Assay Detail
Binding
CHEMBL927003
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Displacement of [3H]diprenorphine from human mu opioid receptor expressed in CHO-K1 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.61 | 8.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL257355 | — | — | 1 | 8.23 |
| CHEMBL257140 | — | — | 1 | 8.19 |
| CHEMBL429677 | — | — | 1 | 8.05 |
| CHEMBL411557 | DYNORPHIN A (1-17) | — | 1 | 8.03 |
| CHEMBL402820 | — | — | 1 | 7.85 |
| CHEMBL402189 | — | — | 1 | 7.82 |
| CHEMBL401594 | — | — | 1 | 7.68 |
| CHEMBL254960 | — | — | 1 | 7.60 |
| CHEMBL254754 | — | — | 1 | 7.57 |
| CHEMBL257139 | — | — | 1 | 7.47 |
| CHEMBL254959 | — | — | 1 | 7.38 |
| CHEMBL402135 | — | — | 1 | 7.33 |
| CHEMBL38576 | ICI-199,441 | — | 1 | 7.28 |
| CHEMBL437784 | — | — | 1 | 7.28 |
| CHEMBL403273 | — | — | 1 | 6.35 |
| CHEMBL258172 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL257355 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL257140 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL429677 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL411557 | DYNORPHIN A (1-17) | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL402820 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL402189 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL401594 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL254960 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL254754 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL257139 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL254959 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL402135 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL38576 | ICI-199,441 | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL437784 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL403273 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL258172 | — | Ki | > | 1000.0 | nM | - |