Dexchlorpheniramine
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Also known as Chlorphenamine, (s)-Chlorpheniramine d-formChlorpheniramine, (s)-Chlorpheniramined-DapritonDexclorfeniraminaSID90340867(S)-ChlorpheniramineSID29216403MMV1740297
Summary
Dexchlorpheniramine (CHEMBL1201353) is an approved small molecule (ATC R06AB02) targeting HRH1; indicated across 1 condition including allergic disease.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: R06AB02 (+1 more)
- Targets: 1 (HRH1)
- Indications: 1 condition
- Clinical trials: 12
- Chemistry: 274.79 Da · C16H19ClN2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1201353 |
| Name | Dexchlorpheniramine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 33036 |
| ChEBI | CHEBI:4464 |
| ATC | R06AB02, R06AB52 |
| Molecular formula | C16H19ClN2 |
| Molecular weight | 274.79 |
| InChIKey | SOYKEARSMXGVTM-HNNXBMFYSA-N |
SMILES: CN(C)CC[C@@H](C1=CC=C(C=C1)Cl)C2=CC=CC=N2
IUPAC name: (3S)-3-(4-chlorophenyl)-N,N-dimethyl-3-pyridin-2-ylpropan-1-amine
Also known as: Chlorphenamine, (s)-, Chlorpheniramine d-form, Chlorpheniramine, (s)-, Chlorpheniramine, d-, Dapriton, Dexchlorpheniramine, Dexclorfeniramina, SID90340867, (S)-Chlorpheniramine, SID29216403, DEXCHLORPHENIRAMINE
Parent form; salt/anhydrous children: CHEMBL1200927, CHEMBL3183101
Patent coverage: 2,237 distinct patent families (8,566 SureChEMBL compound mentions), from 1 matched compound structure(s). 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 | 8.6 | 0% | P35367 |
Broader ChEMBL bioactivity targets: 21 (assay-derived). Sample: Muscarinic acetylcholine receptor M4, Alpha-2A adrenergic receptor, Histamine H2 receptor, Alpha-2B adrenergic receptor, Muscarinic acetylcholine receptor M5, Muscarinic acetylcholine receptor M2, 5-hydroxytryptamine receptor 1A, Muscarinic acetylcholine receptor M1, Sodium-dependent noradrenaline transporter, Alpha-1D adrenergic receptor.
Bioactivity
ChEMBL activities: 37 potent at pChembl ≥ 5 of 48 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| HRH1 | 9.14 | Ki | 0.73 | nM | CHEMBL_ACT_7678844 |
| HRH1 | 8.2 | IC50 | 6.29 | nM | CHEMBL_ACT_7678843 |
| SLC6A4 | 7.89 | Ki | 13 | nM | CHEMBL_ACT_7681006 |
| HRH1 | 7.7 | AC50 | 20 | nM | CHEMBL_ACT_25211990 |
| SLC6A4 | 7.6 | IC50 | 25 | nM | CHEMBL_ACT_7681005 |
| SLC6A4 | 7.1 | AC50 | 80 | nM | CHEMBL_ACT_25149835 |
| CHRM4 | 6.56 | Ki | 276 | nM | CHEMBL_ACT_7678878 |
| CHRM1 | 6.48 | Ki | 333 | nM | CHEMBL_ACT_7678872 |
| CHRM3 | 6.26 | Ki | 547 | nM | CHEMBL_ACT_7678876 |
| SIGMAR1 | 6.16 | Ki | 697 | nM | CHEMBL_ACT_7681008 |
| SLC6A3 | 6.13 | Ki | 739 | nM | CHEMBL_ACT_7678818 |
| CHRM5 | 6.13 | Ki | 749 | nM | CHEMBL_ACT_7678880 |
| KCNH2 | 6.05 | AC50 | 890 | nM | CHEMBL_ACT_25117089 |
| SLC6A3 | 6.03 | IC50 | 931 | nM | CHEMBL_ACT_7678817 |
| CHRM5 | 5.98 | IC50 | 1043 | nM | CHEMBL_ACT_7678879 |
| HTR2A | 5.98 | Ki | 1055 | nM | CHEMBL_ACT_7680994 |
| HTR2C | 5.92 | Ki | 1217 | nM | CHEMBL_ACT_7680998 |
| CHRM1 | 5.86 | IC50 | 1383 | nM | CHEMBL_ACT_7678871 |
| SIGMAR1 | 5.78 | IC50 | 1658 | nM | CHEMBL_ACT_7681007 |
| CHRM4 | 5.7 | IC50 | 1976 | nM | CHEMBL_ACT_7678877 |
| ADRA2B | 5.68 | Ki | 2103 | nM | CHEMBL_ACT_7711196 |
| HTR2C | 5.63 | IC50 | 2322 | nM | CHEMBL_ACT_7680997 |
| CHRM2 | 5.6 | Ki | 2487 | nM | CHEMBL_ACT_7678874 |
| CHRM3 | 5.59 | IC50 | 2579 | nM | CHEMBL_ACT_7678875 |
| SLC6A3 | 5.54 | AC50 | 2900 | nM | CHEMBL_ACT_25123441 |
| HTR2A | 5.43 | IC50 | 3692 | nM | CHEMBL_ACT_7680993 |
| ADRA2B | 5.34 | IC50 | 4607 | nM | CHEMBL_ACT_7711195 |
| SLC6A2 | 5.31 | Ki | 4925 | nM | CHEMBL_ACT_7711206 |
| SLC6A2 | 5.3 | IC50 | 4966 | nM | CHEMBL_ACT_7711205 |
| HRH3 | 5.2 | AC50 | 6300 | nM | CHEMBL_ACT_25200177 |
Target pathways
Aggregated over 1 target gene(s): HRH1.
Top Reactome pathways
2 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Histamine receptors | 1 | HRH1 |
| G alpha (q) signalling events | 1 | HRH1 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| 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 |
| chemical synaptic transmission | 1 |
| memory | 1 |
| visual learning | 1 |
| regulation of vascular permeability | 1 |
| positive regulation of vasoconstriction | 1 |
| regulation of synaptic plasticity | 1 |
| cellular response to histamine | 1 |
| signal transduction | 1 |
| phospholipase C-activating serotonin receptor signaling pathway | 1 |
Indications & clinical
Indications
1 indication (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| allergic disease | 2 | MONDO:0005271 | MONDO:0005271 |
Clinical trials
Total trials: 12.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 10 |
| PHASE1 | 1 |
| Not specified | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT04702256 | PHASE3 | RECRUITING | Induction Therapy for Lupus Nephritis With no Added Oral Steroids: A Trial Comparing Oral Corticosteroids Plus Mycophenolate Mofetil (MMF) Versus Obinutuzumab and MMF |
| NCT00995397 | PHASE3 | UNKNOWN | Non-inferiority Clinical Trial of Dexchlorpheniramine (Cream Versus Lotion) in the Relief of Insect Bite Related Symptoms |
| NCT01085721 | PHASE3 | UNKNOWN | Comparison Between Dexchlorpheniramine and Dexchlorpheniramine/Pseudoephedrine/Guaifenesin in Respiratory Infections |
| NCT01085851 | PHASE3 | UNKNOWN | Non-inferiority Clinical Trial of Dexchlorpheniramine (Cream Versus Lotion) in the Relief of Sunburn Related Symptoms |
| NCT01233934 | PHASE3 | UNKNOWN | Comparative Study of Two Forms of Topical Dexchlorpheniramine Maleate (Cream Versus Gel) for Insect Bites |
| NCT01237925 | PHASE3 | UNKNOWN | Non-inferiority Clinical Trial of Dexchlorpheniramine (Cream Versus Gel) in the Relief of Sunburn Related Symptoms |
| NCT01529229 | PHASE3 | COMPLETED | Comparison of Desloratadine Associated With Prednisolone Oral Solution Versus Dexchlorpheniramine Associated With Betamethasone for Persistent Allergic Rhinitis Treatment |
| NCT01529242 | PHASE3 | TERMINATED | Comparison of Desloratadine Associated With Prednisolone Oral Solution Versus Dexchlorpheniramine Associated With Betamethasone for Cutaneous Rash Treatment |
| NCT01720485 | PHASE3 | UNKNOWN | Comparison of Desloratadine Associated With Prednisolone (Tablet)Versus Dexchlorpheniramine Associated With Betamethasone (Tablet) for Adult Persistent Allergic Rhinitis Treatment |
| NCT03368664 | PHASE3 | TERMINATED | A Study to Evaluate Efficacy, Safety, and Tolerability of Alemtuzumab in Pediatric Patients With RRMS With Disease Activity on Prior DMT |
| NCT02583594 | PHASE1 | COMPLETED | A Study to Characterize Subcutaneous or Intravenous Alemtuzumab in Patients With Progressive Multiple Sclerosis |
| NCT00846950 | Not specified | COMPLETED | Effects of H1-Antagonist on Cognition |
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.
295 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| ACLIDINIUM BROMIDE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| DESLORATADINE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| DIHYDROERGOTAMINE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| PALIPERIDONE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| PRAMIPEXOLE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| ABEMACICLIB | ChEMBL | Phase 4 (approved) | HRH1 |
| ACETOPHENAZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| ACRIVASTINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMIODARONE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMISULPRIDE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMITRIPTYLINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMOXAPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMSACRINE | ChEMBL | Phase 4 (approved) | HRH1 |
| ANTAZOLINE | ChEMBL | Phase 4 (approved) | HRH1 |
| APOMORPHINE | ChEMBL | Phase 4 (approved) | HRH1 |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| ASENAPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| ATOMOXETINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AZATADINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AZELASTINE | ChEMBL | Phase 4 (approved) | HRH1 |
| BENFLUOREX | ChEMBL | Phase 4 (approved) | HRH1 |
| BENPERIDOL | ChEMBL | Phase 4 (approved) | HRH1 |
| BENZBROMARONE | ChEMBL | Phase 4 (approved) | HRH1 |
| BENZTROPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| BEPRIDIL | ChEMBL | Phase 4 (approved) | HRH1 |
| BETAMETHASONE PHOSPHORIC ACID | ChEMBL | Phase 4 (approved) | HRH1 |
| BIPERIDEN | ChEMBL | Phase 4 (approved) | HRH1 |
| BREXPIPRAZOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| BROMPERIDOL | ChEMBL | Phase 4 (approved) | HRH1 |
| BROMPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| BUCLIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| BUPROPION | ChEMBL | Phase 4 (approved) | HRH1 |
| BUSPIRONE | ChEMBL | Phase 4 (approved) | HRH1 |
| BUTRIPTYLINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CABERGOLINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CANDESARTAN CILEXETIL | ChEMBL | Phase 4 (approved) | HRH1 |
| CAPTOPRIL | ChEMBL | Phase 4 (approved) | HRH1 |
| CARBINOXAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CARIPRAZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CETIRIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORDIAZEPOXIDE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORPHENTERMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORPROMAZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORPROTHIXENE | ChEMBL | Phase 4 (approved) | HRH1 |
| CINACALCET | ChEMBL | Phase 4 (approved) | HRH1 |
| CINNARIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CISAPRIDE | ChEMBL | Phase 4 (approved) | HRH1 |
| CITALOPRAM | ChEMBL | Phase 4 (approved) | HRH1 |
| CLEMASTINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CLOFAZIMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CLOMIPRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| CLOZAPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CYCLIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CYCLOBENZAPRINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CYPROHEPTADINE | ChEMBL | Phase 4 (approved) | HRH1 |
| DAUNORUBICIN | ChEMBL | Phase 4 (approved) | HRH1 |
| DESIPRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
Related Atlas pages
- Genes: HRH1
- Drugs: Aclidinium Bromide, Desloratadine, Dihydroergotamine, Paliperidone, Pramipexole, Abemaciclib, Acetophenazine, Acrivastine, Amiodarone, Amisulpride, Amitriptyline, Amoxapine, Amsacrine, Antazoline, Apomorphine, Aripiprazole, Asenapine, Astemizole, Atomoxetine, Azatadine, Azelastine, Benfluorex, Benperidol, Benzbromarone, Benztropine, Bepridil, Betamethasone Phosphoric Acid, Biperiden, Brexpiprazole, Bromperidol, Brompheniramine, Buclizine, Bupropion, Buspirone, Butriptyline, Cabergoline, Candesartan Cilexetil, Captopril, Carbinoxamine, Cariprazine, Cetirizine, Chlordiazepoxide, Chlorphentermine, Chlorpromazine, Chlorprothixene, Cinacalcet, Cinnarizine, Cisapride, Citalopram, Clemastine, Clofazimine, Clomipramine, Clotrimazole, Clozapine, Cyclizine, Cyclobenzaprine, Cyproheptadine, Daunorubicin, Desipramine