Assay Detail
Binding
CHEMBL866345
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Displacement of 2-[125I]iodomelatonin from human recombinant MT2 receptor expressed in NIH3T3 cells
35
Total Activities
33
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
Mapping the melatonin receptor. 7. Subtype selective ligands based on beta-substituted N-acyl-5-methoxytryptamines and beta-substituted N-acyl-5-methoxy-1-methyltryptamines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 35 | 7.67 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL210791 | — | — | 3 | 9.57 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.46 |
| CHEMBL377101 | — | — | 1 | 9.33 |
| CHEMBL207745 | — | — | 1 | 9.13 |
| CHEMBL207625 | — | — | 1 | 9.07 |
| CHEMBL379616 | — | — | 1 | 8.99 |
| CHEMBL426127 | — | — | 1 | 8.94 |
| CHEMBL208307 | — | — | 1 | 8.89 |
| CHEMBL206472 | — | — | 1 | 8.56 |
| CHEMBL210147 | — | — | 1 | 8.53 |
| CHEMBL207960 | — | — | 1 | 8.48 |
| CHEMBL424693 | — | — | 1 | 8.36 |
| CHEMBL209712 | — | — | 1 | 8.12 |
| CHEMBL206790 | — | — | 1 | 7.54 |
| CHEMBL207420 | — | — | 1 | 7.50 |
| CHEMBL382439 | — | — | 1 | 7.48 |
| CHEMBL377871 | — | — | 1 | 7.41 |
| CHEMBL207676 | — | — | 1 | 7.24 |
| CHEMBL377809 | — | — | 1 | 7.21 |
| CHEMBL379403 | — | — | 1 | 7.18 |
| CHEMBL379413 | — | — | 1 | 7.14 |
| CHEMBL206419 | — | — | 1 | 7.07 |
| CHEMBL209711 | — | — | 1 | 7.05 |
| CHEMBL382555 | — | — | 1 | 6.99 |
| CHEMBL382579 | — | — | 1 | 6.86 |
| CHEMBL206471 | — | — | 1 | 6.59 |
| CHEMBL207959 | — | — | 1 | 6.39 |
| CHEMBL426861 | — | — | 1 | 5.98 |
| CHEMBL379504 | — | — | 1 | 5.90 |
| CHEMBL208802 | — | — | 1 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL210791 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL45 | MELATONIN | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL210791 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL377101 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL210791 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL207745 | — | Ki | = | 0.74 | nM | 9.13 |
| CHEMBL207625 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL379616 | — | Ki | = | 1.02 | nM | 8.99 |
| CHEMBL426127 | — | Ki | = | 1.15 | nM | 8.94 |
| CHEMBL208307 | — | Ki | = | 1.29 | nM | 8.89 |
| CHEMBL206472 | — | Ki | = | 2.75 | nM | 8.56 |
| CHEMBL210147 | — | Ki | = | 2.94 | nM | 8.53 |
| CHEMBL207960 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL424693 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL209712 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL206790 | — | Ki | = | 28.9 | nM | 7.54 |
| CHEMBL207420 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL382439 | — | Ki | = | 33.1 | nM | 7.48 |
| CHEMBL377871 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL207676 | — | Ki | = | 57.4 | nM | 7.24 |
| CHEMBL377809 | — | Ki | = | 62.2 | nM | 7.21 |
| CHEMBL379403 | — | Ki | = | 66.1 | nM | 7.18 |
| CHEMBL379413 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL206419 | — | Ki | = | 85.1 | nM | 7.07 |
| CHEMBL209711 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL382555 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL382579 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL206471 | — | Ki | = | 257.0 | nM | 6.59 |
| CHEMBL207959 | — | Ki | = | 407.0 | nM | 6.39 |
| CHEMBL426861 | — | Ki | = | 1047.0 | nM | 5.98 |
| CHEMBL379504 | — | Ki | = | 1259.0 | nM | 5.90 |
| CHEMBL208802 | — | Ki | = | 1445.0 | nM | 5.84 |
| CHEMBL379096 | — | Ki | = | 1738.0 | nM | 5.76 |
| CHEMBL206686 | — | Ki | = | 2344.0 | nM | 5.63 |
| CHEMBL382050 | — | Ki | = | 3767.0 | nM | 5.42 |