Assay Detail
Binding
CHEMBL977779
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Increase of JNK phosphorylation in U50488 treated HEK293 cells expressing GFP tagged kappa opioid receptor
6
Total Activities
5
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 7.02 | 8.30 |
| Activity | 1 | - | - |
| Intrinsic activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL415247 | JDTIC | 1.0 | 1 | 8.30 |
| CHEMBL500830 | DYNORPHIN B | — | 1 | 7.06 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 6.80 |
| CHEMBL290543 | — | — | 2 | 5.91 |
| CHEMBL511142 | BUPRENORPHINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL415247 | JDTIC | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL500830 | DYNORPHIN B | EC50 | = | 87.0 | nM | 7.06 |
| CHEMBL573214 | NORBINALTORPHIMINE | EC50 | = | 158.0 | nM | 6.80 |
| CHEMBL290543 | — | EC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL511142 | BUPRENORPHINE | Activity | - | — | - | |
| CHEMBL290543 | — | Intrinsic activity | = | 1.0 | — | - |