Assay Detail
Binding
CHEMBL710992
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In vitro binding affinity against melatonin receptor using 2-[125I]iodomelatonin (0.05 nM) and chicken brain membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis of 2-amido-2,3-dihydro-1H-phenalene derivatives as new conformationally restricted ligands for melatonin receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.44 | 9.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.34 |
| CHEMBL318179 | — | — | 1 | 9.15 |
| CHEMBL12477 | — | — | 1 | 8.22 |
| CHEMBL12795 | — | — | 1 | 7.54 |
| CHEMBL106276 | — | — | 1 | 7.50 |
| CHEMBL53015 | — | — | 1 | 6.79 |
| CHEMBL104997 | — | — | 1 | 6.78 |
| CHEMBL320810 | — | — | 1 | 6.71 |
| CHEMBL317669 | — | — | 1 | 6.56 |
| CHEMBL33103 | ACETYLSEROTONIN | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL45 | MELATONIN | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL318179 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL12477 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL12795 | — | Ki | = | 28.7 | nM | 7.54 |
| CHEMBL106276 | — | Ki | = | 31.9 | nM | 7.50 |
| CHEMBL53015 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL104997 | — | Ki | = | 168.0 | nM | 6.78 |
| CHEMBL320810 | — | Ki | = | 195.0 | nM | 6.71 |
| CHEMBL317669 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL33103 | ACETYLSEROTONIN | Ki | = | 1640.0 | nM | 5.79 |