Assay Detail
Functional
CHEMBL3583716
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Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
19
Total Activities
19
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
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 |
|---|---|---|---|
| EC50 | 19 | 6.82 | 10.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL45 | MELATONIN | 4.0 | 1 | 10.01 |
| CHEMBL3580908 | — | — | 1 | 7.42 |
| CHEMBL3580910 | — | — | 1 | 6.69 |
| CHEMBL7257 | MEBUFOTENIN | 2.0 | 1 | 6.59 |
| CHEMBL3580907 | — | — | 1 | 6.54 |
| CHEMBL3580919 | — | — | 1 | 6.49 |
| CHEMBL3580909 | — | — | 1 | 6.28 |
| CHEMBL3580913 | — | — | 1 | 6.15 |
| CHEMBL3580916 | — | — | 1 | 6.02 |
| CHEMBL3580911 | — | — | 1 | 6.00 |
| CHEMBL3580912 | — | — | 1 | - |
| CHEMBL3580915 | — | — | 1 | - |
| CHEMBL3580917 | — | — | 1 | - |
| CHEMBL3580918 | — | — | 1 | - |
| CHEMBL3580920 | — | — | 1 | - |
| CHEMBL3580921 | — | — | 1 | - |
| CHEMBL3580922 | — | — | 1 | - |
| CHEMBL3580924 | — | — | 1 | - |
| CHEMBL3580926 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL45 | MELATONIN | EC50 | = | 0.098 | nM | 10.01 |
| CHEMBL3580908 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3580910 | — | EC50 | = | 204.0 | nM | 6.69 |
| CHEMBL7257 | MEBUFOTENIN | EC50 | = | 257.0 | nM | 6.59 |
| CHEMBL3580907 | — | EC50 | = | 289.0 | nM | 6.54 |
| CHEMBL3580919 | — | EC50 | = | 326.0 | nM | 6.49 |
| CHEMBL3580909 | — | EC50 | = | 525.0 | nM | 6.28 |
| CHEMBL3580913 | — | EC50 | = | 711.0 | nM | 6.15 |
| CHEMBL3580916 | — | EC50 | = | 961.0 | nM | 6.02 |
| CHEMBL3580911 | — | EC50 | = | 989.0 | nM | 6.00 |
| CHEMBL3580912 | — | EC50 | - | — | - | |
| CHEMBL3580915 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3580917 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3580918 | — | EC50 | - | — | - | |
| CHEMBL3580920 | — | EC50 | - | — | - | |
| CHEMBL3580921 | — | EC50 | - | — | - | |
| CHEMBL3580922 | — | EC50 | - | — | - | |
| CHEMBL3580924 | — | EC50 | - | — | - | |
| CHEMBL3580926 | — | EC50 | - | — | - |