Assay Detail
Functional
CHEMBL3888048
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HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.
10
Total Activities
10
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 |
Publication
Oligomer-opioid agonist conjugates
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 5.54 | 6.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3923831 | — | — | 1 | 6.21 |
| CHEMBL4107642 | — | — | 1 | 6.19 |
| CHEMBL4110373 | — | — | 1 | 5.92 |
| CHEMBL4108649 | — | — | 1 | 5.64 |
| CHEMBL4106506 | — | — | 1 | 5.51 |
| CHEMBL4112722 | — | — | 1 | 5.41 |
| CHEMBL4112562 | — | — | 1 | 5.38 |
| CHEMBL4110642 | — | — | 1 | 5.37 |
| CHEMBL4108525 | — | — | 1 | 5.36 |
| CHEMBL3937789 | — | — | 1 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3923831 | — | EC50 | = | 624.0 | nM | 6.21 |
| CHEMBL4107642 | — | EC50 | = | 641.0 | nM | 6.19 |
| CHEMBL4110373 | — | EC50 | = | 1189.0 | nM | 5.92 |
| CHEMBL4108649 | — | EC50 | = | 2295.0 | nM | 5.64 |
| CHEMBL4106506 | — | EC50 | = | 3092.0 | nM | 5.51 |
| CHEMBL4112722 | — | EC50 | = | 3933.0 | nM | 5.41 |
| CHEMBL4112562 | — | EC50 | = | 4198.0 | nM | 5.38 |
| CHEMBL4110642 | — | EC50 | = | 4237.0 | nM | 5.37 |
| CHEMBL4108525 | — | EC50 | = | 4417.0 | nM | 5.36 |
| CHEMBL3937789 | — | EC50 | = | 40103.0 | nM | 4.40 |