Molecule Details
| InChIKey | RGCVKNLCSQQDEP-UHFFFAOYSA-N |
|---|---|
| Compound Name | Perphenazine |
| Canonical SMILES | OCCN1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 |
| Clinical Status | Data-mined Candidate |
| Targets (Human+Pathogen) | 16 |
| Pfam Stratification | Cross-Family |
| Avg pChEMBL | 7.56 |
| Source | BindingDB;ChEMBL |
2D Structure
Activity Profile
DrugBank Annotations
| DrugBank ID | DB00850 |
|---|---|
| Drug Name | Perphenazine |
| CAS Number | 58-39-9 |
| Groups | approved investigational |
| ATC Codes | N05AB03 |
| Description | An antipsychotic phenothiazine derivative with actions and uses similar to those of chlorpromazine. |
Categories: Antipsychotic Agents Antipsychotic Agents (First Generation [Typical]) Central Nervous System Agents Central Nervous System Depressants Cytochrome P-450 CYP1A2 Substrates Cytochrome P-450 CYP2C18 Substrates Cytochrome P-450 CYP2C19 Substrates Cytochrome P-450 CYP2C8 Substrates Cytochrome P-450 CYP2C9 Substrates Cytochrome P-450 CYP2D6 Inhibitors Cytochrome P-450 CYP2D6 Inhibitors (strength unknown) Cytochrome P-450 CYP2D6 Substrates Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Substrates Dopamine Agents Dopamine Antagonists Dopamine D2 Receptor Antagonists Drugs causing inadvertant photosensitivity Heterocyclic Compounds, Fused-Ring Nervous System Neurotoxic agents Neurotransmitter Agents Phenothiazines Phenothiazines With Piperazine Structure Photosensitizing Agents Psycholeptics Psychotropic Drugs Sulfur Compounds Tranquilizing Agents
Cross-references: BindingDB: 50130273 ChEBI: 8028 CHEMBL567 ChemSpider: 4586 Drugs Product Database (DPD): 8003 Guide to Pharmacology: 209 IUPHAR: 209 C07427 D00503 PharmGKB: PA450882 PubChem:4748 PubChem:46507058 RxCUI: 8076 Therapeutic Targets Database: DAP000100 Wikipedia: Perphenazine ZINC: ZINC000019228902
Target Activities (16)
| Target | Gene | Organism | Category | Pfam | pChEMBL | Type | Source |
|---|---|---|---|---|---|---|---|
| P35462 | DRD3 | Homo sapiens | Human | PF00001 | 9.9 | Ki | BindingDB |
| P14416 | DRD2 | Homo sapiens | Human | PF00001 | 9.2 | Ki | ChEMBL;BindingDB |
| P28223 | HTR2A | Homo sapiens | Human | PF00001 | 8.2 | Ki | BindingDB |
| P35367 | HRH1 | Homo sapiens | Human | PF00001 | 8.1 | Ki | BindingDB |
| P35348 | ADRA1A | Homo sapiens | Human | PF00001 | 8.0 | Ki | BindingDB |
| P21917 | DRD4 | Homo sapiens | Human | PF00001 | 7.8 | Ki | BindingDB |
| P50406 | HTR6 | Homo sapiens | Human | PF00001 | 7.8 | Ki | BindingDB |
| P34969 | HTR7 | Homo sapiens | Human | PF00001 | 7.6 | Ki | ChEMBL;BindingDB |
| Q06278 | AOX1 | Homo sapiens | Human | PF01315 PF03450 PF00941 PF00111 PF01799 PF02738 PF20256 | 7.5 | IC50 | ChEMBL;BindingDB |
| P18825 | ADRA2C | Homo sapiens | Human | PF00001 | 7.1 | Ki | BindingDB |
| P18089 | ADRA2B | Homo sapiens | Human | PF00001 | 7.0 | Ki | BindingDB |
| P10635 | CYP2D6 | Homo sapiens | Human | PF00067 | 6.9 | IC50 | ChEMBL;BindingDB |
| P28335 | HTR2C | Homo sapiens | Human | PF00001 | 6.9 | Ki | BindingDB |
| P08908 | HTR1A | Homo sapiens | Human | PF00001 | 6.4 | Ki | BindingDB |
| P08913 | ADRA2A | Homo sapiens | Human | PF00001 | 6.3 | Ki | BindingDB |
| P00352 | ALDH1A1 | Homo sapiens | Human | PF00171 | 6.3 | IC50 | ChEMBL;BindingDB |
DrugBank Target Actions (12)
| Target | Gene | Target Name | Action | Type |
|---|---|---|---|---|
| P02768 | ALB | Albumin | regulator | carriers |
| P10635 | CYP2D6 | Cytochrome P450 2D6 | inhibitor | enzymes |
| P05177 | CYP1A2 | Cytochrome P450 1A2 | substrate | enzymes |
| P08684 | CYP3A4 | Cytochrome P450 3A4 | substrate | enzymes |
| P10632 | CYP2C8 | Cytochrome P450 2C8 | substrate | enzymes |
| P10635 | CYP2D6 | Cytochrome P450 2D6 | substrate | enzymes |
| P11712 | CYP2C9 | Cytochrome P450 2C9 | substrate | enzymes |
| P33260 | CYP2C18 | Cytochrome P450 2C18 | substrate | enzymes |
| P33261 | CYP2C19 | Cytochrome P450 2C19 | substrate | enzymes |
| P14416 | DRD2 | D(2) dopamine receptor | antagonist | targets |
| P21728 | DRD1 | D(1A) dopamine receptor | antagonist | targets |
| P0DP23 | CALM1 | Calmodulin | inhibitor | targets |