Compound Detail
CHEMBL726
FLUPHENAZINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL726 |
| Name | FLUPHENAZINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | PLDUPXSUYLZYBN-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
63
Targets
135
Activities
3
Assay Types
7
PK Parameters
20
Publications
3
Known Names
2
Indications
Molecular Properties
437.5
MW (Da)
4.31
ALogP
5
HBA
1
HBD
29.9
PSA (Ų)
0.73
QED
0
Ro5 Violations
6
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1959 |
| Availability | Prescription |
| Chirality | Achiral |
Indications
Psychotic Disorders Schizophrenia
ATC Classification
N05AB02
fluphenazine
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOLEPTICS
Activity Summary
IC50 72 meas. best 9.23
Ki 61 meas. best 9.7
EC50 2 meas. best 5.4
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| D(3) dopamine receptor CHEMBL234 | Ki | 9.7 | 8.8933 | 0.2 | 3 |
| D(2) dopamine receptor CHEMBL217 | Ki | 9.27 | 8.9833 | 0.5 | 3 |
| D(3) dopamine receptor CHEMBL234 | IC50 | 9.23 | 9.23 | 0.6 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | Ki | 8.84 | 8.18 | 1.5 | 2 |
| D(2) dopamine receptor CHEMBL217 | IC50 | 8.79 | 8.79 | 1.6 | 1 |
| Histamine H1 receptor CHEMBL231 | Ki | 8.33 | 7.8033 | 4.7 | 3 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | IC50 | 8.29 | 8.29 | 5.1 | 1 |
| Alpha-1A adrenergic receptor CHEMBL229 | Ki | 8.19 | 8.19 | 6.5 | 1 |
| 5-hydroxytryptamine receptor 7 CHEMBL3155 | Ki | 8.1 | 8.1 | 8.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | Ki | 8.07 | 8.07 | 8.6 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | Ki | 8.02 | 8.02 | 9.6 | 1 |
| D(1A) dopamine receptor CHEMBL2056 | Ki | 7.96 | 7.1533 | 11.0 | 3 |
| Alpha-2B adrenergic receptor CHEMBL1942 | Ki | 7.89 | 7.49 | 13.0 | 2 |
| Alpha-1D adrenergic receptor CHEMBL223 | Ki | 7.8 | 7.8 | 16.0 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | Ki | 7.72 | 7.72 | 19.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | IC50 | 7.7 | 7.7 | 20.0 | 1 |
| D(1B) dopamine receptor CHEMBL1850 | Ki | 7.68 | 7.68 | 21.0 | 2 |
| Alpha-2C adrenergic receptor CHEMBL1916 | Ki | 7.66 | 7.6 | 22.0 | 2 |
| D(1A) dopamine receptor CHEMBL2056 | IC50 | 7.64 | 7.64 | 23.0 | 1 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | Ki | 7.62 | 7.52 | 24.0 | 2 |
| Alpha-1A adrenergic receptor CHEMBL319 | IC50 | 7.62 | 7.62 | 24.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | Ki | 7.6 | 7.6 | 25.0 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | IC50 | 7.54 | 7.54 | 29.0 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | IC50 | 7.48 | 7.48 | 33.0 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | IC50 | 7.47 | 7.47 | 34.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | Ki | 7.46 | 7.46 | 35.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | IC50 | 7.41 | 7.41 | 39.0 | 1 |
| Histamine H1 receptor CHEMBL231 | IC50 | 7.4 | 7.4 | 40.0 | 1 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | IC50 | 7.28 | 7.28 | 52.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | IC50 | 7.17 | 7.17 | 67.0 | 1 |
| Adenylate cyclase CHEMBL2095179 | IC50 | 7.1 | 7.1 | 80.0 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | Ki | 7.1 | 6.8 | 80.0 | 2 |
| Unchecked CHEMBL612545 | Ki | 7.01 | 5.6033 | 97.0 | 6 |
| D(4) dopamine receptor CHEMBL219 | Ki | 6.89 | 6.29 | 130.0 | 2 |
| 5-hydroxytryptamine receptor 1A CHEMBL214 | Ki | 6.84 | 6.84 | 145.7 | 1 |
| Alpha-2C adrenergic receptor CHEMBL1916 | IC50 | 6.81 | 6.81 | 154.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 6.8 | 5.4244 | 158.0 | 9 |
| Alpha-2A adrenergic receptor CHEMBL1867 | IC50 | 6.67 | 6.67 | 215.0 | 1 |
| Muscarinic acetylcholine receptor M4 CHEMBL1821 | Ki | 6.32 | 6.32 | 484.0 | 1 |
| Plasmodium falciparum CHEMBL364 | IC50 | 6.3 | 6.3 | 500.0 | 2 |
| Muscarinic acetylcholine receptor M1 CHEMBL216 | Ki | 6.19 | 6.19 | 646.0 | 1 |
| Sodium-dependent serotonin transporter CHEMBL228 | Ki | 6.1 | 6.1 | 793.0 | 1 |
| Androgen receptor CHEMBL3072 | Ki | 6.1 | 6.1 | 800.0 | 1 |
| 5-hydroxytryptamine receptor 1B CHEMBL3459 | Ki | 6.06 | 6.06 | 869.0 | 1 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | Ki | 6.03 | 6.03 | 939.0 | 1 |
| Muscarinic acetylcholine receptor M3 CHEMBL245 | Ki | 6.0 | 6.0 | 1002.0 | 1 |
| Histamine H2 receptor CHEMBL1941 | Ki | 5.92 | 5.92 | 1205.0 | 1 |
| Histamine H2 receptor CHEMBL1941 | IC50 | 5.91 | 5.91 | 1226.0 | 1 |
| Sodium-dependent serotonin transporter CHEMBL228 | IC50 | 5.83 | 5.83 | 1492.0 | 1 |
| Sodium-dependent dopamine transporter CHEMBL238 | Ki | 5.79 | 5.79 | 1631.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 1581.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 121.0 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 71.6 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 9.9 | mL.min-1.kg-1 | Homo sapiens |
| F | 2.7 | % | Homo sapiens |
| Fu | 0.012 | - | Not specified |
| Fu | 0.455 | - | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine