Assay Detail
Functional
CHEMBL3993989
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Intrinsic activity at human MT2 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
20
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
New quinolinic derivatives as melatonergic ligands: Synthesis and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 9.55 | 10.05 |
| Emax | 10 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4084612 | — | — | 2 | 10.05 |
| CHEMBL4095210 | — | — | 2 | 10.00 |
| CHEMBL10878 | AGOMELATINE | 4.0 | 2 | 9.74 |
| CHEMBL4102177 | — | — | 2 | 9.70 |
| CHEMBL4071572 | — | — | 2 | 9.70 |
| CHEMBL4062947 | — | — | 2 | 9.70 |
| CHEMBL4082097 | — | — | 2 | 9.40 |
| CHEMBL4079784 | — | — | 2 | 9.15 |
| CHEMBL4089965 | — | — | 2 | 9.10 |
| CHEMBL4079699 | — | — | 2 | 8.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4084612 | — | EC50 | = | 0.09 | nM | 10.05 |
| CHEMBL4095210 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL10878 | AGOMELATINE | EC50 | = | 0.18 | nM | 9.74 |
| CHEMBL4102177 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4071572 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4062947 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4082097 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4079784 | — | EC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4089965 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4079699 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL10878 | AGOMELATINE | Emax | = | 91.0 | % | - |
| CHEMBL4102177 | — | Emax | = | 103.0 | % | - |
| CHEMBL4079784 | — | Emax | = | 103.0 | % | - |
| CHEMBL4089965 | — | Emax | = | 73.0 | % | - |
| CHEMBL4082097 | — | Emax | = | 72.0 | % | - |
| CHEMBL4071572 | — | Emax | = | 100.0 | % | - |
| CHEMBL4084612 | — | Emax | = | 102.0 | % | - |
| CHEMBL4062947 | — | Emax | = | 126.0 | % | - |
| CHEMBL4095210 | — | Emax | = | 52.0 | % | - |
| CHEMBL4079699 | — | Emax | = | 90.0 | % | - |