Assay Detail
Binding
CHEMBL764114
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In vitro inhibitory activity against bovine adrenal phenylethanolamine N-methyltransferase(PNMT)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Phenylethanolamine N-methyltransferase (CHEMBL2331) ↗| Type | SINGLE PROTEIN |
| Organism | Bos taurus |
Publication
Synthesis, biochemical evaluation, and classical and three-dimensional quantitative structure-activity relationship studies of 7-substituted-1,2,3,4-tetrahydroisoquinolines and their relative affinities toward phenylethanolamine N-methyltransferase and the alpha2-adrenoceptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 5.74 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27499 | — | — | 1 | 6.75 |
| CHEMBL281864 | — | — | 1 | 6.54 |
| CHEMBL28329 | — | — | 1 | 6.21 |
| CHEMBL27599 | — | — | 1 | 5.89 |
| CHEMBL26711 | — | — | 1 | 5.57 |
| CHEMBL14346 | 1,2,3,4-TETRAHYDROISOQUINOLINE | — | 1 | 5.01 |
| CHEMBL25316 | — | — | 1 | 4.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27499 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL281864 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL28329 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL27599 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL26711 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL14346 | 1,2,3,4-TETRAHYDROISOQUINOLINE | Ki | = | 9700.0 | nM | 5.01 |
| CHEMBL25316 | — | Ki | = | 61000.0 | nM | 4.21 |