Assay Detail
Binding
CHEMBL3745570
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Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
23
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 | 23 | 8.25 | 10.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1946221 | — | — | 2 | 10.27 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.34 |
| CHEMBL3741890 | — | — | 2 | 8.92 |
| CHEMBL322339 | — | — | 2 | 8.30 |
| CHEMBL3742090 | — | — | 2 | 8.30 |
| CHEMBL3739674 | — | — | 2 | 8.21 |
| CHEMBL3260986 | — | — | 2 | 8.10 |
| CHEMBL3739824 | — | — | 2 | 8.05 |
| CHEMBL3741561 | — | — | 2 | 8.05 |
| CHEMBL3740377 | — | — | 2 | 7.93 |
| CHEMBL3740052 | — | — | 2 | 7.46 |
| CHEMBL429392 | — | — | 2 | 6.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1946221 | — | Ki | = | 0.054 | nM | 10.27 |
| CHEMBL1946221 | — | Ki | = | 0.0537 | nM | 10.27 |
| CHEMBL45 | MELATONIN | Ki | = | 0.4571 | nM | 9.34 |
| CHEMBL3741890 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3741890 | — | Ki | = | 1.23 | nM | 8.91 |
| CHEMBL3742090 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL3742090 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL322339 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL322339 | — | Ki | = | 5.754 | nM | 8.24 |
| CHEMBL3739674 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL3739674 | — | Ki | = | 6.166 | nM | 8.21 |
| CHEMBL3260986 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL3260986 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL3741561 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3739824 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3741561 | — | Ki | = | 9.333 | nM | 8.03 |
| CHEMBL3740377 | — | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL3740377 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3739824 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL3740052 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL3740052 | — | Ki | = | 35.48 | nM | 7.45 |
| CHEMBL429392 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL429392 | — | Ki | = | 112.2 | nM | 6.95 |