Assay Detail
Functional
CHEMBL5035391
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Agonist activity at KOR (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
20
Total Activities
11
Compounds Tested
3
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 | 16 | 7.11 | 7.93 |
| logEC50 | 2 | - | - |
| pEC50 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL440765 | U-69593 | — | 2 | 7.93 |
| CHEMBL5085455 | — | — | 2 | 7.41 |
| CHEMBL5091560 | — | — | 2 | 7.15 |
| CHEMBL5090298 | — | — | 2 | 7.09 |
| CHEMBL5082892 | — | — | 2 | 6.87 |
| CHEMBL5094675 | — | — | 2 | 6.86 |
| CHEMBL5086601 | — | — | 2 | 6.50 |
| CHEMBL31421 | — | — | 2 | - |
| CHEMBL70 | MORPHINE | 4.0 | 2 | - |
| CHEMBL5085013 | — | — | 1 | - |
| CHEMBL5086463 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL440765 | U-69593 | EC50 | = | 11.75 | nM | 7.93 |
| CHEMBL440765 | U-69593 | EC50 | = | 11.9 | nM | 7.92 |
| CHEMBL5085455 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5085455 | — | EC50 | = | 38.9 | nM | 7.41 |
| CHEMBL5091560 | — | EC50 | = | 71.2 | nM | 7.15 |
| CHEMBL5091560 | — | EC50 | = | 70.79 | nM | 7.15 |
| CHEMBL5090298 | — | EC50 | = | 81.3 | nM | 7.09 |
| CHEMBL5090298 | — | EC50 | = | 81.28 | nM | 7.09 |
| CHEMBL5082892 | — | EC50 | = | 136.0 | nM | 6.87 |
| CHEMBL5082892 | — | EC50 | = | 138.04 | nM | 6.86 |
| CHEMBL5094675 | — | EC50 | = | 138.04 | nM | 6.86 |
| CHEMBL5094675 | — | EC50 | = | 139.0 | nM | 6.86 |
| CHEMBL5086601 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5086601 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL5086463 | — | logEC50 | - | — | - | |
| CHEMBL5085013 | — | logEC50 | - | — | - | |
| CHEMBL70 | MORPHINE | EC50 | - | — | - | |
| CHEMBL31421 | — | EC50 | - | — | - | |
| CHEMBL31421 | — | pEC50 | - | — | - | |
| CHEMBL70 | MORPHINE | pEC50 | - | — | - |