Assay Detail
Functional
CHEMBL5035397
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Agonist activity at NPFF2R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
18
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293-A |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of Multifunctional and Orally Active Cyclic Peptide Agonists of Opioid/Neuropeptide FF Receptors that Produce Potent, Long-Lasting, and Peripherally Restricted Antinociception with Diminished Side Effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 6.87 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429731 | — | — | 2 | 7.37 |
| CHEMBL5085455 | — | — | 2 | 7.30 |
| CHEMBL5085013 | — | — | 2 | 7.09 |
| CHEMBL5086601 | — | — | 2 | 6.95 |
| CHEMBL5094675 | — | — | 2 | 6.88 |
| CHEMBL5086463 | — | — | 2 | 6.72 |
| CHEMBL5091560 | — | — | 2 | 6.58 |
| CHEMBL5090298 | — | — | 2 | 6.52 |
| CHEMBL5082892 | — | — | 2 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429731 | — | EC50 | = | 42.66 | nM | 7.37 |
| CHEMBL429731 | — | EC50 | = | 42.4 | nM | 7.37 |
| CHEMBL5085455 | — | EC50 | = | 49.8 | nM | 7.30 |
| CHEMBL5085455 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL5085013 | — | EC50 | = | 81.28 | nM | 7.09 |
| CHEMBL5085013 | — | EC50 | = | 81.5 | nM | 7.09 |
| CHEMBL5086601 | — | EC50 | = | 112.0 | nM | 6.95 |
| CHEMBL5086601 | — | EC50 | = | 112.2 | nM | 6.95 |
| CHEMBL5094675 | — | EC50 | = | 133.0 | nM | 6.88 |
| CHEMBL5094675 | — | EC50 | = | 131.83 | nM | 6.88 |
| CHEMBL5086463 | — | EC50 | = | 190.55 | nM | 6.72 |
| CHEMBL5086463 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5091560 | — | EC50 | = | 263.03 | nM | 6.58 |
| CHEMBL5091560 | — | EC50 | = | 265.0 | nM | 6.58 |
| CHEMBL5090298 | — | EC50 | = | 303.0 | nM | 6.52 |
| CHEMBL5090298 | — | EC50 | = | 309.03 | nM | 6.51 |
| CHEMBL5082892 | — | EC50 | = | 349.0 | nM | 6.46 |
| CHEMBL5082892 | — | EC50 | = | 354.81 | nM | 6.45 |