Assay Detail
Binding
CHEMBL3590955
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Antagonist activity against human kappa opioid receptor expressed in human U2OS cells co-expressing beta-arrestin2 pre-treated for 15 mins before U69,593 stimulation for 90 mins by DiscoveRx beta-arrestin2 recruitment based PathHunter assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.64 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 8.60 |
| CHEMBL3590199 | — | — | 1 | 7.08 |
| CHEMBL3590200 | — | — | 1 | 7.03 |
| CHEMBL3590195 | — | — | 1 | 6.98 |
| CHEMBL3590197 | — | — | 1 | 6.98 |
| CHEMBL3590196 | — | — | 1 | 6.73 |
| CHEMBL3590194 | — | — | 1 | 6.46 |
| CHEMBL3590192 | — | — | 1 | 6.41 |
| CHEMBL3590193 | — | — | 1 | 6.41 |
| CHEMBL1455766 | — | — | 1 | 6.39 |
| CHEMBL3590191 | — | — | 1 | 6.32 |
| CHEMBL3590201 | — | — | 1 | 6.15 |
| CHEMBL3590198 | — | — | 1 | 6.06 |
| CHEMBL1724868 | — | — | 1 | 6.03 |
| CHEMBL3590190 | — | — | 1 | 6.03 |
| CHEMBL3590189 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3590199 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL3590200 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL3590195 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL3590197 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL3590196 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL3590194 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3590192 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL3590193 | — | IC50 | = | 388.0 | nM | 6.41 |
| CHEMBL1455766 | — | IC50 | = | 403.0 | nM | 6.39 |
| CHEMBL3590191 | — | IC50 | = | 478.0 | nM | 6.32 |
| CHEMBL3590201 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL3590198 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL1724868 | — | IC50 | = | 937.0 | nM | 6.03 |
| CHEMBL3590190 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL3590189 | — | IC50 | - | — | - |