Assay Detail
Binding
CHEMBL5327154
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Binding affinity to human NTSR1 transfected in HEK293 cells assessed as inhibition constant incubated for 60 mins in the presence of [Leu3H]NT(8-13) by radioligand competition binding assay
7
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 6 | 7.97 | 8.38 |
| Kd | 1 | 9.17 | 9.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL415788 | — | — | 1 | 9.17 |
| CHEMBL5434985 | — | — | 1 | 8.38 |
| CHEMBL5420374 | — | — | 1 | 8.26 |
| CHEMBL5441066 | — | — | 1 | 8.16 |
| CHEMBL5402152 | — | — | 1 | 7.82 |
| CHEMBL5409459 | — | — | 1 | 7.22 |
| CHEMBL423487 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL415788 | — | Kd | = | 0.68 | nM | 9.17 |
| CHEMBL5434985 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL5420374 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL5441066 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL5402152 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL5409459 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL423487 | — | Ki | > | 50000.0 | nM | - |