Assay Detail
Binding
CHEMBL754616
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Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of guinea pig brain
13
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
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 | 13 | 8.51 | 10.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL575508 | — | — | 1 | 10.28 |
| CHEMBL485832 | GUANIDINONALTRINDOLE | — | 1 | 9.74 |
| CHEMBL415247 | JDTIC | 1.0 | 1 | 9.49 |
| CHEMBL2112473 | — | — | 1 | 9.20 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 8.96 |
| CHEMBL10872 | — | — | 1 | 8.68 |
| CHEMBL10986 | — | — | 1 | 8.42 |
| CHEMBL326471 | — | — | 1 | 8.01 |
| CHEMBL2112474 | — | — | 1 | 7.81 |
| CHEMBL2111681 | — | — | 2 | 7.80 |
| CHEMBL2112475 | — | — | 1 | 7.76 |
| CHEMBL2112472 | — | — | 1 | 6.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL575508 | — | Ki | = | 0.053 | nM | 10.28 |
| CHEMBL485832 | GUANIDINONALTRINDOLE | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL415247 | JDTIC | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL2112473 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 1.09 | nM | 8.96 |
| CHEMBL10872 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL10986 | — | Ki | = | 3.84 | nM | 8.42 |
| CHEMBL326471 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL2112474 | — | Ki | = | 15.5 | nM | 7.81 |
| CHEMBL2111681 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2112475 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL2111681 | — | Ki | = | 20.4 | nM | 7.69 |
| CHEMBL2112472 | — | Ki | = | 146.0 | nM | 6.84 |