Assay Detail
Binding
CHEMBL3868339
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of (2S)-N-(2-pyrrol-1-ylphenyl)-1-[2-[1-(tritritiomethyl)benzimidazol-2-yl]sulfanylacetyl]pyrrolidine-2-carboxamide from human OX2 receptor expressed on CHO cell membrane measured after 3 hrs by TopCount method
48
Total Activities
48
Compounds Tested
1
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 selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 48 | 6.51 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3915136 | — | — | 1 | 8.55 |
| CHEMBL3951917 | — | — | 1 | 8.05 |
| CHEMBL3928138 | — | — | 1 | 7.96 |
| CHEMBL3959896 | — | — | 1 | 7.85 |
| CHEMBL3891586 | — | — | 1 | 7.75 |
| CHEMBL3972735 | — | — | 1 | 7.57 |
| CHEMBL3900983 | — | — | 1 | 6.97 |
| CHEMBL3971815 | — | — | 1 | 6.92 |
| CHEMBL3930252 | — | — | 1 | 6.71 |
| CHEMBL3923070 | — | — | 1 | 6.66 |
| CHEMBL3892723 | — | — | 1 | 6.57 |
| CHEMBL3924149 | — | — | 1 | 6.56 |
| CHEMBL3919876 | — | — | 1 | 6.55 |
| CHEMBL3929466 | — | — | 1 | 6.42 |
| CHEMBL2413367 | — | — | 1 | 6.38 |
| CHEMBL3906164 | — | — | 1 | 6.33 |
| CHEMBL3941376 | — | — | 1 | 6.33 |
| CHEMBL3928942 | — | — | 1 | 6.28 |
| CHEMBL3394848 | — | — | 1 | 6.28 |
| CHEMBL3958483 | — | — | 1 | 6.20 |
| CHEMBL3900658 | — | — | 1 | 6.07 |
| CHEMBL3944339 | — | — | 1 | 6.06 |
| CHEMBL3979470 | — | — | 1 | 6.04 |
| CHEMBL3897218 | — | — | 1 | 6.03 |
| CHEMBL3955752 | — | — | 1 | 6.00 |
| CHEMBL3963945 | — | — | 1 | 5.98 |
| CHEMBL3984937 | — | — | 1 | 5.94 |
| CHEMBL3934291 | — | — | 1 | 5.91 |
| CHEMBL3981114 | — | — | 1 | 5.85 |
| CHEMBL3946473 | — | — | 1 | 5.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3915136 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL3951917 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3928138 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3959896 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3891586 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL3972735 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL3900983 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL3971815 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL3930252 | — | Ki | = | 193.0 | nM | 6.71 |
| CHEMBL3923070 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL3892723 | — | Ki | = | 271.0 | nM | 6.57 |
| CHEMBL3924149 | — | Ki | = | 277.0 | nM | 6.56 |
| CHEMBL3919876 | — | Ki | = | 281.0 | nM | 6.55 |
| CHEMBL3929466 | — | Ki | = | 379.0 | nM | 6.42 |
| CHEMBL2413367 | — | Ki | = | 417.0 | nM | 6.38 |
| CHEMBL3906164 | — | Ki | = | 467.0 | nM | 6.33 |
| CHEMBL3941376 | — | Ki | = | 467.0 | nM | 6.33 |
| CHEMBL3928942 | — | Ki | = | 521.0 | nM | 6.28 |
| CHEMBL3394848 | — | Ki | = | 521.0 | nM | 6.28 |
| CHEMBL3958483 | — | Ki | = | 627.0 | nM | 6.20 |
| CHEMBL3900658 | — | Ki | = | 861.0 | nM | 6.07 |
| CHEMBL3944339 | — | Ki | = | 871.0 | nM | 6.06 |
| CHEMBL3979470 | — | Ki | = | 907.0 | nM | 6.04 |
| CHEMBL3897218 | — | Ki | = | 933.0 | nM | 6.03 |
| CHEMBL3955752 | — | Ki | = | 1009.0 | nM | 6.00 |
| CHEMBL3963945 | — | Ki | = | 1038.0 | nM | 5.98 |
| CHEMBL3984937 | — | Ki | = | 1137.0 | nM | 5.94 |
| CHEMBL3934291 | — | Ki | = | 1227.0 | nM | 5.91 |
| CHEMBL3981114 | — | Ki | = | 1409.0 | nM | 5.85 |
| CHEMBL3946473 | — | Ki | = | 1470.0 | nM | 5.83 |
| CHEMBL3892010 | — | Ki | = | 1564.0 | nM | 5.81 |
| CHEMBL3961795 | — | Ki | = | 1617.0 | nM | 5.79 |
| CHEMBL3973097 | — | Ki | = | 2143.0 | nM | 5.67 |
| CHEMBL3925396 | — | Ki | = | 4306.0 | nM | 5.37 |
| CHEMBL3889779 | — | Ki | > | 1770.0 | nM | - |
| CHEMBL3958817 | — | Ki | > | 4379.0 | nM | - |
| CHEMBL3979157 | — | Ki | > | 4379.0 | nM | - |
| CHEMBL3950125 | — | Ki | > | 2633.0 | nM | - |
| CHEMBL3907717 | — | Ki | > | 2633.0 | nM | - |
| CHEMBL3978250 | — | Ki | > | 4379.0 | nM | - |
| CHEMBL3976856 | — | Ki | > | 1407.0 | nM | - |
| CHEMBL3920035 | — | Ki | > | 1935.0 | nM | - |
| CHEMBL3955784 | — | Ki | > | 3370.0 | nM | - |
| CHEMBL3932393 | — | Ki | > | 12660.0 | nM | - |
| CHEMBL3966617 | — | Ki | > | 12720.0 | nM | - |
| CHEMBL3936875 | — | Ki | > | 2096.0 | nM | - |
| CHEMBL3911086 | — | Ki | > | 5868.0 | nM | - |
| CHEMBL3902070 | — | Ki | > | 3327.0 | nM | - |