Assay Detail
Binding
CHEMBL829668
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In vitro binding affinity against human phenylethanolamine N-Methyltransferase
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Phenylethanolamine N-methyltransferase (CHEMBL4617) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.79 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL287837 | — | — | 1 | 8.51 |
| CHEMBL366785 | — | — | 1 | 7.64 |
| CHEMBL175519 | — | — | 1 | 7.55 |
| CHEMBL41647 | — | — | 1 | 7.28 |
| CHEMBL176112 | — | — | 1 | 7.20 |
| CHEMBL178695 | — | — | 1 | 6.89 |
| CHEMBL95873 | — | — | 1 | 6.82 |
| CHEMBL175527 | — | — | 1 | 6.77 |
| CHEMBL177062 | — | — | 1 | 6.72 |
| CHEMBL177621 | — | — | 1 | 6.66 |
| CHEMBL175935 | — | — | 1 | 6.64 |
| CHEMBL290890 | — | — | 1 | 6.57 |
| CHEMBL26717 | — | — | 1 | 6.55 |
| CHEMBL121531 | — | — | 1 | 6.09 |
| CHEMBL355581 | — | — | 1 | 5.92 |
| CHEMBL177861 | — | — | 1 | 5.85 |
| CHEMBL435536 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL287837 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL366785 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL175519 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL41647 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL176112 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL178695 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL95873 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL175527 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL177062 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL177621 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL175935 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL290890 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL26717 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL121531 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL355581 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL177861 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL435536 | — | Ki | = | 1700.0 | nM | 5.77 |