Assay Detail
Binding
CHEMBL753745
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Inhibition of [3H]DAMGO binding to Opioid receptor mu 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 | 6.86 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL415247 | JDTIC | 1.0 | 1 | 8.43 |
| CHEMBL575508 | — | — | 1 | 7.43 |
| CHEMBL485832 | GUANIDINONALTRINDOLE | — | 1 | 7.43 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 7.19 |
| CHEMBL2112473 | — | — | 1 | 6.97 |
| CHEMBL2112475 | — | — | 1 | 6.86 |
| CHEMBL2112474 | — | — | 1 | 6.79 |
| CHEMBL10986 | — | — | 1 | 6.77 |
| CHEMBL2111681 | — | — | 2 | 6.68 |
| CHEMBL326471 | — | — | 1 | 6.22 |
| CHEMBL2112472 | — | — | 1 | 6.12 |
| CHEMBL10872 | — | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL415247 | JDTIC | Ki | = | 3.73 | nM | 8.43 |
| CHEMBL575508 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL485832 | GUANIDINONALTRINDOLE | Ki | = | 36.9 | nM | 7.43 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL2112473 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL2112475 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL2112474 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL10986 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL2111681 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL326471 | — | Ki | = | 596.0 | nM | 6.22 |
| CHEMBL2111681 | — | Ki | = | 633.0 | nM | 6.20 |
| CHEMBL2112472 | — | Ki | = | 764.0 | nM | 6.12 |
| CHEMBL10872 | — | Ki | = | 775.0 | nM | 6.11 |