Assay Detail
Binding
CHEMBL761982
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Ability to inhibit phenylethanolamine N-methyl-transferase (PNMT)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Phenylethanolamine N-methyltransferase (CHEMBL2331) ↗| Type | SINGLE PROTEIN |
| Organism | Bos taurus |
Publication
Synthesis and evaluation of 4-fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.12 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL287837 | — | — | 1 | 6.66 |
| CHEMBL38681 | — | — | 1 | 6.58 |
| CHEMBL59441 | — | — | 1 | 6.54 |
| CHEMBL41647 | — | — | 1 | 6.47 |
| CHEMBL95184 | — | — | 1 | 6.41 |
| CHEMBL95928 | — | — | 1 | 6.27 |
| CHEMBL97282 | — | — | 1 | 6.27 |
| CHEMBL26717 | — | — | 1 | 6.25 |
| CHEMBL39928 | — | — | 1 | 6.19 |
| CHEMBL95873 | — | — | 1 | 6.18 |
| CHEMBL40081 | — | — | 1 | 5.96 |
| CHEMBL316704 | — | — | 1 | 5.89 |
| CHEMBL95450 | — | — | 1 | 5.70 |
| CHEMBL320367 | — | — | 1 | 5.68 |
| CHEMBL6409 | CGS-19281A | — | 1 | 5.57 |
| CHEMBL318333 | — | — | 1 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL287837 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL38681 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL59441 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL41647 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL95184 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL95928 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL97282 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL26717 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL39928 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL95873 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL40081 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL316704 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL95450 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL320367 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL6409 | CGS-19281A | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL318333 | — | Ki | = | 5300.0 | nM | 5.28 |