Assay Detail
Binding
CHEMBL755519
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-BRL 52537 from opioid receptor kappa site in guinea pig
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 | 8.94 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2114223 | — | — | 1 | 9.70 |
| CHEMBL89307 | — | — | 1 | 9.66 |
| CHEMBL2114225 | — | — | 2 | 9.62 |
| CHEMBL71294 | — | — | 1 | 9.51 |
| CHEMBL88168 | — | — | 1 | 9.34 |
| CHEMBL87010 | — | — | 1 | 9.33 |
| CHEMBL2114226 | — | — | 1 | 9.29 |
| CHEMBL329114 | — | — | 1 | 9.22 |
| CHEMBL88393 | — | — | 1 | 9.21 |
| CHEMBL433508 | — | — | 1 | 9.19 |
| CHEMBL290543 | — | — | 1 | 8.66 |
| CHEMBL330449 | — | — | 1 | 7.00 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 6.52 |
| CHEMBL329343 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2114223 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL89307 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL2114225 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL71294 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL88168 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL87010 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL2114226 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL329114 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL88393 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL433508 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL290543 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL330449 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL70 | MORPHINE | Ki | = | 301.0 | nM | 6.52 |
| CHEMBL329343 | — | Ki | > | 100.0 | nM | - |
| CHEMBL2114225 | — | Ki | > | 1000.0 | nM | - |