Assay Detail
Binding
CHEMBL1217617
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Displacement of [3H]DPDPE from rat mu opioid receptor
15
Total Activities
10
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
Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.98 | 9.30 |
| IC50 | 5 | 5.86 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL595972 | — | — | 1 | 9.30 |
| CHEMBL38874 | DAMGO | — | 1 | 9.07 |
| CHEMBL200199 | BIPHALIN | — | 1 | 8.85 |
| CHEMBL507340 | — | — | 2 | 7.80 |
| CHEMBL31421 | — | — | 1 | 6.21 |
| CHEMBL1214027 | — | — | 2 | 6.00 |
| CHEMBL1214026 | — | — | 2 | 5.70 |
| CHEMBL1214025 | — | — | 2 | 5.68 |
| CHEMBL1214024 | — | — | 2 | 5.64 |
| CHEMBL1214076 | — | — | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL595972 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL38874 | DAMGO | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL200199 | BIPHALIN | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL507340 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL507340 | — | IC50 | = | 36.31 | nM | 7.44 |
| CHEMBL31421 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL1214027 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1214026 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL1214027 | — | IC50 | = | 2041.74 | nM | 5.69 |
| CHEMBL1214025 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL1214024 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL1214076 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL1214026 | — | IC50 | = | 3715.35 | nM | 5.43 |
| CHEMBL1214025 | — | IC50 | = | 4168.69 | nM | 5.38 |
| CHEMBL1214024 | — | IC50 | = | 4365.16 | nM | 5.36 |