Assay Detail
Binding
CHEMBL3745571
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Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT2 expressed in CHO cells after 1 hr by gamma counting analysis
22
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel difluoroacetamide analogues of agomelatine and melatonin: probing the melatonin receptors for MT1selectivity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 8.06 | 9.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1946221 | — | — | 2 | 9.07 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.02 |
| CHEMBL322339 | — | — | 2 | 8.75 |
| CHEMBL3742090 | — | — | 2 | 8.75 |
| CHEMBL3739674 | — | — | 2 | 8.11 |
| CHEMBL3741890 | — | — | 2 | 8.09 |
| CHEMBL3739824 | — | — | 2 | 8.05 |
| CHEMBL3741561 | — | — | 2 | 8.05 |
| CHEMBL3740377 | — | — | 2 | 7.84 |
| CHEMBL3740052 | — | — | 2 | 7.36 |
| CHEMBL3260986 | — | — | 2 | 7.06 |
| CHEMBL429392 | — | — | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1946221 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL1946221 | — | Ki | = | 0.8511 | nM | 9.07 |
| CHEMBL45 | MELATONIN | Ki | = | 0.955 | nM | 9.02 |
| CHEMBL322339 | — | Ki | = | 1.778 | nM | 8.75 |
| CHEMBL3742090 | — | Ki | = | 1.778 | nM | 8.75 |
| CHEMBL322339 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3742090 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3739674 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL3739674 | — | Ki | = | 7.762 | nM | 8.11 |
| CHEMBL3741890 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL3741890 | — | Ki | = | 8.128 | nM | 8.09 |
| CHEMBL3741561 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3739824 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3741561 | — | Ki | = | 8.913 | nM | 8.05 |
| CHEMBL3740377 | — | Ki | = | 14.45 | nM | 7.84 |
| CHEMBL3740377 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3739824 | — | Ki | = | 21.38 | nM | 7.67 |
| CHEMBL3740052 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL3740052 | — | Ki | = | 43.65 | nM | 7.36 |
| CHEMBL3260986 | — | Ki | = | 87.1 | nM | 7.06 |
| CHEMBL3260986 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL429392 | — | Ki | = | 354.81 | nM | 6.45 |