Assay Detail
Binding
CHEMBL1763820
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in HEK293 cells
16
Total Activities
16
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
Design and synthesis of 1-(2-alkanamidoethyl)-6-methoxy-7-azaindole derivatives as potent melatonin agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.61 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1760946 | — | — | 1 | 9.55 |
| CHEMBL1760944 | — | — | 1 | 9.52 |
| CHEMBL1760947 | — | — | 1 | 9.52 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.47 |
| CHEMBL1760945 | — | — | 1 | 9.22 |
| CHEMBL1760957 | — | — | 1 | 9.17 |
| CHEMBL1760956 | — | — | 1 | 8.30 |
| CHEMBL1760955 | — | — | 1 | 7.52 |
| CHEMBL137969 | — | — | 1 | 6.93 |
| CHEMBL1760951 | — | — | 1 | 6.26 |
| CHEMBL1760950 | — | — | 1 | 6.13 |
| CHEMBL1760952 | — | — | 1 | 6.03 |
| CHEMBL1760954 | — | — | 1 | 5.96 |
| CHEMBL1760949 | — | — | 1 | 5.40 |
| CHEMBL1760953 | — | — | 1 | 5.13 |
| CHEMBL1760948 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1760946 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL1760944 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL1760947 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL45 | MELATONIN | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL1760945 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1760957 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL1760956 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL1760955 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL137969 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL1760951 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL1760950 | — | Ki | = | 742.0 | nM | 6.13 |
| CHEMBL1760952 | — | Ki | = | 929.0 | nM | 6.03 |
| CHEMBL1760954 | — | Ki | = | 1090.0 | nM | 5.96 |
| CHEMBL1760949 | — | Ki | = | 4007.0 | nM | 5.40 |
| CHEMBL1760953 | — | Ki | = | 7440.0 | nM | 5.13 |
| CHEMBL1760948 | — | Ki | > | 10000.0 | nM | - |