Assay Detail
Binding
CHEMBL3755089
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Displacement of [3H]R-alpha-methyl histamine from recombinant human H3 receptor
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Benzamide derivatives and their constrained analogs as histamine H3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 8.07 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3753475 | — | — | 1 | 9.10 |
| CHEMBL3753703 | — | — | 1 | 9.00 |
| CHEMBL3753315 | — | — | 1 | 8.92 |
| CHEMBL3753814 | — | — | 1 | 8.80 |
| CHEMBL3754200 | — | — | 1 | 8.74 |
| CHEMBL3753901 | — | — | 1 | 8.68 |
| CHEMBL3754209 | — | — | 1 | 8.60 |
| CHEMBL3753170 | — | — | 1 | 8.24 |
| CHEMBL3753093 | — | — | 1 | 8.24 |
| CHEMBL3753147 | — | — | 1 | 8.17 |
| CHEMBL3751915 | — | — | 1 | 8.15 |
| CHEMBL3753304 | — | — | 1 | 8.14 |
| CHEMBL3752081 | — | — | 1 | 8.08 |
| CHEMBL3752655 | — | — | 1 | 8.07 |
| CHEMBL3753764 | — | — | 1 | 8.04 |
| CHEMBL3753102 | — | — | 1 | 7.98 |
| CHEMBL3752705 | — | — | 1 | 7.94 |
| CHEMBL3752796 | — | — | 1 | 7.74 |
| CHEMBL3754205 | — | — | 1 | 7.57 |
| CHEMBL3752696 | — | — | 1 | 6.99 |
| CHEMBL3754674 | — | — | 1 | 6.42 |
| CHEMBL3754726 | — | — | 1 | 5.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3753475 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3753703 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3753315 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3753814 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL3754200 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL3753901 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3754209 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL3753170 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL3753093 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL3753147 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL3751915 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL3753304 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL3752081 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL3752655 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL3753764 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL3753102 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL3752705 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL3752796 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL3754205 | — | Ki | = | 26.9 | nM | 7.57 |
| CHEMBL3752696 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL3754674 | — | Ki | = | 384.3 | nM | 6.42 |
| CHEMBL3754726 | — | Ki | = | 1357.0 | nM | 5.87 |