Assay Detail
Binding
CHEMBL759288
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Binding affinity against opioid receptor kappa 1 using [3H]-U-69,593 as radioligand in guinea pig brain membranes.
37
Total Activities
37
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
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 7.92 | 10.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | — | 1 | 10.47 |
| CHEMBL301160 | BUTORPHAN | — | 1 | 10.10 |
| CHEMBL433272 | — | — | 1 | 10.06 |
| CHEMBL301804 | — | — | 1 | 9.74 |
| CHEMBL299220 | — | — | 1 | 9.74 |
| CHEMBL300033 | — | — | 1 | 9.74 |
| CHEMBL48241 | — | — | 1 | 9.32 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | — | 1 | 9.21 |
| CHEMBL49143 | — | — | 1 | 8.74 |
| CHEMBL592 | LEVORPHANOL | 4.0 | 1 | 8.64 |
| CHEMBL295237 | — | — | 1 | 8.60 |
| CHEMBL296282 | — | — | 1 | 8.57 |
| CHEMBL297292 | — | — | 1 | 8.41 |
| CHEMBL300877 | — | — | 1 | 8.33 |
| CHEMBL48157 | — | — | 1 | 8.22 |
| CHEMBL295402 | — | — | 1 | 8.13 |
| CHEMBL49106 | — | — | 1 | 8.11 |
| CHEMBL48390 | — | — | 1 | 8.11 |
| CHEMBL298688 | — | — | 1 | 8.07 |
| CHEMBL42055 | E-FLUPENTIXOL | 2.0 | 1 | 7.77 |
| CHEMBL298027 | — | — | 1 | 7.62 |
| CHEMBL48936 | — | — | 1 | 7.60 |
| CHEMBL432120 | — | — | 1 | 7.33 |
| CHEMBL299189 | — | — | 1 | 7.23 |
| CHEMBL298571 | — | — | 1 | 7.22 |
| CHEMBL48420 | — | — | 1 | 6.96 |
| CHEMBL49318 | — | — | 1 | 6.92 |
| CHEMBL296304 | — | — | 1 | 6.70 |
| CHEMBL48816 | — | — | 1 | 6.60 |
| CHEMBL298446 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | Ki | = | 0.034 | nM | 10.47 |
| CHEMBL301160 | BUTORPHAN | Ki | = | 0.079 | nM | 10.10 |
| CHEMBL433272 | — | Ki | = | 0.087 | nM | 10.06 |
| CHEMBL301804 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL299220 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL300033 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL48241 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL49143 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL592 | LEVORPHANOL | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL295237 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL296282 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL297292 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL300877 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL48157 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL295402 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL49106 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL48390 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL298688 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL42055 | E-FLUPENTIXOL | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL298027 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL48936 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL432120 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL299189 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL298571 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL48420 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL49318 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL296304 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL48816 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL298446 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL48974 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL299132 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL297467 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL46320 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL300023 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL47488 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL296328 | — | Ki | = | 850.0 | nM | 6.07 |