Assay Detail
Functional
CHEMBL3888047
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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.
28
Total Activities
28
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 | 28 | 5.58 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3923831 | — | — | 1 | 7.54 |
| CHEMBL4110373 | — | — | 1 | 7.07 |
| CHEMBL4107642 | — | — | 1 | 7.03 |
| CHEMBL4106506 | — | — | 1 | 6.89 |
| CHEMBL4108649 | — | — | 1 | 6.80 |
| CHEMBL4112562 | — | — | 1 | 6.57 |
| CHEMBL4112722 | — | — | 1 | 6.38 |
| CHEMBL656 | OXYCODONE | 4.0 | 1 | 6.32 |
| CHEMBL4110642 | — | — | 1 | 6.29 |
| CHEMBL4108525 | — | — | 1 | 5.97 |
| CHEMBL4111500 | — | — | 1 | 5.55 |
| CHEMBL4111282 | — | — | 1 | 5.50 |
| CHEMBL4112727 | — | — | 1 | 5.43 |
| CHEMBL4110656 | — | — | 1 | 5.42 |
| CHEMBL4112234 | — | — | 1 | 5.30 |
| CHEMBL4108425 | — | — | 1 | 5.30 |
| CHEMBL3937789 | — | — | 1 | 5.29 |
| CHEMBL4114370 | — | — | 1 | 5.13 |
| CHEMBL3895828 | — | — | 1 | 5.07 |
| CHEMBL2448883 | — | — | 1 | 4.98 |
| CHEMBL4109078 | — | — | 1 | 4.90 |
| CHEMBL4108254 | — | — | 1 | 4.75 |
| CHEMBL3934684 | — | — | 1 | 4.71 |
| CHEMBL3967811 | — | — | 1 | 4.66 |
| CHEMBL3933053 | — | — | 1 | 4.63 |
| CHEMBL3984515 | — | — | 1 | 4.35 |
| CHEMBL3911284 | — | — | 1 | 4.32 |
| CHEMBL3956767 | — | — | 1 | 4.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3923831 | — | EC50 | = | 28.5 | nM | 7.54 |
| CHEMBL4110373 | — | EC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4107642 | — | EC50 | = | 93.3 | nM | 7.03 |
| CHEMBL4106506 | — | EC50 | = | 128.0 | nM | 6.89 |
| CHEMBL4108649 | — | EC50 | = | 157.0 | nM | 6.80 |
| CHEMBL4112562 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4112722 | — | EC50 | = | 415.0 | nM | 6.38 |
| CHEMBL656 | OXYCODONE | EC50 | = | 478.0 | nM | 6.32 |
| CHEMBL4110642 | — | EC50 | = | 508.0 | nM | 6.29 |
| CHEMBL4108525 | — | EC50 | = | 1061.0 | nM | 5.97 |
| CHEMBL4111500 | — | EC50 | = | 2827.0 | nM | 5.55 |
| CHEMBL4111282 | — | EC50 | = | 3162.0 | nM | 5.50 |
| CHEMBL4112727 | — | EC50 | = | 3715.0 | nM | 5.43 |
| CHEMBL4110656 | — | EC50 | = | 3841.0 | nM | 5.42 |
| CHEMBL4112234 | — | EC50 | = | 5005.0 | nM | 5.30 |
| CHEMBL4108425 | — | EC50 | = | 5037.0 | nM | 5.30 |
| CHEMBL3937789 | — | EC50 | = | 5145.0 | nM | 5.29 |
| CHEMBL4114370 | — | EC50 | = | 7448.0 | nM | 5.13 |
| CHEMBL3895828 | — | EC50 | = | 8574.0 | nM | 5.07 |
| CHEMBL2448883 | — | EC50 | = | 10418.0 | nM | 4.98 |
| CHEMBL4109078 | — | EC50 | = | 12519.0 | nM | 4.90 |
| CHEMBL4108254 | — | EC50 | = | 17948.0 | nM | 4.75 |
| CHEMBL3934684 | — | EC50 | = | 19740.0 | nM | 4.71 |
| CHEMBL3967811 | — | EC50 | = | 22083.0 | nM | 4.66 |
| CHEMBL3933053 | — | EC50 | = | 23235.0 | nM | 4.63 |
| CHEMBL3984515 | — | EC50 | = | 44729.0 | nM | 4.35 |
| CHEMBL3911284 | — | EC50 | = | 48242.0 | nM | 4.32 |
| CHEMBL3956767 | — | EC50 | = | 97381.0 | nM | 4.01 |