Procaterol
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Also known as MeptinSID11113915SID26752069rel-ProcaterolSID144204492SID170465820
Summary
Procaterol (CHEMBL160519) is a phase-3 clinical-stage small molecule (ATC R03AC16) targeting ADRB2; indicated across 2 conditions including obstructive lung disease and asthma.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- ATC class: R03AC16 (+1 more)
- Targets: 1 (ADRB2)
- Indications: 2 conditions
- Clinical trials: 10
- Chemistry: 290.36 Da · C16H22N2O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL160519 |
| Name | Procaterol |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 4916 |
| ATC | R03AC16, R03CC08 |
| Molecular formula | C16H22N2O3 |
| Molecular weight | 290.36 |
| InChIKey | FKNXQNWAXFXVNW-UHFFFAOYSA-N |
SMILES: CCC(C(C1=C2C=CC(=O)NC2=C(C=C1)O)O)NC(C)C
IUPAC name: 8-hydroxy-5-[1-hydroxy-2-(propan-2-ylamino)butyl]-1H-quinolin-2-one
Also known as: Meptin, Procaterol, SID11113915, SID26752069, rel-Procaterol, SID144204492, SID170465820, PROCATEROL, procaterol
Parent form; salt/anhydrous children: CHEMBL1322218
Patent coverage: 2,434 distinct patent families (10,101 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 10,095 (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 |
|---|---|---|---|---|---|
| ADRB2 | β2-adrenoceptor | Agonist | 7.1 | 0.4% | P07550 |
Broader ChEMBL bioactivity targets: 13 (assay-derived). Sample: Lysine-specific demethylase 4E, Prelamin-A/C, 4’-phosphopantetheinyl transferase ffp, Thyrotropin receptor, Menin/Histone-lysine N-methyltransferase MLL, Beta-2 adrenergic receptor, Beta-1 adrenergic receptor, D(2) dopamine receptor, Prostaglandin G/H synthase 2, Cytochrome P450 2D6.
Bioactivity
ChEMBL activities: 7 potent at pChembl ≥ 5 of 19 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| TSHR | 7.9 | Potency | 12.6 | nM | CHEMBL_ACT_3911050 |
| TSHR | 7.9 | Potency | 12.6 | nM | CHEMBL_ACT_4617006 |
| ADRB2 | 7.48 | Ki | 33 | nM | CHEMBL_ACT_16581631 |
| ADRB2 | 7.1 | Kd | 79.43 | nM | CHEMBL_ACT_13449575 |
| ADRB2 | 6.7 | AC50 | 200 | nM | CHEMBL_ACT_25123343 |
| LMNA | 6.05 | Potency | 891.3 | nM | CHEMBL_ACT_3628026 |
| PTGS2 | 5.06 | AC50 | 8800 | nM | CHEMBL_ACT_25166759 |
Target pathways
Aggregated over 1 target gene(s): ADRB2.
Top Reactome pathways
16 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signal Transduction | 1 | ADRB2 |
| Membrane Trafficking | 1 | ADRB2 |
| Signaling by GPCR | 1 | ADRB2 |
| Class A/1 (Rhodopsin-like receptors) | 1 | ADRB2 |
| Amine ligand-binding receptors | 1 | ADRB2 |
| GPCR downstream signalling | 1 | ADRB2 |
| Adrenoceptors | 1 | ADRB2 |
| Metabolism of proteins | 1 | ADRB2 |
| G alpha (s) signalling events | 1 | ADRB2 |
| GPCR ligand binding | 1 | ADRB2 |
| Vesicle-mediated transport | 1 | ADRB2 |
| Deubiquitination | 1 | ADRB2 |
| Ub-specific processing proteases | 1 | ADRB2 |
| Post-translational protein modification | 1 | ADRB2 |
| Cargo recognition for clathrin-mediated endocytosis | 1 | ADRB2 |
| Clathrin-mediated endocytosis | 1 | ADRB2 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| diet induced thermogenesis | 1 |
| norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure | 1 |
| regulation of sodium ion transport | 1 |
| transcription by RNA polymerase II | 1 |
| receptor-mediated endocytosis | 1 |
| smooth muscle contraction | 1 |
| cell surface receptor signaling pathway | 1 |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | 1 |
| endosome to lysosome transport | 1 |
| response to cold | 1 |
| positive regulation of cardiac muscle cell apoptotic process | 1 |
| negative regulation of cardiac muscle cell apoptotic process | 1 |
| positive regulation of bone mineralization | 1 |
| heat generation | 1 |
| negative regulation of multicellular organism growth | 1 |
Indications & clinical
Indications
2 indications (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 |
|---|---|---|---|
| obstructive lung disease | 3 | MONDO:0002267 | HP:0006536 |
| asthma | 3 | MONDO:0004979 | MONDO:0004979 |
Clinical trials
Total trials: 10.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 4 |
| PHASE3 | 2 |
| PHASE1 | 2 |
| PHASE2 | 1 |
| Not specified | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00394485 | PHASE4 | TERMINATED | Tiotropium + Procaterol vs Tiotropium + Placebo in COPD Patients |
| NCT01091337 | PHASE4 | COMPLETED | Comparative Study on the Efficacy and Safety of Procaterol Versus Salbutamol Given Via Metered Dose Inhaler With Spacer in the Management of Acute Asthma Attack in the Emergency Room |
| NCT01170429 | PHASE4 | UNKNOWN | Efficacy and Safety Study of Procaterol Hydrochloride to Treat Patients With Cough Variant Asthma (CVA) |
| NCT06346691 | PHASE4 | COMPLETED | Effects of Oral Doxofylline and Procaterol on Chronic Obstructive Pulmonary Disease |
| NCT00990847 | PHASE3 | COMPLETED | Nebulized Procaterol Versus Nebule Salbutamol for the Treatment of Moderate Acute Asthma |
| NCT01095016 | PHASE3 | COMPLETED | A Study to Evaluate the Efficacy and Safety of Meptin® Swinghaler and Berotec N® Metered Aerosol in Mild to Moderate Stable Asthma Patients |
| NCT02162784 | PHASE2 | COMPLETED | Efficacy Study of SYN006 HFA MDI in Asthma Patients |
| NCT02165033 | PHASE1 | COMPLETED | Multiple-dose Pharmacokinetics Study of SYN006 HFA MDI Administered Orally to Healthy Volunteers |
| NCT02165046 | PHASE1 | COMPLETED | Bioavailability Study of SYN006, Pulmicort pMDI and Meptin Air in Healthy Adult. |
| NCT02349919 | Not specified | UNKNOWN | Effect of Oral Procaterol on Postinfectious Persistent Cough |
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.
188 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| DESLORATADINE | ChEMBL + PubChem | Phase 4 (approved) | ADRB2 |
| DIHYDROERGOTAMINE | ChEMBL + PubChem | Phase 4 (approved) | ADRB2 |
| OLODATEROL | ChEMBL + PubChem | Phase 4 (approved) | ADRB2 |
| PRAMIPEXOLE | ChEMBL + PubChem | Phase 4 (approved) | ADRB2 |
| ACEBUTOLOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| ADENOSINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| ALBUTEROL | ChEMBL | Phase 4 (approved) | ADRB2 |
| AMITRIPTYLINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| AMLODIPINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| AMOXAPINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| ARFORMOTEROL | ChEMBL | Phase 4 (approved) | ADRB2 |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | ADRB2 |
| ATENOLOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| BENPERIDOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| BETAXOLOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| BISOPROLOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| BREXPIPRAZOLE | ChEMBL | Phase 4 (approved) | ADRB2 |
| BROMOCRIPTINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| CANDESARTAN CILEXETIL | ChEMBL | Phase 4 (approved) | ADRB2 |
| CARTEOLOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| CARVEDILOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| CELIPROLOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| CHLORHEXIDINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| CLEMASTINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| CLOMIPRAMINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | ADRB2 |
| CLOZAPINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| DARIFENACIN | ChEMBL | Phase 4 (approved) | ADRB2 |
| DEXAMETHASONE | ChEMBL | Phase 4 (approved) | ADRB2 |
| DIPIVEFRIN | ChEMBL | Phase 4 (approved) | ADRB2 |
| DOBUTAMINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| DOMPERIDONE | ChEMBL | Phase 4 (approved) | ADRB2 |
| DOPAMINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| DOXAZOSIN | ChEMBL | Phase 4 (approved) | ADRB2 |
| ELAGOLIX | ChEMBL | Phase 4 (approved) | ADRB2 |
| EPINEPHRINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| EPINEPHRINE BITARTRATE | ChEMBL | Phase 4 (approved) | ADRB2 |
| ERGOTAMINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| ESMOLOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| FENOTEROL | ChEMBL | Phase 4 (approved) | ADRB2 |
| FLUSPIRILENE | ChEMBL | Phase 4 (approved) | ADRB2 |
| FORMOTEROL | ChEMBL | Phase 4 (approved) | ADRB2 |
| HALOPERIDOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| INDACATEROL | ChEMBL | Phase 4 (approved) | ADRB2 |
| ISOETHARINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| ISOPROTERENOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| LABETALOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| LEVOBUNOLOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| LEVOSALBUTAMOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| LOFEPRAMINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| LOPERAMIDE | ChEMBL | Phase 4 (approved) | ADRB2 |
| LOXAPINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| MEBEVERINE | ChEMBL | Phase 4 (approved) | ADRB2 |
| METAPROTERENOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| METOPROLOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| MIFEPRISTONE | ChEMBL | Phase 4 (approved) | ADRB2 |
| MONTELUKAST | ChEMBL | Phase 4 (approved) | ADRB2 |
| NADOLOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| NEBIVOLOL | ChEMBL | Phase 4 (approved) | ADRB2 |
| NITAZOXANIDE | ChEMBL | Phase 4 (approved) | ADRB2 |
Related Atlas pages
- Genes: ADRB2
- Diseases: obstructive lung disease, asthma
- Drugs: Desloratadine, Dihydroergotamine, Olodaterol, Pramipexole, Acebutolol, Adenosine, Albuterol, Amitriptyline, Amlodipine, Amoxapine, Arformoterol, Aripiprazole, Atenolol, Benperidol, Betaxolol, Bisoprolol, Brexpiprazole, Bromocriptine, Candesartan Cilexetil, Carteolol, Carvedilol, Celiprolol, Chlorhexidine, Clemastine, Clomipramine, Clotrimazole, Clozapine, Darifenacin, Dexamethasone, Dipivefrin, Dobutamine, Domperidone, Dopamine, Doxazosin, Elagolix, Epinephrine, Ergotamine, Esmolol, Fenoterol, Fluspirilene, Formoterol, Haloperidol, Indacaterol, Isoetharine, Isoproterenol, Labetalol, Levobunolol, Levosalbutamol, Lofepramine, Loperamide, Loxapine, Mebeverine, Metaproterenol, Metoprolol, Mifepristone, Montelukast, Nadolol, Nebivolol, Nitazoxanide