Amibegron

Summary

Amibegron (CHEMBL1193948) is a phase-3 clinical-stage small molecule targeting ADRB3; indicated across 3 conditions including anxiety and major depressive disorder.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (ADRB3)
• Indications: 3 conditions
• Clinical trials: 4
• Chemistry: 403.9 Da · C22H26ClNO4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1193948
Name	Amibegron
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	3035442
Molecular formula	C22H26ClNO4
Molecular weight	403.9
InChIKey	RDJQCOBTKKAQAH-FPOVZHCZSA-N

SMILES: CCOC(=O)COC1=CC2=C(CC[C@@H](C2)NC[C@@H](C3=CC(=CC=C3)Cl)O)C=C1

IUPAC name: ethyl 2-[[(7S)-7-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-5,6,7,8-tetrahydronaphthalen-2-yl]oxy]acetate

Also known as: Amibegron, SR-58611, SR58611, AMIBEGRON, amibegron

Parent form; salt/anhydrous children: CHEMBL545437

Patent coverage: 82 distinct patent families (184 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 129 (70%) 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
ADRB3	β3-adrenoceptor	Full agonist	5.2	0.1%	P13945

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): ADRB3.

Top Reactome pathways

8 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	1	ADRB3
Signaling by GPCR	1	ADRB3
Class A/1 (Rhodopsin-like receptors)	1	ADRB3
Amine ligand-binding receptors	1	ADRB3
GPCR downstream signalling	1	ADRB3
Adrenoceptors	1	ADRB3
G alpha (s) signalling events	1	ADRB3
GPCR ligand binding	1	ADRB3

Dominant GO biological processes

GO term	Targets
diet induced thermogenesis	1
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure	1
carbohydrate metabolic process	1
generation of precursor metabolites and energy	1
energy reserve metabolic process	1
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	1
response to cold	1
heat generation	1
negative regulation of multicellular organism growth	1
eating behavior	1
positive regulation of MAPK cascade	1
negative regulation of smooth muscle contraction	1
brown fat cell differentiation	1

Indications & clinical

Indications

3 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
anxiety	3	MONDO:0011918	EFO:0005230
major depressive disorder	3	MONDO:0002009	MONDO:0002009
depressive disorder	3	MONDO:0002050	MONDO:0002050

Clinical trials

Total trials: 4.

Phase distribution

Phase	Trials
PHASE3	4

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00385307	PHASE3	COMPLETED	Efficacy and Safety of SR58611A in Patients With Major Depressive Disorder (SIRIUS)
NCT00825019	PHASE3	COMPLETED	Efficacy and Safety of One Single Dose of SR58611 Compared to Placebo and Paroxetine
NCT00825058	PHASE3	COMPLETED	Efficacy and Safety of SR58611 Compared to Placebo and Paroxetine
NCT00855530	PHASE3	COMPLETED	Long Term Safety and Tolerability of SR58611 in Patients With Major Depressive Disorder

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.

107 molecules share ≥1 primary target. Top 100 by shared-target count:

Molecule	Source	Status	Shared targets
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	ADRB3
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	ADRB3
RIFAMPIN	ChEMBL + PubChem	Phase 4 (approved)	ADRB3
TEGASEROD	ChEMBL + PubChem	Phase 4 (approved)	ADRB3
AMIODARONE	ChEMBL	Phase 4 (approved)	ADRB3
AMLODIPINE	ChEMBL	Phase 4 (approved)	ADRB3
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRB3
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	ADRB3
BEPRIDIL	ChEMBL	Phase 4 (approved)	ADRB3
BISOPROLOL	ChEMBL	Phase 4 (approved)	ADRB3
BOSUTINIB	ChEMBL	Phase 4 (approved)	ADRB3
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	ADRB3
CARVEDILOL	ChEMBL	Phase 4 (approved)	ADRB3
CELECOXIB	ChEMBL	Phase 4 (approved)	ADRB3
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	ADRB3
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	ADRB3
DANAZOL	ChEMBL	Phase 4 (approved)	ADRB3
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	ADRB3
DISOPYRAMIDE	ChEMBL	Phase 4 (approved)	ADRB3
DOXAZOSIN	ChEMBL	Phase 4 (approved)	ADRB3
EBASTINE	ChEMBL	Phase 4 (approved)	ADRB3
ECONAZOLE	ChEMBL	Phase 4 (approved)	ADRB3
EPINEPHRINE	ChEMBL	Phase 4 (approved)	ADRB3
ETHINYL ESTRADIOL	ChEMBL	Phase 4 (approved)	ADRB3
FELODIPINE	ChEMBL	Phase 4 (approved)	ADRB3
FENOFIBRATE	ChEMBL	Phase 4 (approved)	ADRB3
FENOTEROL	ChEMBL	Phase 4 (approved)	ADRB3
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	ADRB3
FORMOTEROL	ChEMBL	Phase 4 (approved)	ADRB3
HALOPERIDOL	ChEMBL	Phase 4 (approved)	ADRB3
IBUPROFEN	ChEMBL	Phase 4 (approved)	ADRB3
ISOPROTERENOL	ChEMBL	Phase 4 (approved)	ADRB3
IVACAFTOR	ChEMBL	Phase 4 (approved)	ADRB3
LABETALOL	ChEMBL	Phase 4 (approved)	ADRB3
LEVOBUNOLOL	ChEMBL	Phase 4 (approved)	ADRB3
LORATADINE	ChEMBL	Phase 4 (approved)	ADRB3
LOVASTATIN	ChEMBL	Phase 4 (approved)	ADRB3
MEMANTINE	ChEMBL	Phase 4 (approved)	ADRB3
MICONAZOLE	ChEMBL	Phase 4 (approved)	ADRB3
MIRABEGRON	ChEMBL	Phase 4 (approved)	ADRB3
MONTELUKAST	ChEMBL	Phase 4 (approved)	ADRB3
NEFAZODONE	ChEMBL	Phase 4 (approved)	ADRB3
NELFINAVIR	ChEMBL	Phase 4 (approved)	ADRB3
NOREPINEPHRINE	ChEMBL	Phase 4 (approved)	ADRB3
OXICONAZOLE	ChEMBL	Phase 4 (approved)	ADRB3
PAMIDRONIC ACID	ChEMBL	Phase 4 (approved)	ADRB3
PERGOLIDE	ChEMBL	Phase 4 (approved)	ADRB3
PHENYLEPHRINE	ChEMBL	Phase 4 (approved)	ADRB3
PIMOZIDE	ChEMBL	Phase 4 (approved)	ADRB3
PINDOLOL	ChEMBL	Phase 4 (approved)	ADRB3
PRACTOLOL	ChEMBL	Phase 4 (approved)	ADRB3
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	ADRB3
PROPAFENONE	ChEMBL	Phase 4 (approved)	ADRB3
PROPRANOLOL	ChEMBL	Phase 4 (approved)	ADRB3
RALOXIFENE	ChEMBL	Phase 4 (approved)	ADRB3
RITONAVIR	ChEMBL	Phase 4 (approved)	ADRB3
SALMETEROL	ChEMBL	Phase 4 (approved)	ADRB3
SIMVASTATIN	ChEMBL	Phase 4 (approved)	ADRB3
SIROLIMUS	ChEMBL	Phase 4 (approved)	ADRB3
SOTALOL	ChEMBL	Phase 4 (approved)	ADRB3
SULOCTIDIL	ChEMBL	Phase 4 (approved)	ADRB3
TACROLIMUS	ChEMBL	Phase 4 (approved)	ADRB3
TAMOXIFEN	ChEMBL	Phase 4 (approved)	ADRB3
TERFENADINE	ChEMBL	Phase 4 (approved)	ADRB3
THIORIDAZINE	ChEMBL	Phase 4 (approved)	ADRB3
TICLOPIDINE	ChEMBL	Phase 4 (approved)	ADRB3
TIMOLOL	ChEMBL	Phase 4 (approved)	ADRB3
VIBEGRON	ChEMBL	Phase 4 (approved)	ADRB3
CANDESARTAN	ChEMBL	Phase 3	ADRB3
ENCLOMIPHENE	ChEMBL	Phase 3	ADRB3
NITRENDIPINE	ChEMBL	Phase 3	ADRB3
ALPRENOLOL	ChEMBL	Phase 2	ADRB3
BOPINDOLOL	ChEMBL	Phase 2	ADRB3
BUCLADESINE	ChEMBL	Phase 2	ADRB3
CIGLITAZONE	ChEMBL	Phase 2	ADRB3
CIMATEROL	ChEMBL	Phase 2	ADRB3
FLESTOLOL	ChEMBL	Phase 2	ADRB3
LEVISOPRENALINE	ChEMBL	Phase 2	ADRB3
LEVOPROPRANOLOL	ChEMBL	Phase 2	ADRB3
MILVETEROL	ChEMBL	Phase 2	ADRB3
PENFLURIDOL	ChEMBL	Phase 2	ADRB3
RAFABEGRON	ChEMBL	Phase 2	ADRB3
SOLABEGRON	ChEMBL	Phase 2	ADRB3
SOTERENOL	ChEMBL	Phase 2	ADRB3
TRETOQUINOL	ChEMBL	Phase 2	ADRB3
VEMTOBERANT	ChEMBL	Phase 2	ADRB3
XAMOTEROL	ChEMBL	Phase 2	ADRB3
ZENIDOLOL	ChEMBL	Phase 2	ADRB3
Acyclovir	PubChem	Approved	ADRB3
Allopurinol	PubChem	Approved	ADRB3
Alogliptin	PubChem	Approved	ADRB3
Bosentan	PubChem	Approved	ADRB3
Clozapine	PubChem	Approved	ADRB3
Desloratadine	PubChem	Approved	ADRB3
Fidaxomicin	PubChem	Approved	ADRB3
Glycopyrrolate	PubChem	Approved	ADRB3
Linagliptin	PubChem	Approved	ADRB3
Methotrexate	PubChem	Approved	ADRB3
Olanzapine	PubChem	Approved	ADRB3
Olmesartan Medoxomil	PubChem	Approved	ADRB3