Molecule Details
| InChIKey | UEQUQVLFIPOEMF-UHFFFAOYSA-N |
|---|---|
| Compound Name | Mianserin |
| Canonical SMILES | CN1CCN2c3ccccc3Cc3ccccc3C2C1 |
| Clinical Status | Clinical Multi-Target |
| Targets (Human+Pathogen) | 21 |
| Pfam Stratification | Cross-Family |
| Avg pChEMBL | 7.14 |
| Source | ChEMBL;BindingDB;TTD_MultiTarget |
2D Structure
Activity Profile
DrugBank Annotations
| DrugBank ID | DB06148 |
|---|---|
| Drug Name | Mianserin |
| CAS Number | 24219-97-4 |
| Groups | approved withdrawn |
| ATC Codes | N06AX03 |
| Description | A tetracyclic compound with antidepressant effects. Mianserin was previously available internationally, however in most markets it has been phased out in favour of [mirtazapine]. |
Categories: Adrenergic Agents Agents that produce hypertension Antidepressive Agents Antidepressive Agents, Second-Generation Antidepressive Agents, Tetracyclic Central Nervous System Agents Central Nervous System Depressants Combined Inhibitors of Serotonin/Norepinephrine Reuptake Cytochrome P-450 CYP1A2 Substrates Cytochrome P-450 CYP2B6 Substrates Cytochrome P-450 CYP2D6 Substrates Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 Substrates Dibenzazepines Dopamine Antagonists Dopamine D2 Receptor Antagonists Heterocyclic Compounds, Fused-Ring Histamine Agents Histamine Antagonists Histamine H1 Antagonists Nervous System Neurotransmitter Agents Psychoanaleptics Psychotropic Drugs Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome Serotonin 5-HT2 Receptor Antagonists Serotonin 5-HT2A Receptor Antagonists Serotonin 5-HT2C Receptor Antagonists Serotonin Agents Serotonin Modulators Serotonin Receptor Antagonists
Cross-references: BindingDB: 50222218 ChEBI: 51137 CHEMBL6437 ChemSpider: 4040 Guide to Pharmacology: 135 IUPHAR: 135 PharmGKB: PA134687937 PubChem:4184 PubChem:46508096 RxCUI: 6929 Therapeutic Targets Database: DAP000293 Wikipedia: Mianserin
Target Activities (21)
| Target | Gene | Organism | Category | Pfam | pChEMBL | Type | Source |
|---|---|---|---|---|---|---|---|
| P35367 | HRH1 | Homo sapiens | Human | PF00001 | 8.8 | IC50 | ChEMBL;BindingDB |
| P28223 | HTR2A | Homo sapiens | Human | PF00001 | 8.5 | Ki | ChEMBL;BindingDB |
| P28335 | HTR2C | Homo sapiens | Human | PF00001 | 8.4 | Ki | ChEMBL;BindingDB |
| P41595 | HTR2B | Homo sapiens | Human | PF00001 | 8.1 | Ki | ChEMBL;BindingDB |
| P08913 | ADRA2A | Homo sapiens | Human | PF00001 | 7.7 | IC50 | ChEMBL;BindingDB |
| P18089 | ADRA2B | Homo sapiens | Human | PF00001 | 7.5 | IC50 | ChEMBL |
| P35348 | ADRA1A | Homo sapiens | Human | PF00001 | 7.4 | pIC50 | TTD_MultiTarget |
| P18825 | ADRA2C | Homo sapiens | Human | PF00001 | 7.4 | IC50 | ChEMBL;BindingDB |
| P50406 | HTR6 | Homo sapiens | Human | PF00001 | 7.3 | Ki | ChEMBL;BindingDB |
| P25100 | ADRA1D | Homo sapiens | Human | PF00001 | 7.2 | IC50 | ChEMBL |
| P34969 | HTR7 | Homo sapiens | Human | PF00001 | 7.2 | Ki | ChEMBL;BindingDB |
| P23975 | SLC6A2 | Homo sapiens | Human | PF00209 | 6.8 | IC50 | ChEMBL |
| P08912 | CHRM5 | Homo sapiens | Human | PF00001 | 6.6 | IC50 | ChEMBL |
| P08173 | CHRM4 | Homo sapiens | Human | PF00001 | 6.5 | Ki | ChEMBL |
| P20309 | CHRM3 | Homo sapiens | Human | PF00001 | 6.5 | Ki | ChEMBL |
| P11229 | CHRM1 | Homo sapiens | Human | PF00001 | 6.5 | Ki | ChEMBL |
| P08172 | CHRM2 | Homo sapiens | Human | PF00001 | 6.4 | Ki | ChEMBL |
| P21728 | DRD1 | Homo sapiens | Human | PF00001 | 6.4 | IC50 | ChEMBL |
| P28221 | HTR1D | Homo sapiens | Human | PF00001 | 6.4 | IC50 | ChEMBL;BindingDB |
| P08908 | HTR1A | Homo sapiens | Human | PF00001 | 6.4 | IC50 | ChEMBL;BindingDB |
| P25021 | HRH2 | Homo sapiens | Human | PF00001 | 6.0 | IC50 | ChEMBL |
DrugBank Target Actions (24)
| Target | Gene | Target Name | Action | Type |
|---|---|---|---|---|
| P05177 | CYP1A2 | Cytochrome P450 1A2 | substrate | enzymes |
| P08684 | CYP3A4 | Cytochrome P450 3A4 | substrate | enzymes |
| P10635 | CYP2D6 | Cytochrome P450 2D6 | substrate | enzymes |
| P20813 | CYP2B6 | Cytochrome P450 2B6 | substrate | enzymes |
| P41145 | OPRK1 | Kappa-type opioid receptor | agonist | targets |
| P08913 | ADRA2A | Alpha-2A adrenergic receptor | antagonist | targets |
| P14416 | DRD2 | D(2) dopamine receptor | antagonist | targets |
| P18089 | ADRA2B | Alpha-2B adrenergic receptor | antagonist | targets |
| P18825 | ADRA2C | Alpha-2C adrenergic receptor | antagonist | targets |
| P28223 | HTR2A | 5-hydroxytryptamine receptor 2A | antagonist | targets |
| P28335 | HTR2C | 5-hydroxytryptamine receptor 2C | antagonist | targets |
| P34969 | HTR7 | 5-hydroxytryptamine receptor 7 | antagonist | targets |
| P35348 | ADRA1A | Alpha-1 adrenergic receptors | antagonist | targets |
| P35367 | HRH1 | Histamine H1 receptor | antagonist | targets |
| P21728 | DRD1 | D(1) dopamine receptor | binder | targets |
| P30939 | HTR1F | 5-hydroxytryptamine receptor 1F | binder | targets |
| P35462 | DRD3 | D(3) dopamine receptor | binder | targets |
| P41595 | HTR2B | 5-hydroxytryptamine receptor 2B | binder | targets |
| P50406 | HTR6 | 5-hydroxytryptamine receptor 6 | binder | targets |
| Q01959 | SLC6A3 | Sodium-dependent dopamine transporter | binder | targets |
| Q9H3N8 | HRH4 | Histamine H4 receptor | binder | targets |
| P08908 | HTR1A | 5-hydroxytryptamine receptor 1A | blocker | targets |
| P23975 | SLC6A2 | Sodium-dependent noradrenaline transporter | inhibitor | targets |
| P31645 | SLC6A4 | Sodium-dependent serotonin transporter | inhibitor | targets |