Assay Detail
Binding
CHEMBL963081
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]PGE2 from human EP3 receptor
67
Total Activities
67
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 | 67 | 7.95 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL479434 | — | — | 1 | 9.30 |
| CHEMBL465947 | — | — | 1 | 9.15 |
| CHEMBL482379 | — | — | 1 | 8.92 |
| CHEMBL519598 | — | — | 1 | 8.89 |
| CHEMBL518396 | — | — | 1 | 8.89 |
| CHEMBL482380 | — | — | 1 | 8.85 |
| CHEMBL479427 | — | — | 1 | 8.77 |
| CHEMBL480011 | — | — | 1 | 8.74 |
| CHEMBL466184 | — | — | 1 | 8.70 |
| CHEMBL464031 | — | — | 1 | 8.70 |
| CHEMBL464063 | — | — | 1 | 8.66 |
| CHEMBL465923 | — | — | 1 | 8.60 |
| CHEMBL481582 | — | — | 1 | 8.55 |
| CHEMBL467632 | — | — | 1 | 8.52 |
| CHEMBL520290 | — | — | 1 | 8.52 |
| CHEMBL479433 | — | — | 1 | 8.47 |
| CHEMBL481589 | — | — | 1 | 8.44 |
| CHEMBL479435 | — | — | 1 | 8.44 |
| CHEMBL517180 | — | — | 1 | 8.44 |
| CHEMBL480992 | — | — | 1 | 8.41 |
| CHEMBL517165 | — | — | 1 | 8.35 |
| CHEMBL480809 | — | — | 1 | 8.33 |
| CHEMBL520933 | — | — | 1 | 8.33 |
| CHEMBL518110 | — | — | 1 | 8.28 |
| CHEMBL518109 | — | — | 1 | 8.24 |
| CHEMBL481004 | — | — | 1 | 8.24 |
| CHEMBL520425 | — | — | 1 | 8.23 |
| CHEMBL466595 | — | — | 1 | 8.21 |
| CHEMBL517385 | — | — | 1 | 8.12 |
| CHEMBL481984 | — | — | 1 | 8.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL479434 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL465947 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL482379 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL519598 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL518396 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL482380 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL479427 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL480011 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL466184 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL464031 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL464063 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL465923 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL481582 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL467632 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL520290 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL479433 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL481589 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL479435 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL517180 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL480992 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL517165 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL480809 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL520933 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL518110 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL481004 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL518109 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL520425 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL466595 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL517385 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL481984 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL516708 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL481782 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL520741 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL464059 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL464032 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL516686 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL512993 | — | IC50 | = | 11.9 | nM | 7.92 |
| CHEMBL465915 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL480012 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL464905 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL464074 | — | IC50 | = | 16.7 | nM | 7.78 |
| CHEMBL464271 | — | IC50 | = | 18.3 | nM | 7.74 |
| CHEMBL464237 | — | IC50 | = | 18.8 | nM | 7.73 |
| CHEMBL521103 | — | IC50 | = | 18.8 | nM | 7.73 |
| CHEMBL469303 | — | IC50 | = | 20.2 | nM | 7.70 |
| CHEMBL482177 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL464270 | — | IC50 | = | 24.1 | nM | 7.62 |
| CHEMBL464042 | — | IC50 | = | 27.8 | nM | 7.56 |
| CHEMBL465122 | — | IC50 | = | 27.6 | nM | 7.56 |
| CHEMBL464906 | — | IC50 | = | 30.0 | nM | 7.52 |