Assay Detail
Binding
CHEMBL1014541
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Displacement of [125I]I-Tyr(3)NT from human NTR1
39
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| IC50 | 20 | 7.73 | 9.42 |
| Ki | 19 | 7.78 | 9.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL468951 | — | — | 2 | 9.54 |
| CHEMBL504768 | — | — | 2 | 9.14 |
| CHEMBL506981 | REMINERTANT | 3.0 | 1 | 9.00 |
| CHEMBL342252 | — | — | 2 | 8.98 |
| CHEMBL407196 | NEUROTENSIN | — | 2 | 8.79 |
| CHEMBL344337 | — | — | 2 | 8.74 |
| CHEMBL505695 | — | — | 2 | 8.70 |
| CHEMBL450258 | — | — | 2 | 8.52 |
| CHEMBL501575 | — | — | 2 | 8.31 |
| CHEMBL453924 | — | — | 2 | 8.26 |
| CHEMBL505906 | — | — | 2 | 8.09 |
| CHEMBL499673 | — | — | 2 | 7.98 |
| CHEMBL447400 | — | — | 2 | 7.69 |
| CHEMBL508380 | — | — | 2 | 6.98 |
| CHEMBL508507 | — | — | 2 | 6.87 |
| CHEMBL266571 | — | — | 2 | 6.75 |
| CHEMBL445035 | — | — | 2 | 6.52 |
| CHEMBL500173 | — | — | 2 | 6.20 |
| CHEMBL500734 | — | — | 2 | 6.19 |
| CHEMBL501956 | — | — | 2 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL468951 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL468951 | — | IC50 | = | 0.383 | nM | 9.42 |
| CHEMBL504768 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL504768 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL506981 | REMINERTANT | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL342252 | — | Ki | = | 1.05 | nM | 8.98 |
| CHEMBL342252 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL407196 | NEUROTENSIN | Ki | = | 1.64 | nM | 8.79 |
| CHEMBL344337 | — | Ki | = | 1.81 | nM | 8.74 |
| CHEMBL505695 | — | Ki | = | 2.01 | nM | 8.70 |
| CHEMBL407196 | NEUROTENSIN | IC50 | = | 2.19 | nM | 8.66 |
| CHEMBL344337 | — | IC50 | = | 2.42 | nM | 8.62 |
| CHEMBL505695 | — | IC50 | = | 2.68 | nM | 8.57 |
| CHEMBL450258 | — | Ki | = | 2.99 | nM | 8.52 |
| CHEMBL450258 | — | IC50 | = | 3.99 | nM | 8.40 |
| CHEMBL501575 | — | Ki | = | 4.87 | nM | 8.31 |
| CHEMBL453924 | — | Ki | = | 5.49 | nM | 8.26 |
| CHEMBL501575 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL453924 | — | IC50 | = | 7.32 | nM | 8.13 |
| CHEMBL505906 | — | Ki | = | 8.07 | nM | 8.09 |
| CHEMBL499673 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL505906 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL499673 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL447400 | — | Ki | = | 20.3 | nM | 7.69 |
| CHEMBL447400 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL508380 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL508507 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL508380 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL266571 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL508507 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL266571 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL445035 | — | Ki | = | 303.0 | nM | 6.52 |
| CHEMBL445035 | — | IC50 | = | 403.0 | nM | 6.39 |
| CHEMBL500173 | — | Ki | = | 631.0 | nM | 6.20 |
| CHEMBL500734 | — | Ki | = | 647.0 | nM | 6.19 |
| CHEMBL500173 | — | IC50 | = | 842.0 | nM | 6.08 |
| CHEMBL500734 | — | IC50 | = | 863.0 | nM | 6.06 |
| CHEMBL501956 | — | Ki | = | 2170.0 | nM | 5.66 |
| CHEMBL501956 | — | IC50 | = | 2900.0 | nM | 5.54 |