Assay Detail
Binding
CHEMBL4375457
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Allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assay
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 43 | 6.00 | 7.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4583177 | — | — | 1 | 7.01 |
| CHEMBL4542358 | — | — | 1 | 6.80 |
| CHEMBL4517098 | — | — | 1 | 6.80 |
| CHEMBL4466155 | — | — | 1 | 6.66 |
| CHEMBL4454815 | — | — | 1 | 6.57 |
| CHEMBL4468649 | — | — | 1 | 6.47 |
| CHEMBL4576388 | — | — | 1 | 6.47 |
| CHEMBL4447601 | — | — | 1 | 6.36 |
| CHEMBL4534863 | — | — | 1 | 6.32 |
| CHEMBL4445632 | — | — | 1 | 6.30 |
| CHEMBL4461671 | — | — | 1 | 6.25 |
| CHEMBL4449708 | — | — | 1 | 6.25 |
| CHEMBL4468696 | — | — | 1 | 6.23 |
| CHEMBL4552414 | — | — | 1 | 6.22 |
| CHEMBL4453565 | — | — | 1 | 6.19 |
| CHEMBL4557702 | — | — | 1 | 6.15 |
| CHEMBL4561093 | — | — | 1 | 6.13 |
| CHEMBL4474616 | — | — | 1 | 6.09 |
| CHEMBL4452254 | — | — | 1 | 6.09 |
| CHEMBL4528434 | — | — | 1 | 6.05 |
| CHEMBL4460206 | — | — | 1 | 6.04 |
| CHEMBL4570744 | — | — | 1 | 6.00 |
| CHEMBL4564639 | — | — | 1 | 6.00 |
| CHEMBL4470647 | — | — | 1 | 5.98 |
| CHEMBL4473181 | — | — | 1 | 5.98 |
| CHEMBL4451959 | — | — | 1 | 5.97 |
| CHEMBL4593175 | — | — | 1 | 5.95 |
| CHEMBL4438479 | — | — | 1 | 5.90 |
| CHEMBL4440438 | — | — | 1 | 5.84 |
| CHEMBL4438637 | — | — | 1 | 5.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4583177 | — | EC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4542358 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4517098 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4466155 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4454815 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4468649 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4576388 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4447601 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4534863 | — | EC50 | = | 478.0 | nM | 6.32 |
| CHEMBL4445632 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4461671 | — | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4449708 | — | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4468696 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4552414 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4453565 | — | EC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4557702 | — | EC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4561093 | — | EC50 | = | 732.0 | nM | 6.13 |
| CHEMBL4474616 | — | EC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4452254 | — | EC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4528434 | — | EC50 | = | 888.0 | nM | 6.05 |
| CHEMBL4460206 | — | EC50 | = | 920.0 | nM | 6.04 |
| CHEMBL4570744 | — | EC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL4564639 | — | EC50 | = | 990.0 | nM | 6.00 |
| CHEMBL4470647 | — | EC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL4473181 | — | EC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL4451959 | — | EC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL4593175 | — | EC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL4438479 | — | EC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL4440438 | — | EC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL4438637 | — | EC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL4572231 | — | EC50 | = | 1720.0 | nM | 5.76 |
| CHEMBL4586953 | — | EC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL4460973 | — | EC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL2431120 | — | EC50 | = | 2870.0 | nM | 5.54 |
| CHEMBL4453074 | — | EC50 | = | 3010.0 | nM | 5.52 |
| CHEMBL4474648 | — | EC50 | = | 3360.0 | nM | 5.47 |
| CHEMBL4448328 | — | EC50 | = | 3810.0 | nM | 5.42 |
| CHEMBL4437603 | — | EC50 | = | 3880.0 | nM | 5.41 |
| CHEMBL4464635 | — | EC50 | = | 4230.0 | nM | 5.37 |
| CHEMBL4554583 | — | EC50 | = | 6720.0 | nM | 5.17 |
| CHEMBL4460691 | — | EC50 | = | 6710.0 | nM | 5.17 |
| CHEMBL4434705 | — | EC50 | = | 10020.0 | nM | 5.00 |
| CHEMBL4458329 | — | EC50 | > | 20000.0 | nM | - |