Assay Detail
Binding
CHEMBL927608
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]clonidine from adrenergic alpha-1 receptor in Sprague-Dawley rat cortex
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis of 4,5,6,7-tetrahydrothieno[3,2-c]pyridines and comparison with their isosteric 1,2,3,4-tetrahydroisoquinolines as inhibitors of phenylethanolamine N-methyltransferase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 5.42 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL287837 | — | — | 1 | 7.68 |
| CHEMBL357424 | — | — | 1 | 6.70 |
| CHEMBL281864 | — | — | 1 | 6.64 |
| CHEMBL14346 | 1,2,3,4-TETRAHYDROISOQUINOLINE | — | 1 | 6.46 |
| CHEMBL398475 | — | — | 1 | 6.42 |
| CHEMBL399179 | — | — | 1 | 6.31 |
| CHEMBL60434 | — | — | 1 | 6.12 |
| CHEMBL200375 | — | — | 1 | 5.96 |
| CHEMBL252803 | — | — | 1 | 5.92 |
| CHEMBL1526 | — | — | 1 | 5.82 |
| CHEMBL253218 | — | — | 1 | 5.64 |
| CHEMBL610 | PHENETHYLAMINE | — | 1 | 5.40 |
| CHEMBL399178 | — | — | 1 | 5.39 |
| CHEMBL281289 | — | — | 1 | 5.37 |
| CHEMBL253010 | — | — | 1 | 5.01 |
| CHEMBL252605 | — | — | 1 | 4.89 |
| CHEMBL252806 | — | — | 1 | 4.80 |
| CHEMBL253860 | — | — | 1 | 4.75 |
| CHEMBL522 | BENZYLAMINE | — | 1 | 4.70 |
| CHEMBL237711 | — | — | 1 | 4.57 |
| CHEMBL398678 | — | — | 1 | 4.54 |
| CHEMBL400515 | — | — | 1 | 4.54 |
| CHEMBL59719 | — | — | 1 | 4.51 |
| CHEMBL252602 | — | — | 1 | 4.50 |
| CHEMBL252606 | — | — | 1 | 4.33 |
| CHEMBL26717 | — | — | 1 | 4.00 |
| CHEMBL253859 | — | — | 1 | - |
| CHEMBL253219 | — | — | 1 | - |
| CHEMBL252808 | — | — | 1 | - |
| CHEMBL399864 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL287837 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL357424 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL281864 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL14346 | 1,2,3,4-TETRAHYDROISOQUINOLINE | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL398475 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL399179 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL60434 | — | Ki | = | 760.0 | nM | 6.12 |
| CHEMBL200375 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL252803 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL1526 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL253218 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL610 | PHENETHYLAMINE | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL399178 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL281289 | — | Ki | = | 4300.0 | nM | 5.37 |
| CHEMBL253010 | — | Ki | = | 9800.0 | nM | 5.01 |
| CHEMBL252605 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL252806 | — | Ki | = | 16000.0 | nM | 4.80 |
| CHEMBL253860 | — | Ki | = | 18000.0 | nM | 4.75 |
| CHEMBL522 | BENZYLAMINE | Ki | = | 20000.0 | nM | 4.70 |
| CHEMBL237711 | — | Ki | = | 27000.0 | nM | 4.57 |
| CHEMBL398678 | — | Ki | = | 29000.0 | nM | 4.54 |
| CHEMBL400515 | — | Ki | = | 29000.0 | nM | 4.54 |
| CHEMBL59719 | — | Ki | = | 31000.0 | nM | 4.51 |
| CHEMBL252602 | — | Ki | = | 32000.0 | nM | 4.50 |
| CHEMBL252606 | — | Ki | = | 47000.0 | nM | 4.33 |
| CHEMBL26717 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL253859 | — | Ki | = | 1500000.0 | nM | - |
| CHEMBL253219 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL252808 | — | Ki | = | 130000.0 | nM | - |
| CHEMBL399864 | — | Ki | > | 500000.0 | nM | - |