Assay Detail
Binding
CHEMBL989166
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR
26
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
QSAR study of imidazoline antihypertensive drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.37 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19236 | MOXONIDINE | 4.0 | 1 | 8.38 |
| CHEMBL360803 | PI-CLONIDINE | — | 2 | 8.32 |
| CHEMBL762 | OXYMETAZOLINE | 4.0 | 2 | 8.21 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 2 | 7.94 |
| CHEMBL862 | GUANFACINE | 4.0 | 1 | 7.72 |
| CHEMBL1079 | TIZANIDINE | 4.0 | 2 | 7.55 |
| CHEMBL420 | GUANABENZ | 4.0 | 2 | 7.46 |
| CHEMBL57895 | EFAROXAN | 2.0 | 2 | 7.28 |
| CHEMBL134 | CLONIDINE | 4.0 | 2 | 7.26 |
| CHEMBL289480 | RILMENIDINE | 4.0 | 2 | 7.23 |
| CHEMBL13852 | CIRAZOLINE | 2.0 | 2 | 7.00 |
| CHEMBL761 | NAPHAZOLINE | 4.0 | 2 | 6.92 |
| CHEMBL1162356 | — | — | 2 | 6.63 |
| CHEMBL10316 | IDAZOXAN | 3.0 | 2 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19236 | MOXONIDINE | Ki | = | 4.198 | nM | 8.38 |
| CHEMBL360803 | PI-CLONIDINE | Ki | = | 4.797 | nM | 8.32 |
| CHEMBL360803 | PI-CLONIDINE | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL762 | OXYMETAZOLINE | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL762 | OXYMETAZOLINE | Ki | = | 6.194 | nM | 8.21 |
| CHEMBL597 | PHENTOLAMINE | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL597 | PHENTOLAMINE | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL862 | GUANFACINE | Ki | = | 19.01 | nM | 7.72 |
| CHEMBL1079 | TIZANIDINE | Ki | = | 28.3 | nM | 7.55 |
| CHEMBL1079 | TIZANIDINE | Ki | = | 28.31 | nM | 7.55 |
| CHEMBL420 | GUANABENZ | Ki | = | 34.67 | nM | 7.46 |
| CHEMBL420 | GUANABENZ | Ki | = | 34.7 | nM | 7.46 |
| CHEMBL57895 | EFAROXAN | Ki | = | 52.4 | nM | 7.28 |
| CHEMBL57895 | EFAROXAN | Ki | = | 52.36 | nM | 7.28 |
| CHEMBL134 | CLONIDINE | Ki | = | 54.95 | nM | 7.26 |
| CHEMBL134 | CLONIDINE | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL289480 | RILMENIDINE | Ki | = | 59.16 | nM | 7.23 |
| CHEMBL289480 | RILMENIDINE | Ki | = | 59.2 | nM | 7.23 |
| CHEMBL13852 | CIRAZOLINE | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL13852 | CIRAZOLINE | Ki | = | 99.08 | nM | 7.00 |
| CHEMBL761 | NAPHAZOLINE | Ki | = | 121.6 | nM | 6.92 |
| CHEMBL761 | NAPHAZOLINE | Ki | = | 121.62 | nM | 6.92 |
| CHEMBL1162356 | — | Ki | = | 232.0 | nM | 6.63 |
| CHEMBL1162356 | — | Ki | = | 231.74 | nM | 6.63 |
| CHEMBL10316 | IDAZOXAN | Ki | = | 1256.03 | nM | 5.90 |
| CHEMBL10316 | IDAZOXAN | Ki | = | 1255.0 | nM | 5.90 |