Compound Detail
CHEMBL479
THIORIDAZINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL479 |
| Name | THIORIDAZINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | KLBQZWRITKRQQV-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
67
Targets
146
Activities
3
Assay Types
11
PK Parameters
20
Publications
12
Known Names
6
Indications
3
Mechanisms
Molecular Properties
370.6
MW (Da)
5.89
ALogP
4
HBA
0
HBD
6.5
PSA (Ų)
0.62
QED
1
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1962 |
| Availability | Withdrawn |
| Chirality | Racemic |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Serotonin 2a (5-HT2a) receptor antagonist | ANTAGONIST | 5-hydroxytryptamine receptor 2A | ✓ | ✓ |
| Serotonin 2c (5-HT2c) receptor antagonist | ANTAGONIST | 5-hydroxytryptamine receptor 2C | ✓ | ✓ |
| D2-like dopamine receptor antagonist | ANTAGONIST | D2-like dopamine receptor | ✓ | ✓ |
Indications
Psychotic Disorders Anxiety Dementia Depressive Disorder Schizophrenia Leukemia, Myeloid, Acute
ATC Classification
N05AC02
thioridazine
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOLEPTICS
Drug Warnings
Withdrawn
cardiotoxicity
Cardiac arrythmias
Black Box Warning
General Warning
Activity Summary
IC50 104 meas. best 8.7
Ki 40 meas. best 8.9
Kd 2 meas. best 6.43
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2A CHEMBL224 | Ki | 8.9 | 7.99 | 1.2 | 2 |
| Muscarinic acetylcholine receptor M1 CHEMBL216 | Ki | 8.77 | 8.77 | 1.7 | 1 |
| Muscarinic acetylcholine receptor CHEMBL1907609 | IC50 | 8.7 | 7.835 | 2.0 | 2 |
| Alpha-1A adrenergic receptor CHEMBL319 | Ki | 8.69 | 8.69 | 2.1 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | Ki | 8.59 | 8.59 | 2.6 | 1 |
| D(2) dopamine receptor CHEMBL339 | IC50 | 8.55 | 7.8475 | 2.8 | 4 |
| Alpha-1D adrenergic receptor CHEMBL223 | Ki | 8.54 | 8.54 | 2.9 | 1 |
| D(3) dopamine receptor CHEMBL234 | Ki | 8.47 | 8.47 | 3.4 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | IC50 | 8.36 | 8.36 | 4.4 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | IC50 | 8.33 | 8.33 | 4.7 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | IC50 | 8.29 | 8.29 | 5.1 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | IC50 | 8.23 | 8.23 | 5.9 | 1 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | Ki | 8.18 | 8.18 | 6.6 | 1 |
| Muscarinic acetylcholine receptor M1 CHEMBL216 | IC50 | 8.15 | 8.15 | 7.0 | 1 |
| L5178Y CHEMBL614720 | IC50 | 8.13 | 6.515 | 7.4 | 4 |
| D(2) dopamine receptor CHEMBL217 | Ki | 8.1 | 7.8633 | 8.0 | 3 |
| Histamine H1 receptor CHEMBL231 | Ki | 8.07 | 8.07 | 8.4 | 1 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | IC50 | 8.03 | 8.03 | 9.2 | 1 |
| D(3) dopamine receptor CHEMBL234 | IC50 | 8.01 | 8.01 | 9.9 | 1 |
| Muscarinic acetylcholine receptor M4 CHEMBL1821 | Ki | 7.96 | 7.96 | 11.0 | 1 |
| Adrenergic receptor alpha-1 CHEMBL1907610 | IC50 | 7.77 | 7.3833 | 17.0 | 3 |
| D(1A) dopamine receptor CHEMBL265 | IC50 | 7.76 | 6.9167 | 17.3 | 3 |
| Serotonin 2 (5-HT2) receptor CHEMBL2093870 | IC50 | 7.75 | 7.485 | 18.0 | 2 |
| Muscarinic acetylcholine receptor M3 CHEMBL245 | Ki | 7.72 | 7.72 | 19.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | Ki | 7.64 | 7.64 | 23.0 | 1 |
| Alpha-2C adrenergic receptor CHEMBL1916 | Ki | 7.6 | 7.6 | 25.0 | 1 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240 | IC50 | 7.48 | 6.9942 | 33.0 | 12 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | Ki | 7.48 | 7.315 | 33.0 | 2 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | Ki | 7.47 | 7.47 | 34.0 | 1 |
| D(2) dopamine receptor CHEMBL217 | IC50 | 7.46 | 7.46 | 35.0 | 1 |
| Muscarinic acetylcholine receptor M2 CHEMBL211 | Ki | 7.42 | 7.42 | 38.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | IC50 | 7.36 | 7.36 | 44.0 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | Ki | 7.3 | 7.3 | 50.0 | 1 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | IC50 | 7.22 | 7.22 | 60.0 | 1 |
| 5-hydroxytryptamine receptor 7 CHEMBL3155 | Ki | 7.16 | 6.95 | 70.0 | 2 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | IC50 | 7.15 | 7.15 | 71.0 | 1 |
| Histamine H1 receptor CHEMBL231 | IC50 | 7.14 | 7.14 | 72.0 | 1 |
| Muscarinic acetylcholine receptor M4 CHEMBL1821 | IC50 | 7.1 | 7.1 | 80.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | Ki | 7.09 | 7.09 | 82.0 | 1 |
| Dopamine receptor CHEMBL2093868 | IC50 | 7.07 | 7.07 | 85.0 | 1 |
| Muscarinic acetylcholine receptor M3 CHEMBL245 | IC50 | 7.05 | 7.05 | 90.0 | 1 |
| D(1A) dopamine receptor CHEMBL2056 | Ki | 7.01 | 7.01 | 97.0 | 1 |
| Histamine H1 receptor CHEMBL4701 | IC50 | 7.0 | 7.0 | 99.0 | 1 |
| Muscarinic acetylcholine receptor M2 CHEMBL211 | IC50 | 6.97 | 6.97 | 106.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | IC50 | 6.89 | 6.89 | 129.0 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | IC50 | 6.88 | 6.88 | 133.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | Ki | 6.82 | 6.82 | 153.0 | 1 |
| Alpha-2C adrenergic receptor CHEMBL1916 | IC50 | 6.77 | 6.77 | 171.0 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | Ki | 6.76 | 6.76 | 174.0 | 1 |
| D(1A) dopamine receptor CHEMBL2056 | IC50 | 6.71 | 6.71 | 194.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 50.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 114.0 | uL.min-1.(10^6cells)-1 | Rattus norvegicus |
| F | 49.0 | % | Homo sapiens |
| Fu | 0.001 | - | Rattus norvegicus |
| Fu | 0.002 | - | Rattus norvegicus |
| Fu | 0.049 | - | Homo sapiens |
| Fu | 0.00067 | - | Rattus norvegicus |
| Fu | 0.001 | - | Rattus norvegicus |
| Fu | 0.0003 | - | Sus scrofa |
| Fu | 0.0031 | - | Rattus norvegicus |
| Vd | 3333.0 | L.kg-1 | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine