Assay Detail
Binding
CHEMBL3762920
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
20
Total Activities
20
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
Melatonergic ligands: Design, synthesis and pharmacological evaluation of novel series of naphthofuranic derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 8.03 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10878 | AGOMELATINE | 4.0 | 1 | 9.92 |
| CHEMBL323332 | — | — | 1 | 9.82 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.64 |
| CHEMBL3758679 | — | — | 1 | 8.72 |
| CHEMBL3758717 | — | — | 1 | 8.68 |
| CHEMBL3759802 | — | — | 1 | 8.55 |
| CHEMBL3758225 | — | — | 1 | 8.34 |
| CHEMBL3759084 | — | — | 1 | 8.24 |
| CHEMBL3758720 | — | — | 1 | 8.00 |
| CHEMBL3759160 | — | — | 1 | 8.00 |
| CHEMBL3759080 | — | — | 1 | 7.77 |
| CHEMBL3759816 | — | — | 1 | 7.70 |
| CHEMBL3759606 | — | — | 1 | 7.63 |
| CHEMBL3759372 | — | — | 1 | 7.37 |
| CHEMBL3759859 | — | — | 1 | 7.14 |
| CHEMBL3759677 | — | — | 1 | 6.85 |
| CHEMBL3760044 | — | — | 1 | 6.80 |
| CHEMBL3759054 | — | — | 1 | 6.80 |
| CHEMBL3759180 | — | — | 1 | 6.68 |
| CHEMBL3759661 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10878 | AGOMELATINE | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL323332 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL45 | MELATONIN | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL3758679 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL3758717 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3759802 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL3758225 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL3759084 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL3758720 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3759160 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL3759080 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3759816 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL3759606 | — | Ki | = | 23.6 | nM | 7.63 |
| CHEMBL3759372 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL3759859 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL3759677 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL3760044 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL3759054 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL3759180 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL3759661 | — | Ki | - | — | - |