Assay Detail
Binding
CHEMBL714922
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Inhibitory activity against melatonin receptor in the quail optica tecta using 2-[125] iodomelatonin as radiolabeled ligand
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Coturnix |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Conformationally restrained melatonin analogues: synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.42 | 10.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL15060 | — | — | 1 | 10.21 |
| CHEMBL33415 | — | — | 1 | 9.89 |
| CHEMBL61991 | — | — | 1 | 8.85 |
| CHEMBL61380 | — | — | 1 | 8.77 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 8.66 |
| CHEMBL34730 | — | — | 1 | 8.44 |
| CHEMBL60832 | — | — | 1 | 8.00 |
| CHEMBL60719 | — | — | 1 | 7.54 |
| CHEMBL292108 | — | — | 1 | 7.14 |
| CHEMBL60033 | — | — | 1 | 6.64 |
| CHEMBL61418 | — | — | 1 | 5.92 |
| CHEMBL64517 | — | — | 1 | 5.89 |
| CHEMBL60001 | — | — | 1 | 5.52 |
| CHEMBL58015 | — | — | 1 | 5.37 |
| CHEMBL61505 | — | — | 1 | 4.48 |
| CHEMBL60946 | — | — | 1 | - |
| CHEMBL64368 | — | — | 1 | - |
| CHEMBL61216 | — | — | 1 | - |
| CHEMBL302883 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL15060 | — | IC50 | = | 0.062 | nM | 10.21 |
| CHEMBL33415 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL61991 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL61380 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL45 | MELATONIN | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL34730 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL60832 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL60719 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL292108 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL60033 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL61418 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL64517 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL60001 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL58015 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL61505 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL60946 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL64368 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL61216 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL302883 | — | IC50 | > | 10000.0 | nM | - |