Vilazodone
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Also known as EMD 515259EMD 68843 BASEEMD-515259Emd-68843 baseVilazodonaVILAZODONE HYDROCHLORIDE
Summary
Vilazodone (CHEMBL439849) is an approved small-molecule antidepressant (ATC N06AX24) targeting HTR1A, DRD2, and DRD3; indicated across 4 conditions including depressive disorder and generalized anxiety disorder.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: N06AX24
- Targets: 6 (HTR1A, DRD2, DRD3…)
- Indications: 4 conditions
- Clinical trials: 23
- Chemistry: 441.5 Da · C26H27N5O2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL439849 |
| Name | Vilazodone |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 6918314 |
| ChEBI | CHEBI:70707 |
| ATC | N06AX24 |
| Molecular formula | C26H27N5O2 |
| Molecular weight | 441.5 |
| InChIKey | SGEGOXDYSFKCPT-UHFFFAOYSA-N |
SMILES: C1CN(CCN1CCCCC2=CNC3=C2C=C(C=C3)C#N)C4=CC5=C(C=C4)OC(=C5)C(=O)N
IUPAC name: 5-[4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl]-1-benzofuran-2-carboxamide
ChEBI definition: A 1-benzofuran that is 5-(piperazin-1-yl}-1-benzofuran-2-carboxamide having a (5-cyanoindol-3-yl)butyl group attached at position N-4 on the piperazine ring. Used for the treatment of major depressive disorder.
Pharmacological roles (ChEBI): antidepressant, serotonergic agonist, serotonin uptake inhibitor.
Also known as: EMD 515259, EMD 68843 BASE, EMD-515259, Emd-68843 base, Vilazodona, Vilazodone, VILAZODONE, VILAZODONE HYDROCHLORIDE
Parent form; salt/anhydrous children: CHEMBL1615374
Patent coverage: 626 distinct patent families (1,555 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 1,291 (83%) 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 |
|---|---|---|---|---|---|
| HTR1A | 5-HT1A receptor | Partial agonist | 9.52 | 0% | P08908 |
| DRD2 | D2 receptor | Agonist | 6.18 | 0% | P14416 |
| DRD3 | D3 receptor | Agonist | 7.15 | 0% | P35462 |
| HRH1 | H1 receptor | Agonist | 6.5 | 0% | P35367 |
| SLC6A4 | SERT | Inhibition | 9.3 | 0.7% | P31645 |
| HTR4 | 5-HT4 receptor | Agonist | 6.6 | 0% | Q13639 |
Broader ChEMBL bioactivity targets: 24 (assay-derived). Sample: Serotonin 3 (5-HT3) receptor, Adrenergic receptor alpha-1, Adrenergic receptor alpha-2, 5-hydroxytryptamine receptor 1A, D(2) dopamine receptor, Sodium-dependent noradrenaline transporter, Sodium-dependent serotonin transporter, Sodium-dependent dopamine transporter, Voltage-gated inwardly rectifying potassium channel KCNH2, 5-hydroxytryptamine receptor 1A, Sodium-dependent serotonin transporter, D(3) dopamine receptor, 5-hydroxytryptamine receptor 7, Acetylcholinesterase, Acetylcholinesterase, 5-hydroxytryptamine receptor 2A, 5-hydroxytryptamine receptor 7, 5-hydroxytryptamine receptor 2C, D(4) dopamine receptor, 5-hydroxytryptamine receptor 6.
Bioactivity
ChEMBL activities: 47 potent at pChembl ≥ 5 of 50 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| HTR1A | 9.96 | IC50 | 0.11 | nM | CHEMBL_ACT_23295777 |
| HTR1A | 9.92 | EC50 | 0.12 | nM | CHEMBL_ACT_18291168 |
| HTR1A | 9.92 | EC50 | 0.12 | nM | CHEMBL_ACT_18996974 |
| HTR1A | 9.7 | IC50 | 0.2 | nM | CHEMBL_ACT_19114059 |
| HTR1A | 9.7 | Ki | 0.2 | nM | CHEMBL_ACT_19283857 |
| HTR1A | 9.52 | Ki | 0.3 | nM | CHEMBL_ACT_10913281 |
| P19327 | 9.52 | IC50 | 0.3 | nM | CHEMBL_ACT_1467775 |
| HTR1A | 9.52 | EC50 | 0.3 | nM | CHEMBL_ACT_26120074 |
| SLC6A4 | 9.4 | IC50 | 0.4 | nM | CHEMBL_ACT_18291221 |
| SLC6A4 | 9.4 | IC50 | 0.4 | nM | CHEMBL_ACT_24416218 |
| SLC6A4 | 9.4 | IC50 | 0.4 | nM | CHEMBL_ACT_24917639 |
| SLC6A4 | 9.32 | IC50 | 0.48 | nM | CHEMBL_ACT_25447759 |
| SLC6A4 | 9.3 | Ki | 0.5 | nM | CHEMBL_ACT_10913304 |
| P31652 | 9.3 | IC50 | 0.5 | nM | CHEMBL_ACT_1467788 |
| P31652 | 9.3 | IC50 | 0.5 | nM | CHEMBL_ACT_19114067 |
| P31652 | 9.3 | IC50 | 0.5 | nM | CHEMBL_ACT_19283888 |
| P31652 | 9.3 | IC50 | 0.5 | nM | CHEMBL_ACT_26120075 |
| P31652 | 9.17 | IC50 | 0.67 | nM | CHEMBL_ACT_23295744 |
| SLC6A4 | 9.17 | IC50 | 0.67 | nM | CHEMBL_ACT_26120115 |
| HTR1A | 9.1 | EC50 | 0.79 | nM | CHEMBL_ACT_24416193 |
| HTR1A | 8.99 | EC50 | 1.02 | nM | CHEMBL_ACT_26120090 |
| P31652 | 8.96 | IC50 | 1.1 | nM | CHEMBL_ACT_1466031 |
| SLC6A4 | 8.72 | Ki | 1.9 | nM | CHEMBL_ACT_18891579 |
| P19327 | 8.36 | IC50 | 4.4 | nM | CHEMBL_ACT_1466030 |
| HTR1A | 8.01 | Ki | 9.7 | nM | CHEMBL_ACT_18891608 |
| P31652 | 7.6 | IC50 | 25 | nM | CHEMBL_ACT_24966874 |
| HTR1A | 7.55 | Ki | 28 | nM | CHEMBL_ACT_24966879 |
| P19020 | 7.15 | IC50 | 71 | nM | CHEMBL_ACT_1467668 |
| P61169 | 7.02 | IC50 | 95 | nM | CHEMBL_ACT_1466032 |
| SLC6A2 | 6.8 | IC50 | 158.1 | nM | CHEMBL_ACT_24416283 |
| Q62758 | 6.6 | IC50 | 252 | nM | CHEMBL_ACT_1467785 |
| SLC6A3 | 6.53 | IC50 | 295 | nM | CHEMBL_ACT_24416286 |
| DRD2 | 6.18 | Ki | 666 | nM | CHEMBL_ACT_10913396 |
| P61169 | 6.18 | IC50 | 666 | nM | CHEMBL_ACT_1467667 |
| P14842 | 5.82 | IC50 | 1510 | nM | CHEMBL_ACT_1467782 |
| ADRA1D | 5.7 | IC50 | 1980 | nM | CHEMBL_ACT_1467773 |
| P08909 | 5.7 | IC50 | 2000 | nM | CHEMBL_ACT_1467783 |
| P31388 | 5.52 | IC50 | 3000 | nM | CHEMBL_ACT_1467786 |
| P32305 | 5.52 | IC50 | 3000 | nM | CHEMBL_ACT_1467787 |
| P30729 | 5.47 | IC50 | 3400 | nM | CHEMBL_ACT_1467669 |
| HTR7 | 5.41 | Ki | 3900 | nM | CHEMBL_ACT_19283870 |
| P28565 | 5.4 | IC50 | 4000 | nM | CHEMBL_ACT_1467780 |
| P35563 | 5.37 | IC50 | 4300 | nM | CHEMBL_ACT_1467784 |
| P28564 | 5.3 | IC50 | 5000 | nM | CHEMBL_ACT_1467666 |
| KCNH2 | 5.26 | IC50 | 5550 | nM | CHEMBL_ACT_24416254 |
| KCNH2 | 5.25 | IC50 | 5600 | nM | CHEMBL_ACT_24917700 |
| ADRA2A | 5.22 | IC50 | 6000 | nM | CHEMBL_ACT_1467774 |
Target pathways
Aggregated over 6 target gene(s): HTR1A, DRD2, DRD3, HRH1, SLC6A4, HTR4.
Top Reactome pathways
17 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signal Transduction | 2 | HTR1A, HTR4 |
| Signaling by GPCR | 2 | HTR1A, HTR4 |
| Class A/1 (Rhodopsin-like receptors) | 2 | HTR1A, HTR4 |
| Amine ligand-binding receptors | 2 | HTR1A, HTR4 |
| Dopamine receptors | 2 | DRD2, DRD3 |
| Serotonin receptors | 2 | HTR1A, HTR4 |
| GPCR ligand binding | 2 | HTR1A, HTR4 |
| Neurotransmitter clearance | 1 | SLC6A4 |
| Transmission across Chemical Synapses | 1 | SLC6A4 |
| Neuronal System | 1 | SLC6A4 |
| Serotonin clearance from the synaptic cleft | 1 | SLC6A4 |
| GPCR downstream signalling | 1 | HTR4 |
| Histamine receptors | 1 | HRH1 |
| G alpha (q) signalling events | 1 | HRH1 |
| G alpha (s) signalling events | 1 | HTR4 |
| G alpha (i) signalling events | 1 | DRD3 |
| SLC-mediated transport of neurotransmitters | 1 | SLC6A4 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| G protein-coupled receptor signaling pathway | 5 |
| signal transduction | 5 |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | 3 |
| chemical synaptic transmission | 3 |
| visual learning | 3 |
| response to xenobiotic stimulus | 3 |
| behavioral response to cocaine | 3 |
| adenylate cyclase-inhibiting serotonin receptor signaling pathway | 2 |
| adult behavior | 2 |
| adenylate cyclase-activating G protein-coupled receptor signaling pathway | 2 |
| G protein-coupled serotonin receptor signaling pathway | 2 |
| response to hypoxia | 2 |
| G protein-coupled receptor internalization | 2 |
| intracellular calcium ion homeostasis | 2 |
| adenylate cyclase-inhibiting dopamine receptor signaling pathway | 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 |
|---|---|---|---|
| depressive disorder | 4 | MONDO:0002050 | MONDO:0002009 |
2 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 |
|---|---|---|---|
| generalized anxiety disorder | 3 | MONDO:0001942 | EFO:1001892 |
| cannabis dependence | 2 | MONDO:0005689 | EFO:0007191 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 23.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 9 |
| PHASE4 | 6 |
| PHASE2 | 4 |
| Not specified | 3 |
| PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01473381 | PHASE4 | COMPLETED | Safety and Efficacy of Vilazodone in Major Depressive Disorder |
| NCT01473394 | PHASE4 | COMPLETED | Safety, Efficacy, and Tolerability of Vilazodone in Major Depressive Disorder |
| NCT01573598 | PHASE4 | COMPLETED | Safety and Efficacy of Vilazodone in Major Depressive Disorder |
| NCT01856127 | PHASE4 | TERMINATED | Does Vilazodone Help With Antidepressant-associated Sexual Dysfunction? |
| NCT01999920 | PHASE4 | COMPLETED | Vilazodone for Separation Anxiety Disorder |
| NCT02028026 | PHASE4 | WITHDRAWN | The Effects of Vilazodone on Glutamate in the Anterior Cingulate Cortex in Anxious Unipolar Depressives |
| NCT00285376 | PHASE3 | COMPLETED | Effectiveness Study of Vilazodone to Treat Depression and to Discover Genetic Markers Associated With Response |
| NCT00644358 | PHASE3 | COMPLETED | A One Year Open Label Study Assessing the Safety and Tolerability of Vilazodone in Patients With Major Depressive Disorder (MDD) |
| NCT00683592 | PHASE3 | COMPLETED | Randomized, Double-Blind, Placebo Controlled Study of Vilazodone’s Efficacy, Safety, and Biomarkers of Response in Major Depressive Disorder (MDD) |
| NCT01629966 | PHASE3 | COMPLETED | Safety, Efficacy and Tolerability of Vilazodone in Generalized Anxiety Disorder |
| NCT01844115 | PHASE3 | COMPLETED | Safety, Efficacy and Tolerability of Vilazodone in (GAD) Generalized Anxiety Disorder |
| NCT01878292 | PHASE3 | COMPLETED | Safety and Efficacy of Vilazodone in Adolescent Patients With Major Depressive Disorder |
| NCT02015546 | PHASE3 | COMPLETED | Switching From Generic Selective Serotonin Reuptake Inhibitors (SSRIs) and Selective Serotonin and Norepinephrine Reuptake Inhibitors (SNRIs) to Three Different Dose Initiation Strategies With Vilazodone |
| NCT02372799 | PHASE3 | COMPLETED | Safety and Efficacy of Vilazodone in Pediatric Patients With Major Depressive Disorder (VLZ-MD-22) |
| NCT02436239 | PHASE3 | COMPLETED | A Study of Vilazodone in Pediatric Patients With Major Depressive Disorder |
| NCT00290914 | PHASE2 | COMPLETED | Safety and Efficacy Study of Vilazodone and Discovering Genetic Markers Associated With Response in Patients With Major Depressive Disorder |
| NCT01574183 | PHASE2 | COMPLETED | Vilazodone Treatment for Marijuana Dependence |
| NCT01742832 | PHASE2 | COMPLETED | Double-Blind Treatment of Major Depressive Disorder With Vilazodone |
| NCT01828515 | PHASE2 | COMPLETED | Vilazodone for Corticosteroid-Induced Memory Impairment |
| NCT02097147 | PHASE1 | COMPLETED | Study to Evaluate the Sexual Functioning of Healthy Adults After Receiving Vilazodone, Paroxetine or Placebo |
| NCT01680900 | Not specified | COMPLETED | Vilazodone for Menopausal Hot Flashes |
| NCT01712321 | Not specified | UNKNOWN | Study of Vilazodone to Treat Social Anxiety Disorder |
| NCT02893371 | Not specified | TERMINATED | Longitudinal Comparative Effectiveness of Bipolar Disorder Therapies |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
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.
847 molecules share ≥1 primary target. Top 100 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CYPROHEPTADINE | ChEMBL + PubChem | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, HTR4, SLC6A4 |
| HALOPERIDOL | ChEMBL + PubChem | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, HTR4, SLC6A4 |
| IMIPRAMINE | ChEMBL + PubChem | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, HTR4, SLC6A4 |
| CISAPRIDE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, HTR4, SLC6A4 |
| DESLORATADINE | ChEMBL + PubChem | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| DIHYDROERGOTAMINE | ChEMBL + PubChem | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| TEGASEROD | ChEMBL + PubChem | Phase 4 (approved) | DRD2, DRD3, HTR1A, HTR4, SLC6A4 |
| ACETOPHENAZINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| AMITRIPTYLINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| AMOXAPINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| APOMORPHINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| ASENAPINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| BREXPIPRAZOLE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| BROMPERIDOL | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| CABERGOLINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| CARIPRAZINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| CHLORPROMAZINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| CHLORPROTHIXENE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| CINACALCET | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| CINNARIZINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| CLEMASTINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| CLOMIPRAMINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| CLOZAPINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| CYCLOBENZAPRINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| DIBENZEPIN | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| DOMPERIDONE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| DOXEPIN | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| DULOXETINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| EBASTINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| EPALRESTAT | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| FLUPHENAZINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| ILOPERIDONE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| KETANSERIN | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| LOXAPINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| MIANSERIN | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| NAFTOPIDIL | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| NEFAZODONE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| NORTRIPTYLINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| OLANZAPINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| PERPHENAZINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| PIMOZIDE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| PIPERACETAZINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| PRENYLAMINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| PROCHLORPERAZINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| PROMAZINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| PROMETHAZINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| RISPERIDONE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| ROTIGOTINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| SERTINDOLE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| SERTRALINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| SUNITINIB | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| TERFENADINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| THIETHYLPERAZINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| THIORIDAZINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| TRAZODONE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| TRIFLUOPERAZINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| ZIPRASIDONE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| MELITRACEN | ChEMBL | Phase 3 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| OPIPRAMOL | ChEMBL | Phase 3 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| OTILONIUM BROMIDE | ChEMBL | Phase 3 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| URAPIDIL | ChEMBL | Phase 3 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| ZUCLOPENTHIXOL | ChEMBL | Phase 3 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| AMOSULALOL | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| BENZETHONIUM | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| CLOTHIAPINE | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| DOMIPHEN | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| FANANSERIN | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| FLUNARIZINE | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| IFENPRODIL | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| MEQUITAZINE | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| METERGOLINE | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| NEMONAPRIDE | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| NIGULDIPINE | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| PENFLURIDOL | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| PIZOTYLINE | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| RITANSERIN | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| SPIPERONE | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| SPIRAMIDE | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| THIOPROPERAZINE | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| ZOTEPINE | ChEMBL | Phase 2 | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| Afatinib | PubChem | Approved | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| Apixaban | PubChem | Approved | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| Binimetinib | PubChem | Approved | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| Bosentan | PubChem | Approved | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| chenodiol | PubChem | Approved | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| Fidaxomicin | PubChem | Approved | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| Fulvestrant | PubChem | Approved | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| Imipenem | PubChem | Approved | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| Linagliptin | PubChem | Approved | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| Propoxyphene | PubChem | Approved | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| Pyrazinamide | PubChem | Approved | DRD2, DRD3, HRH1, HTR1A, SLC6A4 |
| GENTIAN VIOLET | ChEMBL + PubChem | Phase 4 (approved) | DRD2, DRD3, HTR1A, SLC6A4 |
| PRAMIPEXOLE | ChEMBL + PubChem | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | DRD3, HRH1, HTR1A, SLC6A4 |
| TAMSULOSIN | ChEMBL + PubChem | Phase 4 (approved) | DRD2, DRD3, HRH1, HTR1A |
| AMIODARONE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, SLC6A4 |
| AZELASTINE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HRH1, SLC6A4 |
| BAZEDOXIFENE | ChEMBL | Phase 4 (approved) | DRD2, DRD3, HTR1A, SLC6A4 |
Related Atlas pages
- Genes: HTR1A, DRD2, DRD3, HRH1, SLC6A4, HTR4
- Indicated for: depressive disorder
- In clinical trials for: generalized anxiety disorder, cannabis dependence
- Drugs: Cyproheptadine, Haloperidol, Imipramine, Cisapride, Desloratadine, Dihydroergotamine, Tegaserod, Acetophenazine, Amitriptyline, Amoxapine, Apomorphine, Aripiprazole, Asenapine, Astemizole, Brexpiprazole, Bromperidol, Cabergoline, Cariprazine, Chlorpromazine, Chlorprothixene, Cinacalcet, Cinnarizine, Clemastine, Clomipramine, Clozapine, Cyclobenzaprine, Dibenzepin, Domperidone, Doxepin, Duloxetine, Ebastine, Epalrestat, Fluphenazine, Iloperidone, Ketanserin, Loxapine, Mianserin, Naftopidil, Nefazodone, Nortriptyline, Olanzapine, Perphenazine, Pimozide, Piperacetazine, Prenylamine, Prochlorperazine, Promazine, Promethazine, Risperidone, Rotigotine, Sertindole, Sertraline, Sunitinib, Terfenadine, Thiethylperazine, Thioridazine, Trazodone, Trifluoperazine, Ziprasidone, Melitracen, Opipramol, Otilonium Bromide, Urapidil, Zuclopenthixol, Afatinib, Apixaban, Binimetinib, Bosentan, chenodiol, Fidaxomicin, Fulvestrant, Imipenem, Linagliptin, Propoxyphene, Pyrazinamide, Pramipexole, Regorafenib, Tamsulosin, Amiodarone, Azelastine, Bazedoxifene