Assay Detail
Functional
CHEMBL1764014
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
18
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 |
|---|---|---|---|
| EC50 | 9 | 7.82 | 8.82 |
| ECmax | 9 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL45 | MELATONIN | 4.0 | 2 | 8.82 |
| CHEMBL1760947 | — | — | 2 | 8.68 |
| CHEMBL1760945 | — | — | 2 | 8.40 |
| CHEMBL1760946 | — | — | 2 | 8.29 |
| CHEMBL1760944 | — | — | 2 | 7.92 |
| CHEMBL1760957 | — | — | 2 | 7.80 |
| CHEMBL1760956 | — | — | 2 | 7.50 |
| CHEMBL1760955 | — | — | 2 | 7.03 |
| CHEMBL137969 | — | — | 2 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL45 | MELATONIN | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1760947 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL1760945 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1760946 | — | EC50 | = | 5.1 | nM | 8.29 |
| CHEMBL1760944 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1760957 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1760956 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1760955 | — | EC50 | = | 93.0 | nM | 7.03 |
| CHEMBL137969 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1760956 | — | ECmax | = | 37.0 | % | - |
| CHEMBL45 | MELATONIN | ECmax | = | 101.0 | % | - |
| CHEMBL1760945 | — | ECmax | = | 99.0 | % | - |
| CHEMBL1760944 | — | ECmax | = | 96.0 | % | - |
| CHEMBL1760947 | — | ECmax | = | 93.0 | % | - |
| CHEMBL1760955 | — | ECmax | = | 82.0 | % | - |
| CHEMBL137969 | — | ECmax | = | 92.0 | % | - |
| CHEMBL1760946 | — | ECmax | = | 87.0 | % | - |
| CHEMBL1760957 | — | ECmax | = | 83.0 | % | - |