Risperidone

Summary

Risperidone (CHEMBL85) is an approved small-molecule serotonergic antagonist (ATC N05AX08) targeting HTR6, HTR7, and HTR1A; indicated across 34 conditions including psychotic disorder and autism.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N05AX08
• Targets: 16 (HTR6, HTR7, HTR1A…)
• Indications: 34 conditions
• Clinical trials: 384
• Chemistry: 410.5 Da · C23H27FN4O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL85
Name	Risperidone
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5073
ChEBI	CHEBI:8871
ATC	N05AX08
Molecular formula	C23H27FN4O2
Molecular weight	410.5
InChIKey	RAPZEAPATHNIPO-UHFFFAOYSA-N

SMILES: CC1=C(C(=O)N2CCCCC2=N1)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F

IUPAC name: 3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one

ChEBI definition: A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.

Pharmacological roles (ChEBI): serotonergic antagonist, α-adrenergic antagonist, H1-receptor antagonist, second generation antipsychotic, dopaminergic antagonist, psychotropic drug, EC 3.4.21.26 (prolyl oligopeptidase) inhibitor.

Also known as: LY-03004, LY03004, N05AX08, NSC-759895, Okedi, Perseris, Perseris kit, R 64 766, R-64,766, R-64766, RCN-3028, RCN3028

Patent coverage: 11,060 distinct patent families (41,869 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 41,767 (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
HTR6	5-HT6 receptor	Antagonist	5.6	0.2%	P50406
HTR7	5-HT7 receptor	Inverse agonist	8.7	0.8%	P34969
HTR1A	5-HT1A receptor	Antagonist	6.5	0%	P08908
DRD2	D2 receptor	Antagonist	9.36	0%	P14416
DRD3	D3 receptor	Antagonist	7	0%	P35462
ADRA1A	α1A-adrenoceptor	Antagonist	8.7		P35348
ADRA1B	α1B-adrenoceptor	Antagonist	8	0%	P35368
ADRA1D	α1D-adrenoceptor	Antagonist	7.4	0.2%	P25100
ADRA2A	α2A-adrenoceptor	Antagonist	7.3	0.1%	P08913
HRH1	H1 receptor	Antagonist	7.8	0%	P35367
HTR1B	5-HT1B receptor	Antagonist	7.3	0.2%	P28222
HTR1D	5-HT1D receptor	Antagonist	8	0%	P28221
HTR1E	5-ht1e receptor	Antagonist	5.9	0%	P28566
HTR1F	5-HT1F receptor	Antagonist	5.9	0.1%	P30939
HTR2A	5-HT2A receptor	Inverse agonist	10	0%	P28223
HTR2C	5-HT2C receptor	Inverse agonist	7.6	0%	P28335

Broader ChEMBL bioactivity targets: 69 (assay-derived). Sample: Survival motor neuron protein, Peripheral myelin protein 22, Solute carrier family 22 member 2, Multidrug and toxin extrusion protein 1, 5-hydroxytryptamine receptor 2B, D(1B) dopamine receptor, Alpha-2A adrenergic receptor, 5-hydroxytryptamine receptor 1B, Adrenergic receptor alpha-1, Alpha-2C adrenergic receptor.

Bioactivity

ChEMBL activities: 386 potent at pChembl ≥ 5 of 404 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HTR2A	10	Ki	0.1	nM	CHEMBL_ACT_7807022
P08909	9.85	Ki	0.14	nM	CHEMBL_ACT_1006961
HTR2A	9.82	Ki	0.15	nM	CHEMBL_ACT_15083428
P14842	9.82	Ki	0.15	nM	CHEMBL_ACT_2248449
P14842	9.8	Ki	0.16	nM	CHEMBL_ACT_1290209
HTR2A	9.8	Ki	0.16	nM	CHEMBL_ACT_448150
P14842	9.79	Ki	0.16	nM	CHEMBL_ACT_1988736
HTR2A	9.77	Ki	0.17	nM	CHEMBL_ACT_22475676
P14842	9.74	Ki	0.18	nM	CHEMBL_ACT_13318948
P14842	9.74	Ki	0.18	nM	CHEMBL_ACT_16834554
P14842	9.74	Ki	0.18	nM	CHEMBL_ACT_18813863
P14842	9.72	Ki	0.19	nM	CHEMBL_ACT_22792304
HTR2A	9.72	Ki	0.19	nM	CHEMBL_ACT_23202244
P08909	9.7	Ki	0.2	nM	CHEMBL_ACT_238255
P08909	9.7	Ki	0.2	nM	CHEMBL_ACT_312175
P14842	9.7	Ki	0.2	nM	CHEMBL_ACT_585501
HTR2A	9.64	Ki	0.23	nM	CHEMBL_ACT_25617982
P14842	9.6	Ki	0.25	nM	CHEMBL_ACT_13937336
P14842	9.6	Ki	0.25	nM	CHEMBL_ACT_16399871
HTR2A	9.54	Ki	0.29	nM	CHEMBL_ACT_2577191
P14842	9.51	Ki	0.31	nM	CHEMBL_ACT_15766712
P14842	9.51	Ki	0.31	nM	CHEMBL_ACT_229769
P14842	9.51	Ki	0.31	nM	CHEMBL_ACT_519028
HTR2A	9.46	IC50	0.35	nM	CHEMBL_ACT_7807021
HTR2A	9.43	Ki	0.37	nM	CHEMBL_ACT_19099533
HTR2A	9.41	Ki	0.39	nM	CHEMBL_ACT_22892530
HTR2A	9.41	Ki	0.39	nM	CHEMBL_ACT_680061
HTR7	9.4	Ki	0.4	nM	CHEMBL_ACT_18653071
P43140	9.4	Ki	0.4	nM	CHEMBL_ACT_7804804
DRD2	9.36	Ki	0.44	nM	CHEMBL_ACT_680057

Target pathways

Aggregated over 16 target gene(s): HTR6, HTR7, HTR1A, DRD2, DRD3, ADRA1A, ADRA1B, ADRA1D, ADRA2A, HRH1, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2C.

Top Reactome pathways

26 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	13	ADRA1A, ADRA1B, ADRA1D, ADRA2A, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2C, HTR6, HTR7
Signaling by GPCR	13	ADRA1A, ADRA1B, ADRA1D, ADRA2A, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2C, HTR6, HTR7
Class A/1 (Rhodopsin-like receptors)	13	ADRA1A, ADRA1B, ADRA1D, ADRA2A, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2C, HTR6, HTR7
Amine ligand-binding receptors	13	ADRA1A, ADRA1B, ADRA1D, ADRA2A, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2C, HTR6, HTR7
GPCR ligand binding	13	ADRA1A, ADRA1B, ADRA1D, ADRA2A, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2C, HTR6, HTR7
GPCR downstream signalling	12	ADRA1A, ADRA1B, ADRA1D, ADRA2A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2C, HTR6, HTR7
Serotonin receptors	9	HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2C, HTR6, HTR7
G alpha (q) signalling events	6	ADRA1A, ADRA1B, ADRA1D, HRH1, HTR2A, HTR2C
G alpha (i) signalling events	6	ADRA2A, DRD3, HTR1B, HTR1D, HTR1E, HTR1F
Adrenoceptors	4	ADRA1A, ADRA1B, ADRA1D, ADRA2A
G alpha (12/13) signalling events	3	ADRA1A, ADRA1B, ADRA1D
Dopamine receptors	2	DRD2, DRD3
G alpha (s) signalling events	2	HTR6, HTR7
Hemostasis	1	ADRA2A
Metabolism	1	ADRA2A
Integration of energy metabolism	1	ADRA2A
Histamine receptors	1	HRH1
Adrenaline signalling through Alpha-2 adrenergic receptor	1	ADRA2A
Metabolism of proteins	1	ADRA2A
Adrenaline,noradrenaline inhibits insulin secretion	1	ADRA2A
G alpha (z) signalling events	1	ADRA2A
Regulation of insulin secretion	1	ADRA2A
Surfactant metabolism	1	ADRA2A
Platelet activation, signaling and aggregation	1	ADRA2A
Platelet Aggregation (Plug Formation)	1	ADRA2A
RHOBTB3 ATPase cycle	1	HTR7

Dominant GO biological processes

GO term	Targets
signal transduction	16
G protein-coupled receptor signaling pathway	16
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	10
chemical synaptic transmission	10
phospholipase C-activating G protein-coupled receptor signaling pathway	6
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	5
G protein-coupled serotonin receptor signaling pathway	5
adenylate cyclase-inhibiting serotonin receptor signaling pathway	5
adenylate cyclase-activating G protein-coupled receptor signaling pathway	5
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	5
positive regulation of cell population proliferation	4
regulation of vasoconstriction	4
intracellular calcium ion homeostasis	4
response to xenobiotic stimulus	4
positive regulation of ERK1 and ERK2 cascade	4

Indications & clinical

Indications

34 indications (7 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
psychotic disorder	4	MONDO:0005485	EFO:0005407
autism	4	MONDO:0005260	EFO:0003758
schizoaffective disorder	4	MONDO:0005487	EFO:0005411
bipolar disorder	4	MONDO:0004985	EFO:0009963
anxiety	3	MONDO:0011918	EFO:0005230
dementia	3	MONDO:0001627	HP:0000726
oppositional defiant disorder	3	MONDO:0000495	HP:0010865
developmental disability	3	MONDO:0005287	EFO:0003852
neurodevelopmental disorder	3	MONDO:0700092	EFO:0010642
major depressive disorder	3	MONDO:0002009	MONDO:0002009
conduct disorder	3	MONDO:0005352	EFO:0004216
vascular dementia	3	MONDO:0004648	EFO:0004718
depressive disorder	3	MONDO:0002050	MONDO:0002050
Alzheimer disease	3	MONDO:0004975	MONDO:0004975
Rett syndrome	3	MONDO:0010726	MONDO:0010726
intellectual disability	3	MONDO:0001071	HP:0001249
mental disorder	3	MONDO:0005084	EFO:0000677
cocaine dependence	2	MONDO:0005186	EFO:0002610
methamphetamine dependence	2	MONDO:0005419	EFO:0004701
post-traumatic stress disorder	2	MONDO:0005146	EFO:0001358
autism spectrum disorder	2	MONDO:0005258	EFO:0003756
Tourette syndrome	2	MONDO:0007661	EFO:0004895
drug dependence	2	MONDO:0005303	EFO:0003890
obsessive-compulsive disorder	2	MONDO:0008114	EFO:0004242
drug-induced dyskinesia	1	MONDO:0006732	EFO:1000904
schizotypal personality disorder	1	MONDO:0001087	MONDO:0001087
Huntington disease	1	MONDO:0007739	MONDO:0007739
opiate dependence	0	MONDO:0005530	EFO:0005611

6 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 384.

Phase distribution

Phase	Trials
PHASE4	130
PHASE3	86
Not specified	69
PHASE2	46
PHASE1	36
PHASE2/PHASE3	8
PHASE1/PHASE2	6
EARLY_PHASE1	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00768820	PHASE4	RECRUITING	The Psychiatric and Cognitive Phenotypes in Velocardiofacial Syndrome
NCT04478838	PHASE4	RECRUITING	Extended (Alternate Day) Antipsychotic Dosing
NCT04580134	PHASE4	RECRUITING	CLOZAPINE Response in Biotype-1
NCT06969755	PHASE4	RECRUITING	Biomarkers to Enhance Early Schizophrenia Treatment
NCT07047651	PHASE4	ACTIVE_NOT_RECRUITING	Τhe Combination of Pharmacotherapy With RECOVERYTRSGR and RECOVERYTRSBDGR.
NCT07483294	PHASE4	RECRUITING	Cerebellum-based Imaging Neural Markers for Antipsychotic Response
NCT00000374	PHASE4	COMPLETED	Treatment for First-Episode Schizophrenia
NCT00014001	PHASE4	COMPLETED	CATIE- Schizophrenia Trial
NCT00018668	PHASE4	COMPLETED	Antipsychotic Response in Schizophrenia
NCT00034580	PHASE4	COMPLETED	Olanzapine Versus Active Comparator in the Treatment of Bipolar I Disorder
NCT00044655	PHASE4	COMPLETED	Switching Medication to Treat Schizophrenia
NCT00048802	PHASE4	COMPLETED	Treatment and Outcome of Early Onset Bipolar Disorder
NCT00053703	PHASE4	COMPLETED	Treatment of Early Onset Schizophrenia Spectrum Disorders (TEOSS)
NCT00056498	PHASE4	COMPLETED	Risperidone Treatment in Schizophrenia Patients Who Are Currently Taking Clozapine
NCT00061802	PHASE4	COMPLETED	Efficacy and Safety of Two Atypical Antipsychotics vs. Placebo in Patients With an Acute Exacerbation of Either Schizophrenia or Schizoaffective Disorder
NCT00108368	PHASE4	COMPLETED	The Effects of Risperidone and Olanzapine on Thinking
NCT00130923	PHASE4	COMPLETED	Risperidone Long-acting Versus Oral Risperidone in Patients With Schizophrenia and Alcohol Use Disorder
NCT00140426	PHASE4	COMPLETED	A Double-blind, Placebo Controlled Trial of Risperidone for the Treatment of Anorexia Nervosa
NCT00157378	PHASE4	UNKNOWN	Optimization of Acute Treatment in First Episode Schizophrenia
NCT00167479	PHASE4	COMPLETED	A Study of Risperidone Monotherapy in Bipolar Anxiety
NCT00177567	PHASE4	COMPLETED	Treatment of Geriatric Bipolar Mood Disorders: A Pilot Study
NCT00178854	PHASE4	WITHDRAWN	Risperidone (Risperdal) Augmentation in Depressed Partial Responders to SRI Treatment
NCT00181935	PHASE4	COMPLETED	Risperidone Versus Olanzapine for Mania in Preschool Children 4 to 6 Years of Age With Bipolar Disorder
NCT00182013	PHASE4	COMPLETED	Open-Label Comparative Study of Risperidone Versus Olanzapine Versus Quetiapine for Mania in Children and Adolescents With Bipolar I and Bipolar II Disorder
NCT00183625	PHASE4	COMPLETED	Supported Employment and Skills Training in Conjunction With Pharmacotherapy in Schizophrenia Patients
NCT00190749	PHASE4	COMPLETED	Safety Study of Olanzapine and a Comparator in Patients With Schizophrenia and Schizoaffective Disorder
NCT00203528	PHASE4	COMPLETED	Divalproex ER vs. Risperidone for Bipolar Disorder With Comorbid Substance Use Disorder
NCT00203723	PHASE4	TERMINATED	Use of Risperidone in ECT for Treatment Resistant Depression
NCT00203788	PHASE4	COMPLETED	Improving Work Outcome in People With Recent-onset Schizophrenia
NCT00204347	PHASE4	COMPLETED	Effective Measurement of Risperidone Treatment Outcome for Persons With Borderline Personality Disorder
NCT00205699	PHASE4	COMPLETED	Metabolic Effects of Antipsychotics in Children
NCT00206102	PHASE4	COMPLETED	A Study of the Cataractogenic Potential of Seroquel and Risperdal in the Treatment of Participants With Schizophrenia or Schizoaffective Disorder
NCT00208143	PHASE4	COMPLETED	Seroquel Therapy for Substance Use Disorders Comorbid With Schizophrenia
NCT00208182	PHASE4	COMPLETED	Risperidone in the Treatment of PTSD in Women Survivors of Domestic Abuse and Rape Trauma
NCT00208819	PHASE4	COMPLETED	A Comparison of Two Standard Therapies in the Management of Dementia With Agitation
NCT00216528	PHASE4	COMPLETED	A Study to Evaluate Symptomatic Remission in Schizophrenia With Long Acting Risperidone Microspheres
NCT00216554	PHASE4	COMPLETED	The Safety and Efficacy of Risperidone as Adjunctive Therapy to Mood Stabilizers in the Long-term Treatment of Bipolar Mania
NCT00216632	PHASE4	COMPLETED	A Study of Treatment Success in Changing From Olanzapine to Long-acting Injectable Risperidone (RISPERDAL® CONSTA™)
NCT00224315	PHASE4	COMPLETED	Clozapine-Augmentation With Ziprasidone or Risperidone, a Randomized, Prospective Trial
NCT00236379	PHASE4	COMPLETED	A Study of the Effects of Risperidone and Olanzapine on Blood Glucose (Sugar) in Patients With Schizophrenia or Schizoaffective Disorder

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (1) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of DPWG Guideline for risperidone and CYP2D6	DPWG	CYP2D6	yes	yes

PharmGKB also curates 78 clinical and 385 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.

1,026 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2C, HTR6, HTR7
BREXPIPRAZOLE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1B, HTR1D, HTR1E, HTR2A, HTR2C, HTR6, HTR7
CLOZAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1B, HTR1E, HTR1F, HTR2A, HTR2C, HTR6, HTR7
OLANZAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1B, HTR1E, HTR1F, HTR2A, HTR2C, HTR6, HTR7
QUETIAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1E, HTR1F, HTR2A, HTR2C, HTR6, HTR7
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1B, HTR1D, HTR2A, HTR2C, HTR6, HTR7
AZELASTINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1B, HTR1D, HTR1E, HTR2A, HTR2C, HTR6, HTR7
CARIPRAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1B, HTR1D, HTR2A, HTR2C, HTR6, HTR7
NEFAZODONE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1B, HTR1D, HTR2A, HTR2C, HTR6, HTR7
CYPROHEPTADINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1E, HTR1F, HTR2A, HTR2C, HTR6, HTR7
ERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2C, HTR6
IMIPRAMINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, DRD2, DRD3, HRH1, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2C, HTR6, HTR7
ZIPRASIDONE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1E, HTR2A, HTR2C, HTR6, HTR7
YOHIMBINE	ChEMBL + PubChem	Phase 3 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR6
LATREPIRDINE	ChEMBL	Phase 3	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1D, HTR1E, HTR2A, HTR2C, HTR6, HTR7
RITANSERIN	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1B, HTR1E, HTR2A, HTR2C, HTR6, HTR7
ASENAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1E, HTR2A, HTR2C, HTR6
HALOPERIDOL	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6, HTR7
MIANSERIN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1D, HTR2A, HTR2C, HTR6, HTR7
SERTINDOLE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1B, HTR2A, HTR2C, HTR6
TEGASEROD	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HTR1A, HTR1D, HTR2A, HTR2C, HTR6, HTR7
VILAZODONE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1B, HTR1D, HTR6, HTR7
NIGULDIPINE	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1B, HTR2C, HTR6, HTR7
SPIRAMIDE	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1D, HTR2A, HTR6, HTR7
METHYLERGONOVINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1E, HTR1F, HTR2A, HTR2C, HTR6
PRAMIPEXOLE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1B, HTR1E, HTR2A, HTR7
AMOXAPINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6, HTR7
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6, HTR7
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6, HTR7
CISAPRIDE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR7
DOXEPIN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6, HTR7
EBASTINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6, HTR7
KETANSERIN	ChEMBL	Phase 4 (approved)	ADRA1A, DRD2, DRD3, HRH1, HTR1A, HTR1B, HTR1D, HTR2A, HTR2C, HTR6, HTR7
KETOTIFEN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1B, HTR2A, HTR2C, HTR6, HTR7
OXYMETAZOLINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD3, HTR1A, HTR1B, HTR1D, HTR2A, HTR2C, HTR6
PROMAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6, HTR7
SILODOSIN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR1B, HTR1D, HTR7
TERFENADINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6
THIORIDAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6, HTR7
XYLOMETAZOLINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HTR1A, HTR1B, HTR1D, HTR2A, HTR2C
FANANSERIN	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6, HTR7
METERGOLINE	ChEMBL	Phase 2	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6, HTR7
PIZOTYLINE	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR7
SPIPERONE	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6, HTR7
PALIPERIDONE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA2A, DRD2, DRD3, HRH1, HTR1B, HTR1D, HTR2A, HTR2C, HTR7
Pyrazinamide	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6, HTR7
TAMSULOSIN	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR7
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6
AMLODIPINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, ADRA2A, DRD2, DRD3, HTR1A, HTR2A, HTR2C, HTR6
BUSPIRONE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR7
CARVEDILOL	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HTR1A, HTR2A, HTR2C, HTR6, HTR7
CINACALCET	ChEMBL	Phase 4 (approved)	ADRA1B, DRD2, DRD3, HRH1, HTR1A, HTR1D, HTR2A, HTR2C, HTR6, HTR7
CLEMASTINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6
LOXAPINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6, HTR7
MAPROTILINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6
METHYSERGIDE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6, HTR7
NORTRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6
PERGOLIDE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, ADRA2A, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2C, HTR6