Assay Detail
Binding
CHEMBL927005
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Displacement of [3H]diprenorphine from human kappa/mu opioid chimera 4 receptor
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 8.53 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL411557 | DYNORPHIN A (1-17) | — | 1 | 9.74 |
| CHEMBL257139 | — | — | 1 | 9.30 |
| CHEMBL402135 | — | — | 1 | 9.15 |
| CHEMBL38576 | ICI-199,441 | — | 1 | 9.00 |
| CHEMBL402820 | — | — | 1 | 8.92 |
| CHEMBL257140 | — | — | 1 | 8.77 |
| CHEMBL402189 | — | — | 1 | 8.66 |
| CHEMBL254959 | — | — | 1 | 8.60 |
| CHEMBL254960 | — | — | 1 | 8.55 |
| CHEMBL401594 | — | — | 1 | 8.32 |
| CHEMBL437784 | — | — | 1 | 8.17 |
| CHEMBL257355 | — | — | 1 | 8.08 |
| CHEMBL403273 | — | — | 1 | 7.17 |
| CHEMBL258172 | — | — | 1 | 6.92 |
| CHEMBL429677 | — | — | 1 | - |
| CHEMBL254754 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL411557 | DYNORPHIN A (1-17) | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL257139 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL402135 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL38576 | ICI-199,441 | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL402820 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL257140 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL402189 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL254959 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL254960 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL401594 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL437784 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL257355 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL403273 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL258172 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL429677 | — | Ki | - | — | - | |
| CHEMBL254754 | — | Ki | - | — | - |