Assay Detail
Binding
CHEMBL4734922
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Displacement of [3H]UR-PI294 from human SP-FLAG-tagged H3R expressed in HEK293T cells measured after 60 to 120 mins by liquid scintillation counting analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structural modifications in the distal, regulatory region of histamine H receptor antagonists leading to the identification of a potent anti-obesity agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.66 | 8.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4783744 | — | — | 1 | 8.50 |
| CHEMBL4741145 | — | — | 1 | 8.23 |
| CHEMBL4776141 | — | — | 1 | 8.11 |
| CHEMBL4743583 | — | — | 1 | 8.11 |
| CHEMBL4758080 | — | — | 1 | 8.07 |
| CHEMBL4786308 | — | — | 1 | 7.75 |
| CHEMBL4800672 | — | — | 1 | 7.69 |
| CHEMBL4750996 | — | — | 1 | 7.64 |
| CHEMBL14638 | CIPROXIFAN | — | 1 | 7.31 |
| CHEMBL4781093 | — | — | 1 | 7.22 |
| CHEMBL4744110 | — | — | 1 | 7.17 |
| CHEMBL4740135 | — | — | 1 | 6.96 |
| CHEMBL4783066 | — | — | 1 | 6.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4783744 | — | Ki | = | 3.17 | nM | 8.50 |
| CHEMBL4741145 | — | Ki | = | 5.84 | nM | 8.23 |
| CHEMBL4776141 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL4743583 | — | Ki | = | 7.86 | nM | 8.11 |
| CHEMBL4758080 | — | Ki | = | 8.43 | nM | 8.07 |
| CHEMBL4786308 | — | Ki | = | 17.63 | nM | 7.75 |
| CHEMBL4800672 | — | Ki | = | 20.28 | nM | 7.69 |
| CHEMBL4750996 | — | Ki | = | 22.98 | nM | 7.64 |
| CHEMBL14638 | CIPROXIFAN | Ki | = | 48.9 | nM | 7.31 |
| CHEMBL4781093 | — | Ki | = | 60.67 | nM | 7.22 |
| CHEMBL4744110 | — | Ki | = | 67.19 | nM | 7.17 |
| CHEMBL4740135 | — | Ki | = | 109.06 | nM | 6.96 |
| CHEMBL4783066 | — | Ki | = | 139.74 | nM | 6.86 |