Assay Detail
Binding
CHEMBL698416
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In vitro inhibitory activity against Histamine H3 receptor for K+ evoked depolarization-induced release of [3H]histamine from synaptosomes of rat cerebral cortex
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 8.41 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL278462 | CIPRALISANT | 2.0 | 1 | 9.92 |
| CHEMBL14638 | CIPROXIFAN | — | 1 | 9.31 |
| CHEMBL309302 | — | — | 1 | 9.24 |
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 9.22 |
| CHEMBL76440 | — | — | 1 | 8.68 |
| CHEMBL309600 | — | — | 1 | 8.64 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.40 |
| CHEMBL80348 | — | — | 1 | 8.36 |
| CHEMBL80885 | — | — | 1 | 7.52 |
| CHEMBL76381 | — | — | 1 | 7.40 |
| CHEMBL419654 | — | — | 1 | 7.22 |
| CHEMBL77039 | — | — | 1 | 6.95 |
| CHEMBL78981 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL278462 | CIPRALISANT | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL14638 | CIPROXIFAN | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL309302 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL76440 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL309600 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL80348 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL80885 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL76381 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL419654 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL77039 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL78981 | — | Ki | > | 500.0 | nM | - |