Assay Detail
Binding
CHEMBL889157
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Binding affinity to human histamine H3 receptor
16
Total Activities
15
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
A new class of histamine H3 receptor antagonists derived from ligand based design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.59 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL425994 | — | — | 1 | 9.52 |
| CHEMBL27979 | A-349,821 | — | 1 | 9.31 |
| CHEMBL129542 | JNJ-5207852 | — | 2 | 9.24 |
| CHEMBL351231 | — | — | 1 | 8.62 |
| CHEMBL230939 | — | — | 1 | 8.62 |
| CHEMBL230089 | — | — | 1 | 7.92 |
| CHEMBL231042 | — | — | 1 | 7.75 |
| CHEMBL396196 | — | — | 1 | 7.33 |
| CHEMBL231145 | — | — | 1 | 7.06 |
| CHEMBL231146 | — | — | 1 | 6.87 |
| CHEMBL231144 | — | — | 1 | 6.82 |
| CHEMBL397959 | — | — | 1 | 5.99 |
| CHEMBL230087 | — | — | 1 | 5.96 |
| CHEMBL396197 | — | — | 1 | 5.86 |
| CHEMBL230088 | — | — | 1 | 5.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL425994 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL27979 | A-349,821 | Ki | = | 0.4898 | nM | 9.31 |
| CHEMBL129542 | JNJ-5207852 | Ki | = | 0.5754 | nM | 9.24 |
| CHEMBL129542 | JNJ-5207852 | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL351231 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL230939 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL230089 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL231042 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL396196 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL231145 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL231146 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL231144 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL397959 | — | Ki | = | 1021.0 | nM | 5.99 |
| CHEMBL230087 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL396197 | — | Ki | = | 1393.0 | nM | 5.86 |
| CHEMBL230088 | — | Ki | = | 1810.0 | nM | 5.74 |