Assay Detail
Binding
CHEMBL753519
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against opioid receptor kappa, in guinea pig brain membrane, using [3H]bremazocine as the radioligand.
16
Total Activities
16
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
Structure/activity studies related to 2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]acetamides: a novel series of potent and selective kappa-opioid agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.25 | 8.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38576 | ICI-199,441 | — | 1 | 8.16 |
| CHEMBL56653 | — | — | 1 | 8.16 |
| CHEMBL105942 | — | — | 1 | 8.00 |
| CHEMBL109205 | — | — | 1 | 7.97 |
| CHEMBL320882 | — | — | 1 | 7.91 |
| CHEMBL321061 | — | — | 1 | 7.85 |
| CHEMBL106471 | — | — | 1 | 7.61 |
| CHEMBL105984 | — | — | 1 | 7.41 |
| CHEMBL56651 | — | — | 1 | 7.28 |
| CHEMBL110924 | — | — | 1 | 7.24 |
| CHEMBL105783 | — | — | 1 | 7.18 |
| CHEMBL290543 | — | — | 1 | 7.02 |
| CHEMBL106510 | — | — | 1 | 7.00 |
| CHEMBL420115 | — | — | 1 | 5.99 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 5.62 |
| CHEMBL106345 | — | — | 1 | 5.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38576 | ICI-199,441 | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL56653 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL105942 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL109205 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL320882 | — | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL321061 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL106471 | — | IC50 | = | 24.5 | nM | 7.61 |
| CHEMBL105984 | — | IC50 | = | 38.7 | nM | 7.41 |
| CHEMBL56651 | — | IC50 | = | 52.5 | nM | 7.28 |
| CHEMBL110924 | — | IC50 | = | 57.8 | nM | 7.24 |
| CHEMBL105783 | — | IC50 | = | 65.4 | nM | 7.18 |
| CHEMBL290543 | — | IC50 | = | 95.5 | nM | 7.02 |
| CHEMBL106510 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL420115 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL70 | MORPHINE | IC50 | = | 2390.0 | nM | 5.62 |
| CHEMBL106345 | — | IC50 | = | 2750.0 | nM | 5.56 |