Assay Detail
Functional
CHEMBL4834853
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| EC50 | 23 | 9.38 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.96 |
| CHEMBL4874954 | — | — | 1 | 9.85 |
| CHEMBL4852096 | — | — | 1 | 9.85 |
| CHEMBL4848885 | — | — | 1 | 9.74 |
| CHEMBL4854625 | — | — | 1 | 9.70 |
| CHEMBL4867553 | — | — | 1 | 9.62 |
| CHEMBL4859295 | — | — | 1 | 9.60 |
| CHEMBL4852440 | — | — | 1 | 9.49 |
| CHEMBL4859677 | — | — | 1 | 9.48 |
| CHEMBL4873903 | — | — | 1 | 9.38 |
| CHEMBL4869463 | — | — | 1 | 9.12 |
| CHEMBL4872217 | — | — | 1 | 9.01 |
| CHEMBL4854836 | — | — | 1 | 8.72 |
| CHEMBL4846505 | — | — | 1 | 8.67 |
| CHEMBL4860729 | — | — | 1 | 8.45 |
| 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 | EC50 | = | 0.11 | nM | 9.96 |
| CHEMBL4874954 | — | EC50 | = | 0.14 | nM | 9.85 |
| CHEMBL4852096 | — | EC50 | = | 0.14 | nM | 9.85 |
| CHEMBL4848885 | — | EC50 | = | 0.18 | nM | 9.74 |
| CHEMBL4854625 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4867553 | — | EC50 | = | 0.24 | nM | 9.62 |
| CHEMBL4859295 | — | EC50 | = | 0.25 | nM | 9.60 |
| CHEMBL4852440 | — | EC50 | = | 0.32 | nM | 9.49 |
| CHEMBL4859677 | — | EC50 | = | 0.33 | nM | 9.48 |
| CHEMBL4873903 | — | EC50 | = | 0.42 | nM | 9.38 |
| CHEMBL4869463 | — | EC50 | = | 0.75 | nM | 9.12 |
| CHEMBL4872217 | — | EC50 | = | 0.97 | nM | 9.01 |
| CHEMBL4854836 | — | EC50 | = | 1.92 | nM | 8.72 |
| CHEMBL4846505 | — | EC50 | = | 2.13 | nM | 8.67 |
| CHEMBL4860729 | — | EC50 | = | 3.58 | nM | 8.45 |
| CHEMBL4875780 | — | EC50 | - | — | - | |
| CHEMBL4861281 | — | EC50 | - | — | - | |
| CHEMBL4849193 | — | EC50 | - | — | - | |
| CHEMBL4867364 | — | EC50 | - | — | - | |
| CHEMBL4867474 | — | EC50 | - | — | - | |
| CHEMBL4854434 | — | EC50 | - | — | - | |
| CHEMBL4867993 | — | EC50 | - | — | - | |
| CHEMBL113692 | — | EC50 | - | — | - |