Assay Detail
Binding
CHEMBL4767831
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Displacement of [125l]-lodomelatonin from hamster brain cell QR2 incubated for 60 mins by scintillation counting analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cricetinae |
| Tissue | Brain |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Tuning melatonin receptor subtype selectivity in oxadiazolone-based analogues: Discovery of QR2 ligands and NRF2 activators with neurogenic properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.25 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4783454 | — | — | 1 | 8.49 |
| CHEMBL4783536 | — | — | 1 | 8.18 |
| CHEMBL4781688 | — | — | 1 | 8.03 |
| CHEMBL4794450 | — | — | 1 | 7.46 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 7.11 |
| CHEMBL4791901 | — | — | 1 | 6.96 |
| CHEMBL4796759 | — | — | 1 | 6.66 |
| CHEMBL4797429 | — | — | 1 | 6.60 |
| CHEMBL4797226 | — | — | 1 | 6.57 |
| CHEMBL4794879 | — | — | 1 | 6.48 |
| CHEMBL3580919 | — | — | 1 | - |
| CHEMBL4794019 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4783454 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL4783536 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL4781688 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL4794450 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL45 | MELATONIN | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL4791901 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL4796759 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL4797429 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL4797226 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL4794879 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL3580919 | — | Ki | > | 100.0 | nM | - |
| CHEMBL4794019 | — | Ki | > | 10000.0 | nM | - |