Assay Detail
Binding
CHEMBL754736
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Binding affinity towards Opioid receptor kappa 1 on guinea pig cerebellum membranes by [3H]U-69593 displacement.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebellum |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
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 | 20 | 5.90 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2371019 | — | — | 1 | 6.60 |
| CHEMBL2370013 | — | — | 1 | 6.36 |
| CHEMBL2371026 | — | — | 1 | 6.12 |
| CHEMBL557035 | — | — | 1 | 6.08 |
| CHEMBL2371014 | — | — | 1 | 5.93 |
| CHEMBL2369139 | — | — | 1 | 5.92 |
| CHEMBL2371015 | — | — | 1 | 5.89 |
| CHEMBL2371013 | — | — | 1 | 5.60 |
| CHEMBL2371025 | — | — | 1 | 5.55 |
| CHEMBL2371016 | — | — | 1 | 5.47 |
| CHEMBL2371020 | — | — | 1 | 5.36 |
| CHEMBL2371018 | — | — | 1 | - |
| CHEMBL2371009 | — | — | 1 | - |
| CHEMBL3350370 | — | — | 1 | - |
| CHEMBL2371024 | — | — | 1 | - |
| CHEMBL2371023 | — | — | 1 | - |
| CHEMBL191751 | — | — | 1 | - |
| CHEMBL2371027 | — | — | 1 | - |
| CHEMBL2372509 | — | — | 1 | - |
| CHEMBL2371017 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2371019 | — | Ki | = | 253.0 | nM | 6.60 |
| CHEMBL2370013 | — | Ki | = | 442.0 | nM | 6.36 |
| CHEMBL2371026 | — | Ki | = | 766.0 | nM | 6.12 |
| CHEMBL557035 | — | Ki | = | 838.0 | nM | 6.08 |
| CHEMBL2371014 | — | Ki | = | 1180.0 | nM | 5.93 |
| CHEMBL2369139 | — | Ki | = | 1190.0 | nM | 5.92 |
| CHEMBL2371015 | — | Ki | = | 1282.0 | nM | 5.89 |
| CHEMBL2371013 | — | Ki | = | 2509.0 | nM | 5.60 |
| CHEMBL2371025 | — | Ki | = | 2844.0 | nM | 5.55 |
| CHEMBL2371016 | — | Ki | = | 3396.0 | nM | 5.47 |
| CHEMBL2371020 | — | Ki | = | 4324.0 | nM | 5.36 |
| CHEMBL2371018 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2371009 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3350370 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2371024 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2371023 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL191751 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2371027 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2372509 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2371017 | — | Ki | > | 10000.0 | nM | - |