 | — | — | 1 | 8.44 |
| CHEMBL517165 | — | — | 1 | 8.44 |
| CHEMBL520933 | — | — | 1 | 8.41 |
| CHEMBL479433 | — | — | 1 | 8.39 |
| CHEMBL481004 | — | — | 1 | 8.38 |
| CHEMBL464042 | — | — | 1 | 8.30 |
| CHEMBL518396 | — | — | 1 | 8.28 |
| CHEMBL480609 | — | — | 1 | 8.25 |
| CHEMBL480012 | — | — | 1 | 8.24 |
| CHEMBL513305 | — | — | 1 | 8.12 |
| CHEMBL466595 | — | — | 1 | 8.10 |
| CHEMBL517385 | — | — | 1 | 8.01 |
| CHEMBL464063 | — | — | 1 | 8.00 |
| CHEMBL465923 | — | — | 1 | 7.98 |
| CHEMBL469303 | — | — | 1 | 7.97 |
| CHEMBL521103 | — | — | 1 | 7.94 |
| CHEMBL479427 | — | — | 1 | 7.89 |
| CHEMBL482177 | — | — | 1 | 7.88 |
| CHEMBL481783 | — | — | 1 | 7.86 |
| CHEMBL516708 | — | — | 1 | 7.84 |
| CHEMBL517180 | — | — | 1 | 7.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL465122 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL464032 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL466184 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL519598 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL520741 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL464271 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL464031 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL481589 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL480011 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL480809 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL517165 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL520933 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL479433 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL481004 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL464042 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL518396 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL480609 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL480012 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL513305 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL466595 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL517385 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL464063 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL465923 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL469303 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL521103 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL479427 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL482177 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL481783 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL516708 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL517180 | — | IC50 | = | 16.3 | nM | 7.79 |
| CHEMBL512993 | — | IC50 | = | 19.7 | nM | 7.71 |
| CHEMBL479434 | — | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL464270 | — | IC50 | = | 24.6 | nM | 7.61 |
| CHEMBL480992 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL520290 | — | IC50 | = | 27.5 | nM | 7.56 |
| CHEMBL464905 | — | IC50 | = | 31.3 | nM | 7.50 |
| CHEMBL518109 | — | IC50 | = | 33.2 | nM | 7.48 |
| CHEMBL464059 | — | IC50 | = | 33.7 | nM | 7.47 |
| CHEMBL518110 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL481782 | — | IC50 | = | 40.3 | nM | 7.39 |
| CHEMBL479435 | — | IC50 | = | 43.2 | nM | 7.37 |
| CHEMBL482380 | — | IC50 | = | 48.7 | nM | 7.31 |
| CHEMBL481984 | — | IC50 | = | 58.3 | nM | 7.23 |
| CHEMBL482379 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL465947 | — | IC50 | = | 651.0 | nM | 6.19 |