Compound Detail
CHEMBL278462
CIPRALISANT 🧪 Phase II
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🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL278462 |
| Name | CIPRALISANT |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | CVKJAXCQPFOAIN-VXGBXAGGSA-N |
2
Targets
7
Activities
1
Assay Types
0
PK Parameters
6
Publications
3
Known Names
Molecular Properties
216.3
MW (Da)
3.34
ALogP
1
HBA
1
HBD
28.7
PSA (Ų)
0.75
QED
0
Ro5 Violations
2
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Activity Summary
Ki 7 meas. best 9.92
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Histamine H3 receptor CHEMBL4124 | Ki | 9.92 | 9.838 | 0.1 | 5 |
| Histamine H3 receptor CHEMBL264 | Ki | 8.67 | 8.535 | 2.1 | 2 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Histamine H3 receptor | Ki | = | 0.12 | nM | 9.92 | Binding affinity at histamine H3 receptor in rat cortical membranes by [3H]Nalph... | 10072687 |
| Histamine H3 receptor | Ki | = | 0.12 | nM | 9.92 | In vitro inhibitory activity against Histamine H3 receptor for K+ evoked depolar... | 11055360 |
| Histamine H3 receptor | Ki | = | 0.1259 | nM | 9.9 | Binding affinity of compound against Histamine H3 receptor | 10197963 |
| Histamine H3 receptor | Ki | = | 0.18 | nM | 9.74 | Binding affinity to rat cortical histamine H3 receptor | 21062081 |
| Histamine H3 receptor | Ki | = | 0.195 | nM | 9.71 | Binding affinity towards rat cortical H3 receptor | 12657274 |
| Histamine H3 receptor | Ki | = | 2.138 | nM | 8.67 | Binding affinity for human recombinant H3 receptor | 12657274 |
| Histamine H3 receptor | Ki | = | 3.981 | nM | 8.4 | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor exp... | 18433114 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 12657274 | 10.1016/s0960-894x(03)00118-5 | Histamine H3 receptor | 2 |
| 11055360 | 10.1016/s0960-894x(00)00473-x | Histamine H3 receptor | 2 |
| 10197963 | 10.1021/jm980408v | Histamine H3 receptor | 2 |
| 10072687 | 10.1021/jm980310g | Histamine H3 receptor | 1 |
| 18433114 | 10.1021/jm7014149 | Histamine H3 receptor | 1 |
| 21062081 | 10.1021/jm100064d | Histamine H3 receptor | 1 |
Data from ChEMBL 36 via Core Engine