Assay Detail
Binding
CHEMBL1175732
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DAMGO from rat mu opioid receptor expressed in mouse HN9.10 cells
26
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of trivalent ligands targeting opioid, cholecystokinin, and melanocortin receptors for the treatment of pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.80 | 9.89 |
| IC50 | 13 | 7.46 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1172253 | — | — | 2 | 9.89 |
| CHEMBL1172252 | — | — | 2 | 9.16 |
| CHEMBL235743 | — | — | 2 | 8.55 |
| CHEMBL1172428 | — | — | 2 | 8.31 |
| CHEMBL1172248 | — | — | 2 | 8.23 |
| CHEMBL1172245 | — | — | 2 | 8.13 |
| CHEMBL1172247 | — | — | 2 | 8.07 |
| CHEMBL1172251 | — | — | 2 | 7.85 |
| CHEMBL1172249 | — | — | 2 | 7.75 |
| CHEMBL2372623 | — | — | 2 | 7.33 |
| CHEMBL1172429 | — | — | 2 | 6.60 |
| CHEMBL1172244 | — | — | 2 | 5.91 |
| CHEMBL1172246 | — | — | 2 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1172253 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL1172253 | — | IC50 | = | 0.2512 | nM | 9.60 |
| CHEMBL1172252 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL1172252 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL235743 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL1172428 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL1172248 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL235743 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL1172245 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL1172247 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL1172428 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1172248 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL1172251 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1172249 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL1172247 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL1172245 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL1172251 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL1172249 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL2372623 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL2372623 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1172429 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL1172429 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL1172244 | — | Ki | = | 1240.0 | nM | 5.91 |
| CHEMBL1172246 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL1172244 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL1172246 | — | IC50 | = | 3981.07 | nM | 5.40 |