Assay Detail
Functional
CHEMBL698409
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro Histamine H3 receptor antagonist activity in an assay with K+-evoked depolarization-induced release of [3H]histamine from synaptosomes of rat cerebral cortex
8
Total Activities
8
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
General construction pattern of histamine H3-receptor antagonists: change of a paradigm.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.62 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 9.22 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.40 |
| CHEMBL292250 | — | — | 1 | 7.38 |
| CHEMBL296450 | — | — | 1 | 7.25 |
| CHEMBL303121 | — | — | 1 | 7.06 |
| CHEMBL60410 | — | — | 1 | 6.40 |
| CHEMBL305594 | — | — | 1 | - |
| CHEMBL61729 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL292250 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL296450 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL303121 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL60410 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL305594 | — | Ki | > | 500.0 | nM | - |
| CHEMBL61729 | — | Ki | > | 500.0 | nM | - |