Assay Detail
Binding
CHEMBL4252022
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Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
30
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of new naphtho- and quinolinocyclopentane derivatives as potent melatoninergic (MT1/MT2) and serotoninergic (5-HT2C) dual ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 8.66 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10878 | AGOMELATINE | 4.0 | 1 | 10.00 |
| CHEMBL4278248 | — | — | 1 | 10.00 |
| CHEMBL4293386 | — | — | 1 | 9.52 |
| CHEMBL4278575 | — | — | 1 | 9.52 |
| CHEMBL4281712 | — | — | 1 | 9.40 |
| CHEMBL4279639 | — | — | 3 | 9.40 |
| CHEMBL4292336 | — | — | 1 | 9.22 |
| CHEMBL4288497 | — | — | 1 | 9.22 |
| CHEMBL4280601 | — | — | 1 | 9.10 |
| CHEMBL4286896 | — | — | 1 | 9.10 |
| CHEMBL4280791 | — | — | 1 | 9.00 |
| CHEMBL4283539 | — | — | 1 | 9.00 |
| CHEMBL4291381 | — | — | 1 | 8.70 |
| CHEMBL4285145 | — | — | 1 | 8.70 |
| CHEMBL4290302 | — | — | 1 | 8.70 |
| CHEMBL4281915 | — | — | 3 | 8.52 |
| CHEMBL4288925 | — | — | 1 | 8.40 |
| CHEMBL4292109 | — | — | 1 | 8.40 |
| CHEMBL4294790 | — | — | 1 | 8.30 |
| CHEMBL4277185 | — | — | 1 | 8.30 |
| CHEMBL4289115 | — | — | 1 | 8.22 |
| CHEMBL4286494 | — | — | 1 | 8.15 |
| CHEMBL4278446 | — | — | 1 | 8.15 |
| CHEMBL4284223 | — | — | 1 | 8.05 |
| CHEMBL4277390 | — | — | 1 | 7.54 |
| CHEMBL4288690 | — | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10878 | AGOMELATINE | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL4278248 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL4293386 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL4278575 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL4281712 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4279639 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4292336 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL4288497 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL4279639 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL4280601 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL4286896 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL4280791 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4283539 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4285145 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4291381 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4290302 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4281915 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4281915 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4288925 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4292109 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4294790 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL4277185 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL4289115 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4286494 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4278446 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4284223 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4277390 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL4279639 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL4288690 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL4281915 | — | Ki | = | 99.0 | nM | 7.00 |