Assay Detail
Binding
CHEMBL751037
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Binding affinity against cloned human Opioid receptor kappa 1 transfected into chinese hamster ovary cells using [3H]U-69593 as radioligand
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | ovary |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 8.85 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2112374 | — | — | 1 | 9.74 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 9.70 |
| CHEMBL2112373 | — | — | 1 | 9.31 |
| CHEMBL610044 | — | — | 1 | 9.20 |
| CHEMBL610045 | — | — | 1 | 9.18 |
| CHEMBL610043 | — | — | 1 | 9.07 |
| CHEMBL610038 | — | — | 1 | 9.02 |
| CHEMBL610042 | — | — | 1 | 8.85 |
| CHEMBL610032 | — | — | 1 | 8.79 |
| CHEMBL610033 | — | — | 1 | 8.67 |
| CHEMBL610799 | — | — | 1 | 8.62 |
| CHEMBL610041 | — | — | 1 | 8.62 |
| CHEMBL610035 | — | — | 1 | 8.56 |
| CHEMBL610040 | — | — | 1 | 8.56 |
| CHEMBL610036 | — | — | 1 | 8.49 |
| CHEMBL610037 | — | — | 1 | 8.41 |
| CHEMBL610039 | — | — | 1 | 8.32 |
| CHEMBL610034 | — | — | 1 | 8.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2112374 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL2112373 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL610044 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL610045 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL610043 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL610038 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL610042 | — | Ki | = | 1.42 | nM | 8.85 |
| CHEMBL610032 | — | Ki | = | 1.61 | nM | 8.79 |
| CHEMBL610033 | — | Ki | = | 2.14 | nM | 8.67 |
| CHEMBL610799 | — | Ki | = | 2.38 | nM | 8.62 |
| CHEMBL610041 | — | Ki | = | 2.41 | nM | 8.62 |
| CHEMBL610035 | — | Ki | = | 2.72 | nM | 8.56 |
| CHEMBL610040 | — | Ki | = | 2.74 | nM | 8.56 |
| CHEMBL610036 | — | Ki | = | 3.26 | nM | 8.49 |
| CHEMBL610037 | — | Ki | = | 3.91 | nM | 8.41 |
| CHEMBL610039 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL610034 | — | Ki | = | 6.96 | nM | 8.16 |