Assay Detail
Functional
CHEMBL3887482
Review assay metadata, readout intent, target linkage, and publication context from the same page.
cAMP 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 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and 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. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
33
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Prostaglandin E2 receptor EP4 subtype (CHEMBL1836) ↗| 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 | 33 | 9.26 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3975743 | — | — | 2 | 11.00 |
| CHEMBL3937596 | — | — | 2 | 10.79 |
| CHEMBL3897335 | — | — | 1 | 10.64 |
| CHEMBL3902065 | — | — | 1 | 10.42 |
| CHEMBL3895047 | — | — | 1 | 10.33 |
| CHEMBL3893847 | — | — | 1 | 10.23 |
| CHEMBL3916499 | — | — | 1 | 10.10 |
| CHEMBL3891907 | — | — | 1 | 9.82 |
| CHEMBL3982139 | — | — | 1 | 9.82 |
| CHEMBL62570 | — | — | 1 | 9.66 |
| CHEMBL3918816 | — | — | 1 | 9.62 |
| CHEMBL3955128 | — | — | 1 | 9.43 |
| CHEMBL3977939 | — | — | 1 | 9.43 |
| CHEMBL64804 | — | — | 1 | 9.32 |
| CHEMBL3923027 | — | — | 1 | 9.21 |
| CHEMBL3949856 | — | — | 1 | 9.14 |
| CHEMBL3959605 | — | — | 1 | 8.96 |
| CHEMBL3911081 | — | — | 1 | 8.30 |
| CHEMBL3973091 | — | — | 1 | 8.09 |
| CHEMBL3949313 | — | — | 1 | 7.29 |
| CHEMBL3986266 | — | — | 1 | 7.21 |
| CHEMBL3966743 | — | — | 1 | 6.70 |
| CHEMBL3978072 | — | — | 1 | - |
| CHEMBL3900979 | — | — | 1 | - |
| CHEMBL3939998 | — | — | 1 | - |
| CHEMBL3969565 | — | — | 1 | - |
| CHEMBL3945327 | — | — | 1 | - |
| CHEMBL3935235 | — | — | 1 | - |
| CHEMBL3964981 | — | — | 1 | - |
| CHEMBL3982730 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3975743 | — | EC50 | = | 0.01 | nM | 11.00 |
| CHEMBL3937596 | — | EC50 | = | 0.0162 | nM | 10.79 |
| CHEMBL3897335 | — | EC50 | = | 0.023 | nM | 10.64 |
| CHEMBL3902065 | — | EC50 | = | 0.038 | nM | 10.42 |
| CHEMBL3895047 | — | EC50 | = | 0.047 | nM | 10.33 |
| CHEMBL3893847 | — | EC50 | = | 0.059 | nM | 10.23 |
| CHEMBL3916499 | — | EC50 | = | 0.079 | nM | 10.10 |
| CHEMBL3982139 | — | EC50 | = | 0.15 | nM | 9.82 |
| CHEMBL3891907 | — | EC50 | = | 0.15 | nM | 9.82 |
| CHEMBL62570 | — | EC50 | = | 0.22 | nM | 9.66 |
| CHEMBL3918816 | — | EC50 | = | 0.24 | nM | 9.62 |
| CHEMBL3977939 | — | EC50 | = | 0.37 | nM | 9.43 |
| CHEMBL3955128 | — | EC50 | = | 0.37 | nM | 9.43 |
| CHEMBL64804 | — | EC50 | = | 0.48 | nM | 9.32 |
| CHEMBL3923027 | — | EC50 | = | 0.61 | nM | 9.21 |
| CHEMBL3949856 | — | EC50 | = | 0.73 | nM | 9.14 |
| CHEMBL3959605 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3975743 | — | EC50 | = | 3.15 | nM | 8.50 |
| CHEMBL3911081 | — | EC50 | = | 5.02 | nM | 8.30 |
| CHEMBL3937596 | — | EC50 | = | 5.68 | nM | 8.25 |
| CHEMBL3973091 | — | EC50 | = | 8.09 | nM | 8.09 |
| CHEMBL3949313 | — | EC50 | = | 50.8 | nM | 7.29 |
| CHEMBL3986266 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3966743 | — | EC50 | = | 198.0 | nM | 6.70 |
| CHEMBL3978072 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3935235 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3939998 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3969565 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3945327 | — | EC50 | = | 1.4e-07 | nM | - |
| CHEMBL3964981 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3982730 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3968443 | — | EC50 | = | 2.7e-06 | nM | - |
| CHEMBL3900979 | — | EC50 | = | 0.0029 | nM | - |