Assay Detail
Binding
CHEMBL1768189
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Displacement of [3H]neurotensin from human NTS1 receptor expressed in CHO cells
36
Total Activities
35
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of highly potent and neurotensin receptor 2 selective neurotensin mimetics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 35 | 6.61 | 9.64 |
| Kd | 1 | 9.23 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1766935 | — | — | 1 | 9.64 |
| CHEMBL1766928 | — | — | 1 | 9.62 |
| CHEMBL407196 | NEUROTENSIN | — | 1 | 9.23 |
| CHEMBL1766929 | — | — | 1 | 9.21 |
| CHEMBL254769 | — | — | 1 | 8.80 |
| CHEMBL258221 | — | — | 1 | 8.57 |
| CHEMBL1766936 | — | — | 1 | 8.47 |
| CHEMBL1766923 | — | — | 1 | 8.34 |
| CHEMBL1766937 | — | — | 1 | 8.08 |
| CHEMBL1766939 | — | — | 1 | 8.08 |
| CHEMBL1766924 | — | — | 1 | 7.96 |
| CHEMBL411195 | — | — | 1 | 7.77 |
| CHEMBL1766925 | — | — | 1 | 7.58 |
| CHEMBL266230 | — | — | 1 | 7.33 |
| CHEMBL1766930 | — | — | 1 | 7.15 |
| CHEMBL172313 | — | — | 1 | 7.00 |
| CHEMBL253527 | — | — | 1 | 6.68 |
| CHEMBL1766931 | — | — | 1 | 6.66 |
| CHEMBL1766938 | — | — | 1 | 6.60 |
| CHEMBL1766932 | — | — | 1 | 6.05 |
| CHEMBL1766927 | — | — | 1 | 5.96 |
| CHEMBL1766926 | — | — | 1 | 5.89 |
| CHEMBL1766934 | — | — | 1 | 5.89 |
| CHEMBL1766942 | — | — | 1 | 5.58 |
| CHEMBL2369509 | — | — | 2 | 5.52 |
| CHEMBL1766940 | — | — | 1 | 5.43 |
| CHEMBL1766945 | — | — | 1 | 5.08 |
| CHEMBL1766947 | — | — | 1 | 5.07 |
| CHEMBL1766943 | — | — | 1 | 5.00 |
| CHEMBL1766933 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1766935 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL1766928 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL407196 | NEUROTENSIN | Kd | = | 0.59 | nM | 9.23 |
| CHEMBL1766929 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL254769 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL258221 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL1766936 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL1766923 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL1766937 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL1766939 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL1766924 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL411195 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1766925 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL266230 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL1766930 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL172313 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL253527 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL1766931 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL1766938 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL1766932 | — | Ki | = | 890.0 | nM | 6.05 |
| CHEMBL1766927 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL1766926 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL1766934 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL1766942 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL2369509 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL2369509 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL1766940 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL1766945 | — | Ki | = | 8300.0 | nM | 5.08 |
| CHEMBL1766947 | — | Ki | = | 8500.0 | nM | 5.07 |
| CHEMBL1766943 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL1766933 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL1766825 | — | Ki | = | 28000.0 | nM | 4.55 |
| CHEMBL254770 | — | Ki | = | 30000.0 | nM | 4.52 |
| CHEMBL1766946 | — | Ki | = | 32000.0 | nM | 4.50 |
| CHEMBL1766941 | — | Ki | = | 47000.0 | nM | 4.33 |
| CHEMBL1766944 | — | Ki | = | 80000.0 | nM | 4.10 |