Assay Detail
Functional
CHEMBL697536
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Antagonist activity against Histamine H3 receptor in an assay with K+ -evolved depolarization-induced release of [3H]histamine from rat synaptosomes.
22
Total Activities
22
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 | 22 | 8.41 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL114085 | — | — | 1 | 9.60 |
| CHEMBL321835 | — | — | 1 | 9.50 |
| CHEMBL326081 | — | — | 1 | 9.40 |
| CHEMBL324724 | — | — | 1 | 9.30 |
| CHEMBL322481 | — | — | 1 | 9.00 |
| CHEMBL115091 | — | — | 1 | 8.90 |
| CHEMBL113404 | — | — | 1 | 8.80 |
| CHEMBL326624 | — | — | 1 | 8.80 |
| CHEMBL420124 | — | — | 1 | 8.70 |
| CHEMBL112670 | — | — | 1 | 8.60 |
| CHEMBL116270 | — | — | 1 | 8.40 |
| CHEMBL112301 | — | — | 1 | 8.30 |
| CHEMBL113181 | — | — | 1 | 8.30 |
| CHEMBL112099 | — | — | 1 | 8.30 |
| CHEMBL112676 | — | — | 1 | 8.20 |
| CHEMBL112681 | — | — | 1 | 8.10 |
| CHEMBL112629 | — | — | 1 | 7.90 |
| CHEMBL325645 | — | — | 1 | 7.90 |
| CHEMBL112753 | — | — | 1 | 7.60 |
| CHEMBL112202 | — | — | 1 | 7.50 |
| CHEMBL115169 | — | — | 1 | 7.50 |
| CHEMBL113403 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL114085 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL321835 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL326081 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL324724 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL322481 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL115091 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL113404 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL326624 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL420124 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL112670 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL116270 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL112301 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL113181 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL112099 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL112676 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL112681 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL112629 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL325645 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL112753 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL112202 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL115169 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL113403 | — | Ki | = | 398.11 | nM | 6.40 |