Assay Detail
Binding
CHEMBL3583714
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Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-2 transfected in CHO cell membranes after 120 mins
22
Total Activities
22
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
Novel N-Acetyl Bioisosteres of Melatonin: Melatonergic Receptor Pharmacology, Physicochemical Studies, and Phenotypic Assessment of Their Neurogenic Potential.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 7.58 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.82 |
| CHEMBL3580910 | — | — | 1 | 9.35 |
| CHEMBL3580908 | — | — | 1 | 9.00 |
| CHEMBL3580907 | — | — | 1 | 8.42 |
| CHEMBL3580919 | — | — | 1 | 8.40 |
| CHEMBL3580909 | — | — | 1 | 8.31 |
| CHEMBL7257 | MEBUFOTENIN | 2.0 | 1 | 7.80 |
| CHEMBL3580915 | — | — | 1 | 7.80 |
| CHEMBL3580926 | — | — | 1 | 7.77 |
| CHEMBL3580913 | — | — | 1 | 7.36 |
| CHEMBL3580917 | — | — | 1 | 7.17 |
| CHEMBL3580918 | — | — | 1 | 6.80 |
| CHEMBL3580916 | — | — | 1 | 6.72 |
| CHEMBL3580924 | — | — | 1 | 6.66 |
| CHEMBL3580912 | — | — | 1 | 6.30 |
| CHEMBL3580921 | — | — | 1 | 6.28 |
| CHEMBL3580920 | — | — | 1 | 6.27 |
| CHEMBL3580922 | — | — | 1 | 6.25 |
| CHEMBL3580923 | — | — | 1 | - |
| CHEMBL3580925 | — | — | 1 | - |
| CHEMBL3580914 | — | — | 1 | - |
| CHEMBL3580911 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL45 | MELATONIN | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL3580910 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL3580908 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3580907 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL3580919 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3580909 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL7257 | MEBUFOTENIN | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL3580915 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL3580926 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3580913 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL3580917 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL3580918 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL3580916 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL3580924 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL3580912 | — | Ki | = | 498.0 | nM | 6.30 |
| CHEMBL3580921 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL3580920 | — | Ki | = | 535.0 | nM | 6.27 |
| CHEMBL3580922 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL3580923 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3580925 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3580914 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3580911 | — | Ki | > | 1000.0 | nM | - |