Assay Detail
Binding
CHEMBL927004
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Displacement of [3H]diprenorphine from human kappa 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 | 9.22 | 10.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38576 | ICI-199,441 | — | 1 | 10.36 |
| CHEMBL257140 | — | — | 1 | 9.72 |
| CHEMBL411557 | DYNORPHIN A (1-17) | — | 1 | 9.68 |
| CHEMBL402135 | — | — | 1 | 9.66 |
| CHEMBL402820 | — | — | 1 | 9.51 |
| CHEMBL254959 | — | — | 1 | 9.30 |
| CHEMBL257139 | — | — | 1 | 9.27 |
| CHEMBL402189 | — | — | 1 | 9.26 |
| CHEMBL401594 | — | — | 1 | 9.17 |
| CHEMBL403273 | — | — | 1 | 9.15 |
| CHEMBL257355 | — | — | 1 | 8.96 |
| CHEMBL437784 | — | — | 1 | 8.89 |
| CHEMBL429677 | — | — | 1 | 8.85 |
| CHEMBL254960 | — | — | 1 | 8.80 |
| CHEMBL258172 | — | — | 1 | 8.55 |
| CHEMBL254754 | — | — | 1 | 8.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38576 | ICI-199,441 | Ki | = | 0.044 | nM | 10.36 |
| CHEMBL257140 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL411557 | DYNORPHIN A (1-17) | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL402135 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL402820 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL254959 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL257139 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL402189 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL401594 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL403273 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL257355 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL437784 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL429677 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL254960 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL258172 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL254754 | — | Ki | = | 3.8 | nM | 8.42 |