Assay Detail
Binding
CHEMBL4372802
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Displacement of [3H]diprenorphine from human KOR expressed in HEK293T cell membranes after 120 mins by scintillation counting method
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 10 | 7.88 | 9.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281786 | DIPRENORPHINE | 2.0 | 1 | 9.16 |
| CHEMBL4069231 | — | — | 1 | 8.32 |
| CHEMBL4582146 | — | — | 1 | 8.04 |
| CHEMBL4462000 | — | — | 1 | 7.96 |
| CHEMBL4467644 | — | — | 1 | 7.96 |
| CHEMBL4561040 | — | — | 1 | 7.80 |
| CHEMBL4483681 | — | — | 1 | 7.75 |
| CHEMBL4438714 | — | — | 1 | 7.38 |
| CHEMBL4463652 | — | — | 1 | 7.34 |
| CHEMBL4555496 | — | — | 1 | 7.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281786 | DIPRENORPHINE | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL4069231 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL4582146 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL4462000 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4467644 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4561040 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4483681 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4438714 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL4463652 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL4555496 | — | Ki | = | 77.0 | nM | 7.11 |