Assay Detail
Functional
CHEMBL691845
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antagonistic activity against histamine H3-receptor in an assay with K+-evoked depolarisation-induced release of [3H]histamine of synaptosomes of rat cerebral cortex
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Diphenylmethyl ethers: synthesis and histamine H3-receptor antagonist in vitro and in vivo activity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.65 | 9.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 9.20 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.40 |
| CHEMBL291369 | — | — | 1 | 7.70 |
| CHEMBL61618 | — | — | 1 | 7.70 |
| CHEMBL59679 | — | — | 1 | 7.60 |
| CHEMBL443322 | — | — | 1 | 7.60 |
| CHEMBL60342 | — | — | 1 | 7.60 |
| CHEMBL62244 | — | — | 1 | 7.10 |
| CHEMBL59851 | — | — | 1 | 6.90 |
| CHEMBL60606 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL291369 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL61618 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL59679 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL443322 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL60342 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL62244 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL59851 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL60606 | — | Ki | = | 199.53 | nM | 6.70 |