Assay Detail
Binding
CHEMBL838520
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In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 9.12 | 10.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL178853 | — | — | 1 | 10.08 |
| CHEMBL178682 | — | — | 1 | 10.07 |
| CHEMBL179539 | — | — | 1 | 10.00 |
| CHEMBL179263 | — | — | 1 | 9.71 |
| CHEMBL178192 | — | — | 1 | 9.69 |
| CHEMBL369502 | — | — | 1 | 9.69 |
| CHEMBL368699 | — | — | 1 | 9.67 |
| CHEMBL362662 | — | — | 1 | 9.66 |
| CHEMBL179472 | — | — | 1 | 9.64 |
| CHEMBL360885 | — | — | 1 | 9.61 |
| CHEMBL178950 | — | — | 1 | 9.58 |
| CHEMBL555146 | — | — | 1 | 9.57 |
| CHEMBL361801 | — | — | 1 | 9.57 |
| CHEMBL179372 | — | — | 1 | 9.45 |
| CHEMBL179702 | — | — | 1 | 9.39 |
| CHEMBL179015 | — | — | 1 | 9.36 |
| CHEMBL351231 | — | — | 1 | 9.35 |
| CHEMBL359462 | — | — | 1 | 9.31 |
| CHEMBL426603 | — | — | 1 | 9.29 |
| CHEMBL178410 | — | — | 1 | 9.28 |
| CHEMBL178191 | — | — | 1 | 9.28 |
| CHEMBL180368 | — | — | 1 | 9.16 |
| CHEMBL180125 | — | — | 1 | 9.06 |
| CHEMBL362607 | — | — | 1 | 8.75 |
| CHEMBL368398 | — | — | 1 | 8.67 |
| CHEMBL14638 | CIPROXIFAN | — | 1 | 7.20 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 7.14 |
| CHEMBL361355 | — | — | 1 | 7.03 |
| CHEMBL302196 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL178853 | — | Ki | = | 0.08318 | nM | 10.08 |
| CHEMBL178682 | — | Ki | = | 0.08511 | nM | 10.07 |
| CHEMBL179539 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL179263 | — | Ki | = | 0.195 | nM | 9.71 |
| CHEMBL178192 | — | Ki | = | 0.2042 | nM | 9.69 |
| CHEMBL369502 | — | Ki | = | 0.2042 | nM | 9.69 |
| CHEMBL368699 | — | Ki | = | 0.2138 | nM | 9.67 |
| CHEMBL362662 | — | Ki | = | 0.2188 | nM | 9.66 |
| CHEMBL179472 | — | Ki | = | 0.2291 | nM | 9.64 |
| CHEMBL360885 | — | Ki | = | 0.2455 | nM | 9.61 |
| CHEMBL178950 | — | Ki | = | 0.263 | nM | 9.58 |
| CHEMBL555146 | — | Ki | = | 0.2692 | nM | 9.57 |
| CHEMBL361801 | — | Ki | = | 0.2692 | nM | 9.57 |
| CHEMBL179372 | — | Ki | = | 0.3548 | nM | 9.45 |
| CHEMBL179702 | — | Ki | = | 0.4074 | nM | 9.39 |
| CHEMBL179015 | — | Ki | = | 0.4365 | nM | 9.36 |
| CHEMBL351231 | — | Ki | = | 0.4467 | nM | 9.35 |
| CHEMBL359462 | — | Ki | = | 0.4898 | nM | 9.31 |
| CHEMBL426603 | — | Ki | = | 0.5129 | nM | 9.29 |
| CHEMBL178410 | — | Ki | = | 0.5248 | nM | 9.28 |
| CHEMBL178191 | — | Ki | = | 0.5248 | nM | 9.28 |
| CHEMBL180368 | — | Ki | = | 0.6918 | nM | 9.16 |
| CHEMBL180125 | — | Ki | = | 0.871 | nM | 9.06 |
| CHEMBL362607 | — | Ki | = | 1.778 | nM | 8.75 |
| CHEMBL368398 | — | Ki | = | 2.138 | nM | 8.67 |
| CHEMBL14638 | CIPROXIFAN | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL361355 | — | Ki | = | 93.33 | nM | 7.03 |
| CHEMBL302196 | — | Ki | = | 758.58 | nM | 6.12 |