Assay Detail
Binding
CHEMBL694443
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Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Dual antagonists of platelet activating factor and histamine. 3. Synthesis, biological activity and conformational implications of substituted N-acyl-bis-arylcycloheptapiperazines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 6.46 | 8.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL505 | CHLORPHENIRAMINE | 4.0 | 1 | 8.26 |
| CHEMBL117406 | — | — | 1 | 8.19 |
| CHEMBL118807 | — | — | 1 | 8.19 |
| CHEMBL332936 | — | — | 1 | 7.31 |
| CHEMBL410734 | — | — | 1 | 6.85 |
| CHEMBL324336 | — | — | 1 | 6.54 |
| CHEMBL10971 | SCH-37370 | — | 1 | 6.50 |
| CHEMBL117745 | — | — | 1 | 6.01 |
| CHEMBL326289 | — | — | 1 | 5.60 |
| CHEMBL2111767 | — | — | 1 | 5.44 |
| CHEMBL326978 | — | — | 1 | 5.44 |
| CHEMBL116144 | — | — | 1 | 5.44 |
| CHEMBL331159 | — | — | 1 | 5.43 |
| CHEMBL326821 | — | — | 1 | 5.27 |
| CHEMBL2448125 | — | — | 1 | - |
| CHEMBL325470 | — | — | 1 | - |
| CHEMBL325718 | — | — | 1 | - |
| CHEMBL333594 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL505 | CHLORPHENIRAMINE | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL117406 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL118807 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL332936 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL410734 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL324336 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL10971 | SCH-37370 | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL117745 | — | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL326289 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL2111767 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL326978 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL116144 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL331159 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL326821 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL2448125 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL325470 | — | Ki | >= | 7100.0 | nM | - |
| CHEMBL325718 | — | Ki | >= | 3800.0 | nM | - |
| CHEMBL333594 | — | Ki | >= | 5000.0 | nM | - |