Assay Detail
Functional
CHEMBL2320404
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at mouse EP1 receptor expressed in CHOK1 cells assessed as inhibition of 17PTPGE2-induced calcium influx
28
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Prostaglandin E2 receptor EP1 subtype (CHEMBL2181) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Development of an in vivo active, dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 28 | 6.27 | 7.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2315055 | — | — | 2 | 7.39 |
| CHEMBL1207972 | — | — | 2 | 7.32 |
| CHEMBL2315056 | — | — | 2 | 7.27 |
| CHEMBL2315059 | — | — | 2 | 6.67 |
| CHEMBL2315057 | — | — | 2 | 6.67 |
| CHEMBL2315049 | — | — | 2 | 6.52 |
| CHEMBL2315052 | — | — | 2 | 6.35 |
| CHEMBL2315046 | — | — | 2 | 6.26 |
| CHEMBL2315048 | — | — | 2 | 6.04 |
| CHEMBL2315050 | — | — | 2 | 5.86 |
| CHEMBL2315053 | — | — | 2 | 5.66 |
| CHEMBL2315054 | — | — | 2 | 5.58 |
| CHEMBL2315051 | — | — | 2 | 5.36 |
| CHEMBL2315047 | — | — | 2 | 4.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2315055 | — | Kd | = | 40.7 | nM | 7.39 |
| CHEMBL2315055 | — | Kd | = | 40.74 | nM | 7.39 |
| CHEMBL1207972 | — | Kd | = | 47.9 | nM | 7.32 |
| CHEMBL1207972 | — | Kd | = | 47.86 | nM | 7.32 |
| CHEMBL2315056 | — | Kd | = | 53.7 | nM | 7.27 |
| CHEMBL2315056 | — | Kd | = | 56.23 | nM | 7.25 |
| CHEMBL2315059 | — | Kd | = | 214.0 | nM | 6.67 |
| CHEMBL2315057 | — | Kd | = | 214.0 | nM | 6.67 |
| CHEMBL2315059 | — | Kd | = | 213.8 | nM | 6.67 |
| CHEMBL2315057 | — | Kd | = | 213.8 | nM | 6.67 |
| CHEMBL2315049 | — | Kd | = | 302.0 | nM | 6.52 |
| CHEMBL2315049 | — | Kd | = | 302.0 | nM | 6.52 |
| CHEMBL2315052 | — | Kd | = | 446.68 | nM | 6.35 |
| CHEMBL2315052 | — | Kd | = | 447.0 | nM | 6.35 |
| CHEMBL2315046 | — | Kd | = | 549.54 | nM | 6.26 |
| CHEMBL2315046 | — | Kd | = | 549.0 | nM | 6.26 |
| CHEMBL2315048 | — | Kd | = | 912.01 | nM | 6.04 |
| CHEMBL2315048 | — | Kd | = | 912.0 | nM | 6.04 |
| CHEMBL2315050 | — | Kd | = | 1380.0 | nM | 5.86 |
| CHEMBL2315050 | — | Kd | = | 1380.38 | nM | 5.86 |
| CHEMBL2315053 | — | Kd | = | 2190.0 | nM | 5.66 |
| CHEMBL2315053 | — | Kd | = | 2187.76 | nM | 5.66 |
| CHEMBL2315054 | — | Kd | = | 2630.0 | nM | 5.58 |
| CHEMBL2315054 | — | Kd | = | 2630.27 | nM | 5.58 |
| CHEMBL2315051 | — | Kd | = | 4360.0 | nM | 5.36 |
| CHEMBL2315051 | — | Kd | = | 4365.16 | nM | 5.36 |
| CHEMBL2315047 | — | Kd | = | 15800.0 | nM | 4.80 |
| CHEMBL2315047 | — | Kd | = | 15848.93 | nM | 4.80 |