Assay Detail
Binding
CHEMBL5053857
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Binding affinity in Nluc-hH3R assessed in HEK293 cells by NanoBRET binding assay
10
Total Activities
10
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
A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H<sub>3</sub> Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.05 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129542 | JNJ-5207852 | — | 1 | 10.22 |
| CHEMBL5081713 | — | — | 1 | 9.80 |
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 9.30 |
| CHEMBL462605 | PITOLISANT | 4.0 | 1 | 9.04 |
| CHEMBL19439 | IMETIT | — | 1 | 7.90 |
| CHEMBL1433079 | — | — | 1 | 7.71 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 7.28 |
| CHEMBL268229 | — | — | 1 | 7.20 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 6.23 |
| CHEMBL11919 | — | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129542 | JNJ-5207852 | Ki | = | 0.06026 | nM | 10.22 |
| CHEMBL5081713 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL462605 | PITOLISANT | Ki | = | 0.912 | nM | 9.04 |
| CHEMBL19439 | IMETIT | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL1433079 | — | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 52.48 | nM | 7.28 |
| CHEMBL268229 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL90 | HISTAMINE | Ki | = | 588.84 | nM | 6.23 |
| CHEMBL11919 | — | Ki | = | 1621.81 | nM | 5.79 |