Assay Detail
Binding
CHEMBL651979
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Binding affinity towards alpha-1 adrenergic receptor of rat frontal cortex using [3H]- WB- 4101 as a radioligand
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Frontal cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Analogues of the 5-HT1A serotonin antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine with reduced alpha 1-adrenergic affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.53 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8618 | NAN-190 | — | 1 | 9.10 |
| CHEMBL282902 | — | — | 1 | 7.85 |
| CHEMBL27254 | — | — | 1 | 7.82 |
| CHEMBL26306 | — | — | 1 | 7.82 |
| CHEMBL27377 | — | — | 1 | 7.77 |
| CHEMBL27996 | — | — | 1 | 7.68 |
| CHEMBL26587 | — | — | 1 | 7.66 |
| CHEMBL24515 | — | — | 1 | 7.64 |
| CHEMBL287186 | — | — | 1 | 7.64 |
| CHEMBL26189 | — | — | 1 | 7.60 |
| CHEMBL26533 | — | — | 1 | 7.19 |
| CHEMBL21008 | — | — | 1 | 7.13 |
| CHEMBL27098 | — | — | 1 | 7.08 |
| CHEMBL26539 | — | — | 1 | 7.08 |
| CHEMBL410826 | — | — | 1 | 6.96 |
| CHEMBL26030 | — | — | 1 | 6.42 |
| CHEMBL316090 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8618 | NAN-190 | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL282902 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL27254 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL26306 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL27377 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL27996 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL26587 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL24515 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL287186 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL26189 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL26533 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL21008 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL27098 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL26539 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL410826 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL26030 | — | Ki | = | 378.0 | nM | 6.42 |
| CHEMBL316090 | — | Ki | < | 1000.0 | nM | - |