Assay Detail
Functional
CHEMBL2353035
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human kappa opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding after 60 mins by liquid scintillation counting
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 9: Synthesis, characterization and molecular modeling of pyridinyl isosteres of N-BPE-8-CAC (1), a high affinity ligand for opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 8.11 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2347237 | — | — | 1 | 8.59 |
| CHEMBL377789 | — | — | 1 | 8.52 |
| CHEMBL58646 | — | — | 1 | 8.36 |
| CHEMBL2347235 | — | — | 1 | 8.30 |
| CHEMBL2347238 | — | — | 1 | 8.11 |
| CHEMBL2347239 | — | — | 1 | 7.85 |
| CHEMBL2347236 | — | — | 1 | 7.72 |
| CHEMBL290543 | — | — | 1 | 7.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2347237 | — | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL377789 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL58646 | — | EC50 | = | 4.4 | nM | 8.36 |
| CHEMBL2347235 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2347238 | — | EC50 | = | 7.8 | nM | 8.11 |
| CHEMBL2347239 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2347236 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL290543 | — | EC50 | = | 36.0 | nM | 7.44 |