Practolol
drugOn this page
Also known as AY-21,011AY-21011DalzicEraldinI.C.I. 50,172I.C.I.-50,172ICI-50172SID56463034SID144204479dl-practololPractololeSID170466619
Summary
Practolol (CHEMBL6995) is an approved small-molecule β-adrenergic antagonist (ATC C07AB01) targeting ADRB1; indicated across 1 condition including cardiovascular disorder.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: C07AB01
- Targets: 1 (ADRB1)
- Indications: 1 condition
- Chemistry: 266.34 Da · C14H22N2O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL6995 |
| Name | Practolol |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 4883 |
| ChEBI | CHEBI:258351 |
| ATC | C07AB01 |
| Molecular formula | C14H22N2O3 |
| Molecular weight | 266.34 |
| InChIKey | DURULFYMVIFBIR-UHFFFAOYSA-N |
SMILES: CC(C)NCC(COC1=CC=C(C=C1)NC(=O)C)O
IUPAC name: N-[4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl]acetamide
ChEBI definition: N-(4-Hydroxyphenyl)acetamide in which the hydrogen of the phenolic hydroxy group is substituted by a 3-(isopropylaminoamino)-2-hydroxypropyl group. A selective beta blocker, it has been used in the emergency treatment of cardiac arrhythmias.
Pharmacological roles (ChEBI): β-adrenergic antagonist, anti-arrhythmia drug.
Also known as: AY-21,011, AY-21011, Dalzic, Eraldin, I.C.I. 50,172, I.C.I.-50,172, ICI-50172, Practolol, SID56463034, PRACTOLOL, practolol, SID144204479
Patent coverage: 1,037 distinct patent families (4,261 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 |
|---|---|---|---|---|---|
| ADRB1 | β1-adrenoceptor | Antagonist | 6.8 | 0% | P08588 |
Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: Adrenergic receptor beta, Beta-1 adrenergic receptor, Beta-2 adrenergic receptor, Kappa-type opioid receptor, Beta-1 adrenergic receptor, Beta-2 adrenergic receptor, Beta-2 adrenergic receptor, Beta-2 adrenergic receptor, Beta-2 adrenergic receptor.
Bioactivity
ChEMBL activities: 10 potent at pChembl ≥ 5 of 15 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| P54833 | 6.73 | Kd | 186.2 | nM | CHEMBL_ACT_1023532 |
| ADRB2 | 6.6 | Kd | 251.2 | nM | CHEMBL_ACT_227776 |
| P18090 | 6.47 | Kd | 338.8 | nM | CHEMBL_ACT_14613522 |
| Q8K4Z4 | 5.8 | Kd | 1585 | nM | CHEMBL_ACT_131708 |
| ADRB2 | 5.8 | Kd | 1585 | nM | CHEMBL_ACT_227777 |
| ADRB2 | 5.78 | Kd | 1660 | nM | CHEMBL_ACT_670466 |
| OPRK1 | 5.55 | AC50 | 2806 | nM | CHEMBL_ACT_25129116 |
| Q8K4Z4 | 5.35 | Kd | 4467 | nM | CHEMBL_ACT_527491 |
| ADRB1 | 5.31 | AC50 | 4900 | nM | CHEMBL_ACT_25121440 |
| Q8K4Z4 | 5.2 | Kd | 6310 | nM | CHEMBL_ACT_14606283 |
Target pathways
Aggregated over 1 target gene(s): ADRB1.
Top Reactome pathways
8 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signal Transduction | 1 | ADRB1 |
| Signaling by GPCR | 1 | ADRB1 |
| Class A/1 (Rhodopsin-like receptors) | 1 | ADRB1 |
| Amine ligand-binding receptors | 1 | ADRB1 |
| GPCR downstream signalling | 1 | ADRB1 |
| Adrenoceptors | 1 | ADRB1 |
| G alpha (s) signalling events | 1 | ADRB1 |
| GPCR ligand binding | 1 | ADRB1 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| positive regulation of heart rate by epinephrine-norepinephrine | 1 |
| positive regulation of the force of heart contraction by epinephrine-norepinephrine | 1 |
| diet induced thermogenesis | 1 |
| norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure | 1 |
| adenylate cyclase-activating G protein-coupled receptor signaling pathway | 1 |
| response to cold | 1 |
| positive regulation of cardiac muscle cell apoptotic process | 1 |
| heat generation | 1 |
| negative regulation of multicellular organism growth | 1 |
| fear response | 1 |
| positive regulation of MAPK cascade | 1 |
| regulation of circadian sleep/wake cycle, sleep | 1 |
| brown fat cell differentiation | 1 |
| adenylate cyclase-activating adrenergic receptor signaling pathway | 1 |
| positive regulation of cold-induced thermogenesis | 1 |
Indications & clinical
Indications
1 indication (1 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 |
|---|---|---|---|
| cardiovascular disorder | 4 | MONDO:0004995 | EFO:0000319 |
Clinical trials
Total trials: 0.
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.
179 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| OLODATEROL | ChEMBL + PubChem | Phase 4 (approved) | ADRB1 |
| TAMSULOSIN | ChEMBL + PubChem | Phase 4 (approved) | ADRB1 |
| ACEBUTOLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| ALBUTEROL | ChEMBL | Phase 4 (approved) | ADRB1 |
| AMIODARONE | ChEMBL | Phase 4 (approved) | ADRB1 |
| AMITRIPTYLINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| ARFORMOTEROL | ChEMBL | Phase 4 (approved) | ADRB1 |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | ADRB1 |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | ADRB1 |
| ATENOLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| AZELASTINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| BENFLUOREX | ChEMBL | Phase 4 (approved) | ADRB1 |
| BENPERIDOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| BENZBROMARONE | ChEMBL | Phase 4 (approved) | ADRB1 |
| BEPRIDIL | ChEMBL | Phase 4 (approved) | ADRB1 |
| BETAXOLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| BISOPROLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| BREXPIPRAZOLE | ChEMBL | Phase 4 (approved) | ADRB1 |
| BROMOCRIPTINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| CANDESARTAN CILEXETIL | ChEMBL | Phase 4 (approved) | ADRB1 |
| CARIPRAZINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| CARTEOLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| CARVEDILOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| CELIPROLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| CHLORHEXIDINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| CHLORPROTHIXENE | ChEMBL | Phase 4 (approved) | ADRB1 |
| CINACALCET | ChEMBL | Phase 4 (approved) | ADRB1 |
| CLEMASTINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| CLOMIPRAMINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | ADRB1 |
| CODEINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| DARIFENACIN | ChEMBL | Phase 4 (approved) | ADRB1 |
| DAUNORUBICIN | ChEMBL | Phase 4 (approved) | ADRB1 |
| DECITABINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| DIETHYLSTILBESTROL | ChEMBL | Phase 4 (approved) | ADRB1 |
| DOBUTAMINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| DOMPERIDONE | ChEMBL | Phase 4 (approved) | ADRB1 |
| DULOXETINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| EBASTINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| ECONAZOLE | ChEMBL | Phase 4 (approved) | ADRB1 |
| EFAVIRENZ | ChEMBL | Phase 4 (approved) | ADRB1 |
| EPALRESTAT | ChEMBL | Phase 4 (approved) | ADRB1 |
| EPINEPHRINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| ERGOTAMINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| ESMOLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| FENOTEROL | ChEMBL | Phase 4 (approved) | ADRB1 |
| FLUSPIRILENE | ChEMBL | Phase 4 (approved) | ADRB1 |
| FORMOTEROL | ChEMBL | Phase 4 (approved) | ADRB1 |
| INDACATEROL | ChEMBL | Phase 4 (approved) | ADRB1 |
| INDOCYANINE GREEN ACID FORM | ChEMBL | Phase 4 (approved) | ADRB1 |
| ISOCONAZOLE | ChEMBL | Phase 4 (approved) | ADRB1 |
| ISOPROTERENOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| LABETALOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| LASOFOXIFENE | ChEMBL | Phase 4 (approved) | ADRB1 |
| LEVOBUNOLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| LORCASERIN | ChEMBL | Phase 4 (approved) | ADRB1 |
| METARAMINOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| METHYLERGONOVINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| METOPROLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| MICONAZOLE | ChEMBL | Phase 4 (approved) | ADRB1 |
Related Atlas pages
- Genes: ADRB1
- Diseases: cardiovascular disorder
- Drugs: Olodaterol, Tamsulosin, Acebutolol, Albuterol, Amiodarone, Amitriptyline, Arformoterol, Aripiprazole, Astemizole, Atenolol, Azelastine, Benfluorex, Benperidol, Benzbromarone, Bepridil, Betaxolol, Bisoprolol, Brexpiprazole, Bromocriptine, Candesartan Cilexetil, Cariprazine, Carteolol, Carvedilol, Celiprolol, Chlorhexidine, Chlorprothixene, Cinacalcet, Clemastine, Clomipramine, Clotrimazole, Codeine, Darifenacin, Daunorubicin, Decitabine, Diethylstilbestrol, Dobutamine, Domperidone, Duloxetine, Ebastine, Econazole, Efavirenz, Epalrestat, Epinephrine, Ergotamine, Esmolol, Fenoterol, Fluspirilene, Formoterol, Indacaterol, Indocyanine Green Acid Form, Isoconazole, Isoproterenol, Labetalol, Lasofoxifene, Levobunolol, Lorcaserin, Metaraminol, Methylergonovine, Metoprolol