Assay Detail
Binding
CHEMBL838519
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In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | C6 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 8.95 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL368398 | — | — | 1 | 10.10 |
| CHEMBL359462 | — | — | 1 | 9.64 |
| CHEMBL178853 | — | — | 1 | 9.39 |
| CHEMBL14638 | CIPROXIFAN | — | 1 | 9.29 |
| CHEMBL362662 | — | — | 1 | 9.28 |
| CHEMBL178682 | — | — | 1 | 9.27 |
| CHEMBL179539 | — | — | 1 | 9.24 |
| CHEMBL179263 | — | — | 1 | 9.19 |
| CHEMBL361355 | — | — | 1 | 9.15 |
| CHEMBL369502 | — | — | 1 | 9.14 |
| CHEMBL362607 | — | — | 1 | 9.11 |
| CHEMBL361801 | — | — | 1 | 9.04 |
| CHEMBL555146 | — | — | 1 | 9.00 |
| CHEMBL179472 | — | — | 1 | 9.00 |
| CHEMBL179372 | — | — | 1 | 8.98 |
| CHEMBL178950 | — | — | 1 | 8.87 |
| CHEMBL351231 | — | — | 1 | 8.87 |
| CHEMBL179015 | — | — | 1 | 8.85 |
| CHEMBL179702 | — | — | 1 | 8.78 |
| CHEMBL368699 | — | — | 1 | 8.76 |
| CHEMBL426603 | — | — | 1 | 8.71 |
| CHEMBL360885 | — | — | 1 | 8.69 |
| CHEMBL302196 | — | — | 1 | 8.60 |
| CHEMBL180368 | — | — | 1 | 8.59 |
| CHEMBL178410 | — | — | 1 | 8.57 |
| CHEMBL180125 | — | — | 1 | 8.48 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.44 |
| CHEMBL178191 | — | — | 1 | 8.34 |
| CHEMBL178192 | — | — | 1 | 8.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL368398 | — | Ki | = | 0.07943 | nM | 10.10 |
| CHEMBL359462 | — | Ki | = | 0.2291 | nM | 9.64 |
| CHEMBL178853 | — | Ki | = | 0.4074 | nM | 9.39 |
| CHEMBL14638 | CIPROXIFAN | Ki | = | 0.5129 | nM | 9.29 |
| CHEMBL362662 | — | Ki | = | 0.5248 | nM | 9.28 |
| CHEMBL178682 | — | Ki | = | 0.537 | nM | 9.27 |
| CHEMBL179539 | — | Ki | = | 0.5754 | nM | 9.24 |
| CHEMBL179263 | — | Ki | = | 0.6457 | nM | 9.19 |
| CHEMBL361355 | — | Ki | = | 0.7079 | nM | 9.15 |
| CHEMBL369502 | — | Ki | = | 0.7244 | nM | 9.14 |
| CHEMBL362607 | — | Ki | = | 0.7762 | nM | 9.11 |
| CHEMBL361801 | — | Ki | = | 0.912 | nM | 9.04 |
| CHEMBL555146 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL179472 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL179372 | — | Ki | = | 1.047 | nM | 8.98 |
| CHEMBL178950 | — | Ki | = | 1.349 | nM | 8.87 |
| CHEMBL351231 | — | Ki | = | 1.349 | nM | 8.87 |
| CHEMBL179015 | — | Ki | = | 1.413 | nM | 8.85 |
| CHEMBL179702 | — | Ki | = | 1.66 | nM | 8.78 |
| CHEMBL368699 | — | Ki | = | 1.738 | nM | 8.76 |
| CHEMBL426603 | — | Ki | = | 1.95 | nM | 8.71 |
| CHEMBL360885 | — | Ki | = | 2.042 | nM | 8.69 |
| CHEMBL302196 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL180368 | — | Ki | = | 2.57 | nM | 8.59 |
| CHEMBL178410 | — | Ki | = | 2.692 | nM | 8.57 |
| CHEMBL180125 | — | Ki | = | 3.311 | nM | 8.48 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 3.631 | nM | 8.44 |
| CHEMBL178191 | — | Ki | = | 4.571 | nM | 8.34 |
| CHEMBL178192 | — | Ki | = | 5.754 | nM | 8.24 |