Assay Detail
Binding
CHEMBL975272
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Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in HEL293 cells
17
Total Activities
17
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
Fluorinated non-imidazole histamine H3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 9.08 | 10.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL470609 | — | — | 1 | 10.17 |
| CHEMBL513193 | — | — | 1 | 10.03 |
| CHEMBL472466 | — | — | 1 | 9.70 |
| CHEMBL470601 | — | — | 1 | 9.62 |
| CHEMBL513729 | — | — | 1 | 9.59 |
| CHEMBL471437 | — | — | 1 | 9.55 |
| CHEMBL470599 | — | — | 1 | 9.55 |
| CHEMBL452877 | — | — | 1 | 9.51 |
| CHEMBL129542 | JNJ-5207852 | — | 1 | 9.24 |
| CHEMBL470610 | — | — | 1 | 9.08 |
| CHEMBL470600 | — | — | 1 | 9.00 |
| CHEMBL462605 | PITOLISANT | 4.0 | 1 | 8.57 |
| CHEMBL193978 | — | — | 1 | 8.55 |
| CHEMBL129257 | — | — | 1 | 7.96 |
| CHEMBL469388 | — | — | 1 | 7.76 |
| CHEMBL449484 | — | — | 1 | 7.37 |
| CHEMBL471877 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL470609 | — | Ki | = | 0.068 | nM | 10.17 |
| CHEMBL513193 | — | Ki | = | 0.094 | nM | 10.03 |
| CHEMBL472466 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL470601 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL513729 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL471437 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL470599 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL452877 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL129542 | JNJ-5207852 | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL470610 | — | Ki | = | 0.84 | nM | 9.08 |
| CHEMBL470600 | — | Ki | = | 0.99 | nM | 9.00 |
| CHEMBL462605 | PITOLISANT | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL193978 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL129257 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL469388 | — | Ki | = | 17.3 | nM | 7.76 |
| CHEMBL449484 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL471877 | — | Ki | > | 1000.0 | nM | - |