Assay Detail
ADMET
CHEMBL4701870
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Agonist activity at human NTS1 expressed in HEK293 cells co-expressing Galphaq/RlucII/GFP10-Ggamma1/Gbeta1 assessed as increase in Galphaq activation incubated for 10 mins in presence of coelenterazine 400A by BRET assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 8.53 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL415788 | — | — | 1 | 9.82 |
| CHEMBL4789659 | — | — | 1 | 9.62 |
| CHEMBL4744531 | — | — | 1 | 9.59 |
| CHEMBL4776986 | — | — | 1 | 9.07 |
| CHEMBL4798887 | — | — | 1 | 8.89 |
| CHEMBL4597094 | — | — | 1 | 8.77 |
| CHEMBL4749016 | — | — | 1 | 8.74 |
| CHEMBL4758754 | — | — | 1 | 8.41 |
| CHEMBL4745899 | — | — | 1 | 8.17 |
| CHEMBL4747286 | — | — | 1 | 7.82 |
| CHEMBL4761165 | — | — | 1 | 7.72 |
| CHEMBL4742666 | — | — | 1 | 5.72 |
| CHEMBL4750783 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL415788 | — | EC50 | = | 0.15 | nM | 9.82 |
| CHEMBL4789659 | — | EC50 | = | 0.24 | nM | 9.62 |
| CHEMBL4744531 | — | EC50 | = | 0.26 | nM | 9.59 |
| CHEMBL4776986 | — | EC50 | = | 0.86 | nM | 9.07 |
| CHEMBL4798887 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4597094 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4749016 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4758754 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4745899 | — | EC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4747286 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4761165 | — | EC50 | = | 19.1 | nM | 7.72 |
| CHEMBL4742666 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4750783 | — | EC50 | - | — | - |