Assay Detail
Binding
CHEMBL644243
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Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and structure-activity relationships of a new model of arylpiperazines. 3.1 2-[omega-(4-arylpiperazin-1-yl)alkyl]perhydropyrrolo- [1,2-c]imidazoles and -perhydroimidazo[1,5-a]pyridines: study of the influence of the terminal amide fragment on 5-HT1A affinity/selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.28 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL289873 | — | — | 1 | 8.51 |
| CHEMBL42810 | — | — | 1 | 8.08 |
| CHEMBL46881 | — | — | 1 | 8.07 |
| CHEMBL290039 | — | — | 1 | 8.02 |
| CHEMBL43992 | — | — | 1 | 8.00 |
| CHEMBL42644 | — | — | 1 | 7.92 |
| CHEMBL88715 | — | — | 1 | 7.35 |
| CHEMBL89677 | — | — | 1 | 7.19 |
| CHEMBL424432 | — | — | 1 | 7.19 |
| CHEMBL46918 | — | — | 1 | 7.19 |
| CHEMBL315472 | — | — | 1 | 7.14 |
| CHEMBL417709 | — | — | 1 | 7.14 |
| CHEMBL45253 | — | — | 1 | 7.04 |
| CHEMBL42706 | — | — | 1 | 6.96 |
| CHEMBL90384 | — | — | 1 | 6.94 |
| CHEMBL89380 | — | — | 1 | 6.66 |
| CHEMBL90165 | — | — | 1 | 6.62 |
| CHEMBL314997 | — | — | 1 | 6.56 |
| CHEMBL88594 | — | — | 1 | 6.49 |
| CHEMBL89950 | — | — | 1 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL289873 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL42810 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL46881 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL290039 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL43992 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL42644 | — | Ki | = | 12.1 | nM | 7.92 |
| CHEMBL88715 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL89677 | — | Ki | = | 64.3 | nM | 7.19 |
| CHEMBL424432 | — | Ki | = | 64.9 | nM | 7.19 |
| CHEMBL46918 | — | Ki | = | 64.9 | nM | 7.19 |
| CHEMBL315472 | — | Ki | = | 72.6 | nM | 7.14 |
| CHEMBL417709 | — | Ki | = | 72.4 | nM | 7.14 |
| CHEMBL45253 | — | Ki | = | 90.4 | nM | 7.04 |
| CHEMBL42706 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL90384 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL89380 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL90165 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL314997 | — | Ki | = | 278.0 | nM | 6.56 |
| CHEMBL88594 | — | Ki | = | 323.0 | nM | 6.49 |
| CHEMBL89950 | — | Ki | = | 363.0 | nM | 6.44 |