Assay Detail
Binding
CHEMBL643682
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of [3H]clonidine binding at the alpha-2 adrenergic receptor.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Enantiospecific synthesis of 3-fluoromethyl-, 3-hydroxymethyl-, and 3-chloromethyl-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 | 37 | 5.20 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL287837 | — | — | 1 | 7.68 |
| CHEMBL14346 | 1,2,3,4-TETRAHYDROISOQUINOLINE | — | 1 | 6.46 |
| CHEMBL293023 | — | — | 1 | 6.31 |
| CHEMBL59994 | — | — | 1 | 6.17 |
| CHEMBL60434 | — | — | 1 | 6.12 |
| CHEMBL342625 | — | — | 1 | 6.01 |
| CHEMBL337144 | — | — | 1 | 5.92 |
| CHEMBL343389 | — | — | 1 | 5.64 |
| CHEMBL137286 | — | — | 1 | 5.54 |
| CHEMBL136304 | — | — | 1 | 5.51 |
| CHEMBL121531 | — | — | 1 | 5.42 |
| CHEMBL61490 | — | — | 1 | 5.36 |
| CHEMBL294079 | — | — | 1 | 5.24 |
| CHEMBL39928 | — | — | 1 | 5.19 |
| CHEMBL342411 | — | — | 1 | 5.18 |
| CHEMBL60068 | — | — | 1 | 5.18 |
| CHEMBL62034 | — | — | 1 | 4.89 |
| CHEMBL61489 | — | — | 1 | 4.77 |
| CHEMBL136475 | — | — | 1 | 4.77 |
| CHEMBL304872 | — | — | 1 | 4.72 |
| CHEMBL137607 | — | — | 1 | 4.43 |
| CHEMBL293700 | — | — | 1 | 4.42 |
| CHEMBL138677 | — | — | 1 | 4.33 |
| CHEMBL57966 | — | — | 1 | 4.28 |
| CHEMBL97282 | — | — | 1 | 4.12 |
| CHEMBL135959 | — | — | 1 | 4.01 |
| CHEMBL337156 | — | — | 1 | 4.00 |
| CHEMBL26717 | — | — | 1 | 4.00 |
| CHEMBL336026 | — | — | 1 | - |
| CHEMBL136361 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL287837 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL14346 | 1,2,3,4-TETRAHYDROISOQUINOLINE | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL293023 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL59994 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL60434 | — | Ki | = | 760.0 | nM | 6.12 |
| CHEMBL342625 | — | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL337144 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL343389 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL137286 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL136304 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL121531 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL61490 | — | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL294079 | — | Ki | = | 5700.0 | nM | 5.24 |
| CHEMBL39928 | — | Ki | = | 6400.0 | nM | 5.19 |
| CHEMBL60068 | — | Ki | = | 6600.0 | nM | 5.18 |
| CHEMBL342411 | — | Ki | = | 6600.0 | nM | 5.18 |
| CHEMBL62034 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL136475 | — | Ki | = | 17000.0 | nM | 4.77 |
| CHEMBL61489 | — | Ki | = | 17000.0 | nM | 4.77 |
| CHEMBL304872 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL137607 | — | Ki | = | 37000.0 | nM | 4.43 |
| CHEMBL293700 | — | Ki | = | 38000.0 | nM | 4.42 |
| CHEMBL138677 | — | Ki | = | 47000.0 | nM | 4.33 |
| CHEMBL57966 | — | Ki | = | 53000.0 | nM | 4.28 |
| CHEMBL97282 | — | Ki | = | 76000.0 | nM | 4.12 |
| CHEMBL135959 | — | Ki | = | 97000.0 | nM | 4.01 |
| CHEMBL26717 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL337156 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL336026 | — | Ki | = | 360000.0 | nM | - |
| CHEMBL136361 | — | Ki | = | 270000.0 | nM | - |
| CHEMBL95873 | — | Ki | = | 680000.0 | nM | - |
| CHEMBL40081 | — | Ki | = | 460000.0 | nM | - |
| CHEMBL290890 | — | Ki | = | 160000.0 | nM | - |
| CHEMBL139495 | — | Ki | = | 140000.0 | nM | - |
| CHEMBL41647 | — | Ki | = | 1400000.0 | nM | - |
| CHEMBL135957 | — | Ki | = | 101000.0 | nM | - |
| CHEMBL135908 | — | Ki | = | 580000.0 | nM | - |