Doxepin
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Also known as DoxepinaDoxepineSinepinSinequanadapinSID174006603rac-Doxepine
Summary
Doxepin (CHEMBL1628227) is an approved small-molecule antidepressant (ATC D04AX01) targeting HRH1, SLC6A2, and SLC6A4; indicated across 10 conditions including depressive disorder and anxiety.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: D04AX01 (+1 more)
- Targets: 3 (HRH1, SLC6A2, SLC6A4)
- Indications: 10 conditions
- Clinical trials: 14
- Chemistry: 279.4 Da · C19H21NO
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1628227 |
| Name | Doxepin |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 3158 |
| ChEBI | CHEBI:4710 |
| ATC | D04AX01, N06AA12 |
| Molecular formula | C19H21NO |
| Molecular weight | 279.4 |
| InChIKey | ODQWQRRAPPTVAG-UHFFFAOYSA-N |
SMILES: CN(C)CCC=C1C2=CC=CC=C2COC3=CC=CC=C31
IUPAC name: 3-(6H-benzo[c][1]benzoxepin-11-ylidene)-N,N-dimethylpropan-1-amine
ChEBI definition: A dibenzooxepine that is 6,11-dihydrodibenzo[b,e]oxepine substituted by a 3-(dimethylamino)propylidene group at position 11. It is used as an antidepressant drug.
Pharmacological roles (ChEBI): antidepressant.
Also known as: Doxepin, Doxepina, Doxepine, Sinepin, Sinequan, doxepin, adapin, DOXEPINE, SID174006603, DOXEPIN, rac-Doxepine
Parent form; salt/anhydrous children: CHEMBL1628234
Patent coverage: 7,727 distinct patent families (28,171 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 28,169 (100%) 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 |
|---|---|---|---|---|---|
| HRH1 | H1 receptor | Antagonist | 10 | 0% | P35367 |
| SLC6A2 | NET | Inhibition | 7.54 | 0.4% | P23975 |
| SLC6A4 | SERT | Inhibition | 7.17 | 0.7% | P31645 |
Broader ChEMBL bioactivity targets: 35 (assay-derived). Sample: Muscarinic acetylcholine receptor M4, 5-hydroxytryptamine receptor 2B, D(1B) dopamine receptor, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Histamine H2 receptor, Alpha-2B adrenergic receptor, Muscarinic acetylcholine receptor M5, D(1A) dopamine receptor, Serotonin (5-HT) receptor, Muscarinic acetylcholine receptor M2, 5-hydroxytryptamine receptor 1A, Muscarinic acetylcholine receptor M1, D(2) dopamine receptor, D(4) dopamine receptor, Sodium-dependent noradrenaline transporter, Alpha-1D adrenergic receptor, 5-hydroxytryptamine receptor 2A, 5-hydroxytryptamine receptor 2C, Sodium-dependent serotonin transporter.
Bioactivity
ChEMBL activities: 93 potent at pChembl ≥ 5 of 95 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| P43140 | 11 | IC50 | 0.01 | nM | CHEMBL_ACT_764854 |
| HRH1 | 10.18 | Ki | 0.07 | nM | CHEMBL_ACT_7690122 |
| HRH1 | 9.75 | Ki | 0.18 | nM | CHEMBL_ACT_7945362 |
| HRH1 | 9.6 | Ki | 0.25 | nM | CHEMBL_ACT_16792480 |
| HRH1 | 9.24 | IC50 | 0.57 | nM | CHEMBL_ACT_7690121 |
| HRH1 | 9 | AC50 | 1 | nM | CHEMBL_ACT_25211975 |
| CHRM4 | 8.23 | Ki | 5.84 | nM | CHEMBL_ACT_7690156 |
| HTR2A | 7.96 | Ki | 11 | nM | CHEMBL_ACT_7681540 |
| CHRM3 | 7.82 | Ki | 15 | nM | CHEMBL_ACT_7690154 |
| CHRM1 | 7.75 | Ki | 18 | nM | CHEMBL_ACT_7690150 |
| CHRM5 | 7.72 | Ki | 19 | nM | CHEMBL_ACT_7690158 |
| ADRA1A | 7.67 | AC50 | 21.5 | nM | CHEMBL_ACT_25137619 |
| SLC6A4 | 7.66 | Ki | 22 | nM | CHEMBL_ACT_7681552 |
| HTR2C | 7.62 | Ki | 24 | nM | CHEMBL_ACT_7681544 |
| CHRM5 | 7.58 | IC50 | 26 | nM | CHEMBL_ACT_7690157 |
| SLC6A2 | 7.54 | IC50 | 29 | nM | CHEMBL_ACT_7688045 |
| SLC6A2 | 7.54 | Ki | 29 | nM | CHEMBL_ACT_7688046 |
| ADRA2B | 7.5 | Ki | 32 | nM | CHEMBL_ACT_7688036 |
| P15823 | 7.48 | Ki | 33 | nM | CHEMBL_ACT_7688030 |
| HTR2A | 7.42 | IC50 | 38 | nM | CHEMBL_ACT_7681539 |
| HTR2A | 7.38 | AC50 | 42.2 | nM | CHEMBL_ACT_25173431 |
| SLC6A4 | 7.38 | IC50 | 42 | nM | CHEMBL_ACT_7681551 |
| CHRM4 | 7.38 | IC50 | 42 | nM | CHEMBL_ACT_7690155 |
| P43140 | 7.37 | Ki | 43 | nM | CHEMBL_ACT_7688028 |
| HTR2C | 7.34 | IC50 | 46 | nM | CHEMBL_ACT_7681543 |
| HRH2 | 7.28 | AC50 | 52 | nM | CHEMBL_ACT_25114317 |
| HTR2B | 7.25 | Ki | 56 | nM | CHEMBL_ACT_7681542 |
| ADRA1D | 7.24 | Ki | 58 | nM | CHEMBL_ACT_7688032 |
| P15823 | 7.22 | IC50 | 60 | nM | CHEMBL_ACT_7688029 |
| ADRA1A | 7.16 | AC50 | 68.9 | nM | CHEMBL_ACT_25138323 |
| CHRM3 | 7.16 | IC50 | 69 | nM | CHEMBL_ACT_7690153 |
| ADRA2B | 7.15 | IC50 | 71 | nM | CHEMBL_ACT_7688035 |
| HTR2C | 7.14 | AC50 | 72 | nM | CHEMBL_ACT_25131285 |
| CHRM1 | 7.11 | IC50 | 77 | nM | CHEMBL_ACT_7690149 |
| HTR2B | 7.05 | IC50 | 89 | nM | CHEMBL_ACT_7681541 |
| CHRM2 | 7.04 | Ki | 92 | nM | CHEMBL_ACT_7690152 |
| HTR6 | 6.98 | Ki | 105 | nM | CHEMBL_ACT_12059578 |
| P43140 | 6.97 | IC50 | 107 | nM | CHEMBL_ACT_7688027 |
| DRD3 | 6.96 | AC50 | 110 | nM | CHEMBL_ACT_25193003 |
| ADRA1D | 6.93 | IC50 | 118 | nM | CHEMBL_ACT_7688031 |
| SLC6A2 | 6.92 | AC50 | 119.2 | nM | CHEMBL_ACT_25145698 |
| HTR2B | 6.85 | AC50 | 140.4 | nM | CHEMBL_ACT_25163970 |
| HTR6 | 6.83 | Ki | 149 | nM | CHEMBL_ACT_7681550 |
| ADRA2C | 6.82 | Ki | 150 | nM | CHEMBL_ACT_7688038 |
| ADRA1A | 6.8 | AC50 | 157.6 | nM | CHEMBL_ACT_25218590 |
| SLC6A2 | 6.75 | AC50 | 180 | nM | CHEMBL_ACT_25144482 |
| P08909 | 6.7 | IC50 | 200 | nM | CHEMBL_ACT_764853 |
| ADRA2B | 6.68 | AC50 | 210 | nM | CHEMBL_ACT_25143177 |
| HTR6 | 6.66 | AC50 | 217.9 | nM | CHEMBL_ACT_25118891 |
| CHRM5 | 6.66 | AC50 | 219.5 | nM | CHEMBL_ACT_25137377 |
| CHRM1 | 6.6 | AC50 | 250 | nM | CHEMBL_ACT_25134914 |
| CHRM2 | 6.59 | IC50 | 258 | nM | CHEMBL_ACT_7690151 |
| SIGMAR1 | 6.58 | Ki | 265 | nM | CHEMBL_ACT_7681554 |
| DRD1 | 6.54 | AC50 | 286.2 | nM | CHEMBL_ACT_25114908 |
| DRD1 | 6.52 | AC50 | 300.5 | nM | CHEMBL_ACT_25114600 |
| HTR6 | 6.5 | IC50 | 320 | nM | CHEMBL_ACT_7681549 |
| DRD1 | 6.46 | Ki | 344 | nM | CHEMBL_ACT_7690088 |
| ADRA1A | 6.44 | AC50 | 359.9 | nM | CHEMBL_ACT_25217700 |
| CHRM3 | 6.43 | AC50 | 370 | nM | CHEMBL_ACT_25136180 |
| SLC6A4 | 6.38 | AC50 | 419.4 | nM | CHEMBL_ACT_25151025 |
| DRD3 | 6.33 | Ki | 473 | nM | CHEMBL_ACT_7690092 |
| CHRM1 | 6.31 | AC50 | 490.8 | nM | CHEMBL_ACT_25209948 |
| ADRA2A | 6.3 | Ki | 501 | nM | CHEMBL_ACT_7688034 |
| CHRM4 | 6.29 | AC50 | 512.4 | nM | CHEMBL_ACT_25144397 |
| CHRM2 | 6.25 | AC50 | 561.4 | nM | CHEMBL_ACT_25195131 |
| CHRM2 | 6.23 | AC50 | 589 | nM | CHEMBL_ACT_25195434 |
| SIGMAR1 | 6.2 | IC50 | 631 | nM | CHEMBL_ACT_7681553 |
| DRD1 | 6.16 | IC50 | 688 | nM | CHEMBL_ACT_7690087 |
| DRD4 | 6.14 | AC50 | 725.5 | nM | CHEMBL_ACT_25127280 |
| HTR1A | 6.11 | AC50 | 775.8 | nM | CHEMBL_ACT_25164340 |
| ADRA2C | 6.09 | AC50 | 810 | nM | CHEMBL_ACT_25147340 |
| P19327 | 6.06 | Ki | 868 | nM | CHEMBL_ACT_7681536 |
| HTR1A | 6.03 | AC50 | 924.9 | nM | CHEMBL_ACT_25164722 |
| ADRA2C | 5.99 | IC50 | 1029 | nM | CHEMBL_ACT_7688037 |
| DRD3 | 5.95 | AC50 | 1134 | nM | CHEMBL_ACT_25194231 |
| HTR2B | 5.92 | AC50 | 1200 | nM | CHEMBL_ACT_25227023 |
| HTR5A | 5.9 | AC50 | 1264 | nM | CHEMBL_ACT_25163895 |
| ADRA2A | 5.88 | IC50 | 1335 | nM | CHEMBL_ACT_7688033 |
| DRD3 | 5.86 | IC50 | 1393 | nM | CHEMBL_ACT_7690091 |
| DRD2 | 5.85 | AC50 | 1400 | nM | CHEMBL_ACT_25139801 |
| HTR7 | 5.82 | AC50 | 1526 | nM | CHEMBL_ACT_25119039 |
| P19327 | 5.82 | IC50 | 1519 | nM | CHEMBL_ACT_7681535 |
| DRD5 | 5.8 | AC50 | 1569 | nM | CHEMBL_ACT_25127513 |
| P47747 | 5.8 | IC50 | 1600 | nM | CHEMBL_ACT_764858 |
| HRH2 | 5.74 | Ki | 1836 | nM | CHEMBL_ACT_7690124 |
| HRH2 | 5.73 | IC50 | 1867 | nM | CHEMBL_ACT_7690123 |
| HTR2A | 5.7 | AC50 | 2000 | nM | CHEMBL_ACT_25224685 |
| SLC6A4 | 5.6 | AC50 | 2500 | nM | CHEMBL_ACT_25149818 |
| CHRM2 | 5.6 | AC50 | 2500 | nM | CHEMBL_ACT_25213232 |
| OPRK1 | 5.57 | AC50 | 2700 | nM | CHEMBL_ACT_25128948 |
| KCNH2 | 5.4 | AC50 | 4000 | nM | CHEMBL_ACT_25117070 |
| ADRA2A | 5.29 | AC50 | 5176 | nM | CHEMBL_ACT_25156127 |
| ADRA2A | 5.23 | AC50 | 5923 | nM | CHEMBL_ACT_25155801 |
Target pathways
Aggregated over 3 target gene(s): HRH1, SLC6A2, SLC6A4.
Top Reactome pathways
14 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| SLC-mediated transport of neurotransmitters | 2 | SLC6A2, SLC6A4 |
| Neurotransmitter clearance | 1 | SLC6A4 |
| Transmission across Chemical Synapses | 1 | SLC6A4 |
| Neuronal System | 1 | SLC6A4 |
| Disease | 1 | SLC6A2 |
| Serotonin clearance from the synaptic cleft | 1 | SLC6A4 |
| Transport of small molecules | 1 | SLC6A2 |
| Histamine receptors | 1 | HRH1 |
| G alpha (q) signalling events | 1 | HRH1 |
| R-HSA-425366 | 1 | SLC6A2 |
| SLC-mediated transmembrane transport | 1 | SLC6A2 |
| SLC transporter disorders | 1 | SLC6A2 |
| Defective SLC6A2 causes orthostatic intolerance (OI) | 1 | SLC6A2 |
| Disorders of transmembrane transporters | 1 | SLC6A2 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| chemical synaptic transmission | 2 |
| memory | 2 |
| neurotransmitter transport | 2 |
| amino acid transport | 2 |
| response to xenobiotic stimulus | 2 |
| obsolete monoamine transport | 2 |
| sodium ion transmembrane transport | 2 |
| transmembrane transport | 2 |
| neurotransmitter reuptake | 2 |
| inflammatory response | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | 1 |
| phospholipase C-activating G protein-coupled receptor signaling pathway | 1 |
| visual learning | 1 |
| regulation of vascular permeability | 1 |
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:0002050 |
6 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 |
| urticaria | 3 | MONDO:0005492 | EFO:0005531 |
| irritable bowel syndrome | 2 | MONDO:0005052 | EFO:0000555 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| sleep disorder | 2 | MONDO:0100081 | EFO:0008568 |
3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 14.
Phase distribution
| Phase | Trials |
|---|---|
| Not specified | 5 |
| PHASE4 | 4 |
| PHASE3 | 2 |
| PHASE2 | 2 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT07542756 | PHASE4 | NOT_YET_RECRUITING | A SMART Approach to Evaluating the Benefits of Common Prescription and OTC Medications for Insomnia |
| NCT07598734 | PHASE4 | NOT_YET_RECRUITING | Doxepin Alone or Combined With Ramelteon Versus Placebo for Improving Sleep Quality After Primary Total Knee Arthroplasty |
| NCT00465972 | PHASE4 | COMPLETED | The Treatment of Insomnia in Patients With HIV Disease |
| NCT03758079 | PHASE4 | COMPLETED | Comparison of Gabapentin With Doxepin in the Management of Uremic Pruritus |
| NCT02374567 | PHASE3 | TERMINATED | Pharmacovigilance in Gerontopsychiatric Patients |
| NCT05115136 | PHASE3 | UNKNOWN | Using Doxepin for Urticaria |
| NCT00755495 | PHASE2 | COMPLETED | Safety and Efficacy of Ramelteon and Doxepin in Subjects With Chronic Insomnia |
| NCT01268709 | PHASE2 | COMPLETED | Effect of Doxepin and Nortriptyline on Irritable Bowel Syndrome |
| NCT01489982 | EARLY_PHASE1 | COMPLETED | Treatments for Insomnia in Patients With Parkinson’s Disease |
| NCT06017895 | Not specified | RECRUITING | Doxepin Solution for Alleviation of Stubborn Breakthrough Pain Induced by Swallowing in Patients Receiving Radiotherapy for Nasopharyngeal Carcinoma |
| NCT02893371 | Not specified | TERMINATED | Longitudinal Comparative Effectiveness of Bipolar Disorder Therapies |
| NCT04554888 | Not specified | COMPLETED | Characterization of New Human Models of Non-histaminergic Itch and Their Interaction With the TRPM8 Receptor |
| NCT04588532 | Not specified | COMPLETED | Characterization of BAM8-22 as a New Surrogate Model of Non-histaminergic Itch |
| NCT05107999 | Not specified | UNKNOWN | Stigma and Efficacy of Zhizhu Kuanzhong Capsules |
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.
695 molecules share ≥1 primary target. Top 100 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| ACLIDINIUM BROMIDE | ChEMBL + PubChem | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| AMITRIPTYLINE | ChEMBL + PubChem | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| Crizotinib | ChEMBL + PubChem | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| DESLORATADINE | ChEMBL + PubChem | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| DIHYDROERGOTAMINE | ChEMBL + PubChem | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| Olodaterol | ChEMBL + PubChem | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| Tadalafil | ChEMBL + PubChem | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| ACETOPHENAZINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| AMIODARONE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| AMOXAPINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| ASENAPINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| ATOMOXETINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| AZELASTINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| BENFLUOREX | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| BENZTROPINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| BEPRIDIL | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| BREXPIPRAZOLE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| BROMPERIDOL | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| BROMPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| BUPROPION | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| CABERGOLINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| CARBINOXAMINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| CETIRIZINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| CHLORPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| CHLORPHENTERMINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| CHLORPROMAZINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| CHLORPROTHIXENE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| CINACALCET | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| CINNARIZINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| CITALOPRAM | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| CLEMASTINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| CLOMIPRAMINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| CLOZAPINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| CYCLOBENZAPRINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| CYPROHEPTADINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| DAUNORUBICIN | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| DESIPRAMINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| DEXBROMPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| DEXCHLORPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| DIBENZEPIN | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| DIPHENHYDRAMINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| DOMPERIDONE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| DOTHIEPIN | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| DULOXETINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| EBASTINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| EPALRESTAT | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| ESCITALOPRAM | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| FLUOXETINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| FLUPHENAZINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| FLUSPIRILENE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| HALOPERIDOL | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| IDARUBICIN | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| ILOPERIDONE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| IMIPRAMINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| INDOCYANINE GREEN ACID FORM | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| LASOFOXIFENE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| LOFEPRAMINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| LORCASERIN | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| LOXAPINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| MAZINDOL | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| MECLIZINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| MEFLOQUINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| MEPAZINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| METHAPYRILENE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| MIANSERIN | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| NAFTOPIDIL | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| NEFAZODONE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| NEFOPAM | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| NOMIFENSINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| NORTRIPTYLINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| ORPHENADRINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| PERPHENAZINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| PIMOZIDE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| PIPAMAZINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| PIPERACETAZINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| PITOLISANT | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| PONATINIB | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| PRENYLAMINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| PROCHLORPERAZINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| PROMAZINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| PROMETHAZINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| PYRVINIUM | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| RIFAMPIN | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| RISPERIDONE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| ROTIGOTINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| SERTINDOLE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| SERTRALINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| SULOCTIDIL | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| SUNITINIB | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| TERFENADINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| THIETHYLPERAZINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| THIORIDAZINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| THIOTEPA | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| TRIFLUOPERAZINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| TRIPELENNAMINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
| VENLAFAXINE | ChEMBL | Phase 4 (approved) | HRH1, SLC6A2, SLC6A4 |
Related Atlas pages
- Genes: HRH1, SLC6A2, SLC6A4
- Indicated for: depressive disorder
- In clinical trials for: anxiety, dementia, urticaria, irritable bowel syndrome, breast neoplasm, sleep disorder
- Drugs: Aclidinium Bromide, Amitriptyline, Crizotinib, Desloratadine, Dihydroergotamine, Olodaterol, Regorafenib, Tadalafil, Acetophenazine, Amiodarone, Amoxapine, Aripiprazole, Asenapine, Astemizole, Atomoxetine, Azelastine, Benfluorex, Benztropine, Bepridil, Brexpiprazole, Bromperidol, Brompheniramine, Bupropion, Cabergoline, Carbinoxamine, Cetirizine, Chlorpheniramine, Chlorphentermine, Chlorpromazine, Chlorprothixene, Cinacalcet, Cinnarizine, Citalopram, Clemastine, Clomipramine, Clotrimazole, Clozapine, Cyclobenzaprine, Cyproheptadine, Daunorubicin, Desipramine, Dexbrompheniramine, Dibenzepin, Diphenhydramine, Domperidone, Dothiepin, Duloxetine, Ebastine, Epalrestat, Fluoxetine, Fluphenazine, Fluspirilene, Haloperidol, Idarubicin, Iloperidone, Imipramine, Indocyanine Green Acid Form, Lasofoxifene, Lofepramine, Lorcaserin, Loxapine, Mazindol, Meclizine, Mefloquine, Mepazine, Methapyrilene, Mianserin, Naftopidil, Nefazodone, Nefopam, Nomifensine, Nortriptyline, Orphenadrine, Perphenazine, Pimozide, Pipamazine, Piperacetazine, Pitolisant, Ponatinib, Prenylamine, Prochlorperazine, Promazine, Promethazine, Pyrvinium, Rifampin, Risperidone, Rotigotine, Sertindole, Sertraline, Suloctidil, Sunitinib, Terfenadine, Thiethylperazine, Thioridazine, Thiotepa, Trifluoperazine, Tripelennamine, Venlafaxine