Assay Detail
Binding
CHEMBL3583020
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Displacement of [125I]-p-iodoclonidin from I1-imidazoline receptor in rat PC12 cell membranes
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | PC-12 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Antagonism/Agonism modulation to build novel antihypertensives selectively triggering i1-imidazoline receptor activation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.98 | 8.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2092861 | — | — | 1 | 8.97 |
| CHEMBL71429 | — | — | 1 | 8.30 |
| CHEMBL3582266 | — | — | 1 | 7.88 |
| CHEMBL3582264 | — | — | 1 | 7.63 |
| CHEMBL3582261 | — | — | 1 | 7.20 |
| CHEMBL3582260 | — | — | 1 | 7.01 |
| CHEMBL128168 | BIPHENYLINE | — | 1 | 6.90 |
| CHEMBL3582258 | — | — | 1 | 6.81 |
| CHEMBL3582267 | — | — | 1 | 6.71 |
| CHEMBL273485 | — | — | 1 | 6.51 |
| CHEMBL3582265 | — | — | 1 | 5.98 |
| CHEMBL3582259 | — | — | 1 | 5.65 |
| CHEMBL1907832 | — | — | 1 | 5.20 |
| CHEMBL3582263 | — | — | 1 | - |
| CHEMBL3582262 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2092861 | — | Ki | = | 1.072 | nM | 8.97 |
| CHEMBL71429 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL3582266 | — | Ki | = | 13.18 | nM | 7.88 |
| CHEMBL3582264 | — | Ki | = | 23.44 | nM | 7.63 |
| CHEMBL3582261 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL3582260 | — | Ki | = | 97.72 | nM | 7.01 |
| CHEMBL128168 | BIPHENYLINE | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL3582258 | — | Ki | = | 154.88 | nM | 6.81 |
| CHEMBL3582267 | — | Ki | = | 194.98 | nM | 6.71 |
| CHEMBL273485 | — | Ki | = | 309.03 | nM | 6.51 |
| CHEMBL3582265 | — | Ki | = | 1047.13 | nM | 5.98 |
| CHEMBL3582259 | — | Ki | = | 2238.72 | nM | 5.65 |
| CHEMBL1907832 | — | Ki | = | 6309.57 | nM | 5.20 |
| CHEMBL3582263 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3582262 | — | Ki | > | 1000.0 | nM | - |