Assay Detail
Functional
CHEMBL3584513
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells co-expressing C-terminally modified Galphaqi5 assessed as stimulation of calcium release by Fluo-4 AM dye-based fluorescence assay
12
Total Activities
12
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
Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 8.34 | 8.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3582487 | — | — | 1 | 8.98 |
| CHEMBL3580749 | — | — | 1 | 8.87 |
| CHEMBL411557 | DYNORPHIN A (1-17) | — | 1 | 8.75 |
| CHEMBL3580748 | — | — | 1 | 8.65 |
| CHEMBL3580746 | — | — | 1 | 8.55 |
| CHEMBL3580750 | — | — | 1 | 8.44 |
| CHEMBL3580745 | — | — | 1 | 8.32 |
| CHEMBL3580743 | — | — | 1 | 8.31 |
| CHEMBL3582485 | — | — | 1 | 8.12 |
| CHEMBL3582484 | — | — | 1 | 8.00 |
| CHEMBL3580744 | — | — | 1 | 7.93 |
| CHEMBL3582486 | — | — | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3582487 | — | EC50 | = | 1.047 | nM | 8.98 |
| CHEMBL3580749 | — | EC50 | = | 1.349 | nM | 8.87 |
| CHEMBL411557 | DYNORPHIN A (1-17) | EC50 | = | 1.778 | nM | 8.75 |
| CHEMBL3580748 | — | EC50 | = | 2.239 | nM | 8.65 |
| CHEMBL3580746 | — | EC50 | = | 2.818 | nM | 8.55 |
| CHEMBL3580750 | — | EC50 | = | 3.631 | nM | 8.44 |
| CHEMBL3580745 | — | EC50 | = | 4.786 | nM | 8.32 |
| CHEMBL3580743 | — | EC50 | = | 4.898 | nM | 8.31 |
| CHEMBL3582485 | — | EC50 | = | 7.586 | nM | 8.12 |
| CHEMBL3582484 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3580744 | — | EC50 | = | 11.75 | nM | 7.93 |
| CHEMBL3582486 | — | EC50 | = | 72.44 | nM | 7.14 |