Assay Detail
Binding
CHEMBL754712
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity to human Opioid receptor mu 1 on CHO cell membranes using [3H]diprenorphine displacement.
23
Total Activities
23
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
Structure-activity relationships of dynorphin a analogues modified in the address sequence.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 6.33 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.44 |
| CHEMBL216640 | — | — | 1 | 8.25 |
| CHEMBL265813 | — | — | 1 | 8.10 |
| CHEMBL269483 | — | — | 1 | 7.92 |
| CHEMBL407832 | — | — | 1 | 7.62 |
| CHEMBL217379 | — | — | 1 | 7.45 |
| CHEMBL293465 | — | — | 1 | 7.42 |
| CHEMBL63188 | — | — | 1 | 7.39 |
| CHEMBL8234 | ENKEPHALIN | — | 1 | 7.26 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 7.10 |
| CHEMBL2369366 | — | — | 1 | 5.78 |
| CHEMBL2369365 | — | — | 1 | 5.63 |
| CHEMBL2369408 | — | — | 1 | 5.56 |
| CHEMBL2369370 | — | — | 1 | 5.51 |
| CHEMBL413729 | — | — | 1 | 5.28 |
| CHEMBL2369390 | — | — | 1 | 5.22 |
| CHEMBL2369389 | — | — | 1 | 5.21 |
| CHEMBL2369391 | — | — | 1 | 4.90 |
| CHEMBL2369393 | — | — | 1 | 4.82 |
| CHEMBL2369407 | — | — | 1 | 4.81 |
| CHEMBL2369395 | — | — | 1 | 4.79 |
| CHEMBL2369394 | — | — | 1 | 4.71 |
| CHEMBL2369371 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL80 | NALOXONE | Ki | = | 3.63 | nM | 8.44 |
| CHEMBL216640 | — | Ki | = | 5.62 | nM | 8.25 |
| CHEMBL265813 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL269483 | — | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL407832 | — | Ki | = | 23.8 | nM | 7.62 |
| CHEMBL217379 | — | Ki | = | 35.4 | nM | 7.45 |
| CHEMBL293465 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL63188 | — | Ki | = | 40.6 | nM | 7.39 |
| CHEMBL8234 | ENKEPHALIN | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 79.4 | nM | 7.10 |
| CHEMBL2369366 | — | Ki | = | 1660.0 | nM | 5.78 |
| CHEMBL2369365 | — | Ki | = | 2340.0 | nM | 5.63 |
| CHEMBL2369408 | — | Ki | = | 2750.0 | nM | 5.56 |
| CHEMBL2369370 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL413729 | — | Ki | = | 5250.0 | nM | 5.28 |
| CHEMBL2369390 | — | Ki | = | 6030.0 | nM | 5.22 |
| CHEMBL2369389 | — | Ki | = | 6200.0 | nM | 5.21 |
| CHEMBL2369391 | — | Ki | = | 12600.0 | nM | 4.90 |
| CHEMBL2369393 | — | Ki | = | 15100.0 | nM | 4.82 |
| CHEMBL2369407 | — | Ki | = | 15500.0 | nM | 4.81 |
| CHEMBL2369395 | — | Ki | = | 16200.0 | nM | 4.79 |
| CHEMBL2369394 | — | Ki | = | 19500.0 | nM | 4.71 |
| CHEMBL2369371 | — | Ki | > | 100000.0 | nM | - |