Assay Detail
Functional
CHEMBL711326
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Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and structure-affinity-activity relationships of novel benzofuran derivatives as MT(2) melatonin receptor selective ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 7.61 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL287560 | — | — | 1 | 9.77 |
| CHEMBL329263 | — | — | 1 | 7.68 |
| CHEMBL97186 | — | — | 1 | 7.60 |
| CHEMBL33549 | — | — | 1 | 7.43 |
| CHEMBL329086 | — | — | 1 | 6.86 |
| CHEMBL329299 | — | — | 1 | 6.32 |
| CHEMBL440144 | — | — | 1 | - |
| CHEMBL317742 | — | — | 1 | - |
| CHEMBL329960 | — | — | 1 | - |
| CHEMBL96778 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL287560 | — | EC50 | = | 0.17 | nM | 9.77 |
| CHEMBL329263 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL97186 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL33549 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL329086 | — | EC50 | = | 138.0 | nM | 6.86 |
| CHEMBL329299 | — | EC50 | = | 481.0 | nM | 6.32 |
| CHEMBL440144 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL317742 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL329960 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL96778 | — | EC50 | > | 10000.0 | nM | - |