Compound Detail
CHEMBL1909072
PIPAMAZINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL1909072 |
| Name | PIPAMAZINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | OSJJYEUEJRVVOD-UHFFFAOYSA-N |
22
Targets
49
Activities
2
Assay Types
0
PK Parameters
4
Publications
2
Known Names
1
Mechanisms
Molecular Properties
402.0
MW (Da)
4.53
ALogP
4
HBA
1
HBD
49.6
PSA (Ų)
0.80
QED
0
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Availability | Withdrawn |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Unknown | - | - | ✓ | ✓ |
Drug Warnings
Withdrawn
hepatotoxicity
associated with hepatic lesions
Withdrawn
hepatotoxicity
associated with hepatic lesions
Withdrawn
hepatotoxicity
associated with hepatic lesions
Activity Summary
IC50 25 meas. best 8.76
Ki 24 meas. best 9.26
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2A CHEMBL224 | Ki | 9.26 | 9.26 | 0.6 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | Ki | 9.11 | 9.11 | 0.8 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | Ki | 9.02 | 9.02 | 1.0 | 1 |
| Histamine H1 receptor CHEMBL231 | Ki | 8.94 | 8.94 | 1.2 | 1 |
| D(2) dopamine receptor CHEMBL217 | Ki | 8.87 | 8.87 | 1.4 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | Ki | 8.85 | 8.85 | 1.4 | 1 |
| D(3) dopamine receptor CHEMBL234 | Ki | 8.8 | 8.8 | 1.6 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | IC50 | 8.76 | 8.76 | 1.7 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | IC50 | 8.71 | 8.71 | 1.9 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | IC50 | 8.71 | 8.71 | 1.9 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | Ki | 8.68 | 8.68 | 2.1 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | IC50 | 8.59 | 8.59 | 2.6 | 1 |
| D(2) dopamine receptor CHEMBL217 | IC50 | 8.39 | 8.39 | 4.0 | 1 |
| D(3) dopamine receptor CHEMBL234 | IC50 | 8.33 | 8.33 | 4.7 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | IC50 | 8.29 | 8.29 | 5.1 | 1 |
| Alpha-2C adrenergic receptor CHEMBL1916 | Ki | 8.19 | 8.19 | 6.5 | 1 |
| Histamine H1 receptor CHEMBL231 | IC50 | 8.0 | 8.0 | 9.9 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | Ki | 7.96 | 7.96 | 11.0 | 1 |
| D(1A) dopamine receptor CHEMBL2056 | Ki | 7.8 | 7.8 | 16.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | IC50 | 7.66 | 7.66 | 22.0 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | Ki | 7.6 | 7.6 | 25.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | Ki | 7.51 | 7.51 | 31.0 | 1 |
| D(1A) dopamine receptor CHEMBL2056 | IC50 | 7.5 | 7.5 | 32.0 | 1 |
| Alpha-2C adrenergic receptor CHEMBL1916 | IC50 | 7.35 | 7.35 | 45.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | Ki | 7.32 | 7.32 | 48.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | IC50 | 7.31 | 7.31 | 49.0 | 1 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | Ki | 7.28 | 7.28 | 52.0 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | IC50 | 7.18 | 7.18 | 66.0 | 1 |
| Cytochrome P450 2D6 CHEMBL289 | IC50 | 7.0 | 7.0 | 100.0 | 1 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | IC50 | 6.95 | 6.95 | 112.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | IC50 | 6.94 | 6.94 | 114.0 | 1 |
| Sodium-dependent serotonin transporter CHEMBL228 | Ki | 6.46 | 6.46 | 346.0 | 1 |
| Unchecked CHEMBL612545 | Ki | 6.43 | 6.0125 | 372.0 | 4 |
| Sodium-dependent noradrenaline transporter CHEMBL222 | IC50 | 6.35 | 6.35 | 450.0 | 1 |
| Sodium-dependent noradrenaline transporter CHEMBL222 | Ki | 6.35 | 6.35 | 446.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 6.22 | 5.905 | 604.0 | 4 |
| Sodium-dependent serotonin transporter CHEMBL228 | IC50 | 6.19 | 6.19 | 651.0 | 1 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | Ki | 5.99 | 5.99 | 1018.0 | 1 |
| 5-hydroxytryptamine receptor 1B CHEMBL3459 | Ki | 5.86 | 5.86 | 1367.0 | 1 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | IC50 | 5.75 | 5.75 | 1782.0 | 1 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | Ki | 5.65 | 5.65 | 2259.0 | 1 |
| 5-hydroxytryptamine receptor 1B CHEMBL3459 | IC50 | 5.52 | 5.52 | 3007.0 | 1 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | IC50 | 5.5 | 5.5 | 3144.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 26948801 | 10.1016/j.drudis.2016.02.015 | Homo sapiens | 2 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| 21624500 | 10.1016/j.drudis.2011.05.007 | Hepatotoxicity | 1 |
| 22194678 | 10.1371/journal.pcbi.1002310 | Hepatotoxicity | 1 |
Data from ChEMBL 36 via Core Engine