Assay Detail
Binding
CHEMBL1827031
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Displacement of [125I]Iodoproxyfan from recombinant human histamine H3 receptor expressed in HEK293 cells after 60 mins
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel and highly potent histamine H3 receptor ligands. Part 2: exploring the cyclohexylamine-based series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 9.28 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1824245 | — | — | 1 | 9.77 |
| CHEMBL1824231 | — | — | 1 | 9.68 |
| CHEMBL1824233 | — | — | 1 | 9.60 |
| CHEMBL1824235 | — | — | 1 | 9.60 |
| CHEMBL1824247 | — | — | 1 | 9.59 |
| CHEMBL1824246 | — | — | 1 | 9.54 |
| CHEMBL1824230 | — | — | 1 | 9.52 |
| CHEMBL1824239 | — | — | 1 | 9.49 |
| CHEMBL1824234 | — | — | 1 | 9.48 |
| CHEMBL1824232 | — | — | 1 | 9.47 |
| CHEMBL1824241 | — | — | 1 | 9.39 |
| CHEMBL1824244 | — | — | 1 | 9.39 |
| CHEMBL1824248 | — | — | 1 | 9.28 |
| CHEMBL1824237 | — | — | 1 | 9.25 |
| CHEMBL1824243 | — | — | 1 | 9.24 |
| CHEMBL1824236 | — | — | 1 | 9.19 |
| CHEMBL1824249 | — | — | 1 | 9.19 |
| CHEMBL1824240 | — | — | 1 | 9.17 |
| CHEMBL1824242 | — | — | 1 | 9.04 |
| CHEMBL1824238 | — | — | 1 | 9.04 |
| CHEMBL1824229 | — | — | 1 | 8.77 |
| CHEMBL1824250 | — | — | 1 | 8.49 |
| CHEMBL1824251 | — | — | 1 | 8.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1824245 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL1824231 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL1824233 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL1824235 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL1824247 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL1824246 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL1824230 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL1824239 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL1824234 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL1824232 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL1824241 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL1824244 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL1824248 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL1824237 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL1824243 | — | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL1824236 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL1824249 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL1824240 | — | Ki | = | 0.67 | nM | 9.17 |
| CHEMBL1824242 | — | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL1824238 | — | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL1824229 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL1824250 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL1824251 | — | Ki | = | 5.5 | nM | 8.26 |