Blonanserin

Summary

Blonanserin (CHEMBL178803) is an approved small molecule targeting DRD2 and HTR2A; indicated across 1 condition.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Targets: 2 (DRD2, HTR2A)
• Indications: 1 condition
• Clinical trials: 2
• Chemistry: 367.5 Da · C23H30FN3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL178803
Name	Blonanserin
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	125564
Molecular formula	C23H30FN3
Molecular weight	367.5
InChIKey	XVGOZDAJGBALKS-UHFFFAOYSA-N

SMILES: CCN1CCN(CC1)C2=NC3=C(CCCCCC3)C(=C2)C4=CC=C(C=C4)F

IUPAC name: 2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine

Also known as: AD-5423, Blonanserin, Blonanserina, Blonanserine, DSP-5423, SID144206818, BLONANSERIN, BLONANSERIN (LONASEN), blonanserin, BlonanserinÊ, Blonanserin (Lonasen), BlonanserinÂ

Patent coverage: 901 distinct patent families (3,292 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 3,267 (99%) 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
DRD2	D2 receptor	Antagonist	9.85	0%	P14416
HTR2A	5-HT2A receptor	Antagonist	9.09	0%	P28223

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: D(2) dopamine receptor, 5-hydroxytryptamine receptor 2A.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DRD2	9.85	Ki	0.14	nM	CHEMBL_ACT_1421609
HTR2A	9.09	Ki	0.81	nM	CHEMBL_ACT_1421610

Target pathways

Aggregated over 2 target gene(s): DRD2, HTR2A.

Top Reactome pathways

9 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	1	HTR2A
Signaling by GPCR	1	HTR2A
Class A/1 (Rhodopsin-like receptors)	1	HTR2A
Amine ligand-binding receptors	1	HTR2A
GPCR downstream signalling	1	HTR2A
Dopamine receptors	1	DRD2
Serotonin receptors	1	HTR2A
G alpha (q) signalling events	1	HTR2A
GPCR ligand binding	1	HTR2A

Dominant GO biological processes

GO term	Targets
temperature homeostasis	2
intracellular calcium ion homeostasis	2
response to xenobiotic stimulus	2
regulation of dopamine secretion	2
response to cocaine	2
behavioral response to cocaine	2
release of sequestered calcium ion into cytosol	2
negative regulation of synaptic transmission, glutamatergic	2
positive regulation of ERK1 and ERK2 cascade	2
presynaptic modulation of chemical synaptic transmission	2
signal transduction	2
G protein-coupled receptor signaling pathway	2
response to hypoxia	1
response to amphetamine	1
nervous system process involved in regulation of systemic arterial blood pressure	1

Indications & clinical

Indications

1 indication (0 at ChEMBL trial phase 4).

The 1 indication record carries no mapped disease name (EFO/MeSH-only); none shown.

Clinical trials

Total trials: 2.

Phase distribution

Phase	Trials
PHASE4	1
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03784222	PHASE4	TERMINATED	Effects on Social and Cognition Functions of Blonanserin in First Episode Schizophrenia Patients
NCT01516424	PHASE3	COMPLETED	Efficiency Study to Investigate Blonanserin in Treatment of Schizophrenia When Compared With Risperidone

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 3 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

480 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	DRD2, HTR2A
Fidaxomicin	ChEMBL + PubChem	Phase 4 (approved)	DRD2, HTR2A
Propoxyphene	ChEMBL + PubChem	Phase 4 (approved)	DRD2, HTR2A
ACETOPHENAZINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
AMIODARONE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
AMISULPRIDE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
AMLODIPINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
AMOXAPINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
APOMORPHINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
ASENAPINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
AZATADINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
AZELASTINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
BENPERIDOL	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
BENZQUINAMIDE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
BENZTROPINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
BEPRIDIL	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
BOSUTINIB	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
BROMPERIDOL	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
BUSPIRONE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
BUTRIPTYLINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
CABERGOLINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
CANNABIDIOL	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
CARIPRAZINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
CARVEDILOL	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
CINACALCET	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
CINNARIZINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
CISAPRIDE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
CLEMASTINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
CLOZAPINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
CYCLOBENZAPRINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
DARIFENACIN	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
DESIPRAMINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
DESLORATADINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
DIBENZEPIN	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
DIPHENIDOL	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
DOBUTAMINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
DOMPERIDONE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
DOTHIEPIN	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
DOXEPIN	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
DROPERIDOL	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
DULOXETINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
EBASTINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
ECONAZOLE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
ERGOTAMINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
FEXOFENADINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
FLUOXETINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A
FLUSPIRILENE	ChEMBL	Phase 4 (approved)	DRD2, HTR2A