Assay Detail
Functional
CHEMBL852482
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for alpha-2C adrenergic receptor
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 8.81 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL435352 | — | — | 1 | 10.52 |
| CHEMBL176261 | — | — | 1 | 10.00 |
| CHEMBL2112985 | — | — | 1 | 10.00 |
| CHEMBL180470 | — | — | 1 | 10.00 |
| CHEMBL175853 | — | — | 1 | 9.70 |
| CHEMBL176116 | — | — | 1 | 9.70 |
| CHEMBL179237 | — | — | 1 | 9.70 |
| CHEMBL176002 | — | — | 1 | 9.70 |
| CHEMBL175911 | — | — | 1 | 9.52 |
| CHEMBL425324 | — | — | 1 | 9.30 |
| CHEMBL180322 | — | — | 1 | 9.30 |
| CHEMBL369378 | — | — | 1 | 9.30 |
| CHEMBL178588 | — | — | 1 | 8.80 |
| CHEMBL2112969 | — | — | 1 | 8.80 |
| CHEMBL2112978 | — | — | 1 | 8.77 |
| CHEMBL2112973 | — | — | 1 | 8.57 |
| CHEMBL2112971 | — | — | 1 | 8.44 |
| CHEMBL2112982 | — | — | 1 | 8.41 |
| CHEMBL2112977 | — | — | 1 | 8.40 |
| CHEMBL2112970 | — | — | 1 | 8.35 |
| CHEMBL2112983 | — | — | 1 | 8.27 |
| CHEMBL328114 | — | — | 1 | 8.21 |
| CHEMBL2112972 | — | — | 1 | 8.20 |
| CHEMBL2112984 | — | — | 1 | 8.02 |
| CHEMBL2112975 | — | — | 1 | 8.01 |
| CHEMBL426959 | — | — | 1 | 7.96 |
| CHEMBL2112976 | — | — | 1 | 7.92 |
| CHEMBL2112981 | — | — | 1 | 7.82 |
| CHEMBL2112974 | — | — | 1 | 7.64 |
| CHEMBL2112979 | — | — | 1 | 6.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL435352 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL176261 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL2112985 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL180470 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL175853 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL176116 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL179237 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL176002 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL175911 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL425324 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL180322 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL369378 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL178588 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL2112969 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL2112978 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL2112973 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL2112971 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL2112982 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL2112977 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2112970 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL2112983 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL328114 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL2112972 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL2112984 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL2112975 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL426959 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2112976 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2112981 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2112974 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL2112979 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL2112980 | — | Ki | > | 1000.0 | nM | - |