Assay Detail
Binding
CHEMBL5055010
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Displacement of [3H]U69,593 from human kappa opioid receptor expressed in mouse HN9.10 cells assessed as inhibition constant by radioligand binding assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HN9.10 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
C-terminal modified Enkephalin-like tetrapeptides with enhanced affinities at the kappa opioid receptor and monoamine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.18 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5089012 | — | — | 1 | 9.89 |
| CHEMBL5094499 | — | — | 1 | 9.28 |
| CHEMBL5086370 | — | — | 1 | 8.82 |
| CHEMBL5078669 | — | — | 1 | 8.24 |
| CHEMBL5091642 | — | — | 1 | 7.70 |
| CHEMBL5090705 | — | — | 1 | 7.55 |
| CHEMBL5077561 | — | — | 1 | 7.47 |
| CHEMBL5083183 | — | — | 1 | 7.36 |
| CHEMBL5081245 | — | — | 1 | 7.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5089012 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL5094499 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL5086370 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL5078669 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL5091642 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL5090705 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL5077561 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL5083183 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL5081245 | — | Ki | = | 47.0 | nM | 7.33 |