Assay Detail
Binding
CHEMBL3590954
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against HA-tagged human recombinant kappa opioid receptor expressed in CHO cells assessed as inhibition of U69,593-induced ERK phosphorylation pre-incubated with compound before U69,593 stimulation for 10 mins
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 | 8.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 8.34 |
| CHEMBL3590195 | — | — | 1 | 7.31 |
| CHEMBL3590197 | — | — | 1 | 7.12 |
| CHEMBL3590200 | — | — | 1 | 7.06 |
| CHEMBL3590199 | — | — | 1 | 6.97 |
| CHEMBL3590196 | — | — | 1 | 6.84 |
| CHEMBL3590193 | — | — | 1 | 6.59 |
| CHEMBL3590194 | — | — | 1 | 6.50 |
| CHEMBL3590192 | — | — | 1 | 6.40 |
| CHEMBL3590191 | — | — | 1 | 6.39 |
| CHEMBL1455766 | — | — | 1 | 6.23 |
| CHEMBL1724868 | — | — | 1 | 6.12 |
| CHEMBL3590190 | — | — | 1 | 5.95 |
| CHEMBL3590198 | — | — | 1 | 5.92 |
| CHEMBL3590201 | — | — | 1 | 5.87 |
| CHEMBL3590189 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3590195 | — | IC50 | = | 49.1 | nM | 7.31 |
| CHEMBL3590197 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3590200 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3590199 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL3590196 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL3590193 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL3590194 | — | IC50 | = | 314.0 | nM | 6.50 |
| CHEMBL3590192 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3590191 | — | IC50 | = | 406.0 | nM | 6.39 |
| CHEMBL1455766 | — | IC50 | = | 591.0 | nM | 6.23 |
| CHEMBL1724868 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL3590190 | — | IC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL3590198 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3590201 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL3590189 | — | IC50 | - | — | - |