Assay Detail
Binding
CHEMBL753671
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Inhibition of [3H]-DADLE binding to Opioid receptor delta 1 of rat brain tissue
13
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
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 | 6.76 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL485832 | GUANIDINONALTRINDOLE | — | 1 | 7.16 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 7.07 |
| CHEMBL2112475 | — | — | 1 | 6.84 |
| CHEMBL415247 | JDTIC | 1.0 | 1 | 6.52 |
| CHEMBL575508 | — | — | 1 | 6.21 |
| CHEMBL10872 | — | — | 1 | - |
| CHEMBL326471 | — | — | 1 | - |
| CHEMBL2112472 | — | — | 1 | - |
| CHEMBL10986 | — | — | 1 | - |
| CHEMBL2111681 | — | — | 2 | - |
| CHEMBL2112473 | — | — | 1 | - |
| CHEMBL2112474 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL485832 | GUANIDINONALTRINDOLE | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL2112475 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL415247 | JDTIC | Ki | = | 301.0 | nM | 6.52 |
| CHEMBL575508 | — | Ki | = | 616.0 | nM | 6.21 |
| CHEMBL10872 | — | Ki | > | 4900.0 | nM | - |
| CHEMBL326471 | — | Ki | > | 4900.0 | nM | - |
| CHEMBL2112472 | — | Ki | > | 4900.0 | nM | - |
| CHEMBL10986 | — | Ki | > | 3400.0 | nM | - |
| CHEMBL2111681 | — | Ki | > | 5051.0 | nM | - |
| CHEMBL2112473 | — | Ki | > | 4900.0 | nM | - |
| CHEMBL2112474 | — | Ki | > | 3400.0 | nM | - |
| CHEMBL2111681 | — | Ki | > | 5051.0 | nM | - |