Compound Detail
CHEMBL6437
MIANSERIN 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL6437 |
| Name | MIANSERIN |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | UEQUQVLFIPOEMF-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
54
Targets
169
Activities
3
Assay Types
9
PK Parameters
20
Publications
5
Known Names
5
Indications
Molecular Properties
264.4
MW (Da)
3.08
ALogP
2
HBA
0
HBD
6.5
PSA (Ų)
0.72
QED
0
Ro5 Violations
0
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Availability | Withdrawn |
| Chirality | Racemic |
Indications
Depressive Disorder Depressive Disorder Anxiety Dementia Schizophrenia
ATC Classification
N06AX03
mianserin
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOANALEPTICS
Drug Warnings
Withdrawn
General Warning
adverse effects
Activity Summary
Ki 93 meas. best 9.76
IC50 65 meas. best 10.15
Kd 11 meas. best 7.72
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Alpha-1A adrenergic receptor CHEMBL319 | IC50 | 10.15 | 8.4 | 0.1 | 2 |
| Histamine H1 receptor CHEMBL231 | Ki | 9.76 | 9.265 | 0.2 | 2 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | Ki | 9.3 | 8.4292 | 0.5 | 13 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | Ki | 9.22 | 8.465 | 0.6 | 8 |
| Histamine H1 receptor CHEMBL3943 | Ki | 9.07 | 9.07 | 0.9 | 1 |
| Serotonin 2 (5-HT2) receptor CHEMBL2093870 | Ki | 8.96 | 8.525 | 1.1 | 4 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | IC50 | 8.94 | 8.535 | 1.2 | 2 |
| 5-hydroxytryptamine receptor 2C CHEMBL324 | Ki | 8.85 | 8.85 | 1.4 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL322 | Ki | 8.82 | 8.384 | 1.5 | 5 |
| Histamine H1 receptor CHEMBL231 | IC50 | 8.82 | 8.645 | 1.5 | 2 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | IC50 | 8.75 | 8.1367 | 1.8 | 3 |
| Rattus norvegicus CHEMBL376 | Ki | 8.52 | 8.195 | 3.0 | 2 |
| Alpha-2C adrenergic receptor CHEMBL1916 | Ki | 8.42 | 8.0 | 3.8 | 2 |
| Unchecked CHEMBL612545 | Ki | 8.38 | 7.0286 | 4.2 | 7 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | Ki | 8.33 | 8.19 | 4.6 | 2 |
| Alpha-2A adrenergic receptor CHEMBL1867 | Ki | 8.32 | 8.06 | 4.8 | 2 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | IC50 | 8.14 | 8.14 | 7.3 | 1 |
| Rattus norvegicus CHEMBL376 | IC50 | 7.93 | 6.1 | 11.8 | 4 |
| Unchecked CHEMBL612545 | IC50 | 7.85 | 6.484 | 14.0 | 5 |
| Alpha-2A adrenergic receptor CHEMBL4744 | Ki | 7.77 | 7.77 | 17.0 | 1 |
| Unchecked CHEMBL612545 | Kd | 7.72 | 7.545 | 19.0 | 2 |
| Alpha-2A adrenergic receptor CHEMBL1867 | IC50 | 7.68 | 7.525 | 20.9 | 2 |
| Norepinephrine transporter CHEMBL304 | IC50 | 7.66 | 7.66 | 22.0 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | Ki | 7.62 | 7.62 | 24.0 | 1 |
| Norepinephrine transporter CHEMBL304 | Ki | 7.58 | 7.3867 | 26.0 | 3 |
| Adrenergic receptor alpha-1 CHEMBL1907610 | Ki | 7.55 | 7.2267 | 28.0 | 3 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | Ki | 7.4 | 7.3467 | 40.0 | 3 |
| Alpha-1D adrenergic receptor CHEMBL223 | Ki | 7.39 | 7.39 | 41.0 | 1 |
| Alpha-1A adrenergic receptor CHEMBL4892 | Ki | 7.37 | 7.37 | 43.0 | 2 |
| Alpha-2C adrenergic receptor CHEMBL1916 | IC50 | 7.37 | 7.1633 | 42.7 | 3 |
| Alpha-2B adrenergic receptor CHEMBL1942 | IC50 | 7.28 | 7.28 | 52.0 | 1 |
| Adrenergic receptor alpha-2 CHEMBL2093864 | Kd | 7.27 | 6.7525 | 53.7 | 4 |
| 5-hydroxytryptamine receptor 7 CHEMBL3155 | Ki | 7.25 | 6.5167 | 56.0 | 3 |
| Adrenergic receptor alpha-1 CHEMBL1907610 | Kd | 7.24 | 6.63 | 57.5 | 3 |
| Adrenergic receptor alpha-2 CHEMBL2093864 | Ki | 7.21 | 7.165 | 62.0 | 2 |
| 5-hydroxytryptamine receptor 7 CHEMBL3223 | Ki | 7.2 | 7.1 | 63.1 | 2 |
| Alpha-1B adrenergic receptor CHEMBL315 | Ki | 7.18 | 7.18 | 66.0 | 1 |
| Serotonin 3 (5-HT3) receptor CHEMBL2094116 | Ki | 7.16 | 7.16 | 70.0 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | IC50 | 7.08 | 7.08 | 83.0 | 1 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | IC50 | 7.07 | 7.07 | 85.0 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | Ki | 7.04 | 7.04 | 91.0 | 1 |
| 5-hydroxytryptamine receptor 7 CHEMBL3155 | IC50 | 6.94 | 6.94 | 114.8 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | IC50 | 6.92 | 6.92 | 119.0 | 1 |
| Sodium-dependent noradrenaline transporter CHEMBL222 | Ki | 6.79 | 6.79 | 161.0 | 1 |
| Sodium-dependent noradrenaline transporter CHEMBL222 | IC50 | 6.79 | 6.79 | 163.0 | 1 |
| Adrenergic receptor alpha-2 CHEMBL2093864 | IC50 | 6.68 | 6.68 | 210.0 | 1 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | Ki | 6.64 | 6.64 | 230.0 | 1 |
| Serotonin 3 receptor (5HT3) CHEMBL2111333 | Ki | 6.6 | 6.6 | 252.0 | 1 |
| Alpha-1A adrenergic receptor CHEMBL229 | Kd | 6.6 | 6.6 | 251.2 | 1 |
| D(1A) dopamine receptor CHEMBL2056 | Ki | 6.57 | 6.57 | 271.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 1463.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 50.4 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 54.6 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 18.8 | mL.min-1.kg-1 | Homo sapiens |
| F | 49.0 | % | Homo sapiens |
| Fu | 0.14 | - | Not specified |
| Fu | 0.839 | - | Homo sapiens |
| T1/2 | 25.0 | hr | - |
| Vd | 16.0 | L.kg-1 | - |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine