Assay Detail
Binding
CHEMBL1099708
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Displacement of [125I]Iodoproxyfan from human histamine H3 receptor expressed in HEK293 cells after 60 mins by scintillation counting
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Acidic elements in histamine H(3) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.40 | 9.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL459350 | — | — | 1 | 9.50 |
| CHEMBL129542 | JNJ-5207852 | — | 1 | 9.20 |
| CHEMBL1076567 | — | — | 1 | 8.70 |
| CHEMBL1202099 | — | — | 1 | 8.40 |
| CHEMBL1081073 | — | — | 1 | 8.30 |
| CHEMBL1082147 | — | — | 1 | 8.10 |
| CHEMBL1080906 | — | — | 1 | 8.10 |
| CHEMBL1082149 | — | — | 1 | 8.00 |
| CHEMBL1076599 | — | — | 1 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL459350 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL129542 | JNJ-5207852 | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL1076567 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL1202099 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL1081073 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL1082147 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL1080906 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL1082149 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1076599 | — | Ki | = | 50.12 | nM | 7.30 |