Assay Detail
Binding
CHEMBL987963
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 HEK293 cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of 3-phenylnaphthalenic derivatives as new selective MT(2) melatoninergic ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.19 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10878 | AGOMELATINE | 4.0 | 1 | 10.22 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.85 |
| CHEMBL517502 | — | — | 1 | 8.23 |
| CHEMBL491605 | — | — | 1 | 7.61 |
| CHEMBL489170 | — | — | 1 | 7.42 |
| CHEMBL478217 | — | — | 1 | 7.30 |
| CHEMBL490595 | — | — | 1 | 7.29 |
| CHEMBL453138 | — | — | 1 | 7.28 |
| CHEMBL476341 | — | — | 1 | 7.22 |
| CHEMBL490188 | — | — | 1 | 7.09 |
| CHEMBL477835 | — | — | 1 | 7.08 |
| CHEMBL478218 | — | — | 1 | 6.91 |
| CHEMBL518113 | — | — | 1 | 6.90 |
| CHEMBL477833 | — | — | 1 | 6.90 |
| CHEMBL491604 | — | — | 1 | 6.86 |
| CHEMBL491403 | — | — | 1 | 6.69 |
| CHEMBL476131 | — | — | 1 | 6.56 |
| CHEMBL476132 | — | — | 1 | 6.53 |
| CHEMBL477834 | — | — | 1 | 5.86 |
| CHEMBL478438 | — | — | 1 | 5.82 |
| CHEMBL490594 | — | — | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10878 | AGOMELATINE | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL45 | MELATONIN | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL517502 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL491605 | — | Ki | = | 24.7 | nM | 7.61 |
| CHEMBL489170 | — | Ki | = | 38.4 | nM | 7.42 |
| CHEMBL478217 | — | Ki | = | 49.8 | nM | 7.30 |
| CHEMBL490595 | — | Ki | = | 50.7 | nM | 7.29 |
| CHEMBL453138 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL476341 | — | Ki | = | 60.3 | nM | 7.22 |
| CHEMBL490188 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL477835 | — | Ki | = | 82.5 | nM | 7.08 |
| CHEMBL478218 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL518113 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL477833 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL491604 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL491403 | — | Ki | = | 204.0 | nM | 6.69 |
| CHEMBL476131 | — | Ki | = | 275.0 | nM | 6.56 |
| CHEMBL476132 | — | Ki | = | 297.0 | nM | 6.53 |
| CHEMBL477834 | — | Ki | = | 1390.0 | nM | 5.86 |
| CHEMBL478438 | — | Ki | = | 1510.0 | nM | 5.82 |
| CHEMBL490594 | — | Ki | = | 3830.0 | nM | 5.42 |