Assay Detail
Binding
CHEMBL3887484
Review assay metadata, readout intent, target linkage, and publication context from the same page.
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Prostaglandin E2 receptor EP2 subtype (CHEMBL1881) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Difluorolactam compounds as EP4 receptor-selective agonists for use in the treatment of EP4-mediated diseases and conditions
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 6.32 | 7.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL62570 | — | — | 1 | 7.78 |
| CHEMBL64804 | — | — | 1 | 7.23 |
| CHEMBL3937596 | — | — | 1 | 7.19 |
| CHEMBL3975743 | — | — | 1 | 6.83 |
| CHEMBL3945327 | — | — | 1 | 6.80 |
| CHEMBL3955128 | — | — | 1 | 6.69 |
| CHEMBL3916499 | — | — | 1 | 6.49 |
| CHEMBL3966743 | — | — | 1 | 6.13 |
| CHEMBL3949856 | — | — | 1 | 6.12 |
| CHEMBL3902065 | — | — | 1 | 6.00 |
| CHEMBL3968443 | — | — | 1 | 5.99 |
| CHEMBL3900979 | — | — | 1 | 5.88 |
| CHEMBL3895047 | — | — | 1 | 5.79 |
| CHEMBL3923027 | — | — | 1 | 5.71 |
| CHEMBL3893847 | — | — | 1 | 4.10 |
| CHEMBL3897335 | — | — | 1 | - |
| CHEMBL3918816 | — | — | 1 | - |
| CHEMBL3977939 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL62570 | — | EC50 | = | 16.5 | nM | 7.78 |
| CHEMBL64804 | — | EC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3937596 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3975743 | — | EC50 | = | 148.0 | nM | 6.83 |
| CHEMBL3945327 | — | EC50 | = | 157.0 | nM | 6.80 |
| CHEMBL3955128 | — | EC50 | = | 205.0 | nM | 6.69 |
| CHEMBL3916499 | — | EC50 | = | 326.0 | nM | 6.49 |
| CHEMBL3966743 | — | EC50 | = | 743.0 | nM | 6.13 |
| CHEMBL3949856 | — | EC50 | = | 763.0 | nM | 6.12 |
| CHEMBL3902065 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3968443 | — | EC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL3900979 | — | EC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL3895047 | — | EC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL3923027 | — | EC50 | = | 1960.0 | nM | 5.71 |
| CHEMBL3893847 | — | EC50 | = | 79000.0 | nM | 4.10 |
| CHEMBL3897335 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3918816 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3977939 | — | EC50 | > | 10000.0 | nM | - |