Assay Detail
Binding
CHEMBL1005949
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]RX821002 from alpha2 adrenergic receptor in human brain prefrontal cortex tissue by liquid scintillation spectrometry
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Prefrontal cortex |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Guanidine and 2-aminoimidazoline aromatic derivatives as alpha2-adrenoceptor antagonists. 2. Exploring alkyl linkers for new antidepressants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 41 | 7.02 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10332 | — | — | 1 | 9.04 |
| CHEMBL844 | BRIMONIDINE | 4.0 | 1 | 8.85 |
| CHEMBL75389 | — | — | 1 | 8.80 |
| CHEMBL1204394 | — | — | 1 | 8.26 |
| CHEMBL242839 | — | — | 1 | 8.21 |
| CHEMBL270533 | — | — | 1 | 7.96 |
| CHEMBL42139 | — | — | 1 | 7.85 |
| CHEMBL1204395 | — | — | 1 | 7.82 |
| CHEMBL230644 | — | — | 1 | 7.77 |
| CHEMBL1204391 | — | — | 1 | 7.68 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 7.68 |
| CHEMBL271749 | — | — | 1 | 7.58 |
| CHEMBL1203971 | — | — | 1 | 7.33 |
| CHEMBL243061 | — | — | 1 | 7.33 |
| CHEMBL10316 | IDAZOXAN | 3.0 | 1 | 7.29 |
| CHEMBL1204392 | — | — | 1 | 7.12 |
| CHEMBL1204398 | — | — | 1 | 7.11 |
| CHEMBL9441 | — | — | 1 | 7.07 |
| CHEMBL429921 | — | — | 1 | 7.02 |
| CHEMBL270900 | — | — | 1 | 6.92 |
| CHEMBL495211 | — | — | 1 | 6.85 |
| CHEMBL271534 | — | — | 1 | 6.83 |
| CHEMBL1203970 | — | — | 1 | 6.68 |
| CHEMBL430286 | — | — | 1 | 6.62 |
| CHEMBL270122 | — | — | 1 | 6.58 |
| CHEMBL405429 | — | — | 1 | 6.56 |
| CHEMBL1204200 | — | — | 1 | 6.53 |
| CHEMBL1204393 | — | — | 1 | 6.51 |
| CHEMBL1204384 | — | — | 1 | 6.48 |
| CHEMBL270352 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10332 | — | Ki | = | 0.912 | nM | 9.04 |
| CHEMBL844 | BRIMONIDINE | Ki | = | 1.413 | nM | 8.85 |
| CHEMBL75389 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL1204394 | — | Ki | = | 5.495 | nM | 8.26 |
| CHEMBL242839 | — | Ki | = | 6.166 | nM | 8.21 |
| CHEMBL270533 | — | Ki | = | 10.96 | nM | 7.96 |
| CHEMBL42139 | — | Ki | = | 14.13 | nM | 7.85 |
| CHEMBL1204395 | — | Ki | = | 15.14 | nM | 7.82 |
| CHEMBL230644 | — | Ki | = | 16.98 | nM | 7.77 |
| CHEMBL1204391 | — | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL134 | CLONIDINE | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL271749 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL1203971 | — | Ki | = | 46.77 | nM | 7.33 |
| CHEMBL243061 | — | Ki | = | 46.77 | nM | 7.33 |
| CHEMBL10316 | IDAZOXAN | Ki | = | 51.29 | nM | 7.29 |
| CHEMBL1204392 | — | Ki | = | 75.86 | nM | 7.12 |
| CHEMBL1204398 | — | Ki | = | 77.62 | nM | 7.11 |
| CHEMBL9441 | — | Ki | = | 85.11 | nM | 7.07 |
| CHEMBL429921 | — | Ki | = | 95.5 | nM | 7.02 |
| CHEMBL270900 | — | Ki | = | 120.23 | nM | 6.92 |
| CHEMBL495211 | — | Ki | = | 141.25 | nM | 6.85 |
| CHEMBL271534 | — | Ki | = | 147.91 | nM | 6.83 |
| CHEMBL1203970 | — | Ki | = | 208.93 | nM | 6.68 |
| CHEMBL430286 | — | Ki | = | 239.88 | nM | 6.62 |
| CHEMBL270122 | — | Ki | = | 263.03 | nM | 6.58 |
| CHEMBL405429 | — | Ki | = | 275.42 | nM | 6.56 |
| CHEMBL1204200 | — | Ki | = | 295.12 | nM | 6.53 |
| CHEMBL1204393 | — | Ki | = | 309.03 | nM | 6.51 |
| CHEMBL1204384 | — | Ki | = | 331.13 | nM | 6.48 |
| CHEMBL270352 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL44100 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL297076 | — | Ki | = | 407.38 | nM | 6.39 |
| CHEMBL1204397 | — | Ki | = | 416.87 | nM | 6.38 |
| CHEMBL271809 | — | Ki | = | 478.63 | nM | 6.32 |
| CHEMBL497120 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL1204140 | — | Ki | = | 645.65 | nM | 6.19 |
| CHEMBL363001 | — | Ki | = | 758.58 | nM | 6.12 |
| CHEMBL270121 | — | Ki | = | 891.25 | nM | 6.05 |
| CHEMBL404606 | — | Ki | = | 1318.26 | nM | 5.88 |
| CHEMBL271404 | — | Ki | = | 2630.27 | nM | 5.58 |
| CHEMBL1204396 | — | Ki | = | 2818.38 | nM | 5.55 |