Assay Detail
Binding
CHEMBL753447
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Affinity for opioid receptor mu sites
15
Total Activities
14
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
(1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.85 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL70 | MORPHINE | 4.0 | 1 | 8.48 |
| CHEMBL2114225 | — | — | 2 | 7.97 |
| CHEMBL2114223 | — | — | 1 | 7.52 |
| CHEMBL88168 | — | — | 1 | 7.33 |
| CHEMBL89307 | — | — | 1 | 7.33 |
| CHEMBL88393 | — | — | 1 | 6.64 |
| CHEMBL2114226 | — | — | 1 | 6.53 |
| CHEMBL329114 | — | — | 1 | 6.38 |
| CHEMBL87010 | — | — | 1 | 6.35 |
| CHEMBL290543 | — | — | 1 | 6.21 |
| CHEMBL71294 | — | — | 1 | 5.81 |
| CHEMBL433508 | — | — | 1 | 5.63 |
| CHEMBL329343 | — | — | 1 | - |
| CHEMBL330449 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL70 | MORPHINE | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL2114225 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL2114223 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL88168 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL89307 | — | Ki | = | 47.2 | nM | 7.33 |
| CHEMBL88393 | — | Ki | = | 231.0 | nM | 6.64 |
| CHEMBL2114226 | — | Ki | = | 293.0 | nM | 6.53 |
| CHEMBL329114 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL87010 | — | Ki | = | 445.0 | nM | 6.35 |
| CHEMBL290543 | — | Ki | = | 616.0 | nM | 6.21 |
| CHEMBL71294 | — | Ki | = | 1559.0 | nM | 5.81 |
| CHEMBL433508 | — | Ki | = | 2341.0 | nM | 5.63 |
| CHEMBL329343 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL330449 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2114225 | — | Ki | > | 1000.0 | nM | - |