Assay Detail
Functional
CHEMBL750345
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Antagonistic activity in the Opioid receptor kappa 1-mediated [35S]GTP-gamma-S, binding assay against 50 nM U-50,488
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationships of dynorphin a analogues modified in the address sequence.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.88 | 8.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 8.36 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 7.30 |
| CHEMBL2369408 | — | — | 1 | 6.47 |
| CHEMBL2369366 | — | — | 1 | 6.39 |
| CHEMBL2369365 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | IC50 | = | 4.37 | nM | 8.36 |
| CHEMBL80 | NALOXONE | IC50 | = | 49.8 | nM | 7.30 |
| CHEMBL2369408 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL2369366 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL2369365 | — | IC50 | = | 1260.0 | nM | 5.90 |