Assay Detail
Binding
CHEMBL4734937
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human H3R
9
Total Activities
9
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
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 | 9 | 8.55 | 9.56 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129542 | JNJ-5207852 | — | 1 | 9.56 |
| CHEMBL462605 | PITOLISANT | 4.0 | 1 | 9.52 |
| CHEMBL97170 | — | — | 1 | 8.92 |
| CHEMBL498228 | — | — | 1 | 8.70 |
| CHEMBL319000 | — | — | 1 | 8.70 |
| CHEMBL4759150 | — | — | 1 | 8.51 |
| CHEMBL4796748 | — | — | 1 | 8.40 |
| CHEMBL4162433 | — | — | 1 | 7.42 |
| CHEMBL14638 | CIPROXIFAN | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129542 | JNJ-5207852 | Ki | = | 0.2754 | nM | 9.56 |
| CHEMBL462605 | PITOLISANT | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL97170 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL498228 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL319000 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL4759150 | — | Ki | = | 3.12 | nM | 8.51 |
| CHEMBL4796748 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL4162433 | — | Ki | = | 37.8 | nM | 7.42 |
| CHEMBL14638 | CIPROXIFAN | Ki | = | 63.0 | nM | 7.20 |