Assay Detail
Binding
CHEMBL5330540
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]pyrilamine from Sprague-Dawley rat H1 receptor assessed as inhibition constant measured after 30 mins by competitive binding assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
New aryl-/heteroarylpiperazine derivatives of 1,7-dimethyl-8,9-diphenyl-4-azatricyclo[5.2.1.0<sup>2,6</sup>]dec-8-ene-3,5,10-trione: Synthesis and preliminary studies of biological activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.53 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL643 | PROMETHAZINE | 4.0 | 1 | 9.00 |
| CHEMBL5403228 | — | — | 1 | 8.22 |
| CHEMBL5395179 | — | — | 1 | 8.15 |
| CHEMBL5435378 | — | — | 1 | 7.52 |
| CHEMBL5409943 | — | — | 1 | 7.10 |
| CHEMBL5422403 | — | — | 1 | 6.52 |
| CHEMBL5437394 | — | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL643 | PROMETHAZINE | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL5403228 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL5395179 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL5435378 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL5409943 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL5422403 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL5437394 | — | Ki | = | 600.0 | nM | 6.22 |