Assay Detail
Functional
CHEMBL5327158
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Agonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Neurotensin(8-13) analogs as dual NTS1 and NTS2 receptor ligands with enhanced effects on a mouse model of Parkinson's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 7 | 8.54 | 9.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5420374 | — | — | 1 | 9.13 |
| CHEMBL5441066 | — | — | 1 | 9.09 |
| CHEMBL5402152 | — | — | 1 | 9.07 |
| CHEMBL415788 | — | — | 1 | 9.06 |
| CHEMBL5434985 | — | — | 1 | 9.05 |
| CHEMBL5409459 | — | — | 1 | 8.89 |
| CHEMBL423487 | — | — | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5420374 | — | EC50 | = | 0.74 | nM | 9.13 |
| CHEMBL5441066 | — | EC50 | = | 0.82 | nM | 9.09 |
| CHEMBL5402152 | — | EC50 | = | 0.85 | nM | 9.07 |
| CHEMBL415788 | — | EC50 | = | 0.88 | nM | 9.06 |
| CHEMBL5434985 | — | EC50 | = | 0.89 | nM | 9.05 |
| CHEMBL5409459 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL423487 | — | EC50 | = | 3200.0 | nM | 5.50 |