Assay Detail
Functional
CHEMBL5541941
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human OX2R expressed in CHO cells preincubated for 120 mins followed by orexin-A addition by FLIPR assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Nivasorexant (ACT-539313): The First Selective Orexin-1 Receptor Antagonist (SO1RA) Investigated in Clinical Trials.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 6.75 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3981385 | — | — | 1 | 8.77 |
| CHEMBL3739711 | — | — | 1 | 8.51 |
| CHEMBL5594996 | — | — | 1 | 8.43 |
| CHEMBL5564739 | — | — | 1 | 8.36 |
| CHEMBL5584170 | — | — | 1 | 8.32 |
| CHEMBL3917550 | — | — | 1 | 8.15 |
| CHEMBL5568798 | — | — | 1 | 7.92 |
| CHEMBL5571060 | — | — | 1 | 7.70 |
| CHEMBL5591379 | — | — | 1 | 7.47 |
| CHEMBL3905808 | — | — | 1 | 7.47 |
| CHEMBL5575306 | — | — | 1 | 7.40 |
| CHEMBL5573121 | — | — | 1 | 7.40 |
| CHEMBL5573476 | — | — | 1 | 7.24 |
| CHEMBL5567578 | — | — | 1 | 7.02 |
| CHEMBL3904485 | — | — | 1 | 7.00 |
| CHEMBL5569629 | — | — | 1 | 7.00 |
| CHEMBL3895130 | — | — | 1 | 6.74 |
| CHEMBL3951681 | — | — | 1 | 6.67 |
| CHEMBL3915416 | — | — | 1 | 6.67 |
| CHEMBL3892369 | NIVASOREXANT | 2.0 | 1 | 6.64 |
| CHEMBL3946474 | — | — | 1 | 6.58 |
| CHEMBL3971116 | — | — | 1 | 6.55 |
| CHEMBL3924228 | — | — | 1 | 6.41 |
| CHEMBL3938981 | — | — | 1 | 6.39 |
| CHEMBL3936920 | — | — | 1 | 6.22 |
| CHEMBL5573198 | — | — | 1 | 6.18 |
| CHEMBL3933467 | — | — | 1 | 6.11 |
| CHEMBL3949919 | — | — | 1 | 6.11 |
| CHEMBL3969984 | — | — | 1 | 6.08 |
| CHEMBL3960556 | — | — | 1 | 5.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3981385 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3739711 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5594996 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5564739 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5584170 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3917550 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5568798 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5571060 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5591379 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3905808 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5573121 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5575306 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5573476 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5567578 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL5569629 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3904485 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL3895130 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL3951681 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL3915416 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL3892369 | NIVASOREXANT | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL3946474 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL3971116 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL3924228 | — | IC50 | = | 386.0 | nM | 6.41 |
| CHEMBL3938981 | — | IC50 | = | 404.0 | nM | 6.39 |
| CHEMBL3936920 | — | IC50 | = | 595.0 | nM | 6.22 |
| CHEMBL5573198 | — | IC50 | = | 666.0 | nM | 6.18 |
| CHEMBL3933467 | — | IC50 | = | 784.0 | nM | 6.11 |
| CHEMBL3949919 | — | IC50 | = | 784.0 | nM | 6.11 |
| CHEMBL3969984 | — | IC50 | = | 822.0 | nM | 6.08 |
| CHEMBL3960556 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL3963023 | — | IC50 | = | 1107.0 | nM | 5.96 |
| CHEMBL3901346 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL3930115 | — | IC50 | = | 1428.0 | nM | 5.84 |
| CHEMBL5595319 | — | IC50 | = | 1546.0 | nM | 5.81 |
| CHEMBL3936704 | — | IC50 | = | 1827.0 | nM | 5.74 |
| CHEMBL3922678 | — | IC50 | = | 1829.0 | nM | 5.74 |
| CHEMBL3927349 | — | IC50 | = | 1825.0 | nM | 5.74 |
| CHEMBL5571329 | — | IC50 | = | 1961.0 | nM | 5.71 |
| CHEMBL3964366 | — | IC50 | = | 2016.0 | nM | 5.70 |
| CHEMBL3952970 | — | IC50 | = | 2427.0 | nM | 5.62 |
| CHEMBL3957175 | — | IC50 | = | 3505.0 | nM | 5.46 |