Assay Detail
Binding
CHEMBL854130
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Displacement of N-[3H]methylhistamine from rat histamine H3 receptor in rat cortical hemispheres
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Aplysamine-1 and related analogs as histamine H3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.24 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129542 | JNJ-5207852 | — | 1 | 9.00 |
| CHEMBL204872 | — | — | 1 | 8.30 |
| CHEMBL381717 | — | — | 1 | 7.35 |
| CHEMBL382429 | — | — | 1 | 7.30 |
| CHEMBL201861 | — | — | 1 | 7.24 |
| CHEMBL204377 | — | — | 1 | 7.05 |
| CHEMBL380697 | APLYSAMINE | — | 1 | 6.60 |
| CHEMBL203670 | — | — | 1 | 6.59 |
| CHEMBL204113 | — | — | 1 | 6.50 |
| CHEMBL203901 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129542 | JNJ-5207852 | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL204872 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL381717 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL382429 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL201861 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL204377 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL380697 | APLYSAMINE | Ki | = | 249.0 | nM | 6.60 |
| CHEMBL203670 | — | Ki | = | 255.0 | nM | 6.59 |
| CHEMBL204113 | — | Ki | = | 319.0 | nM | 6.50 |
| CHEMBL203901 | — | Ki | = | 345.0 | nM | 6.46 |