Assay Detail
Binding
CHEMBL5392875
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Displacement of [3H]UR-MN259 from SP-FLAG tagged human histamine H3 receptor expressed in HEK293T cells assessed as inhibition constant incubated for 60 min by scintillation counter analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Tritiated Radioligand with High Affinity and Selectivity for the Histamine H<sub>3</sub> Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.08 | 9.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129542 | JNJ-5207852 | — | 1 | 9.98 |
| CHEMBL5430091 | — | — | 1 | 9.55 |
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 8.84 |
| CHEMBL462605 | PITOLISANT | 4.0 | 1 | 8.81 |
| CHEMBL19439 | IMETIT | — | 1 | 8.24 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 7.38 |
| CHEMBL11919 | — | — | 1 | 7.12 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 6.41 |
| CHEMBL268229 | — | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129542 | JNJ-5207852 | Ki | = | 0.1047 | nM | 9.98 |
| CHEMBL5430091 | — | Ki | = | 0.2818 | nM | 9.55 |
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 1.445 | nM | 8.84 |
| CHEMBL462605 | PITOLISANT | Ki | = | 1.549 | nM | 8.81 |
| CHEMBL19439 | IMETIT | Ki | = | 5.754 | nM | 8.24 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 41.69 | nM | 7.38 |
| CHEMBL11919 | — | Ki | = | 75.86 | nM | 7.12 |
| CHEMBL90 | HISTAMINE | Ki | = | 389.05 | nM | 6.41 |
| CHEMBL268229 | — | Ki | = | 426.58 | nM | 6.37 |