Assay Detail
Binding
CHEMBL751031
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Binding affinity towards human cloned Opioid receptor kappa 1 using [3H]U-69593
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 8.88 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 9.70 |
| CHEMBL415247 | JDTIC | 1.0 | 1 | 9.39 |
| CHEMBL575508 | — | — | 1 | 9.00 |
| CHEMBL2112473 | — | — | 1 | 8.74 |
| CHEMBL10872 | — | — | 1 | 8.66 |
| CHEMBL2112474 | — | — | 1 | 7.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL415247 | JDTIC | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL575508 | — | Ki | = | 1.01 | nM | 9.00 |
| CHEMBL2112473 | — | Ki | = | 1.82 | nM | 8.74 |
| CHEMBL10872 | — | Ki | = | 2.18 | nM | 8.66 |
| CHEMBL2112474 | — | Ki | = | 16.2 | nM | 7.79 |