Assay Detail
Binding
CHEMBL3254255
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Displacement of [3H] naloxone from opioid receptor (unknown origin) in presence of 100 mM NaCl
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Stereochemical studies on medicinal agents. 23. Synthesis and biological evaluation of 6-amino derivatives of naloxone and naltrexone.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.17 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201149 | NALTREXONE HYDROCHLORIDE | 4.0 | 1 | 9.23 |
| CHEMBL3249714 | — | — | 1 | 9.15 |
| CHEMBL1718 | NALOXONE HYDROCHLORIDE | 4.0 | 1 | 8.37 |
| CHEMBL3249715 | — | — | 1 | 8.05 |
| CHEMBL3249712 | — | — | 1 | 7.28 |
| CHEMBL3249713 | — | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201149 | NALTREXONE HYDROCHLORIDE | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL3249714 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL1718 | NALOXONE HYDROCHLORIDE | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3249715 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3249712 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3249713 | — | IC50 | = | 110.0 | nM | 6.96 |