Assay Detail
Binding
CHEMBL890061
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Binding affinity to human histamine H3 receptor
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 7.39 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL427845 | — | — | 1 | 8.77 |
| CHEMBL394861 | — | — | 1 | 8.70 |
| CHEMBL233054 | — | — | 1 | 8.70 |
| CHEMBL242820 | — | — | 1 | 8.48 |
| CHEMBL233053 | — | — | 1 | 8.42 |
| CHEMBL234526 | — | — | 1 | 8.40 |
| CHEMBL394801 | — | — | 1 | 8.13 |
| CHEMBL232661 | — | — | 1 | 8.13 |
| CHEMBL395096 | — | — | 1 | 8.06 |
| CHEMBL233471 | — | — | 1 | 8.02 |
| CHEMBL234732 | — | — | 1 | 8.02 |
| CHEMBL394787 | — | — | 1 | 8.01 |
| CHEMBL394800 | — | — | 1 | 7.96 |
| CHEMBL396459 | — | — | 1 | 7.92 |
| CHEMBL233470 | — | — | 1 | 7.85 |
| CHEMBL245130 | — | — | 1 | 7.52 |
| CHEMBL232660 | — | — | 1 | 7.42 |
| CHEMBL233681 | — | — | 1 | 7.40 |
| CHEMBL396945 | — | — | 1 | 7.33 |
| CHEMBL396703 | — | — | 1 | 7.16 |
| CHEMBL234525 | — | — | 1 | 6.97 |
| CHEMBL395022 | — | — | 1 | 6.84 |
| CHEMBL232620 | — | — | 1 | 6.57 |
| CHEMBL396981 | — | — | 1 | 6.57 |
| CHEMBL232621 | — | — | 1 | 6.29 |
| CHEMBL242817 | — | — | 1 | 5.96 |
| CHEMBL232010 | — | — | 1 | 5.84 |
| CHEMBL232218 | — | — | 1 | 5.58 |
| CHEMBL429440 | — | — | 1 | 5.55 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL427845 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL394861 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL233054 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL242820 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL233053 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL234526 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL394801 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL232661 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL395096 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL233471 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL234732 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL394787 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL394800 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL396459 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL233470 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL245130 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL232660 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL233681 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL396945 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL396703 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL234525 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL395022 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL232620 | — | Ki | = | 267.0 | nM | 6.57 |
| CHEMBL396981 | — | Ki | = | 268.0 | nM | 6.57 |
| CHEMBL232621 | — | Ki | = | 509.0 | nM | 6.29 |
| CHEMBL242817 | — | Ki | = | 1108.0 | nM | 5.96 |
| CHEMBL232010 | — | Ki | = | 1440.0 | nM | 5.84 |
| CHEMBL232218 | — | Ki | = | 2606.0 | nM | 5.58 |
| CHEMBL429440 | — | Ki | = | 2840.0 | nM | 5.55 |
| CHEMBL41 | FLUOXETINE | Ki | = | 7300.0 | nM | 5.14 |