Tripelennamine
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Also known as NSC-118946TripelenaminaTRIPELENNAMINE CITRATE
Summary
Tripelennamine (CHEMBL1241) is an approved small molecule (ATC R06AC04) targeting HRH1; indicated across 2 conditions including allergic disease.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: R06AC04 (+1 more)
- Targets: 1 (HRH1)
- Indications: 2 conditions
- Chemistry: 255.36 Da · C16H21N3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1241 |
| Name | Tripelennamine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 5587 |
| ATC | R06AC04, D04AA04 |
| Molecular formula | C16H21N3 |
| Molecular weight | 255.36 |
| InChIKey | UFLGIAIHIAPJJC-UHFFFAOYSA-N |
SMILES: CN(C)CCN(CC1=CC=CC=C1)C2=CC=CC=N2
IUPAC name: N’-benzyl-N,N-dimethyl-N’-pyridin-2-ylethane-1,2-diamine
Also known as: NSC-118946, Tripelenamina, Tripelennamine, TRIPELENNAMINE, TRIPELENNAMINE CITRATE, tripelennamine
Parent form; salt/anhydrous children: CHEMBL1200446, CHEMBL1200769
Patent coverage: 3,091 distinct patent families (11,906 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 11,892 (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 | 8 | 0% | P35367 |
Broader ChEMBL bioactivity targets: 13 (assay-derived). Sample: Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, D(1A) dopamine receptor, Muscarinic acetylcholine receptor M2, Sodium-dependent noradrenaline transporter, 5-hydroxytryptamine receptor 2A, Sodium-dependent serotonin transporter, Alpha-1A adrenergic receptor, Histamine H1 receptor, Kappa-type opioid receptor, Sodium-dependent dopamine transporter, Voltage-gated inwardly rectifying potassium channel KCNH2.
Bioactivity
ChEMBL activities: 13 potent at pChembl ≥ 5 of 17 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| HRH1 | 7.4 | IC50 | 39.81 | nM | CHEMBL_ACT_164845 |
| HRH1 | 7.1 | AC50 | 80 | nM | CHEMBL_ACT_25212045 |
| SLC6A4 | 6.68 | AC50 | 209 | nM | CHEMBL_ACT_25149887 |
| SLC6A4 | 6.4 | AC50 | 394.8 | nM | CHEMBL_ACT_25151068 |
| SLC6A3 | 6.21 | AC50 | 618.6 | nM | CHEMBL_ACT_25124700 |
| SLC6A3 | 5.89 | AC50 | 1300 | nM | CHEMBL_ACT_25123493 |
| SLC6A2 | 5.58 | AC50 | 2615 | nM | CHEMBL_ACT_25145741 |
| KCNH2 | 5.55 | AC50 | 2800 | nM | CHEMBL_ACT_25117165 |
| ADRA2A | 5.51 | AC50 | 3083 | nM | CHEMBL_ACT_25156170 |
| CHRM2 | 5.33 | AC50 | 4716 | nM | CHEMBL_ACT_25195477 |
| OPRK1 | 5.2 | AC50 | 6251 | nM | CHEMBL_ACT_25129014 |
| HTR2A | 5.14 | AC50 | 7300 | nM | CHEMBL_ACT_25224750 |
| ADRA2C | 5.03 | AC50 | 9400 | nM | CHEMBL_ACT_25147410 |
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 approved indication. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).
| Indication | Phase | MONDO | EFO |
|---|---|---|---|
| allergic disease | 4 | MONDO:0005271 | MONDO:0005271 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 0.
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
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 100 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 |
| DEXBROMPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| DEXCHLORPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| DIBENZEPIN | ChEMBL | Phase 4 (approved) | HRH1 |
| DICYCLOMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| DIETHYLPROPION | ChEMBL | Phase 4 (approved) | HRH1 |
| DIMENHYDRINATE | ChEMBL | Phase 4 (approved) | HRH1 |
| DIPHEMANIL | ChEMBL | Phase 4 (approved) | HRH1 |
| DIPHENHYDRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| DOMPERIDONE | ChEMBL | Phase 4 (approved) | HRH1 |
| DOTHIEPIN | ChEMBL | Phase 4 (approved) | HRH1 |
| DOXEPIN | ChEMBL | Phase 4 (approved) | HRH1 |
| DROPERIDOL | ChEMBL | Phase 4 (approved) | HRH1 |
| DULOXETINE | ChEMBL | Phase 4 (approved) | HRH1 |
| DYCLONINE | ChEMBL | Phase 4 (approved) | HRH1 |
| EBASTINE | ChEMBL | Phase 4 (approved) | HRH1 |
| EPALRESTAT | ChEMBL | Phase 4 (approved) | HRH1 |
| ESCITALOPRAM | ChEMBL | Phase 4 (approved) | HRH1 |
| FENTANYL | ChEMBL | Phase 4 (approved) | HRH1 |
| FEXOFENADINE | ChEMBL | Phase 4 (approved) | HRH1 |
| FLUDROCORTISONE | ChEMBL | Phase 4 (approved) | HRH1 |
| FLUOXETINE | ChEMBL | Phase 4 (approved) | HRH1 |
| FLUPHENAZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| FLUSPIRILENE | ChEMBL | Phase 4 (approved) | HRH1 |
| GLYCOPYRRONIUM BROMIDE | ChEMBL | Phase 4 (approved) | HRH1 |
| HALOPERIDOL | ChEMBL | Phase 4 (approved) | HRH1 |
| HISTAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| HYDROXOCOBALAMIN | ChEMBL | Phase 4 (approved) | HRH1 |
| HYDROXYZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| IDARUBICIN | ChEMBL | Phase 4 (approved) | HRH1 |
| ILOPERIDONE | ChEMBL | Phase 4 (approved) | HRH1 |
| IMIPRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| INDOCYANINE GREEN ACID FORM | ChEMBL | Phase 4 (approved) | HRH1 |
| IPRINDOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| KETANSERIN | ChEMBL | Phase 4 (approved) | HRH1 |
| KETOTIFEN | ChEMBL | Phase 4 (approved) | HRH1 |
| LASOFOXIFENE | ChEMBL | Phase 4 (approved) | HRH1 |
| LEVOCETIRIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| LOFEPRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| LORATADINE | ChEMBL | Phase 4 (approved) | HRH1 |
| LORCASERIN | ChEMBL | Phase 4 (approved) | HRH1 |
Related Atlas pages
- Genes: HRH1
- Indicated for: allergic disease
- 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, Chlorpheniramine, Chlorphentermine, Chlorpromazine, Chlorprothixene, Cinacalcet, Cinnarizine, Cisapride, Citalopram, Clemastine, Clofazimine, Clomipramine, Clotrimazole, Clozapine, Cyclizine, Cyclobenzaprine, Cyproheptadine, Daunorubicin, Desipramine, Dexbrompheniramine, Dibenzepin, Dicyclomine, Diethylpropion, Dimenhydrinate, Diphemanil, Diphenhydramine, Domperidone, Dothiepin, Doxepin, Droperidol, Duloxetine, Dyclonine, Ebastine, Epalrestat, Fentanyl, Fexofenadine, Fludrocortisone, Fluoxetine, Fluphenazine, Fluspirilene, Glycopyrronium Bromide, Haloperidol, Histamine, Hydroxocobalamin, Hydroxyzine, Idarubicin, Iloperidone, Imipramine, Indocyanine Green Acid Form, Iprindole, Ketanserin, Ketotifen, Lasofoxifene, Lofepramine, Loratadine, Lorcaserin