Assay Detail
Functional
CHEMBL1107423
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Agonist activity at human recombinant kappa opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding after 45 mins by microplate luminescence assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 6.50 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL440765 | U-69593 | — | 1 | 7.10 |
| CHEMBL1094880 | — | — | 1 | 7.06 |
| CHEMBL1095521 | — | — | 1 | 6.09 |
| CHEMBL1094237 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL440765 | U-69593 | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1094880 | — | EC50 | = | 87.0 | nM | 7.06 |
| CHEMBL1095521 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL1094237 | — | EC50 | = | 1800.0 | nM | 5.75 |