Assay Detail
Binding
CHEMBL2445992
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as beta-arrestin recruitment by chemiluminescence assay
36
Total Activities
36
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 22 | 6.14 | 7.30 |
| pEC50 | 14 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2443272 | — | — | 1 | 7.30 |
| CHEMBL2443262 | OLICERIDINE | 4.0 | 1 | 7.30 |
| CHEMBL2443279 | — | — | 1 | 7.20 |
| CHEMBL2443269 | — | — | 1 | 6.80 |
| CHEMBL2443258 | — | — | 1 | 6.70 |
| CHEMBL2443268 | — | — | 1 | 6.70 |
| CHEMBL2443278 | — | — | 1 | 6.60 |
| CHEMBL2443261 | — | — | 1 | 6.50 |
| CHEMBL2443263 | — | — | 1 | 6.40 |
| CHEMBL2443256 | — | — | 1 | 6.40 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 6.30 |
| CHEMBL2443260 | — | — | 1 | 6.30 |
| CHEMBL2443285 | — | — | 1 | 6.20 |
| CHEMBL2443259 | — | — | 1 | 6.20 |
| CHEMBL2443282 | — | — | 1 | 5.80 |
| CHEMBL2443277 | — | — | 1 | 5.70 |
| CHEMBL2443280 | — | — | 1 | 5.70 |
| CHEMBL2443284 | — | — | 1 | 5.20 |
| CHEMBL2443264 | — | — | 1 | 5.10 |
| CHEMBL2443265 | — | — | 1 | 5.10 |
| CHEMBL2443270 | — | — | 1 | 4.80 |
| CHEMBL2443253 | — | — | 1 | 4.70 |
| CHEMBL2440150 | — | — | 1 | - |
| CHEMBL2443267 | — | — | 1 | - |
| CHEMBL2443266 | — | — | 1 | - |
| CHEMBL2443257 | — | — | 1 | - |
| CHEMBL2443255 | — | — | 1 | - |
| CHEMBL2443273 | — | — | 1 | - |
| CHEMBL2443274 | — | — | 1 | - |
| CHEMBL2443271 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2443272 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL2443262 | OLICERIDINE | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL2443279 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL2443269 | — | EC50 | = | 158.49 | nM | 6.80 |
| CHEMBL2443258 | — | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL2443268 | — | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL2443278 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL2443261 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL2443263 | — | EC50 | = | 398.11 | nM | 6.40 |
| CHEMBL2443256 | — | EC50 | = | 398.11 | nM | 6.40 |
| CHEMBL70 | MORPHINE | EC50 | = | 501.19 | nM | 6.30 |
| CHEMBL2443260 | — | EC50 | = | 501.19 | nM | 6.30 |
| CHEMBL2443285 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL2443259 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL2443282 | — | EC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL2443277 | — | EC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL2443280 | — | EC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL2443284 | — | EC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL2443264 | — | EC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL2443265 | — | EC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL2443270 | — | EC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL2443253 | — | EC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL2443254 | — | pEC50 | - | — | - | |
| CHEMBL511142 | BUPRENORPHINE | pEC50 | - | — | - | |
| CHEMBL2443276 | — | pEC50 | - | — | - | |
| CHEMBL2443281 | — | pEC50 | - | — | - | |
| CHEMBL2443275 | — | pEC50 | - | — | - | |
| CHEMBL2443283 | — | pEC50 | - | — | - | |
| CHEMBL2443271 | — | pEC50 | - | — | - | |
| CHEMBL2443274 | — | pEC50 | - | — | - | |
| CHEMBL2443273 | — | pEC50 | - | — | - | |
| CHEMBL2443255 | — | pEC50 | - | — | - | |
| CHEMBL2443257 | — | pEC50 | - | — | - | |
| CHEMBL2443266 | — | pEC50 | - | — | - | |
| CHEMBL2443267 | — | pEC50 | - | — | - | |
| CHEMBL2440150 | — | pEC50 | - | — | - |