Assay Detail
Functional
CHEMBL698411
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antagonist potency at Histamine H3 receptor measured as K+-evoked [3H]histamine release from synaptosomes of rat cerebral cortex.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
4-Alkynylphenyl imidazolylpropyl ethers as selective histamine H3-receptor antagonists with high oral central nervous system activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.94 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 9.22 |
| CHEMBL309600 | — | — | 1 | 8.64 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.40 |
| CHEMBL132798 | — | — | 1 | 8.12 |
| CHEMBL132686 | — | — | 1 | 7.44 |
| CHEMBL133793 | — | — | 1 | 6.91 |
| CHEMBL134902 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL309600 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL132798 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL132686 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL133793 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL134902 | — | Ki | = | 140.0 | nM | 6.85 |