Mepenzolate
drug drugOn this page
Also known as Mepenzolate bromide free baseMepenzolate cationMepenzolate ionMEPENZOLATE BROMIDE
Summary
Mepenzolate (CHEMBL524004) is an approved small molecule (ATC A03AB12) targeting CHRM2, CHRM3, and CHRM4; indicated across 1 condition.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: A03AB12
- Targets: 3 (CHRM2, CHRM3, CHRM4)
- Indications: 1 condition
- Chemistry: 340.4 Da · C21H26NO3+
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL524004 |
| Name | Mepenzolate |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 4057 |
| ATC | A03AB12 |
| Molecular formula | C21H26NO3+ |
| Molecular weight | 340.4 |
| InChIKey | GKNPSSNBBWDAGH-UHFFFAOYSA-N |
SMILES: C[N+]1(CCCC(C1)OC(=O)C(C2=CC=CC=C2)(C3=CC=CC=C3)O)C
IUPAC name: (1,1-dimethylpiperidin-1-ium-3-yl) 2-hydroxy-2,2-diphenylacetate
Also known as: Mepenzolate, Mepenzolate bromide free base, Mepenzolate cation, Mepenzolate ion, MEPENZOLATE, mepenzolate, MEPENZOLATE BROMIDE
Parent form; salt/anhydrous children: CHEMBL1724
Patent coverage: 4 distinct patent families (6 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 |
|---|---|---|---|---|---|
| CHRM2 | M2 receptor | Antagonist | 9.17 | 0% | P08172 |
| CHRM3 | M3 receptor | Antagonist | 8.59 | 0% | P20309 |
| CHRM4 | M4 receptor | Antagonist | 9.44 | 1.6% | P08173 |
Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Muscarinic acetylcholine receptor M2, Sodium-dependent serotonin transporter, Voltage-gated inwardly rectifying potassium channel KCNH2.
Bioactivity
ChEMBL activities: 1 potent at pChembl ≥ 5 of 3 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| CHRM2 | 8.35 | AC50 | 4.5 | nM | CHEMBL_ACT_25195594 |
Target pathways
Aggregated over 3 target gene(s): CHRM2, CHRM3, CHRM4.
Top Reactome pathways
17 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signal Transduction | 3 | CHRM2, CHRM3, CHRM4 |
| Signaling by GPCR | 3 | CHRM2, CHRM3, CHRM4 |
| Class A/1 (Rhodopsin-like receptors) | 3 | CHRM2, CHRM3, CHRM4 |
| Amine ligand-binding receptors | 3 | CHRM2, CHRM3, CHRM4 |
| GPCR downstream signalling | 3 | CHRM2, CHRM3, CHRM4 |
| Muscarinic acetylcholine receptors | 3 | CHRM2, CHRM3, CHRM4 |
| GPCR ligand binding | 3 | CHRM2, CHRM3, CHRM4 |
| G alpha (i) signalling events | 2 | CHRM2, CHRM4 |
| Metabolism | 1 | CHRM3 |
| Integration of energy metabolism | 1 | CHRM3 |
| Membrane Trafficking | 1 | CHRM2 |
| Acetylcholine regulates insulin secretion | 1 | CHRM3 |
| G alpha (q) signalling events | 1 | CHRM3 |
| Regulation of insulin secretion | 1 | CHRM3 |
| Vesicle-mediated transport | 1 | CHRM2 |
| Cargo recognition for clathrin-mediated endocytosis | 1 | CHRM2 |
| Clathrin-mediated endocytosis | 1 | CHRM2 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| G protein-coupled receptor signaling pathway | 3 |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | 3 |
| adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway | 3 |
| G protein-coupled acetylcholine receptor signaling pathway | 3 |
| chemical synaptic transmission | 3 |
| signal transduction | 3 |
| regulation of smooth muscle contraction | 2 |
| phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathway | 2 |
| nervous system development | 2 |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | 1 |
| adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway | 1 |
| regulation of heart contraction | 1 |
| response to virus | 1 |
| presynaptic modulation of chemical synaptic transmission | 1 |
| smooth muscle contraction | 1 |
Indications & clinical
Indications
1 indication record carries no mapped disease name (EFO/MeSH-only); none shown.
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.
447 molecules share ≥1 primary target. Top 100 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| ACLIDINIUM BROMIDE | ChEMBL + PubChem | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| GENTIAN VIOLET | ChEMBL + PubChem | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| MAVORIXAFOR | ChEMBL + PubChem | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| ACETYLCHOLINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| AMIODARONE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| AMITRIPTYLINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| AMOXAPINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| ATROPINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| BENZTROPINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| BETHANECHOL | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| BIPERIDEN | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| CARBACHOL | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| CARBAMOYLCHOLINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| CEVIMELINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| CHLOROQUINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| CHLORPROMAZINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| CINNARIZINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| CLEMASTINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| CLIDINIUM | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| CLOMIPRAMINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| CLOZAPINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| CYCLIZINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| CYPROHEPTADINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| DARIFENACIN | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| DESLORATADINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| DEXCHLORPHENIRAMINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| DICYCLOMINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| DIMENHYDRINATE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| DIPHENHYDRAMINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| DIPHENIDOL | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| DOXEPIN | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| EBASTINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| ECONAZOLE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| FLUPHENAZINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| GLYCOPYRRONIUM BROMIDE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| HALOPERIDOL | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| HOMATROPINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| HYDROXYCHLOROQUINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| IMIPRAMINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| IPRATROPIUM | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| KETOTIFEN | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| LOXAPINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| MAPROTILINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| MEPAZINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| METHSCOPOLAMINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| METHSCOPOLAMINE BROMIDE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| MIANSERIN | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| MICONAZOLE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| NORTRIPTYLINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| OLANZAPINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| ORPHENADRINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| OXYBUTYNIN | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| PAROXETINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| PERHEXILINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| PILOCARPINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| PIRENZEPINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| PROCHLORPERAZINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| PROMAZINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| PROMETHAZINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| QUETIAPINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| QUINACRINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| RISPERIDONE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| SCOPOLAMINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| SERTRALINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| SOLIFENACIN | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| SULOCTIDIL | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| TAMOXIFEN | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| TERCONAZOLE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| THIORIDAZINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| TIOTROPIUM BROMIDE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| TOLTERODINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| TRIHEXYPHENIDYL | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| TROPICAMIDE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| TROSPIUM CHLORIDE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| XANOMELINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3, CHRM4 |
| BLARCAMESINE | ChEMBL | Phase 3 | CHRM2, CHRM3, CHRM4 |
| DIMETHINDENE | ChEMBL | Phase 3 | CHRM2, CHRM3, CHRM4 |
| ENCLOMIPHENE | ChEMBL | Phase 3 | CHRM2, CHRM3, CHRM4 |
| ABAPERIDONE | ChEMBL | Phase 2 | CHRM2, CHRM3, CHRM4 |
| APROFENE | ChEMBL | Phase 2 | CHRM2, CHRM3, CHRM4 |
| BENZETHONIUM CHLORIDE | ChEMBL | Phase 2 | CHRM2, CHRM3, CHRM4 |
| CIGLITAZONE | ChEMBL | Phase 2 | CHRM2, CHRM3, CHRM4 |
| FLUNARIZINE | ChEMBL | Phase 2 | CHRM2, CHRM3, CHRM4 |
| METHYLBENACTYZIUM BROMIDE | ChEMBL | Phase 2 | CHRM2, CHRM3, CHRM4 |
| OTENZEPAD | ChEMBL | Phase 2 | CHRM2, CHRM3, CHRM4 |
| PF-03635659 | ChEMBL | Phase 2 | CHRM2, CHRM3, CHRM4 |
| SABCOMELINE | ChEMBL | Phase 2 | CHRM2, CHRM3, CHRM4 |
| TALSACLIDINE | ChEMBL | Phase 2 | CHRM2, CHRM3, CHRM4 |
| ZOTEPINE | ChEMBL | Phase 2 | CHRM2, CHRM3, CHRM4 |
| AFATINIB | ChEMBL + PubChem | Phase 4 (approved) | CHRM2, CHRM3 |
| CHENODIOL | ChEMBL + PubChem | Phase 4 (approved) | CHRM2, CHRM3 |
| Linagliptin | ChEMBL + PubChem | Phase 4 (approved) | CHRM2, CHRM3 |
| OLODATEROL | ChEMBL + PubChem | Phase 4 (approved) | CHRM2, CHRM3 |
| Propoxyphene | ChEMBL + PubChem | Phase 4 (approved) | CHRM2, CHRM3 |
| AMBENONIUM | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3 |
| ANISOTROPINE | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3 |
| BENPERIDOL | ChEMBL | Phase 4 (approved) | CHRM2, CHRM3 |
| BETAMETHASONE PHOSPHORIC ACID | ChEMBL | Phase 4 (approved) | CHRM3, CHRM4 |
Related Atlas pages
- Genes: CHRM2, CHRM3, CHRM4
- Drugs: Aclidinium Bromide, Mavorixafor, Acetylcholine, Amiodarone, Amitriptyline, Amoxapine, Astemizole, Atropine, Benztropine, Bethanechol, Biperiden, Carbachol, Cevimeline, Chloroquine, Chlorpromazine, Cinnarizine, Clemastine, Clidinium, Clomipramine, Clotrimazole, Clozapine, Cyclizine, Cyproheptadine, Darifenacin, Desloratadine, Dexchlorpheniramine, Dicyclomine, Dimenhydrinate, Diphenhydramine, Diphenidol, Doxepin, Ebastine, Econazole, Fluphenazine, Glycopyrronium Bromide, Haloperidol, Homatropine, Hydroxychloroquine, Imipramine, Ipratropium, Ketotifen, Loxapine, Maprotiline, Mepazine, Methscopolamine, Mianserin, Miconazole, Nortriptyline, Olanzapine, Orphenadrine, Oxybutynin, Paroxetine, Perhexiline, Pilocarpine, Pirenzepine, Prochlorperazine, Promazine, Promethazine, Quetiapine, Quinacrine, Risperidone, Scopolamine, Sertraline, Solifenacin, Suloctidil, Tamoxifen, Terconazole, Thioridazine, Tiotropium Bromide, Tolterodine, Trihexyphenidyl, Tropicamide, Xanomeline, Blarcamesine, Dimethindene, Enclomiphene, Afatinib, Chenodiol, Linagliptin, Olodaterol, Propoxyphene, Ambenonium, Anisotropine, Benperidol, Betamethasone Phosphoric Acid