Assay Detail
Functional
CHEMBL1286052
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Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 19 | 7.18 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1276248 | — | — | 1 | 8.20 |
| CHEMBL242693 | — | — | 1 | 8.00 |
| CHEMBL396013 | — | — | 1 | 7.73 |
| CHEMBL1278084 | — | — | 1 | 7.60 |
| CHEMBL1276140 | — | — | 1 | 7.60 |
| CHEMBL1276220 | — | — | 1 | 7.45 |
| CHEMBL1276218 | — | — | 1 | 7.40 |
| CHEMBL374584 | — | — | 1 | 7.33 |
| CHEMBL495095 | ALLYPHENYLINE | — | 1 | 7.30 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 7.24 |
| CHEMBL128168 | BIPHENYLINE | — | 1 | 7.24 |
| CHEMBL385310 | — | — | 1 | 7.03 |
| CHEMBL1276247 | — | — | 1 | 7.00 |
| CHEMBL222928 | — | — | 1 | 7.00 |
| CHEMBL242265 | — | — | 1 | 6.95 |
| CHEMBL1276219 | — | — | 1 | 6.90 |
| CHEMBL1276139 | — | — | 1 | 6.73 |
| CHEMBL397753 | — | — | 1 | 6.13 |
| CHEMBL1278085 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1276248 | — | EC50 | = | 6.31 | nM | 8.20 |
| CHEMBL242693 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL396013 | — | EC50 | = | 18.62 | nM | 7.73 |
| CHEMBL1278084 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL1276140 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL1276220 | — | EC50 | = | 35.48 | nM | 7.45 |
| CHEMBL1276218 | — | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL374584 | — | EC50 | = | 46.77 | nM | 7.33 |
| CHEMBL495095 | ALLYPHENYLINE | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL134 | CLONIDINE | EC50 | = | 57.54 | nM | 7.24 |
| CHEMBL128168 | BIPHENYLINE | EC50 | = | 57.54 | nM | 7.24 |
| CHEMBL385310 | — | EC50 | = | 93.33 | nM | 7.03 |
| CHEMBL1276247 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL222928 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL242265 | — | EC50 | = | 112.2 | nM | 6.95 |
| CHEMBL1276219 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL1276139 | — | EC50 | = | 186.21 | nM | 6.73 |
| CHEMBL397753 | — | EC50 | = | 741.31 | nM | 6.13 |
| CHEMBL1278085 | — | EC50 | = | 2511.89 | nM | 5.60 |