Assay Detail
Binding
CHEMBL1670256
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Binding affinity to rat MT1 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO-Galpha16 |
| 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 |
|---|---|---|---|
| EC50 | 34 | 6.97 | 9.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.25 |
| CHEMBL1669703 | — | — | 1 | 9.13 |
| CHEMBL10878 | AGOMELATINE | 4.0 | 1 | 8.68 |
| CHEMBL1218 | RAMELTEON | 4.0 | 1 | 8.51 |
| CHEMBL1669701 | — | — | 1 | 8.41 |
| CHEMBL1669700 | — | — | 1 | 8.01 |
| CHEMBL1669710 | — | — | 1 | 7.75 |
| CHEMBL1669685 | — | — | 1 | 7.19 |
| CHEMBL1669682 | — | — | 1 | 7.01 |
| CHEMBL1669709 | — | — | 1 | 6.77 |
| CHEMBL1669689 | — | — | 1 | 6.68 |
| CHEMBL1669688 | — | — | 1 | 6.42 |
| CHEMBL1669705 | — | — | 1 | 6.41 |
| CHEMBL1669686 | — | — | 1 | 6.21 |
| CHEMBL1669687 | — | — | 1 | 6.19 |
| CHEMBL1669681 | — | — | 1 | 5.89 |
| CHEMBL1669684 | — | — | 1 | 5.77 |
| CHEMBL1669698 | — | — | 1 | 5.77 |
| CHEMBL1669683 | — | — | 1 | 5.64 |
| CHEMBL1669702 | — | — | 1 | 5.46 |
| CHEMBL1669690 | — | — | 1 | 5.12 |
| CHEMBL1669696 | — | — | 1 | - |
| CHEMBL1669695 | — | — | 1 | - |
| CHEMBL1669697 | — | — | 1 | - |
| CHEMBL1669694 | — | — | 1 | - |
| CHEMBL1669693 | — | — | 1 | - |
| CHEMBL1669699 | — | — | 1 | - |
| CHEMBL1669692 | — | — | 1 | - |
| CHEMBL1669691 | — | — | 1 | - |
| CHEMBL1669680 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL45 | MELATONIN | EC50 | = | 0.56 | nM | 9.25 |
| CHEMBL1669703 | — | EC50 | = | 0.74 | nM | 9.13 |
| CHEMBL10878 | AGOMELATINE | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL1218 | RAMELTEON | EC50 | = | 3.1 | nM | 8.51 |
| CHEMBL1669701 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL1669700 | — | EC50 | = | 9.7 | nM | 8.01 |
| CHEMBL1669710 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1669685 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1669682 | — | EC50 | = | 98.0 | nM | 7.01 |
| CHEMBL1669709 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1669689 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1669688 | — | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL1669705 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL1669686 | — | EC50 | = | 610.0 | nM | 6.21 |
| CHEMBL1669687 | — | EC50 | = | 640.0 | nM | 6.19 |
| CHEMBL1669681 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1669698 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1669684 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1669683 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL1669702 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL1669690 | — | EC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL1669707 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1669708 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1669706 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1669704 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1669680 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1669691 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1669692 | — | EC50 | - | — | - | |
| CHEMBL1669699 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1669693 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1669694 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1669697 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1669695 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1669696 | — | EC50 | > | 10000.0 | nM | - |