Assay Detail
Binding
CHEMBL1108334
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Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
17
Total Activities
17
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
Design, synthesis and pharmacological evaluation of novel naphthalenic derivatives as selective MT(1) melatoninergic ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 9.07 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1095196 | — | — | 1 | 10.15 |
| CHEMBL1094212 | — | — | 1 | 10.05 |
| CHEMBL1095831 | — | — | 1 | 9.59 |
| CHEMBL1095197 | — | — | 1 | 9.43 |
| CHEMBL1094546 | — | — | 1 | 9.26 |
| CHEMBL14453 | — | — | 1 | 9.22 |
| CHEMBL1096991 | — | — | 1 | 9.19 |
| CHEMBL1095195 | — | — | 1 | 9.10 |
| CHEMBL1097315 | — | — | 1 | 9.04 |
| CHEMBL1097314 | — | — | 1 | 9.00 |
| CHEMBL1095832 | — | — | 1 | 8.97 |
| CHEMBL1097496 | — | — | 1 | 8.86 |
| CHEMBL1095505 | — | — | 1 | 8.82 |
| CHEMBL1094545 | — | — | 1 | 8.62 |
| CHEMBL1097497 | — | — | 1 | 8.46 |
| CHEMBL1095522 | — | — | 1 | 8.39 |
| CHEMBL1095504 | — | — | 1 | 8.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1095196 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL1094212 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL1095831 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL1095197 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL1094546 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL14453 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1096991 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL1095195 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL1097315 | — | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL1097314 | — | Ki | = | 1.01 | nM | 9.00 |
| CHEMBL1095832 | — | Ki | = | 1.07 | nM | 8.97 |
| CHEMBL1097496 | — | Ki | = | 1.38 | nM | 8.86 |
| CHEMBL1095505 | — | Ki | = | 1.51 | nM | 8.82 |
| CHEMBL1094545 | — | Ki | = | 2.37 | nM | 8.62 |
| CHEMBL1097497 | — | Ki | = | 3.47 | nM | 8.46 |
| CHEMBL1095522 | — | Ki | = | 4.04 | nM | 8.39 |
| CHEMBL1095504 | — | Ki | = | 9.1 | nM | 8.04 |