Assay Detail
Functional
CHEMBL1014542
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at NTR1 in human HT-29 cells assessed as increase in intracellular calcium concentration by FLIPR assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HT-29 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Comparison of N-terminal modifications on neurotensin(8-13) analogues correlates peptide stability but not binding affinity with in vivo efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 19 | 7.74 | 9.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL504768 | — | — | 1 | 9.11 |
| CHEMBL468951 | — | — | 1 | 9.07 |
| CHEMBL342252 | — | — | 1 | 9.00 |
| CHEMBL505695 | — | — | 1 | 8.73 |
| CHEMBL344337 | — | — | 1 | 8.72 |
| CHEMBL407196 | NEUROTENSIN | — | 1 | 8.70 |
| CHEMBL505906 | — | — | 1 | 8.21 |
| CHEMBL499673 | — | — | 1 | 8.19 |
| CHEMBL453924 | — | — | 1 | 8.14 |
| CHEMBL501575 | — | — | 1 | 8.11 |
| CHEMBL447400 | — | — | 1 | 8.10 |
| CHEMBL450258 | — | — | 1 | 7.59 |
| CHEMBL508507 | — | — | 1 | 7.24 |
| CHEMBL508380 | — | — | 1 | 6.82 |
| CHEMBL266571 | — | — | 1 | 6.70 |
| CHEMBL445035 | — | — | 1 | 6.66 |
| CHEMBL500734 | — | — | 1 | 6.12 |
| CHEMBL500173 | — | — | 1 | 6.11 |
| CHEMBL501956 | — | — | 1 | 5.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL504768 | — | EC50 | = | 0.78 | nM | 9.11 |
| CHEMBL468951 | — | EC50 | = | 0.853 | nM | 9.07 |
| CHEMBL342252 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL505695 | — | EC50 | = | 1.85 | nM | 8.73 |
| CHEMBL344337 | — | EC50 | = | 1.89 | nM | 8.72 |
| CHEMBL407196 | NEUROTENSIN | EC50 | = | 1.98 | nM | 8.70 |
| CHEMBL505906 | — | EC50 | = | 6.21 | nM | 8.21 |
| CHEMBL499673 | — | EC50 | = | 6.44 | nM | 8.19 |
| CHEMBL453924 | — | EC50 | = | 7.28 | nM | 8.14 |
| CHEMBL501575 | — | EC50 | = | 7.76 | nM | 8.11 |
| CHEMBL447400 | — | EC50 | = | 7.96 | nM | 8.10 |
| CHEMBL450258 | — | EC50 | = | 25.8 | nM | 7.59 |
| CHEMBL508507 | — | EC50 | = | 57.7 | nM | 7.24 |
| CHEMBL508380 | — | EC50 | = | 151.0 | nM | 6.82 |
| CHEMBL266571 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL445035 | — | EC50 | = | 217.0 | nM | 6.66 |
| CHEMBL500734 | — | EC50 | = | 764.0 | nM | 6.12 |
| CHEMBL500173 | — | EC50 | = | 783.0 | nM | 6.11 |
| CHEMBL501956 | — | EC50 | = | 1860.0 | nM | 5.73 |