Assay Detail
Binding
CHEMBL714104
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Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of naphthalenic dimers as selective MT1 melatoninergic ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 9.83 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14417 | — | — | 1 | 10.52 |
| CHEMBL14136 | — | — | 1 | 10.30 |
| CHEMBL273787 | — | — | 1 | 10.30 |
| CHEMBL10878 | AGOMELATINE | 4.0 | 1 | 10.22 |
| CHEMBL13985 | — | — | 1 | 10.10 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.85 |
| CHEMBL429392 | — | — | 1 | 9.30 |
| CHEMBL14453 | — | — | 1 | 9.22 |
| CHEMBL14514 | — | — | 1 | 8.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14417 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL14136 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL273787 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL10878 | AGOMELATINE | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL13985 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL45 | MELATONIN | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL429392 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL14453 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL14514 | — | Ki | = | 2.05 | nM | 8.69 |