Assay Detail
Binding
CHEMBL1670261
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]melatonin from rat MT2 receptor expressed in CHO-Galpha16 cells
42
Total Activities
34
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 7.62 | 10.52 |
| IC50 | 8 | 7.71 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1218 | RAMELTEON | 4.0 | 1 | 10.52 |
| CHEMBL10878 | AGOMELATINE | 4.0 | 1 | 9.85 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.24 |
| CHEMBL1669703 | — | — | 2 | 8.68 |
| CHEMBL1669700 | — | — | 2 | 8.57 |
| CHEMBL1669701 | — | — | 2 | 8.57 |
| CHEMBL1669710 | — | — | 1 | 8.48 |
| CHEMBL1669709 | — | — | 1 | 8.17 |
| CHEMBL1669702 | — | — | 2 | 8.00 |
| CHEMBL1669685 | — | — | 1 | 8.00 |
| CHEMBL1669704 | — | — | 2 | 7.62 |
| CHEMBL1669707 | — | — | 2 | 7.51 |
| CHEMBL1669682 | — | — | 1 | 7.51 |
| CHEMBL1669686 | — | — | 1 | 7.46 |
| CHEMBL1669705 | — | — | 2 | 7.36 |
| CHEMBL1669706 | — | — | 2 | 7.18 |
| CHEMBL1669688 | — | — | 1 | 7.17 |
| CHEMBL1669708 | — | — | 1 | 7.08 |
| CHEMBL1669691 | — | — | 1 | 6.96 |
| CHEMBL1669681 | — | — | 1 | 6.82 |
| CHEMBL1669698 | — | — | 1 | 6.44 |
| CHEMBL1669699 | — | — | 1 | 6.07 |
| CHEMBL1669697 | — | — | 1 | 6.06 |
| CHEMBL1669692 | — | — | 1 | 5.39 |
| CHEMBL1669690 | — | — | 1 | - |
| CHEMBL1669689 | — | — | 1 | - |
| CHEMBL1669693 | — | — | 1 | - |
| CHEMBL1669687 | — | — | 1 | - |
| CHEMBL1669694 | — | — | 1 | - |
| CHEMBL1669695 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1218 | RAMELTEON | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL10878 | AGOMELATINE | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL45 | MELATONIN | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL1669703 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL1669700 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL1669701 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL1669710 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL1669709 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL1669685 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1669702 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1669704 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1669704 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL1669682 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL1669707 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1669686 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL1669705 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL1669706 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL1669688 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL1669708 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL1669702 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL1669691 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL1669681 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL1669707 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL1669698 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL1669699 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL1669697 | — | Ki | = | 870.0 | nM | 6.06 |
| CHEMBL1669692 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL1669701 | — | IC50 | - | — | - | |
| CHEMBL1669700 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1669703 | — | IC50 | - | — | - | |
| CHEMBL1669705 | — | IC50 | - | — | - | |
| CHEMBL1669696 | — | Ki | - | — | - | |
| CHEMBL1669695 | — | Ki | - | — | - | |
| CHEMBL1669694 | — | Ki | - | — | - | |
| CHEMBL1669690 | — | Ki | - | — | - | |
| CHEMBL1669689 | — | Ki | - | — | - | |
| CHEMBL1669687 | — | Ki | - | — | - | |
| CHEMBL1669693 | — | Ki | - | — | - | |
| CHEMBL1669706 | — | IC50 | - | — | - | |
| CHEMBL1669684 | — | Ki | - | — | - | |
| CHEMBL1669683 | — | Ki | - | — | - | |
| CHEMBL1669680 | — | Ki | - | — | - |