Assay Detail
Functional
CHEMBL698408
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Histamine H3 receptor antagonist activity in an assay with K+ evoked depolarization-induced release of [3H]-histamine from rat synaptosomes.
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 8.29 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL114085 | — | — | 1 | 9.59 |
| CHEMBL321835 | — | — | 1 | 9.52 |
| CHEMBL326081 | — | — | 1 | 9.36 |
| CHEMBL324724 | — | — | 1 | 9.34 |
| CHEMBL14638 | CIPROXIFAN | — | 1 | 9.31 |
| CHEMBL114129 | — | — | 1 | 9.10 |
| CHEMBL322481 | — | — | 1 | 9.03 |
| CHEMBL115091 | — | — | 1 | 8.85 |
| CHEMBL113404 | — | — | 1 | 8.82 |
| CHEMBL326624 | — | — | 1 | 8.82 |
| CHEMBL420124 | — | — | 1 | 8.66 |
| CHEMBL112670 | — | — | 1 | 8.55 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.40 |
| CHEMBL116270 | — | — | 1 | 8.36 |
| CHEMBL112301 | — | — | 1 | 8.35 |
| CHEMBL113181 | — | — | 1 | 8.31 |
| CHEMBL112027 | — | — | 1 | 8.29 |
| CHEMBL112099 | — | — | 1 | 8.27 |
| CHEMBL114326 | — | — | 1 | 8.25 |
| CHEMBL112676 | — | — | 1 | 8.24 |
| CHEMBL112681 | — | — | 1 | 8.08 |
| CHEMBL112629 | — | — | 1 | 7.92 |
| CHEMBL325645 | — | — | 1 | 7.89 |
| CHEMBL324123 | — | — | 1 | 7.62 |
| CHEMBL112753 | — | — | 1 | 7.60 |
| CHEMBL112202 | — | — | 1 | 7.54 |
| CHEMBL115169 | — | — | 1 | 7.51 |
| CHEMBL326993 | — | — | 1 | 7.26 |
| CHEMBL112858 | — | — | 1 | 7.11 |
| CHEMBL324112 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL114085 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL321835 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL326081 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL324724 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL14638 | CIPROXIFAN | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL114129 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL322481 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL115091 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL113404 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL326624 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL420124 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL112670 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL116270 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL112301 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL113181 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL112027 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL112099 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL114326 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL112676 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL112681 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL112629 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL325645 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL324123 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL112753 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL112202 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL115169 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL326993 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL112858 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL324112 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL113403 | — | Ki | = | 371.0 | nM | 6.43 |
| CHEMBL112181 | — | Ki | ~ | 300.0 | nM | - |