Assay Detail
Binding
CHEMBL884786
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Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 8.04 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL597 | PHENTOLAMINE | 4.0 | 1 | 8.38 |
| CHEMBL194323 | — | — | 1 | 8.28 |
| CHEMBL370818 | — | — | 1 | 8.28 |
| CHEMBL362954 | — | — | 1 | 7.70 |
| CHEMBL194849 | — | — | 1 | 7.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL597 | PHENTOLAMINE | Ki | = | 4.12 | nM | 8.38 |
| CHEMBL194323 | — | Ki | = | 5.25 | nM | 8.28 |
| CHEMBL370818 | — | Ki | = | 5.25 | nM | 8.28 |
| CHEMBL362954 | — | Ki | = | 19.9 | nM | 7.70 |
| CHEMBL194849 | — | Ki | = | 26.8 | nM | 7.57 |