Assay Detail
Binding
CHEMBL854129
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Displacement of N-[3H]methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SK-N-MC |
| 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 | 11 | 7.90 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129542 | JNJ-5207852 | — | 1 | 9.40 |
| CHEMBL204872 | — | — | 1 | 9.30 |
| CHEMBL381717 | — | — | 1 | 8.52 |
| CHEMBL204377 | — | — | 1 | 8.22 |
| CHEMBL201861 | — | — | 1 | 8.10 |
| CHEMBL382429 | — | — | 1 | 7.85 |
| CHEMBL203670 | — | — | 1 | 7.75 |
| CHEMBL380697 | APLYSAMINE | — | 1 | 7.52 |
| CHEMBL204113 | — | — | 1 | 7.44 |
| CHEMBL203901 | — | — | 1 | 7.40 |
| CHEMBL70313 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129542 | JNJ-5207852 | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL204872 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL381717 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL204377 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL201861 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL382429 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL203670 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL380697 | APLYSAMINE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL204113 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL203901 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL70313 | — | Ki | = | 4000.0 | nM | 5.40 |