Perphenazine
drug drugOn this page
Also known as ChlorpiprazineDecentanFentazinNSC-150866PerfenazinaPerphenazine component of etrafon-aPerphenazine maleateTrilafonTrilafon-laSID11111645SID11111646SID26747080SID50104233SID57287811SID85231190SID856006SID90340948SID56422427SID26747081
Summary
Perphenazine (CHEMBL567) is an approved small-molecule phenothiazine antipsychotic drug (ATC N05AB03) targeting HTR6, HTR7, and DRD2; indicated across 9 conditions including psychotic disorder and anxiety.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: N05AB03
- Targets: 6 (HTR6, HTR7, DRD2…)
- Indications: 9 conditions
- Clinical trials: 17
- Chemistry: 404 Da · C21H26ClN3OS
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL567 |
| Name | Perphenazine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 4748 |
| ChEBI | CHEBI:8028 |
| ATC | N05AB03 |
| Molecular formula | C21H26ClN3OS |
| Molecular weight | 404 |
| InChIKey | RGCVKNLCSQQDEP-UHFFFAOYSA-N |
SMILES: C1CN(CCN1CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl)CCO
IUPAC name: 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol
ChEBI definition: A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10.
Pharmacological roles (ChEBI): phenothiazine antipsychotic drug, dopaminergic antagonist, antiemetic.
Also known as: Chlorpiprazine, Decentan, Fentazin, NSC-150866, Perfenazina, Perphenazine, Perphenazine component of etrafon-a, Perphenazine maleate, Trilafon, Trilafon-la, perphenazine, SID11111645
Patent coverage: 5,954 distinct patent families (21,883 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 21,767 (99%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| HTR6 | 5-HT6 receptor | Inverse agonist | 7.1 | 0.2% | P50406 |
| HTR7 | 5-HT7 receptor | Inverse agonist | 7.2 | 0.8% | P34969 |
| DRD2 | D2 receptor | Antagonist | 9.59 | 0% | P14416 |
| HRH1 | H1 receptor | Antagonist | 8.1 | 0% | P35367 |
| HTR2A | 5-HT2A receptor | Antagonist | 8.2 | 0% | P28223 |
| HTR2C | 5-HT2C receptor | Antagonist | 6.9 | 0% | P28335 |
Broader ChEMBL bioactivity targets: 66 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Microtubule-associated protein tau, Ubiquitin carboxyl-terminal hydrolase 2, Nuclear receptor ROR-gamma, Survival motor neuron protein, Prelamin-A/C, ATP-dependent DNA helicase Q1, 4’-phosphopantetheinyl transferase ffp, Thrombopoietin, G-protein coupled receptor 35, NPC intracellular cholesterol transporter 1, Geminin, Endonuclease 4, Ras-related protein Rab-9A, Peripheral myelin protein 22, Apelin receptor, Aldehyde oxidase 1, Aldehyde oxidase 1, Aldehyde oxidase 1, Pleiotropic ABC efflux transporter of multiple drugs.
Bioactivity
ChEMBL activities: 55 potent at pChembl ≥ 5 of 100 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| DRD2 | 9.52 | IC50 | 0.3 | nM | CHEMBL_ACT_13317546 |
| DRD2 | 7.77 | AC50 | 17 | nM | CHEMBL_ACT_25140031 |
| HTR2A | 7.68 | AC50 | 20.7 | nM | CHEMBL_ACT_25173514 |
| HTR7 | 7.64 | Ki | 23 | nM | CHEMBL_ACT_82695 |
| ADRA1A | 7.59 | AC50 | 25.8 | nM | CHEMBL_ACT_25137757 |
| CYP2D6 | 7.5 | Potency | 31.6 | nM | CHEMBL_ACT_4969903 |
| CYP2D6 | 7.5 | AC50 | 31.62 | nM | CHEMBL_ACT_6067267 |
| AOX1 | 7.48 | IC50 | 33 | nM | CHEMBL_ACT_5102808 |
| DRD3 | 7.41 | AC50 | 39 | nM | CHEMBL_ACT_25193233 |
| HRH1 | 7.38 | AC50 | 42 | nM | CHEMBL_ACT_25212207 |
| CYP2D6 | 6.92 | IC50 | 120 | nM | CHEMBL_ACT_15450962 |
| ADRA2B | 6.85 | AC50 | 140 | nM | CHEMBL_ACT_25143408 |
| CYP2D6 | 6.7 | Potency | 199.5 | nM | CHEMBL_ACT_4949755 |
| CYP1A2 | 6.5 | AC50 | 316.2 | nM | CHEMBL_ACT_6059963 |
| SMN1 | 6.4 | Potency | 398.1 | nM | CHEMBL_ACT_3886126 |
| ADRA2C | 6.34 | AC50 | 460 | nM | CHEMBL_ACT_25147574 |
| ALDH1A1 | 6.28 | IC50 | 524.2 | nM | CHEMBL_ACT_24348830 |
| HTR2A | 6.24 | AC50 | 570 | nM | CHEMBL_ACT_25224899 |
| TDP1 | 6.15 | Potency | 707.9 | nM | CHEMBL_ACT_3934608 |
| Q9Z0U5 | 6.13 | IC50 | 740 | nM | CHEMBL_ACT_5102821 |
| HTR2B | 6.11 | AC50 | 770 | nM | CHEMBL_ACT_25227247 |
| KCNH2 | 6.05 | AC50 | 900 | nM | CHEMBL_ACT_25117417 |
| OPRK1 | 5.98 | AC50 | 1045 | nM | CHEMBL_ACT_25129158 |
| P33302 | 5.85 | IC50 | 1400 | nM | CHEMBL_ACT_5306636 |
| CYP3A4 | 5.6 | Potency | 2512 | nM | CHEMBL_ACT_4957349 |
| CYP3A4 | 5.6 | Potency | 2512 | nM | CHEMBL_ACT_5026706 |
| HTR1A | 5.57 | AC50 | 2700 | nM | CHEMBL_ACT_25215809 |
| ADRA2A | 5.56 | IC50 | 2775 | nM | CHEMBL_ACT_25751424 |
| ADRB2 | 5.56 | IC50 | 2777 | nM | CHEMBL_ACT_25751425 |
| SMN1 | 5.55 | Potency | 2818 | nM | CHEMBL_ACT_3892312 |
| SLC6A4 | 5.54 | AC50 | 2900 | nM | CHEMBL_ACT_25150045 |
| CX3CR1 | 5.53 | IC50 | 2949 | nM | CHEMBL_ACT_25751427 |
| CYP2C19 | 5.5 | Potency | 3162 | nM | CHEMBL_ACT_4015608 |
| APLNR | 5.49 | IC50 | 3218 | nM | CHEMBL_ACT_25751426 |
| KCNH2 | 5.46 | Ki | 3454 | nM | CHEMBL_ACT_7736473 |
| HTR2C | 5.44 | AC50 | 3600 | nM | CHEMBL_ACT_25131515 |
| Q5FB27 | 5.44 | IC50 | 3600 | nM | CHEMBL_ACT_5102838 |
| GLP1R | 5.41 | IC50 | 3931 | nM | CHEMBL_ACT_25751430 |
| GPR65 | 5.4 | IC50 | 3944 | nM | CHEMBL_ACT_25751434 |
| GPR183 | 5.38 | IC50 | 4172 | nM | CHEMBL_ACT_25751432 |
| KCNH2 | 5.38 | IC50 | 4216 | nM | CHEMBL_ACT_7736472 |
| CYP1A2 | 5.35 | IC50 | 4490 | nM | CHEMBL_ACT_15449393 |
| FPR1 | 5.32 | IC50 | 4803 | nM | CHEMBL_ACT_25751428 |
| GPR119 | 5.29 | IC50 | 5165 | nM | CHEMBL_ACT_25751431 |
| GPR35 | 5.22 | IC50 | 5967 | nM | CHEMBL_ACT_25751433 |
| FPR3 | 5.21 | IC50 | 6243 | nM | CHEMBL_ACT_25751429 |
| O54754 | 5.21 | IC50 | 6100 | nM | CHEMBL_ACT_5102814 |
| P0A6C1 | 5.2 | Potency | 6310 | nM | CHEMBL_ACT_4069460 |
| SLC6A3 | 5.19 | AC50 | 6500 | nM | CHEMBL_ACT_25123653 |
| TDP1 | 5.15 | Potency | 7080 | nM | CHEMBL_ACT_3927968 |
| MTOR | 5.13 | Potency | 7362 | nM | CHEMBL_ACT_4522781 |
| MAPT | 5.05 | Potency | 8912 | nM | CHEMBL_ACT_3967446 |
| MAPT | 5.05 | Potency | 8912 | nM | CHEMBL_ACT_3972097 |
| TP53 | 5 | Potency | 10000 | nM | CHEMBL_ACT_4870157 |
| NPSR1 | 5 | Potency | 10000 | nM | CHEMBL_ACT_4884944 |
Target pathways
Aggregated over 6 target gene(s): HTR6, HTR7, DRD2, HRH1, HTR2A, HTR2C.
Top Reactome pathways
12 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signal Transduction | 4 | HTR2A, HTR2C, HTR6, HTR7 |
| Signaling by GPCR | 4 | HTR2A, HTR2C, HTR6, HTR7 |
| Class A/1 (Rhodopsin-like receptors) | 4 | HTR2A, HTR2C, HTR6, HTR7 |
| Amine ligand-binding receptors | 4 | HTR2A, HTR2C, HTR6, HTR7 |
| GPCR downstream signalling | 4 | HTR2A, HTR2C, HTR6, HTR7 |
| Serotonin receptors | 4 | HTR2A, HTR2C, HTR6, HTR7 |
| GPCR ligand binding | 4 | HTR2A, HTR2C, HTR6, HTR7 |
| G alpha (q) signalling events | 3 | HRH1, HTR2A, HTR2C |
| G alpha (s) signalling events | 2 | HTR6, HTR7 |
| Histamine receptors | 1 | HRH1 |
| Dopamine receptors | 1 | DRD2 |
| RHOBTB3 ATPase cycle | 1 | HTR7 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| signal transduction | 6 |
| G protein-coupled receptor signaling pathway | 6 |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | 5 |
| chemical synaptic transmission | 5 |
| G protein-coupled serotonin receptor signaling pathway | 4 |
| intracellular calcium ion homeostasis | 3 |
| phospholipase C-activating G protein-coupled receptor signaling pathway | 3 |
| release of sequestered calcium ion into cytosol | 3 |
| positive regulation of ERK1 and ERK2 cascade | 3 |
| phospholipase C-activating serotonin receptor signaling pathway | 3 |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | 2 |
| adenylate cyclase-activating serotonin receptor signaling pathway | 2 |
| temperature homeostasis | 2 |
| locomotory behavior | 2 |
| visual learning | 2 |
Indications & clinical
Indications
1 approved indication. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).
| Indication | Phase | MONDO | EFO |
|---|---|---|---|
| psychotic disorder | 4 | MONDO:0005485 | EFO:0005407 |
4 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.
| Disease (in trials) | Phase | MONDO | EFO |
|---|---|---|---|
| anxiety | 3 | MONDO:0011918 | EFO:0005230 |
| dementia | 3 | MONDO:0001627 | HP:0000726 |
| depressive disorder | 3 | MONDO:0002050 | MONDO:0002050 |
| cocaine dependence | 2 | MONDO:0005186 | EFO:0002610 |
4 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 17.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 6 |
| PHASE3 | 4 |
| Not specified | 3 |
| PHASE2 | 2 |
| PHASE1 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00014001 | PHASE4 | COMPLETED | CATIE- Schizophrenia Trial |
| NCT00802100 | PHASE4 | COMPLETED | Comparison of Optimal Antipsychotic Treatments for Adults With Schizophrenia |
| NCT01157351 | PHASE4 | COMPLETED | 15 Month Study for Adults Who Have Been Diagnosed With Schizophrenia and Incarcerated |
| NCT01193166 | PHASE4 | WITHDRAWN | Twelve Month Study Comparing Paliperidone Palmitate and Select Oral Antipsychotics in Adults With Schizophrenia Who Have Been Recently Discharged From an Inpatient Psychiatric Hospital |
| NCT02199743 | PHASE4 | COMPLETED | Lurasidone Effects on Tissue Glutamate in Schizophrenia |
| NCT02307396 | PHASE4 | COMPLETED | Evaluation of the Necessity of Long-term Pharmacological Treatment With Antipsychotics in Schizophrenic Patients |
| NCT00009204 | PHASE3 | COMPLETED | Serotonergic Pharmacotherapy for Agitation of Dementia |
| NCT02374567 | PHASE3 | TERMINATED | Pharmacovigilance in Gerontopsychiatric Patients |
| NCT02431702 | PHASE3 | COMPLETED | A Study to Compare Disease Progression and Modification Following Treatment With Paliperidone Palmitate Long-Acting Injection or Oral Antipsychotics in Participant’s With Recent-onset Schizophrenia or Schizophreniform |
| NCT04606264 | PHASE3 | COMPLETED | Recommendations of Enhanced Recovery Interventions for Patient’s Clinical Team and Collection of Associated Data |
| NCT00737256 | PHASE2 | UNKNOWN | A Double-Blind, Controlled Study of Aripiprazole in Co-Morbid Schizophrenia and Cocaine Dependence |
| NCT05762146 | PHASE2 | UNKNOWN | Networked Drug REpurposing for Mechanism-based neuroPrOtection in Acute Ischaemic STROKE |
| NCT00480246 | PHASE1 | COMPLETED | A Positron Emission Tomography (PET) Study to Assess the Degree of Dopamine-2 (D2) Receptor Occupancy in the Human Brain After Single Doses of BL-1020 or Perphenazine in Healthy Male Subjects Using [11C]Raclopride as PET Tracer |
| NCT04776499 | PHASE1 | COMPLETED | Possible Effects of Propylthiouracil, Riociguat and Perphenazine on Circulation of Healthy Volunteers |
| NCT02600741 | Not specified | COMPLETED | Family Intervention in Recent Onset Schizophrenia Treatment (FIRST) |
| NCT02893371 | Not specified | TERMINATED | Longitudinal Comparative Effectiveness of Bipolar Disorder Therapies |
| NCT03019887 | Not specified | COMPLETED | Correlation Between Cognitive Function and Relapse of Schizophrenia Regarding Dose Reduction |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 2 clinical and 26 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
607 molecules share ≥1 primary target. Top 100 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| BREXPIPRAZOLE | ChEMBL + PubChem | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| DIHYDROERGOTAMINE | ChEMBL + PubChem | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| AMOXAPINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| AZELASTINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| CARIPRAZINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| CHLORPROMAZINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| CINACALCET | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| CLOZAPINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| CYPROHEPTADINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| DOXEPIN | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| FLUPHENAZINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| HALOPERIDOL | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| IMIPRAMINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| KETANSERIN | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| KETOTIFEN | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| LOXAPINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| METHYSERGIDE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| MIANSERIN | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| NEFAZODONE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| OLANZAPINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| PROMAZINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| QUETIAPINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| RISPERIDONE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| THIORIDAZINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| THIOTHIXENE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| ZIPRASIDONE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| LATREPIRDINE | ChEMBL | Phase 3 | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| FANANSERIN | ChEMBL | Phase 2 | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| LYSERGIDE | ChEMBL | Phase 2 | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| MARITUPIRDINE | ChEMBL | Phase 2 | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| METERGOLINE | ChEMBL | Phase 2 | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| PENFLURIDOL | ChEMBL | Phase 2 | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| RITANSERIN | ChEMBL | Phase 2 | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| SPIPERONE | ChEMBL | Phase 2 | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| Pyrazinamide | PubChem | Approved | DRD2, HRH1, HTR2A, HTR2C, HTR6, HTR7 |
| DESLORATADINE | ChEMBL + PubChem | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| PALIPERIDONE | ChEMBL + PubChem | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR7 |
| AMIODARONE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| AMITRIPTYLINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| ASENAPINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| BENZTROPINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| BUSPIRONE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR7 |
| CARVEDILOL | ChEMBL | Phase 4 (approved) | DRD2, HTR2A, HTR2C, HTR6, HTR7 |
| CISAPRIDE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR7 |
| CLEMASTINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| CLOMIPRAMINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| DIBENZEPIN | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR6, HTR7 |
| EBASTINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| FLUOXETINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| FLUSPIRILENE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| HYDROXYZINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR6, HTR7 |
| ILOPERIDONE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| IPRINDOLE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| LURASIDONE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR7 |
| MAPROTILINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| METHYLERGONOVINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| NORTRIPTYLINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| PERGOLIDE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| PIMOZIDE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| PIPAMAZINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| PROCHLORPERAZINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| PROMETHAZINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| SERTINDOLE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| SUNITINIB | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| TEGASEROD | ChEMBL | Phase 4 (approved) | DRD2, HTR2A, HTR2C, HTR6, HTR7 |
| TERFENADINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| IDALOPIRDINE | ChEMBL | Phase 3 | DRD2, HTR2A, HTR2C, HTR6, HTR7 |
| LISURIDE | ChEMBL | Phase 3 | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| ZUCLOPENTHIXOL | ChEMBL | Phase 3 | DRD2, HRH1, HTR2A, HTR2C, HTR6 |
| NIGULDIPINE | ChEMBL | Phase 2 | DRD2, HRH1, HTR2C, HTR6, HTR7 |
| PIZOTYLINE | ChEMBL | Phase 2 | DRD2, HRH1, HTR2A, HTR2C, HTR7 |
| SPIRAMIDE | ChEMBL | Phase 2 | DRD2, HRH1, HTR2A, HTR6, HTR7 |
| Fidaxomicin | ChEMBL + PubChem | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C |
| PRAMIPEXOLE | ChEMBL + PubChem | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR7 |
| Propoxyphene | ChEMBL + PubChem | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C |
| TAMSULOSIN | ChEMBL + PubChem | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR7 |
| AMISULPRIDE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR7 |
| AMLODIPINE | ChEMBL | Phase 4 (approved) | DRD2, HTR2A, HTR2C, HTR6 |
| APOMORPHINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C |
| AZATADINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C |
| BENPERIDOL | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C |
| BROMOCRIPTINE | ChEMBL | Phase 4 (approved) | DRD2, HTR2A, HTR2C, HTR6 |
| BUTRIPTYLINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C |
| CYCLOBENZAPRINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C |
| DESIPRAMINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C |
| DICYCLOMINE | ChEMBL | Phase 4 (approved) | HRH1, HTR2A, HTR2C, HTR6 |
| DIETHYLSTILBESTROL | ChEMBL | Phase 4 (approved) | DRD2, HTR2A, HTR2C, HTR6 |
| DIPHENHYDRAMINE | ChEMBL | Phase 4 (approved) | HRH1, HTR2A, HTR2C, HTR6 |
| DOMPERIDONE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C |
| DOTHIEPIN | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C |
| DROPERIDOL | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C |
| DULOXETINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C |
| ECONAZOLE | ChEMBL | Phase 4 (approved) | DRD2, HTR2A, HTR2C, HTR6 |
| ERGOTAMINE | ChEMBL | Phase 4 (approved) | DRD2, HTR2A, HTR2C, HTR6 |
| LASOFOXIFENE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C |
| LOFEPRAMINE | ChEMBL | Phase 4 (approved) | DRD2, HRH1, HTR2A, HTR2C |
| MEPAZINE | ChEMBL | Phase 4 (approved) | HRH1, HTR2A, HTR2C, HTR6 |
Related Atlas pages
- Genes: HTR6, HTR7, DRD2, HRH1, HTR2A, HTR2C
- Indicated for: psychotic disorder
- In clinical trials for: anxiety, dementia, depressive disorder, cocaine dependence
- Drugs: Brexpiprazole, Dihydroergotamine, Amoxapine, Aripiprazole, Astemizole, Azelastine, Cariprazine, Chlorpromazine, Cinacalcet, Clozapine, Cyproheptadine, Doxepin, Fluphenazine, Haloperidol, Imipramine, Ketanserin, Ketotifen, Loxapine, Methysergide, Mianserin, Nefazodone, Olanzapine, Promazine, Quetiapine, Risperidone, Thioridazine, Thiothixene, Ziprasidone, Latrepirdine, Pyrazinamide, Desloratadine, Paliperidone, Amiodarone, Amitriptyline, Asenapine, Benztropine, Buspirone, Carvedilol, Cisapride, Clemastine, Clomipramine, Clotrimazole, Dibenzepin, Ebastine, Fluoxetine, Fluspirilene, Hydroxyzine, Iloperidone, Iprindole, Lurasidone, Maprotiline, Methylergonovine, Nortriptyline, Pergolide, Pimozide, Pipamazine, Prochlorperazine, Promethazine, Sertindole, Sunitinib, Tegaserod, Terfenadine, Idalopirdine, Lisuride, Zuclopenthixol, Fidaxomicin, Pramipexole, Propoxyphene, Tamsulosin, Amisulpride, Amlodipine, Apomorphine, Azatadine, Benperidol, Bromocriptine, Butriptyline, Cyclobenzaprine, Desipramine, Dicyclomine, Diethylstilbestrol, Diphenhydramine, Domperidone, Dothiepin, Droperidol, Duloxetine, Econazole, Ergotamine, Lasofoxifene, Lofepramine, Mepazine