Molecule Details
| InChIKey | ZPEIMTDSQAKGNT-UHFFFAOYSA-N |
|---|---|
| Compound Name | Chlorpromazine |
| Canonical SMILES | CN(C)CCCN1c2ccccc2Sc2ccc(Cl)cc21 |
| Clinical Status | Clinical Multi-Target |
| Targets (Human+Pathogen) | 35 |
| Pfam Stratification | Cross-Family |
| Avg pChEMBL | 7.16 |
| Source | BindingDB;ChEMBL;TTD_MultiTarget |
2D Structure
Activity Profile
DrugBank Annotations
| DrugBank ID | DB00477 |
|---|---|
| Drug Name | Chlorpromazine |
| CAS Number | 50-53-3 |
| Groups | approved investigational vet_approved |
| ATC Codes | N05AA01 |
| Description | The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class, chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking dopamine receptors. Chlorpromazine has several other actions and therapeutic uses, including as an anti... |
Categories: Adrenergic Antagonists Adrenergic alpha-1 Receptor Antagonists Adrenergic alpha-Antagonists Agents producing tachycardia Agents that produce hypertension Agents that reduce seizure threshold Anticholinergic Agents Antidepressive Agents Antiemetics Antipsychotic Agents Antipsychotic Agents (First Generation [Typical]) Autonomic Agents BSEP/ABCB11 Inhibitors Central Nervous System Agents Central Nervous System Depressants Cholinesterase Inhibitors Cytochrome P-450 CYP1A2 Substrates Cytochrome P-450 CYP2D6 Inhibitors Cytochrome P-450 CYP2D6 Inhibitors (moderate) Cytochrome P-450 CYP2D6 Inhibitors (strength unknown) Cytochrome P-450 CYP2D6 Substrates Cytochrome P-450 CYP2E1 Inhibitors Cytochrome P-450 CYP2E1 Inhibitors (strength unknown) Cytochrome P-450 CYP3A Inducers Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Inducers Cytochrome P-450 CYP3A4 Inducers (strength unknown) Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 CYP3A4 Substrates (strength unknown) Cytochrome P-450 Enzyme Inducers Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Substrates Dopamine Agents Dopamine Antagonists Dopamine D2 Receptor Antagonists Drugs causing inadvertant photosensitivity Drugs that are Mainly Renally Excreted Gastrointestinal Agents Heterocyclic Compounds, Fused-Ring Histamine Antagonists Histamine H1 Antagonists Hyperglycemia-Associated Agents Hypotensive Agents Moderate Risk QTc-Prolonging Agents Muscarinic Antagonists Nervous System Neurotoxic agents Neurotransmitter Agents P-glycoprotein inhibitors P-glycoprotein substrates Peripheral Nervous System Agents Phenothiazines Phenothiazines With Aliphatic Side-Chain Photosensitizing Agents Psycholeptics Psychotropic Drugs QTc Prolonging Agents Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome Serotonin 5-HT1 Receptor Antagonists Serotonin 5-HT1A Receptor Antagonists Serotonin 5-HT2 Receptor Antagonists Serotonin 5-HT2A Receptor Antagonists Serotonin 5-HT2C Receptor Antagonists Serotonin Agents Serotonin Receptor Antagonists Sulfur Compounds Tranquilizing Agents
Cross-references: BindingDB: 50001888 ChEBI: 3647 CHEMBL71 ChemSpider: 2625 Drugs Product Database (DPD): 8017 Guide to Pharmacology: 83 IUPHAR: 83 C06906 D00270 PDB: Z80 PharmGKB: PA448964 PubChem:2726 PubChem:46508395 RxCUI: 2403 Therapeutic Targets Database: DAP000374 Wikipedia: Chlorpromazine ZINC: ZINC000000044027
Target Activities (35)
| Target | Gene | Organism | Category | Pfam | pChEMBL | Type | Source |
|---|---|---|---|---|---|---|---|
| P35348 | ADRA1A | Homo sapiens | Human | PF00001 | 9.1 | Ki | BindingDB |
| P25100 | ADRA1D | Homo sapiens | Human | PF00001 | 8.6 | IC50 | ChEMBL |
| P14416 | DRD2 | Homo sapiens | Human | PF00001 | 8.5 | Ki | ChEMBL;BindingDB |
| P35462 | DRD3 | Homo sapiens | Human | PF00001 | 8.4 | Ki | ChEMBL;BindingDB |
| P28223 | HTR2A | Homo sapiens | Human | PF00001 | 8.2 | Ki | ChEMBL;BindingDB |
| P35367 | HRH1 | Homo sapiens | Human | PF00001 | 8.1 | Ki | ChEMBL;BindingDB |
| P18089 | ADRA2B | Homo sapiens | Human | PF00001 | 7.8 | Ki | ChEMBL;BindingDB |
| P23975 | SLC6A2 | Homo sapiens | Human | PF00209 | 7.7 | IC50 | ChEMBL |
| P21917 | DRD4 | Homo sapiens | Human | PF00001 | 7.6 | Ki | ChEMBL;BindingDB |
| P28335 | HTR2C | Homo sapiens | Human | PF00001 | 7.6 | Ki | ChEMBL;BindingDB |
| P34969 | HTR7 | Homo sapiens | Human | PF00001 | 7.5 | Ki | ChEMBL;BindingDB |
| P08912 | CHRM5 | Homo sapiens | Human | PF00001 | 7.5 | Ki | ChEMBL;BindingDB |
| P50406 | HTR6 | Homo sapiens | Human | PF00001 | 7.4 | Ki | ChEMBL;BindingDB |
| P11229 | CHRM1 | Homo sapiens | Human | PF00001 | 7.3 | Ki | ChEMBL;BindingDB |
| P18825 | ADRA2C | Homo sapiens | Human | PF00001 | 7.3 | Ki | ChEMBL;BindingDB |
| Q9H3N8 | HRH4 | Homo sapiens | Human | PF00001 | 7.3 | Ki | BindingDB |
| P41595 | HTR2B | Homo sapiens | Human | PF00001 | 7.3 | Ki | ChEMBL;BindingDB |
| P31645 | SLC6A4 | Homo sapiens | Human | PF03491 PF00209 | 7.2 | Ki | ChEMBL;BindingDB |
| P20309 | CHRM3 | Homo sapiens | Human | PF00001 | 7.2 | Ki | ChEMBL;BindingDB |
| P08173 | CHRM4 | Homo sapiens | Human | PF00001 | 7.1 | Ki | ChEMBL;BindingDB |
| P21728 | DRD1 | Homo sapiens | Human | PF00001 | 7.0 | Ki | ChEMBL;BindingDB |
| P08172 | CHRM2 | Homo sapiens | Human | PF00001 | 6.8 | Ki | ChEMBL;BindingDB |
| P21918 | DRD5 | Homo sapiens | Human | PF00001 | 6.8 | Ki | ChEMBL;BindingDB |
| P08913 | ADRA2A | Homo sapiens | Human | PF00001 | 6.6 | Ki | ChEMBL;BindingDB |
| Q99720 | SIGMAR1 | Homo sapiens | Human | PF04622 | 6.5 | IC50 | ChEMBL |
| Q06278 | AOX1 | Homo sapiens | Human | PF01315 PF03450 PF00941 PF00111 PF01799 PF02738 PF20256 | 6.2 | IC50 | ChEMBL;BindingDB |
| O15399 | GRIN2D | Homo sapiens | Human | PF01094 PF00060 PF10613 | 6.2 | IC50 | ChEMBL |
| O60391 | GRIN3B | Homo sapiens | Human | PF00060 PF10613 | 6.2 | IC50 | ChEMBL |
| P08183 | ABCB1 | Homo sapiens | Human | PF00664 PF00005 | 6.2 | Ki | ChEMBL;BindingDB |
| Q05586 | GRIN1 | Homo sapiens | Human | PF01094 PF00060 PF10613 | 6.2 | IC50 | ChEMBL |
| Q12879 | GRIN2A | Homo sapiens | Human | PF01094 PF00060 PF10613 PF10565 | 6.2 | IC50 | ChEMBL |
| Q13224 | GRIN2B | Homo sapiens | Human | PF01094 PF00060 PF10613 PF10565 | 6.2 | IC50 | ChEMBL |
| Q14957 | GRIN2C | Homo sapiens | Human | PF01094 PF00060 PF10613 PF10565 | 6.2 | IC50 | ChEMBL |
| Q8TCU5 | GRIN3A | Homo sapiens | Human | PF01094 PF00060 PF10613 | 6.2 | IC50 | ChEMBL |
| P08908 | HTR1A | Homo sapiens | Human | PF00001 | 6.2 | Ki | ChEMBL;BindingDB |
DrugBank Target Actions (32)
| Target | Gene | Target Name | Action | Type |
|---|---|---|---|---|
| P02768 | ALB | Albumin | binder | carriers |
| P08684 | CYP3A4 | Cytochrome P450 3A4 | inducer | enzymes |
| P05181 | CYP2E1 | Cytochrome P450 2E1 | inhibitor | enzymes |
| P06276 | BCHE | Cholinesterase | inhibitor | enzymes |
| P10635 | CYP2D6 | Cytochrome P450 2D6 | inhibitor | enzymes |
| P05177 | CYP1A2 | Cytochrome P450 1A2 | substrate | enzymes |
| P10635 | CYP2D6 | Cytochrome P450 2D6 | substrate | enzymes |
| P08908 | HTR1A | 5-hydroxytryptamine receptor 1A | antagonist | targets |
| P08913 | ADRA2A | Alpha-2 adrenergic receptors | antagonist | targets |
| P11229 | CHRM1 | Muscarinic acetylcholine receptor M1 | antagonist | targets |
| P14416 | DRD2 | D(2) dopamine receptor | antagonist | targets |
| P20309 | CHRM3 | Muscarinic acetylcholine receptor M3 | antagonist | targets |
| P21728 | DRD1 | D(1A) dopamine receptor | antagonist | targets |
| P21917 | DRD4 | D(4) dopamine receptor | antagonist | targets |
| P28223 | HTR2A | 5-hydroxytryptamine receptor 2A | antagonist | targets |
| P28335 | HTR2C | 5-hydroxytryptamine receptor 2C | antagonist | targets |
| P34969 | HTR7 | 5-hydroxytryptamine receptor 7 | antagonist | targets |
| P35348 | ADRA1A | Alpha-1A adrenergic receptor | antagonist | targets |
| P35367 | HRH1 | Histamine H1 receptor | antagonist | targets |
| P35368 | ADRA1B | Alpha-1B adrenergic receptor | antagonist | targets |
| P35462 | DRD3 | D(3) dopamine receptor | antagonist | targets |
| P50406 | HTR6 | 5-hydroxytryptamine receptor 6 | antagonist | targets |
| P02763 | P02763 | alpha1-acid glycoprotein | binder | targets |
| P28223 | HTR2A | 5-hydroxytryptamine 2 receptor | binder | targets |
| Q9H3N8 | HRH4 | Histamine H4 receptor | binder | targets |
| P0DP23 | CALM1 | Calmodulin | inhibitor | targets |
| P17405 | P17405 | Sphingomyelin phosphodiesterase | inhibitor | targets |
| P21918 | DRD5 | D(1B) dopamine receptor | inhibitor | targets |
| Q12809 | KCNH2 | Voltage-gated inwardly rectifying potassium channel KCNH2 | inhibitor | targets |
| O95342 | ABCB11 | Bile salt export pump | inhibitor | transporters |
| P08183 | ABCB1 | ATP-dependent translocase ABCB1 | inhibitor | transporters |
| P08183 | ABCB1 | ATP-dependent translocase ABCB1 | substrate | transporters |