Assay Detail
Functional
CHEMBL3583718
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human melatonin receptor-2 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 | 7.17 | 10.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL45 | MELATONIN | 4.0 | 1 | 10.16 |
| CHEMBL3580908 | — | — | 1 | 8.52 |
| CHEMBL3580910 | — | — | 1 | 7.96 |
| CHEMBL3580919 | — | — | 1 | 7.54 |
| CHEMBL3580915 | — | — | 1 | 7.15 |
| CHEMBL3580907 | — | — | 1 | 7.09 |
| CHEMBL3580926 | — | — | 1 | 6.96 |
| CHEMBL7257 | MEBUFOTENIN | 2.0 | 1 | 6.95 |
| CHEMBL3580909 | — | — | 1 | 6.88 |
| CHEMBL3580913 | — | — | 1 | 6.53 |
| CHEMBL3580917 | — | — | 1 | 6.34 |
| CHEMBL3580912 | — | — | 1 | 6.30 |
| CHEMBL3580916 | — | — | 1 | 6.05 |
| CHEMBL3580921 | — | — | 1 | 5.96 |
| CHEMBL3580918 | — | — | 1 | - |
| CHEMBL3580911 | — | — | 1 | - |
| CHEMBL3580920 | — | — | 1 | - |
| CHEMBL3580922 | — | — | 1 | - |
| CHEMBL3580924 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL45 | MELATONIN | EC50 | = | 0.069 | nM | 10.16 |
| CHEMBL3580908 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3580910 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3580919 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3580915 | — | EC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3580907 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL3580926 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL7257 | MEBUFOTENIN | EC50 | = | 112.0 | nM | 6.95 |
| CHEMBL3580909 | — | EC50 | = | 132.0 | nM | 6.88 |
| CHEMBL3580913 | — | EC50 | = | 295.0 | nM | 6.53 |
| CHEMBL3580917 | — | EC50 | = | 457.0 | nM | 6.34 |
| CHEMBL3580912 | — | EC50 | = | 503.0 | nM | 6.30 |
| CHEMBL3580916 | — | EC50 | = | 881.0 | nM | 6.05 |
| CHEMBL3580921 | — | EC50 | = | 1096.0 | nM | 5.96 |
| CHEMBL3580918 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3580911 | — | EC50 | - | — | - | |
| CHEMBL3580920 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3580922 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3580924 | — | EC50 | > | 1000.0 | nM | - |