Compound Detail
CHEMBL728
PROCHLORPERAZINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL728 |
| Name | PROCHLORPERAZINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | WIKYUJGCLQQFNW-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
39
Targets
80
Activities
3
Assay Types
10
PK Parameters
20
Publications
7
Known Names
11
Indications
1
Mechanisms
Molecular Properties
373.9
MW (Da)
4.58
ALogP
4
HBA
0
HBD
9.7
PSA (Ų)
0.78
QED
0
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1956 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Dopamine D2 receptor antagonist | ANTAGONIST | D(2) dopamine receptor | ✓ | ✓ |
Indications
Anxiety Postoperative Nausea and Vomiting Psychotic Disorders Schizophrenia Genital Neoplasms, Female Headache Migraine Disorders Nausea Nausea Cardiotoxicity Multiple Myeloma
ATC Classification
N05AB04
prochlorperazine
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOLEPTICS
Drug Warnings
Black Box Warning
General Warning
Activity Summary
IC50 46 meas. best 8.15
Ki 31 meas. best 8.7
EC50 3 meas. best 7.06
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2A CHEMBL224 | Ki | 8.7 | 8.7 | 2.0 | 1 |
| Histamine H1 receptor CHEMBL231 | Ki | 8.55 | 8.55 | 2.8 | 1 |
| D(2) dopamine receptor CHEMBL217 | Ki | 8.44 | 8.44 | 3.6 | 1 |
| D(3) dopamine receptor CHEMBL234 | Ki | 8.35 | 8.35 | 4.5 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | Ki | 8.32 | 8.32 | 4.7 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | IC50 | 8.15 | 8.15 | 7.1 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | IC50 | 8.0 | 8.0 | 10.0 | 1 |
| D(2) dopamine receptor CHEMBL217 | IC50 | 7.96 | 7.96 | 11.0 | 1 |
| Alpha-2C adrenergic receptor CHEMBL1916 | Ki | 7.92 | 7.92 | 12.0 | 1 |
| D(3) dopamine receptor CHEMBL234 | IC50 | 7.89 | 7.89 | 13.0 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | Ki | 7.89 | 7.89 | 13.0 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | Ki | 7.8 | 7.8 | 16.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | Ki | 7.64 | 7.64 | 23.0 | 1 |
| Histamine H1 receptor CHEMBL231 | IC50 | 7.62 | 7.62 | 24.0 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | IC50 | 7.5 | 7.5 | 32.0 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | IC50 | 7.47 | 7.47 | 34.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | Ki | 7.39 | 7.39 | 41.0 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | Ki | 7.31 | 7.31 | 49.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | IC50 | 7.27 | 7.27 | 54.0 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | Ki | 7.2 | 7.2 | 63.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | Ki | 7.19 | 7.19 | 65.0 | 1 |
| D(1A) dopamine receptor CHEMBL2056 | Ki | 7.11 | 7.11 | 78.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | IC50 | 7.11 | 7.11 | 78.0 | 1 |
| Alpha-2C adrenergic receptor CHEMBL1916 | IC50 | 7.09 | 7.09 | 82.0 | 1 |
| dengue virus type 2 CHEMBL613966 | EC50 | 7.06 | 7.06 | 88.0 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | IC50 | 7.05 | 7.05 | 89.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | IC50 | 6.99 | 6.99 | 102.0 | 1 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | Ki | 6.91 | 6.91 | 124.0 | 1 |
| D(1A) dopamine receptor CHEMBL2056 | IC50 | 6.81 | 6.81 | 155.0 | 1 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | Ki | 6.8 | 6.8 | 158.0 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | IC50 | 6.77 | 6.77 | 169.0 | 1 |
| Muscarinic acetylcholine receptor M4 CHEMBL1821 | Ki | 6.72 | 6.72 | 190.0 | 1 |
| 5-hydroxytryptamine receptor 4 CHEMBL5017 | Ki | 6.71 | 6.71 | 194.0 | 1 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | IC50 | 6.66 | 6.66 | 220.0 | 1 |
| Muscarinic acetylcholine receptor M1 CHEMBL216 | Ki | 6.61 | 6.61 | 244.0 | 1 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | IC50 | 6.57 | 6.57 | 267.0 | 1 |
| Cytochrome P450 2D6 CHEMBL289 | IC50 | 6.52 | 6.52 | 300.0 | 1 |
| Muscarinic acetylcholine receptor M3 CHEMBL245 | Ki | 6.49 | 6.49 | 321.0 | 1 |
| Sodium-dependent noradrenaline transporter CHEMBL222 | Ki | 6.4 | 6.4 | 396.0 | 1 |
| Sodium-dependent noradrenaline transporter CHEMBL222 | IC50 | 6.4 | 6.4 | 400.0 | 1 |
| Unchecked CHEMBL612545 | Ki | 6.38 | 6.0833 | 416.0 | 3 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | Ki | 6.26 | 6.26 | 543.0 | 1 |
| Sodium-dependent serotonin transporter CHEMBL228 | Ki | 6.21 | 6.21 | 621.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 6.17 | 4.9513 | 676.0 | 8 |
| D(4) dopamine receptor CHEMBL219 | Ki | 6.09 | 6.09 | 810.0 | 1 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | IC50 | 6.02 | 6.02 | 950.0 | 1 |
| Muscarinic acetylcholine receptor M1 CHEMBL216 | IC50 | 5.99 | 5.99 | 1013.0 | 1 |
| Muscarinic acetylcholine receptor M2 CHEMBL211 | Ki | 5.96 | 5.96 | 1107.0 | 1 |
| 5-hydroxytryptamine receptor 4 CHEMBL5017 | IC50 | 5.93 | 5.93 | 1164.0 | 1 |
| Sodium-dependent serotonin transporter CHEMBL228 | IC50 | 5.93 | 5.93 | 1169.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 16.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 29240.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 51.7 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 144.0 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 16.4 | mL.min-1.kg-1 | Homo sapiens |
| F | 20.0 | % | Homo sapiens |
| Fu | 0.003 | - | Not specified |
| Fu | 0.553 | - | Homo sapiens |
| MRT | 23.0 | hr | Homo sapiens |
| T1/2 | 9.0 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine