Assay Detail
Binding
CHEMBL714928
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Inhibition of 2-[125I]iodomelatonin binding to melatonin receptor in quail brain as 1/Ka
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Coturnix |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
2-Substituted 5-methoxy-N-acyltryptamines: synthesis, binding affinity for the melatonin receptor, and evaluation of the biological activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 9.21 | 10.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL289233 | IODOMELATONIN | — | 1 | 10.68 |
| CHEMBL15060 | — | — | 1 | 10.24 |
| CHEMBL33415 | — | — | 1 | 10.24 |
| CHEMBL341392 | — | — | 1 | 9.68 |
| CHEMBL14975 | — | — | 1 | 9.62 |
| CHEMBL127069 | — | — | 1 | 9.37 |
| CHEMBL130759 | — | — | 1 | 9.20 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 8.96 |
| CHEMBL37549 | — | — | 1 | 8.66 |
| CHEMBL34730 | — | — | 1 | 8.66 |
| CHEMBL340115 | — | — | 1 | 8.37 |
| CHEMBL126417 | — | — | 1 | 8.28 |
| CHEMBL131281 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL289233 | IODOMELATONIN | Ki | = | 0.021 | nM | 10.68 |
| CHEMBL15060 | — | Ki | = | 0.057 | nM | 10.24 |
| CHEMBL33415 | — | Ki | = | 0.058 | nM | 10.24 |
| CHEMBL341392 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL14975 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL127069 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL130759 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL45 | MELATONIN | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL37549 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL34730 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL340115 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL126417 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL131281 | — | Ki | = | 18.0 | nM | 7.75 |