Assay Detail
Binding
CHEMBL973057
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Inhibition of MT3 melatonin binding site from hamster brain membrane
22
Total Activities
22
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cricetinae |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design and synthesis of benzofuranic derivatives as new ligands at the melatonin-binding site MT3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.59 | 8.57 |
| Ki | 2 | 9.62 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL494438 | — | — | 1 | 9.72 |
| CHEMBL300728 | — | — | 1 | 9.52 |
| CHEMBL504585 | — | — | 1 | 8.57 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 8.11 |
| CHEMBL493424 | — | — | 1 | 7.96 |
| CHEMBL505744 | — | — | 1 | 7.92 |
| CHEMBL495399 | — | — | 1 | 7.85 |
| CHEMBL446329 | — | — | 1 | 7.80 |
| CHEMBL494566 | — | — | 1 | 7.75 |
| CHEMBL521826 | — | — | 1 | 7.64 |
| CHEMBL495232 | — | — | 1 | 7.62 |
| CHEMBL522674 | — | — | 1 | 7.39 |
| CHEMBL494567 | — | — | 1 | 7.28 |
| CHEMBL521827 | — | — | 1 | 7.25 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 7.19 |
| CHEMBL495241 | — | — | 1 | 7.19 |
| CHEMBL323332 | — | — | 1 | 7.19 |
| CHEMBL505118 | — | — | 1 | 7.17 |
| CHEMBL522528 | — | — | 1 | 7.09 |
| CHEMBL493579 | — | — | 1 | - |
| CHEMBL493414 | — | — | 1 | - |
| CHEMBL493607 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL494438 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL300728 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL504585 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL2 | PRAZOSIN | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL493424 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL505744 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL495399 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL446329 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL494566 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL521826 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL495232 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL522674 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL494567 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL521827 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL45 | MELATONIN | IC50 | = | 64.6 | nM | 7.19 |
| CHEMBL495241 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL323332 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL505118 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL522528 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL493579 | — | IC50 | - | — | - | |
| CHEMBL493414 | — | IC50 | - | — | - | |
| CHEMBL493607 | — | IC50 | - | — | - |