Assay Detail
Binding
CHEMBL839735
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Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor MT2 expressed in NIH3T3 rat fibroblast cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NIH3T3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Analysis of structure-activity relationships for MT2 selective antagonists by melatonin MT1 and MT2 receptor models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.05 | 10.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL285718 | — | — | 1 | 10.80 |
| CHEMBL33549 | — | — | 1 | 9.49 |
| CHEMBL274438 | — | — | 1 | 9.30 |
| CHEMBL189449 | — | — | 1 | 9.18 |
| CHEMBL34327 | — | — | 1 | 8.19 |
| CHEMBL33185 | — | — | 1 | 8.06 |
| CHEMBL187525 | — | — | 1 | 8.01 |
| CHEMBL366004 | — | — | 1 | 6.54 |
| CHEMBL372243 | — | — | 1 | 5.74 |
| CHEMBL195074 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL285718 | — | Ki | = | 0.01585 | nM | 10.80 |
| CHEMBL33549 | — | Ki | = | 0.3236 | nM | 9.49 |
| CHEMBL274438 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL189449 | — | Ki | = | 0.6607 | nM | 9.18 |
| CHEMBL34327 | — | Ki | = | 6.457 | nM | 8.19 |
| CHEMBL33185 | — | Ki | = | 8.71 | nM | 8.06 |
| CHEMBL187525 | — | Ki | = | 9.772 | nM | 8.01 |
| CHEMBL366004 | — | Ki | = | 288.4 | nM | 6.54 |
| CHEMBL372243 | — | Ki | = | 1819.7 | nM | 5.74 |
| CHEMBL195074 | — | Ki | = | 6025.6 | nM | 5.22 |