Assay Detail
Binding
CHEMBL4835155
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Displacement of 2-[125l]-lodomelatonin from human MT2 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
18
Total Activities
18
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 | 18 | 9.60 | 10.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4868554 | — | — | 1 | 10.24 |
| CHEMBL3648356 | — | — | 1 | 10.15 |
| CHEMBL3648354 | — | — | 1 | 10.14 |
| CHEMBL3648362 | — | — | 1 | 10.07 |
| CHEMBL3648358 | — | — | 1 | 10.06 |
| CHEMBL4870108 | — | — | 1 | 9.92 |
| CHEMBL3648355 | — | — | 1 | 9.89 |
| CHEMBL3648367 | — | — | 1 | 9.82 |
| CHEMBL3648366 | — | — | 1 | 9.82 |
| CHEMBL3648365 | — | — | 1 | 9.80 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.68 |
| CHEMBL4864102 | — | — | 1 | 9.64 |
| CHEMBL4869029 | — | — | 1 | 9.46 |
| CHEMBL4872592 | — | — | 1 | 9.12 |
| CHEMBL4874630 | — | — | 1 | 9.02 |
| CHEMBL4848381 | — | — | 1 | 8.96 |
| CHEMBL4874010 | — | — | 1 | 8.85 |
| CHEMBL3648357 | — | — | 1 | 8.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4868554 | — | Ki | = | 0.058 | nM | 10.24 |
| CHEMBL3648356 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL3648354 | — | Ki | = | 0.073 | nM | 10.14 |
| CHEMBL3648362 | — | Ki | = | 0.086 | nM | 10.07 |
| CHEMBL3648358 | — | Ki | = | 0.088 | nM | 10.06 |
| CHEMBL4870108 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL3648355 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL3648367 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL3648366 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL3648365 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL45 | MELATONIN | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL4864102 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL4869029 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL4872592 | — | Ki | = | 0.75 | nM | 9.12 |
| CHEMBL4874630 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL4848381 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4874010 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3648357 | — | Ki | = | 6.1 | nM | 8.21 |