Assay Detail
Functional
CHEMBL754276
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In vitro agonist activity at kappa opioid receptor in rabbit vas deferens.
23
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.47 | 10.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL603370 | — | — | 3 | 10.74 |
| CHEMBL62474 | — | — | 1 | 10.40 |
| CHEMBL66265 | — | — | 1 | 10.00 |
| CHEMBL293406 | — | — | 1 | 9.55 |
| CHEMBL62884 | — | — | 1 | 9.47 |
| CHEMBL294779 | — | — | 1 | 9.47 |
| CHEMBL63810 | — | — | 1 | 9.38 |
| CHEMBL304900 | — | — | 1 | 8.92 |
| CHEMBL408054 | — | — | 1 | 8.46 |
| CHEMBL293408 | — | — | 1 | 8.40 |
| CHEMBL62663 | — | — | 1 | 8.16 |
| CHEMBL62879 | — | — | 1 | 8.00 |
| CHEMBL62567 | — | — | 1 | 7.82 |
| CHEMBL292724 | — | — | 1 | 7.22 |
| CHEMBL440487 | — | — | 1 | 6.52 |
| CHEMBL290543 | — | — | 1 | 6.43 |
| CHEMBL63367 | — | — | 1 | 6.35 |
| CHEMBL430562 | — | — | 1 | 5.54 |
| CHEMBL65052 | — | — | 1 | - |
| CHEMBL292976 | — | — | 1 | - |
| CHEMBL302190 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL603370 | — | IC50 | = | 0.018 | nM | 10.74 |
| CHEMBL62474 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL603370 | — | IC50 | = | 0.041 | nM | 10.39 |
| CHEMBL66265 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL293406 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL62884 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL294779 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL63810 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL304900 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL408054 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL293408 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL603370 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL62663 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL62879 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL62567 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL292724 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL440487 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL290543 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL63367 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL430562 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL65052 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL292976 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL302190 | — | IC50 | > | 10000.0 | nM | - |