Assay Detail
Binding
CHEMBL756647
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Binding affinity towards Opioid receptor mu 1 on rat forebrain membranes by [3H]sufentanil displacement.
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Forebrain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Side chain methyl substitution in the delta-opioid receptor antagonist TIPP has an important effect on the activity profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 6.47 | 8.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL365581 | — | — | 1 | 8.14 |
| CHEMBL2371015 | — | — | 1 | 7.33 |
| CHEMBL2369139 | — | — | 1 | 7.08 |
| CHEMBL2371020 | — | — | 1 | 6.83 |
| CHEMBL557035 | — | — | 1 | 6.75 |
| CHEMBL2371023 | — | — | 1 | 6.55 |
| CHEMBL2371009 | — | — | 1 | 6.45 |
| CHEMBL2371026 | — | — | 1 | 6.30 |
| CHEMBL2364557 | — | — | 1 | 6.18 |
| CHEMBL2371027 | — | — | 1 | 6.09 |
| CHEMBL2371016 | — | — | 1 | 6.01 |
| CHEMBL2371014 | — | — | 1 | 5.80 |
| CHEMBL2371019 | — | — | 1 | 5.69 |
| CHEMBL191751 | — | — | 2 | 5.40 |
| CHEMBL2371013 | — | — | 1 | - |
| CHEMBL2372509 | — | — | 1 | - |
| CHEMBL3350370 | — | — | 1 | - |
| CHEMBL2370013 | — | — | 1 | - |
| CHEMBL2371024 | — | — | 1 | - |
| CHEMBL2371018 | — | — | 1 | - |
| CHEMBL2371025 | — | — | 1 | - |
| CHEMBL2371017 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL365581 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL2371015 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL2369139 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL2371020 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL557035 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL2371023 | — | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL2371009 | — | Ki | = | 352.0 | nM | 6.45 |
| CHEMBL2371026 | — | Ki | = | 498.0 | nM | 6.30 |
| CHEMBL2364557 | — | Ki | = | 658.0 | nM | 6.18 |
| CHEMBL2371027 | — | Ki | = | 810.0 | nM | 6.09 |
| CHEMBL2371016 | — | Ki | = | 973.0 | nM | 6.01 |
| CHEMBL2371014 | — | Ki | = | 1596.0 | nM | 5.80 |
| CHEMBL2371019 | — | Ki | = | 2021.0 | nM | 5.69 |
| CHEMBL191751 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL2371013 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2372509 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3350370 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2370013 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2371024 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2371018 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2371025 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL191751 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2371017 | — | Ki | > | 10000.0 | nM | - |