Compound Detail
CHEMBL564
PROMAZINE 💊 Approved Drug
Enter ChEMBL ID:
Free Research Context
This compound will appear in recent viewed items on the research home for this browser.
Research home
View demo workspace
💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL564 |
| Name | PROMAZINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | ZGUGWUXLJSTTMA-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
40
Targets
78
Activities
3
Assay Types
11
PK Parameters
20
Publications
4
Known Names
1
Indications
Molecular Properties
284.4
MW (Da)
4.24
ALogP
3
HBA
0
HBD
6.5
PSA (Ų)
0.83
QED
0
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1956 |
| Availability | Discontinued |
| Chirality | Achiral |
Indications
Psychotic Disorders
ATC Classification
N05AA03
promazine
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOLEPTICS
Activity Summary
IC50 45 meas. best 8.46
Ki 30 meas. best 9.4
EC50 3 meas. best 5.3
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Histamine H1 receptor CHEMBL231 | Ki | 9.4 | 9.4 | 0.4 | 1 |
| Histamine H1 receptor CHEMBL231 | IC50 | 8.46 | 7.035 | 3.4 | 2 |
| Alpha-1A adrenergic receptor CHEMBL319 | Ki | 8.43 | 8.43 | 3.7 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | Ki | 8.34 | 8.34 | 4.5 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | Ki | 8.21 | 8.21 | 6.2 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | Ki | 8.17 | 8.17 | 6.7 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | IC50 | 8.09 | 8.09 | 8.2 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | Ki | 8.07 | 8.07 | 8.4 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | IC50 | 8.03 | 8.03 | 9.2 | 1 |
| Sodium-dependent noradrenaline transporter CHEMBL222 | IC50 | 7.89 | 7.89 | 13.0 | 1 |
| Sodium-dependent noradrenaline transporter CHEMBL222 | Ki | 7.89 | 7.89 | 13.0 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | IC50 | 7.89 | 7.89 | 13.0 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | IC50 | 7.75 | 7.75 | 18.0 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | IC50 | 7.64 | 7.64 | 23.0 | 1 |
| Alpha-2C adrenergic receptor CHEMBL1916 | Ki | 7.43 | 7.43 | 37.0 | 1 |
| Muscarinic acetylcholine receptor M4 CHEMBL1821 | Ki | 7.38 | 7.38 | 42.0 | 1 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | Ki | 7.34 | 7.34 | 46.0 | 1 |
| Sodium-dependent serotonin transporter CHEMBL228 | Ki | 7.34 | 7.34 | 46.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | Ki | 7.28 | 7.28 | 52.0 | 1 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | IC50 | 7.19 | 7.19 | 64.0 | 1 |
| D(3) dopamine receptor CHEMBL234 | Ki | 7.16 | 7.16 | 69.0 | 1 |
| Sodium-dependent serotonin transporter CHEMBL228 | IC50 | 7.07 | 7.07 | 86.0 | 1 |
| Muscarinic acetylcholine receptor M3 CHEMBL245 | Ki | 7.06 | 7.06 | 88.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | IC50 | 7.0 | 7.0 | 99.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | Ki | 6.94 | 6.94 | 114.0 | 1 |
| Muscarinic acetylcholine receptor M1 CHEMBL216 | Ki | 6.93 | 6.93 | 117.0 | 1 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | Ki | 6.9 | 6.9 | 127.0 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | Ki | 6.9 | 6.9 | 126.0 | 1 |
| Dopamine receptor CHEMBL2096970 | IC50 | 6.89 | 6.89 | 130.0 | 1 |
| D(2) dopamine receptor CHEMBL217 | Ki | 6.78 | 6.78 | 168.0 | 1 |
| D(3) dopamine receptor CHEMBL234 | IC50 | 6.69 | 6.69 | 205.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | Ki | 6.66 | 6.66 | 221.0 | 1 |
| Alpha-2C adrenergic receptor CHEMBL1916 | IC50 | 6.6 | 6.6 | 253.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | IC50 | 6.57 | 6.57 | 271.0 | 1 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | IC50 | 6.56 | 6.56 | 274.0 | 1 |
| Cytochrome P450 2D6 CHEMBL289 | IC50 | 6.52 | 6.52 | 300.0 | 1 |
| Muscarinic acetylcholine receptor M4 CHEMBL1821 | IC50 | 6.52 | 6.52 | 299.0 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | IC50 | 6.47 | 6.47 | 337.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | IC50 | 6.46 | 6.46 | 347.0 | 1 |
| Muscarinic acetylcholine receptor M2 CHEMBL211 | Ki | 6.41 | 6.41 | 387.0 | 1 |
| Muscarinic acetylcholine receptor M3 CHEMBL245 | IC50 | 6.38 | 6.38 | 416.0 | 1 |
| Muscarinic acetylcholine receptor M1 CHEMBL216 | IC50 | 6.31 | 6.31 | 487.0 | 1 |
| Plasmodium falciparum CHEMBL364 | IC50 | 6.31 | 6.305 | 490.0 | 2 |
| D(2) dopamine receptor CHEMBL217 | IC50 | 6.3 | 6.3 | 505.0 | 1 |
| Unchecked CHEMBL612545 | Ki | 6.13 | 5.81 | 732.0 | 5 |
| Dopamine receptor CHEMBL2093868 | IC50 | 5.98 | 5.98 | 1040.0 | 1 |
| Muscarinic acetylcholine receptor M2 CHEMBL211 | IC50 | 5.96 | 5.96 | 1089.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 5.96 | 5.6333 | 1098.0 | 6 |
| D(1A) dopamine receptor CHEMBL2056 | Ki | 5.91 | 5.91 | 1232.0 | 1 |
| Histamine H1 receptor CHEMBL4701 | IC50 | 5.9 | 5.9 | 1258.9 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 14.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 1595.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 30.9 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 51.6 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 14.3 | mL.min-1.kg-1 | Homo sapiens |
| Fu | 0.11 | - | Homo sapiens |
| Fu | 0.11 | - | Homo sapiens |
| Fu | 0.029 | - | Not specified |
| Fu | 0.545 | - | Homo sapiens |
| MRT | 9.6 | hr | Homo sapiens |
| T1/2 | 7.9 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine