Assay Detail
Binding
CHEMBL881341
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In vitro binding affinity for rat histamine H3 receptor using [3H]N-alpha-methylhistamine
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 8.87 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL197747 | — | — | 1 | 9.96 |
| CHEMBL199245 | — | — | 1 | 9.57 |
| CHEMBL196294 | — | — | 1 | 9.46 |
| CHEMBL196467 | — | — | 1 | 9.42 |
| CHEMBL194506 | — | — | 1 | 9.40 |
| CHEMBL445144 | — | — | 1 | 9.24 |
| CHEMBL424842 | — | — | 1 | 9.17 |
| CHEMBL371210 | — | — | 1 | 9.10 |
| CHEMBL194620 | — | — | 1 | 9.06 |
| CHEMBL371258 | — | — | 1 | 9.06 |
| CHEMBL194418 | — | — | 1 | 8.93 |
| CHEMBL196629 | — | — | 1 | 8.92 |
| CHEMBL351231 | — | — | 1 | 8.91 |
| CHEMBL196868 | — | — | 1 | 8.87 |
| CHEMBL198625 | — | — | 1 | 8.85 |
| CHEMBL194857 | — | — | 1 | 8.83 |
| CHEMBL362952 | — | — | 1 | 8.80 |
| CHEMBL366183 | — | — | 1 | 8.72 |
| CHEMBL198703 | — | — | 1 | 8.70 |
| CHEMBL198325 | — | — | 1 | 8.67 |
| CHEMBL380557 | — | — | 1 | 8.63 |
| CHEMBL197608 | — | — | 1 | 8.60 |
| CHEMBL364222 | — | — | 1 | 8.60 |
| CHEMBL199187 | — | — | 1 | 8.57 |
| CHEMBL197890 | — | — | 1 | 8.56 |
| CHEMBL196480 | — | — | 1 | 8.54 |
| CHEMBL372546 | — | — | 1 | 8.48 |
| CHEMBL193607 | — | — | 1 | 8.40 |
| CHEMBL363645 | — | — | 1 | 8.40 |
| CHEMBL425023 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL197747 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL199245 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL196294 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL196467 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL194506 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL445144 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL424842 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL371210 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL194620 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL371258 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL194418 | — | Ki | = | 1.18 | nM | 8.93 |
| CHEMBL196629 | — | Ki | = | 1.19 | nM | 8.92 |
| CHEMBL351231 | — | Ki | = | 1.23 | nM | 8.91 |
| CHEMBL196868 | — | Ki | = | 1.35 | nM | 8.87 |
| CHEMBL198625 | — | Ki | = | 1.42 | nM | 8.85 |
| CHEMBL194857 | — | Ki | = | 1.47 | nM | 8.83 |
| CHEMBL362952 | — | Ki | = | 1.58 | nM | 8.80 |
| CHEMBL366183 | — | Ki | = | 1.92 | nM | 8.72 |
| CHEMBL198703 | — | Ki | = | 2.01 | nM | 8.70 |
| CHEMBL198325 | — | Ki | = | 2.12 | nM | 8.67 |
| CHEMBL380557 | — | Ki | = | 2.36 | nM | 8.63 |
| CHEMBL197608 | — | Ki | = | 2.51 | nM | 8.60 |
| CHEMBL364222 | — | Ki | = | 2.51 | nM | 8.60 |
| CHEMBL199187 | — | Ki | = | 2.71 | nM | 8.57 |
| CHEMBL197890 | — | Ki | = | 2.76 | nM | 8.56 |
| CHEMBL196480 | — | Ki | = | 2.88 | nM | 8.54 |
| CHEMBL372546 | — | Ki | = | 3.27 | nM | 8.48 |
| CHEMBL193607 | — | Ki | = | 3.96 | nM | 8.40 |
| CHEMBL363645 | — | Ki | = | 4.02 | nM | 8.40 |
| CHEMBL425023 | — | Ki | = | 17.9 | nM | 7.75 |