Assay Detail
Functional
CHEMBL4372804
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Agonist activity at human KOR expressed in HEK293T cells assessed as inhibition of Galphai-mediated cAMP accumulation after 15 mins by microbeta counting assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of Novel Quinoxaline-Based κ-Opioid Receptor Agonists for the Treatment of Neuroinflammation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 8.61 | 10.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL445332 | SALVINORIN A | 1.0 | 1 | 10.82 |
| CHEMBL4069231 | — | — | 1 | 8.92 |
| CHEMBL4582146 | — | — | 1 | 8.80 |
| CHEMBL4467644 | — | — | 1 | 8.70 |
| CHEMBL4463652 | — | — | 1 | 8.55 |
| CHEMBL4462000 | — | — | 1 | 8.47 |
| CHEMBL4561040 | — | — | 1 | 8.22 |
| CHEMBL4483681 | — | — | 1 | 8.09 |
| CHEMBL4555496 | — | — | 1 | 8.00 |
| CHEMBL4438714 | — | — | 1 | 7.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL445332 | SALVINORIN A | EC50 | = | 0.015 | nM | 10.82 |
| CHEMBL4069231 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4582146 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4467644 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4463652 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4462000 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4561040 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4483681 | — | EC50 | = | 8.1 | nM | 8.09 |
| CHEMBL4555496 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4438714 | — | EC50 | = | 32.0 | nM | 7.50 |