Assay Detail
Binding
CHEMBL3993987
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Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in HEK or CHO cell membranes after 120 mins
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
New quinolinic derivatives as melatonergic ligands: Synthesis and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 8.74 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4089965 | — | — | 1 | 10.52 |
| CHEMBL4062947 | — | — | 1 | 10.05 |
| CHEMBL4084612 | — | — | 1 | 10.05 |
| CHEMBL4095210 | — | — | 1 | 10.00 |
| CHEMBL4102177 | — | — | 1 | 9.70 |
| CHEMBL10878 | AGOMELATINE | 4.0 | 1 | 9.70 |
| CHEMBL4071572 | — | — | 1 | 9.70 |
| CHEMBL4079784 | — | — | 1 | 9.52 |
| CHEMBL4061905 | — | — | 1 | 9.52 |
| CHEMBL4082097 | — | — | 1 | 9.52 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.51 |
| CHEMBL4079699 | — | — | 1 | 9.40 |
| CHEMBL4070527 | — | — | 1 | 9.30 |
| CHEMBL4100108 | — | — | 1 | 9.00 |
| CHEMBL4094436 | — | — | 1 | 8.40 |
| CHEMBL4097693 | — | — | 1 | 8.22 |
| CHEMBL4073867 | — | — | 1 | 7.66 |
| CHEMBL4097817 | — | — | 1 | 7.58 |
| CHEMBL4096197 | — | — | 1 | 7.40 |
| CHEMBL4068922 | — | — | 1 | 7.14 |
| CHEMBL4080608 | — | — | 1 | 6.60 |
| CHEMBL4092353 | — | — | 1 | 6.37 |
| CHEMBL4105511 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4089965 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL4062947 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL4084612 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL4095210 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL4102177 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL10878 | AGOMELATINE | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4071572 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4079784 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL4061905 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL4082097 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL45 | MELATONIN | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL4079699 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4070527 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL4100108 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4094436 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4097693 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4073867 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4097817 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL4096197 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4068922 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL4080608 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL4092353 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL4105511 | — | Ki | = | 550.0 | nM | 6.26 |