Assay Detail
Binding
CHEMBL713259
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Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
12
Total Activities
12
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
Synthesis of nitroindole derivatives with high affinity and selectivity for melatoninergic binding sites MT(3).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.14 | 10.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL289233 | IODOMELATONIN | — | 1 | 10.89 |
| CHEMBL300056 | — | — | 1 | 10.10 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.92 |
| CHEMBL52755 | — | — | 1 | 9.52 |
| CHEMBL55084 | — | — | 1 | 8.96 |
| CHEMBL33700 | — | — | 1 | 8.59 |
| CHEMBL298335 | — | — | 1 | 7.84 |
| CHEMBL52559 | — | — | 1 | 7.72 |
| CHEMBL300729 | — | — | 1 | 7.31 |
| CHEMBL300195 | — | — | 1 | 5.97 |
| CHEMBL300728 | — | — | 1 | 5.73 |
| CHEMBL53622 | — | — | 1 | 5.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL289233 | IODOMELATONIN | Ki | = | 0.013 | nM | 10.89 |
| CHEMBL300056 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL45 | MELATONIN | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL52755 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL55084 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL33700 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL298335 | — | Ki | = | 14.6 | nM | 7.84 |
| CHEMBL52559 | — | Ki | = | 19.2 | nM | 7.72 |
| CHEMBL300729 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL300195 | — | Ki | = | 1060.0 | nM | 5.97 |
| CHEMBL300728 | — | Ki | = | 1880.0 | nM | 5.73 |
| CHEMBL53622 | — | Ki | = | 8560.0 | nM | 5.07 |