Assay Detail
Binding
CHEMBL4834838
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Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
23
Total Activities
23
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 <b>ACH-000143</b>: A Novel Potent and Peripherally Preferred Melatonin Receptor Agonist that Reduces Liver Triglycerides and Steatosis in Diet-Induced Obese Rats.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 9.00 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.74 |
| CHEMBL4852440 | — | — | 1 | 9.47 |
| CHEMBL4874954 | — | — | 1 | 9.41 |
| CHEMBL4859677 | — | — | 1 | 9.38 |
| CHEMBL4873903 | — | — | 1 | 9.21 |
| CHEMBL4869463 | — | — | 1 | 9.15 |
| CHEMBL4852096 | — | — | 1 | 9.06 |
| CHEMBL4867553 | — | — | 1 | 9.00 |
| CHEMBL4872217 | — | — | 1 | 8.96 |
| CHEMBL4848885 | — | — | 1 | 8.96 |
| CHEMBL4854625 | — | — | 1 | 8.92 |
| CHEMBL4859295 | — | — | 1 | 8.68 |
| CHEMBL4854836 | — | — | 1 | 8.66 |
| CHEMBL4860729 | — | — | 1 | 8.44 |
| CHEMBL4846505 | — | — | 1 | 7.89 |
| CHEMBL4875780 | — | — | 1 | - |
| CHEMBL4861281 | — | — | 1 | - |
| CHEMBL4849193 | — | — | 1 | - |
| CHEMBL4867364 | — | — | 1 | - |
| CHEMBL4867474 | — | — | 1 | - |
| CHEMBL4854434 | — | — | 1 | - |
| CHEMBL4867993 | — | — | 1 | - |
| CHEMBL113692 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL45 | MELATONIN | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL4852440 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL4874954 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL4859677 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL4873903 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL4869463 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL4852096 | — | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL4867553 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4872217 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4848885 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4854625 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL4859295 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL4854836 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL4860729 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL4846505 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4875780 | — | Ki | - | — | - | |
| CHEMBL4861281 | — | Ki | - | — | - | |
| CHEMBL4849193 | — | Ki | - | — | - | |
| CHEMBL4867364 | — | Ki | - | — | - | |
| CHEMBL4867474 | — | Ki | - | — | - | |
| CHEMBL4854434 | — | Ki | - | — | - | |
| CHEMBL4867993 | — | Ki | - | — | - | |
| CHEMBL113692 | — | Ki | - | — | - |