Assay Detail
Functional
CHEMBL5035393
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Agonist activity at DOR (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
22
Total Activities
11
Compounds Tested
2
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 | 20 | 6.79 | 8.34 |
| pEC50 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL31421 | — | — | 2 | 8.34 |
| CHEMBL5086601 | — | — | 2 | 7.55 |
| CHEMBL5090298 | — | — | 2 | 7.13 |
| CHEMBL5091560 | — | — | 2 | 7.02 |
| CHEMBL5082892 | — | — | 2 | 6.43 |
| CHEMBL5085455 | — | — | 2 | 6.26 |
| CHEMBL5086463 | — | — | 2 | 6.24 |
| CHEMBL5094675 | — | — | 2 | 6.18 |
| CHEMBL5085013 | — | — | 2 | 6.04 |
| CHEMBL440765 | U-69593 | — | 2 | - |
| CHEMBL70 | MORPHINE | 4.0 | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL31421 | — | EC50 | = | 4.571 | nM | 8.34 |
| CHEMBL31421 | — | EC50 | = | 6.4 | nM | 8.19 |
| CHEMBL5086601 | — | EC50 | = | 28.18 | nM | 7.55 |
| CHEMBL5086601 | — | EC50 | = | 28.2 | nM | 7.55 |
| CHEMBL5090298 | — | EC50 | = | 74.13 | nM | 7.13 |
| CHEMBL5090298 | — | EC50 | = | 74.2 | nM | 7.13 |
| CHEMBL5091560 | — | EC50 | = | 95.1 | nM | 7.02 |
| CHEMBL5091560 | — | EC50 | = | 95.5 | nM | 7.02 |
| CHEMBL5082892 | — | EC50 | = | 374.0 | nM | 6.43 |
| CHEMBL5082892 | — | EC50 | = | 371.54 | nM | 6.43 |
| CHEMBL5085455 | — | EC50 | = | 549.54 | nM | 6.26 |
| CHEMBL5085455 | — | EC50 | = | 546.0 | nM | 6.26 |
| CHEMBL5086463 | — | EC50 | = | 581.0 | nM | 6.24 |
| CHEMBL5086463 | — | EC50 | = | 575.44 | nM | 6.24 |
| CHEMBL5094675 | — | EC50 | = | 659.0 | nM | 6.18 |
| CHEMBL5094675 | — | EC50 | = | 660.69 | nM | 6.18 |
| CHEMBL5085013 | — | EC50 | = | 923.0 | nM | 6.04 |
| CHEMBL5085013 | — | EC50 | = | 912.01 | nM | 6.04 |
| CHEMBL70 | MORPHINE | pEC50 | - | — | - | |
| CHEMBL440765 | U-69593 | pEC50 | - | — | - | |
| CHEMBL440765 | U-69593 | EC50 | - | — | - | |
| CHEMBL70 | MORPHINE | EC50 | - | — | - |