Assay Detail
Functional
CHEMBL2182837
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Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay
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
Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 7.43 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2180639 | — | — | 1 | 8.44 |
| CHEMBL290543 | — | — | 1 | 8.03 |
| CHEMBL440765 | U-69593 | — | 1 | 7.58 |
| CHEMBL2180638 | — | — | 1 | 7.46 |
| CHEMBL2180640 | — | — | 1 | 7.33 |
| CHEMBL1188090 | — | — | 1 | 7.31 |
| CHEMBL2180637 | — | — | 1 | 7.06 |
| CHEMBL2180641 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2180639 | — | EC50 | = | 3.62 | nM | 8.44 |
| CHEMBL290543 | — | EC50 | = | 9.31 | nM | 8.03 |
| CHEMBL440765 | U-69593 | EC50 | = | 26.1 | nM | 7.58 |
| CHEMBL2180638 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2180640 | — | EC50 | = | 46.2 | nM | 7.33 |
| CHEMBL1188090 | — | EC50 | = | 49.1 | nM | 7.31 |
| CHEMBL2180637 | — | EC50 | = | 86.4 | nM | 7.06 |
| CHEMBL2180641 | — | EC50 | = | 647.0 | nM | 6.19 |