Assay Detail
Binding
CHEMBL1947484
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Displacement of [125I]iodomelatonin form human MT2 receptor expressed in HEK cells after 120 mins
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, synthesis and pharmacological evaluation of new series of naphthalenic analogues as melatoninergic (MT1/MT2) and serotoninergic 5-HT2C dual ligands (I).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 9.01 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1946226 | — | — | 1 | 11.00 |
| CHEMBL1946224 | — | — | 1 | 10.40 |
| CHEMBL342432 | — | — | 1 | 10.22 |
| CHEMBL1946220 | — | — | 1 | 10.15 |
| CHEMBL1946232 | — | — | 1 | 10.15 |
| CHEMBL10878 | AGOMELATINE | 4.0 | 1 | 9.92 |
| CHEMBL1946233 | — | — | 1 | 9.89 |
| CHEMBL1946234 | — | — | 1 | 9.74 |
| CHEMBL139410 | — | — | 1 | 9.55 |
| CHEMBL1946229 | — | — | 1 | 9.49 |
| CHEMBL1946235 | — | — | 1 | 9.41 |
| CHEMBL1946227 | — | — | 1 | 9.32 |
| CHEMBL1946704 | — | — | 1 | 9.25 |
| CHEMBL1946222 | — | — | 1 | 9.23 |
| CHEMBL1946705 | — | — | 1 | 9.01 |
| CHEMBL1946707 | — | — | 1 | 8.98 |
| CHEMBL1946231 | — | — | 1 | 8.96 |
| CHEMBL1946708 | — | — | 1 | 8.92 |
| CHEMBL1946225 | — | — | 1 | 8.87 |
| CHEMBL1946236 | — | — | 1 | 8.46 |
| CHEMBL1946709 | — | — | 1 | 8.42 |
| CHEMBL1946228 | — | — | 1 | 8.38 |
| CHEMBL1946221 | — | — | 1 | 8.37 |
| CHEMBL1946223 | — | — | 1 | 8.06 |
| CHEMBL1946706 | — | — | 1 | 8.06 |
| CHEMBL138201 | — | — | 1 | 8.00 |
| CHEMBL1946702 | — | — | 1 | 7.19 |
| CHEMBL1946230 | — | — | 1 | 7.05 |
| CHEMBL1946703 | — | — | 1 | 6.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1946226 | — | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL1946224 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL342432 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL1946220 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL1946232 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL10878 | AGOMELATINE | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL1946233 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL1946234 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL139410 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL1946229 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL1946235 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL1946227 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL1946704 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL1946222 | — | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL1946705 | — | Ki | = | 0.98 | nM | 9.01 |
| CHEMBL1946707 | — | Ki | = | 1.05 | nM | 8.98 |
| CHEMBL1946231 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1946708 | — | Ki | = | 1.19 | nM | 8.92 |
| CHEMBL1946225 | — | Ki | = | 1.34 | nM | 8.87 |
| CHEMBL1946236 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL1946709 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL1946228 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL1946221 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL1946223 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL1946706 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL138201 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL1946702 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL1946230 | — | Ki | = | 88.3 | nM | 7.05 |
| CHEMBL1946703 | — | Ki | = | 124.0 | nM | 6.91 |