Assay Detail
Binding
CHEMBL764116
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Inhibition of PNMT (Phenylethanolamine N-Methyltransferase) in vitro
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 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 5.63 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL287837 | — | — | 1 | 6.66 |
| CHEMBL38681 | — | — | 1 | 6.58 |
| CHEMBL41647 | — | — | 1 | 6.47 |
| CHEMBL112964 | — | — | 1 | 6.28 |
| CHEMBL26717 | — | — | 1 | 6.25 |
| CHEMBL43021 | — | — | 1 | 6.19 |
| CHEMBL60068 | — | — | 1 | 5.96 |
| CHEMBL112351 | — | — | 1 | 5.70 |
| CHEMBL60434 | — | — | 1 | 5.68 |
| CHEMBL6409 | CGS-19281A | — | 1 | 5.57 |
| CHEMBL294562 | — | — | 1 | 5.04 |
| CHEMBL14346 | 1,2,3,4-TETRAHYDROISOQUINOLINE | — | 1 | 5.00 |
| CHEMBL112038 | — | — | 1 | 4.89 |
| CHEMBL444793 | — | — | 1 | 4.82 |
| CHEMBL59994 | — | — | 1 | 4.62 |
| CHEMBL112357 | — | — | 1 | 4.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL287837 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL38681 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL41647 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL112964 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL26717 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL43021 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL60068 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL112351 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL60434 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL6409 | CGS-19281A | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL294562 | — | Ki | = | 9200.0 | nM | 5.04 |
| CHEMBL14346 | 1,2,3,4-TETRAHYDROISOQUINOLINE | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL112038 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL444793 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL59994 | — | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL112357 | — | Ki | = | 36000.0 | nM | 4.44 |