Assay Detail
Binding
CHEMBL1008299
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Binding affinity to histamine H3 receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 8.93 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL517140 | GSK189254 | 2.0 | 1 | 9.92 |
| CHEMBL351231 | — | — | 1 | 9.40 |
| CHEMBL129542 | JNJ-5207852 | — | 1 | 9.22 |
| CHEMBL498228 | — | — | 1 | 8.70 |
| CHEMBL27979 | A-349,821 | — | 1 | 8.70 |
| CHEMBL319000 | — | — | 1 | 8.40 |
| CHEMBL218790 | — | — | 1 | 8.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL517140 | GSK189254 | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL351231 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL129542 | JNJ-5207852 | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL498228 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL27979 | A-349,821 | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL319000 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL218790 | — | Ki | = | 7.0 | nM | 8.15 |