Assay Detail
Binding
CHEMBL748537
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Inhibitory concentration against Opioid receptor kappa 1 using [3H]- U-69,593 radioligand
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.25 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.30 |
| CHEMBL2112732 | — | — | 1 | 8.70 |
| CHEMBL440765 | U-69593 | — | 1 | 8.68 |
| CHEMBL468469 | — | — | 1 | 8.59 |
| CHEMBL152351 | — | — | 1 | 8.22 |
| CHEMBL347674 | — | — | 1 | 8.13 |
| CHEMBL345208 | — | — | 1 | 8.09 |
| CHEMBL154510 | — | — | 1 | 7.77 |
| CHEMBL352224 | — | — | 1 | 7.68 |
| CHEMBL152327 | — | — | 1 | 7.37 |
| CHEMBL31421 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL2112732 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL440765 | U-69593 | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL468469 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL152351 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL347674 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL345208 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL154510 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL352224 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL152327 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL31421 | — | IC50 | > | 1000.0 | nM | - |