Assay Detail
Functional
CHEMBL4410977
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Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and μ-Opioid Activity of the Primary Metabolites of Carfentanil.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 9.44 | 10.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4588535 | — | — | 1 | 10.85 |
| CHEMBL4578287 | — | — | 1 | 10.55 |
| CHEMBL4548662 | — | — | 1 | 9.70 |
| CHEMBL4524446 | — | — | 1 | 9.55 |
| CHEMBL596 | FENTANYL | 4.0 | 1 | 9.29 |
| CHEMBL4457592 | — | — | 1 | 8.36 |
| CHEMBL4562635 | — | — | 1 | 7.77 |
| CHEMBL290429 | CARFENTANIL | 2.0 | 1 | - |
| CHEMBL4463749 | — | — | 1 | - |
| CHEMBL4563672 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4588535 | — | EC50 | = | 0.014 | nM | 10.85 |
| CHEMBL4578287 | — | EC50 | = | 0.028 | nM | 10.55 |
| CHEMBL4548662 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4524446 | — | EC50 | = | 0.28 | nM | 9.55 |
| CHEMBL596 | FENTANYL | EC50 | = | 0.51 | nM | 9.29 |
| CHEMBL4457592 | — | EC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4562635 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL290429 | CARFENTANIL | EC50 | = | 0.0049 | nM | - |
| CHEMBL4463749 | — | EC50 | = | 0.0051 | nM | - |
| CHEMBL4563672 | — | EC50 | = | 0.0024 | nM | - |