Assay Detail
Binding
CHEMBL4835153
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Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Potent and Orally Bioavailable Melatonin Receptor Agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 9.45 | 10.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4868554 | — | — | 1 | 10.57 |
| CHEMBL3648356 | — | — | 1 | 10.51 |
| CHEMBL3648362 | — | — | 1 | 10.43 |
| CHEMBL3648355 | — | — | 1 | 10.17 |
| CHEMBL3648358 | — | — | 1 | 10.17 |
| CHEMBL4874630 | — | — | 1 | 9.77 |
| CHEMBL4874010 | — | — | 1 | 9.70 |
| CHEMBL3648365 | — | — | 1 | 9.66 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.62 |
| CHEMBL4869029 | — | — | 1 | 9.52 |
| CHEMBL4872592 | — | — | 1 | 9.46 |
| CHEMBL3648366 | — | — | 1 | 9.41 |
| CHEMBL3648367 | — | — | 1 | 9.35 |
| CHEMBL3648354 | — | — | 1 | 9.35 |
| CHEMBL4848381 | — | — | 1 | 8.92 |
| CHEMBL4864102 | — | — | 1 | 8.89 |
| CHEMBL4870108 | — | — | 1 | 8.36 |
| CHEMBL4871181 | — | — | 1 | 8.03 |
| CHEMBL3648357 | — | — | 1 | 7.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4868554 | — | Ki | = | 0.027 | nM | 10.57 |
| CHEMBL3648356 | — | Ki | = | 0.031 | nM | 10.51 |
| CHEMBL3648362 | — | Ki | = | 0.037 | nM | 10.43 |
| CHEMBL3648355 | — | Ki | = | 0.067 | nM | 10.17 |
| CHEMBL3648358 | — | Ki | = | 0.067 | nM | 10.17 |
| CHEMBL4874630 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL4874010 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3648365 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL45 | MELATONIN | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL4869029 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL4872592 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL3648366 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL3648367 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL3648354 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL4848381 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL4864102 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL4870108 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL4871181 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL3648357 | — | Ki | = | 23.0 | nM | 7.64 |