Assay Detail
Binding
CHEMBL754376
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Displacement of [3H]DAMGO from human recombinant Opioid receptor mu 1 on CHO cell membranes.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.62 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.70 |
| CHEMBL38874 | DAMGO | — | 1 | 9.30 |
| CHEMBL2113382 | — | — | 1 | 8.78 |
| CHEMBL2113380 | — | — | 1 | 8.31 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 8.20 |
| CHEMBL2113373 | — | — | 1 | 8.02 |
| CHEMBL2113378 | — | — | 1 | 7.99 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 7.68 |
| CHEMBL2113379 | — | — | 1 | 7.53 |
| CHEMBL2113372 | — | — | 1 | 7.48 |
| CHEMBL2113377 | — | — | 1 | 7.43 |
| CHEMBL2113381 | — | — | 1 | 7.29 |
| CHEMBL2113383 | — | — | 1 | 7.12 |
| CHEMBL401093 | OXYMORPHINDOLE | — | 1 | 6.44 |
| CHEMBL31421 | — | — | 1 | 6.30 |
| CHEMBL2113376 | — | — | 1 | 5.98 |
| CHEMBL440765 | U-69593 | — | 1 | 5.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL38874 | DAMGO | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL2113382 | — | Ki | = | 1.68 | nM | 8.78 |
| CHEMBL2113380 | — | Ki | = | 4.91 | nM | 8.31 |
| CHEMBL567175 | NALTRINDOLE | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL2113373 | — | Ki | = | 9.61 | nM | 8.02 |
| CHEMBL2113378 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL2113379 | — | Ki | = | 29.3 | nM | 7.53 |
| CHEMBL2113372 | — | Ki | = | 33.4 | nM | 7.48 |
| CHEMBL2113377 | — | Ki | = | 37.2 | nM | 7.43 |
| CHEMBL2113381 | — | Ki | = | 51.1 | nM | 7.29 |
| CHEMBL2113383 | — | Ki | = | 76.3 | nM | 7.12 |
| CHEMBL401093 | OXYMORPHINDOLE | Ki | = | 363.0 | nM | 6.44 |
| CHEMBL31421 | — | Ki | = | 504.0 | nM | 6.30 |
| CHEMBL2113376 | — | Ki | = | 1051.0 | nM | 5.98 |
| CHEMBL440765 | U-69593 | Ki | = | 1145.0 | nM | 5.94 |