Compound Detail
CHEMBL708
ZIPRASIDONE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL708 |
| Name | ZIPRASIDONE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | MVWVFYHBGMAFLY-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
28
Targets
97
Activities
2
Assay Types
18
PK Parameters
20
Publications
4
Known Names
15
Indications
Molecular Properties
412.9
MW (Da)
3.81
ALogP
5
HBA
1
HBD
48.5
PSA (Ų)
0.71
QED
0
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2001 |
| Availability | Prescription |
| Chirality | Achiral |
Indications
Psychotic Disorders Psychotic Disorders Anxiety Bipolar Disorder Dementia Depressive Disorder Schizophrenia Autistic Disorder Borderline Personality Disorder Depressive Disorder, Major Mood Disorders Phobia, Social Cardiovascular Diseases Opioid-Related Disorders Substance-Related Disorders
ATC Classification
N05AE04
ziprasidone
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOLEPTICS
Activity Summary
Ki 84 meas. best 10.1
IC50 13 meas. best 9.38
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2A CHEMBL224 | Ki | 10.1 | 9.4556 | 0.1 | 9 |
| Dopamine D2 receptor and Serotonin 2a receptor (D2 and 5HT2a) CHEMBL2111406 | Ki | 9.38 | 9.38 | 0.4 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | IC50 | 9.38 | 9.38 | 0.4 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL322 | Ki | 9.38 | 9.38 | 0.4 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | Ki | 9.3 | 9.3 | 0.5 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | Ki | 9.26 | 8.5671 | 0.6 | 7 |
| D(2) dopamine receptor CHEMBL217 | Ki | 9.1 | 8.5421 | 0.8 | 14 |
| 5-hydroxytryptamine receptor 1A CHEMBL214 | Ki | 8.8 | 8.386 | 1.6 | 5 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | Ki | 8.8 | 8.8 | 1.6 | 1 |
| Adrenergic receptor alpha-1 CHEMBL2094251 | Ki | 8.72 | 8.14 | 1.9 | 4 |
| D(2) dopamine receptor CHEMBL339 | Ki | 8.32 | 8.32 | 4.8 | 2 |
| 5-hydroxytryptamine receptor 7 CHEMBL3155 | Ki | 8.3 | 8.2733 | 5.0 | 3 |
| D(2) dopamine receptor CHEMBL217 | IC50 | 8.3 | 8.3 | 5.0 | 1 |
| Histamine H1 receptor CHEMBL231 | Ki | 8.28 | 7.404 | 5.3 | 5 |
| Alpha-1A adrenergic receptor CHEMBL229 | Ki | 8.22 | 8.22 | 6.0 | 1 |
| D(3) dopamine receptor CHEMBL234 | Ki | 8.2 | 8.12 | 6.3 | 5 |
| Adrenergic receptor alpha-1 CHEMBL1907610 | Ki | 8.1 | 8.0133 | 7.9 | 3 |
| D(1A) dopamine receptor CHEMBL2056 | Ki | 8.02 | 7.13 | 9.5 | 3 |
| Adrenergic receptor alpha-1 CHEMBL2094251 | IC50 | 7.96 | 7.96 | 11.0 | 1 |
| Histamine H1 receptor CHEMBL3943 | Ki | 7.8 | 7.8 | 15.8 | 1 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | Ki | 7.7 | 7.288 | 20.0 | 5 |
| D(4) dopamine receptor CHEMBL219 | Ki | 7.5 | 7.405 | 32.0 | 4 |
| Transporter CHEMBL6184 | Ki | 7.32 | 7.32 | 48.0 | 1 |
| Sodium-dependent serotonin transporter CHEMBL228 | Ki | 7.28 | 7.11 | 53.0 | 3 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240 | IC50 | 6.92 | 6.875 | 120.2 | 8 |
| Histamine H1 receptor CHEMBL4701 | IC50 | 6.82 | 6.82 | 150.0 | 1 |
| Adrenergic receptor alpha-2 CHEMBL2095158 | Ki | 6.41 | 6.41 | 390.0 | 2 |
| Serotonin 3 (5-HT3) receptor CHEMBL2094132 | Ki | 6.4 | 6.4 | 398.1 | 1 |
| Adrenergic receptor alpha-2 CHEMBL2093864 | Ki | 6.3 | 6.3 | 501.2 | 1 |
| Muscarinic acetylcholine receptor M1 CHEMBL216 | Ki | 5.29 | 5.29 | 5100.0 | 1 |
| Aspartate aminotransferase, cytoplasmic CHEMBL2189139 | IC50 | 5.27 | 5.27 | 5390.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 5.1 | mL.min-1.kg-1 | Homo sapiens |
| CL | 5.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 5.1 | mL.min-1.kg-1 | Homo sapiens |
| CL | 5.1 | mL.min-1.kg-1 | Homo sapiens |
| CL | 29.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 118.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 15.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 23.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 28.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 89.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 1.8 | mL.min-1.g-1 | Homo sapiens |
| CL | 15.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 28.0 | mL.min-1.g-1 | Homo sapiens |
| F | 60.0 | % | Homo sapiens |
| Fu | 0.0012 | - | Homo sapiens |
| Fu | 0.0012 | - | Homo sapiens |
| MRT | 3.3 | hr | Homo sapiens |
| T1/2 | 3.1 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine