Apomorphine

Summary

Apomorphine (CHEMBL53) is an approved small-molecule α-adrenergic drug (ATC N04BC07) targeting HTR1A, DRD1, and DRD2; indicated across 5 conditions including erectile dysfunction and parkinson disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N04BC07 (+1 more)
• Targets: 13 (HTR1A, DRD1, DRD2…)
• Indications: 5 conditions
• Clinical trials: 32
• Chemistry: 267.32 Da · C17H17NO2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL53
Name	Apomorphine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	6005
ChEBI	CHEBI:48538
ATC	N04BC07, G04BE07
Molecular formula	C17H17NO2
Molecular weight	267.32
InChIKey	VMWNQDUVQKEIOC-CYBMUJFWSA-N

SMILES: CN1CCC2=C3[C@H]1CC4=C(C3=CC=C2)C(=C(C=C4)O)O

IUPAC name: (6aR)-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-10,11-diol

Pharmacological roles (ChEBI): α-adrenergic drug, serotonergic drug, antidyskinesia agent, dopamine agonist, antiparkinson drug, emetic.

Also known as: APL-130277, Apomorphine, Apomorphinum, VR-040, VR040, R-(-)-Apomorphine, apomorphine, apomorphin, (R)-(-)-Apomorphine, SID11114270, SID26752261, SID50085845

Parent form; salt/anhydrous children: CHEMBL3187985

Patent coverage: 7,436 distinct patent families (25,813 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 25,516 (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
HTR1A	5-HT1A receptor	Partial agonist	6.9	0%	P08908
DRD1	D1 receptor	Full agonist	6.2	0%	P21728
DRD2	D2 receptor	Partial agonist	7.5	0%	P14416
DRD3	D3 receptor	Partial agonist	7.6	0%	P35462
DRD4	D4 receptor	Partial agonist	8.4	0%	P21917
DRD5	D5 receptor	Partial agonist	7.8	0%	P21918
ADRA2A	α2A-adrenoceptor	Partial agonist	6.9	0.1%	P08913
ADRA2B	α2B-adrenoceptor	Antagonist	7.2	0.2%	P18089
ADRA2C	α2C-adrenoceptor	Antagonist	7.4	0%	P18825
TRPA1	TRPA1	Activation	5.1	0.1%	O75762
HTR2A	5-HT2A receptor	Antagonist	6.9	0%	P28223
HTR2B	5-HT2B receptor	Antagonist	6.9	0.4%	P41595
HTR2C	5-HT2C receptor	Antagonist	7	0%	P28335

Broader ChEMBL bioactivity targets: 70 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Pyruvate kinase PKM, Microtubule-associated protein tau, Lysine-specific demethylase 4E, Nuclear receptor ROR-gamma, Fructose-bisphosphate aldolase, Prelamin-A/C, 4’-phosphopantetheinyl transferase ffp, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], Aspartyl aminopeptidase.

Bioactivity

ChEMBL activities: 223 potent at pChembl ≥ 5 of 264 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P61169	9.4	EC50	0.4	nM	CHEMBL_ACT_1796544
P61169	9.4	EC50	0.4	nM	CHEMBL_ACT_827253
DRD2	9.21	Ki	0.62	nM	CHEMBL_ACT_3116206
DRD2	9.18	Kd	0.66	nM	CHEMBL_ACT_1045311
P61169	9	IC50	1	nM	CHEMBL_ACT_163057
P18901	9	IC50	1	nM	CHEMBL_ACT_334112
P20288	9	IC50	1	nM	CHEMBL_ACT_905549
P18901	8.96	IC50	1.1	nM	CHEMBL_ACT_1081762
P18901	8.85	IC50	1.4	nM	CHEMBL_ACT_522358
P30729	8.82	EC50	1.5	nM	CHEMBL_ACT_827249
DRD2	8.8	EC50	1.58	nM	CHEMBL_ACT_19009954
DRD2	8.79	EC50	1.61	nM	CHEMBL_ACT_19009976
DRD2	8.77	EC50	1.7	nM	CHEMBL_ACT_13965391
P61169	8.77	IC50	1.7	nM	CHEMBL_ACT_150829
P18901	8.77	IC50	1.7	nM	CHEMBL_ACT_159466
P61169	8.77	IC50	1.7	nM	CHEMBL_ACT_840986
DRD2	8.74	EC50	1.8	nM	CHEMBL_ACT_1796543
P61169	8.74	Ki	1.8	nM	CHEMBL_ACT_5207139
P18901	8.74	IC50	1.8	nM	CHEMBL_ACT_522357
P61169	8.74	EC50	1.8	nM	CHEMBL_ACT_827252
P61169	8.72	Ki	1.9	nM	CHEMBL_ACT_2107109
P61169	8.66	Ki	2.2	nM	CHEMBL_ACT_677480
P61169	8.59	IC50	2.6	nM	CHEMBL_ACT_1151673
P18901	8.59	IC50	2.6	nM	CHEMBL_ACT_1269152
DRD3	8.59	Ki	2.6	nM	CHEMBL_ACT_5207705
P61169	8.59	IC50	2.6	nM	CHEMBL_ACT_980622
DRD2	8.44	Ki	3.6	nM	CHEMBL_ACT_1796591
P20288	8.43	Ki	3.7	nM	CHEMBL_ACT_1109809
DRD1	8.42	EC50	3.77	nM	CHEMBL_ACT_19009914
DRD2	8.4	EC50	4	nM	CHEMBL_ACT_13355068

Target pathways

Aggregated over 13 target gene(s): HTR1A, DRD1, DRD2, DRD3, DRD4, DRD5, ADRA2A, ADRA2B, ADRA2C, TRPA1, HTR2A, HTR2B, HTR2C.

Top Reactome pathways

24 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	7	ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR2A, HTR2B, HTR2C
Signaling by GPCR	7	ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR2A, HTR2B, HTR2C
Class A/1 (Rhodopsin-like receptors)	7	ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR2A, HTR2B, HTR2C
Amine ligand-binding receptors	7	ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR2A, HTR2B, HTR2C
GPCR ligand binding	7	ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR2A, HTR2B, HTR2C
GPCR downstream signalling	6	ADRA2A, ADRA2B, ADRA2C, HTR2A, HTR2B, HTR2C
Dopamine receptors	5	DRD1, DRD2, DRD3, DRD4, DRD5
G alpha (i) signalling events	5	ADRA2A, ADRA2B, ADRA2C, DRD3, DRD4
Serotonin receptors	4	HTR1A, HTR2A, HTR2B, HTR2C
Hemostasis	3	ADRA2A, ADRA2B, ADRA2C
Adrenoceptors	3	ADRA2A, ADRA2B, ADRA2C
Adrenaline signalling through Alpha-2 adrenergic receptor	3	ADRA2A, ADRA2B, ADRA2C
G alpha (q) signalling events	3	HTR2A, HTR2B, HTR2C
G alpha (z) signalling events	3	ADRA2A, ADRA2B, ADRA2C
Platelet activation, signaling and aggregation	3	ADRA2A, ADRA2B, ADRA2C
Platelet Aggregation (Plug Formation)	3	ADRA2A, ADRA2B, ADRA2C
Metabolism	2	ADRA2A, ADRA2C
Integration of energy metabolism	2	ADRA2A, ADRA2C
Metabolism of proteins	2	ADRA2A, ADRA2C
Adrenaline,noradrenaline inhibits insulin secretion	2	ADRA2A, ADRA2C
G alpha (s) signalling events	2	DRD1, DRD5
Regulation of insulin secretion	2	ADRA2A, ADRA2C
Surfactant metabolism	2	ADRA2A, ADRA2C
TRP channels	1	TRPA1

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	12
signal transduction	12
intracellular calcium ion homeostasis	8
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	6
chemical synaptic transmission	6
response to xenobiotic stimulus	6
positive regulation of MAPK cascade	6
G protein-coupled serotonin receptor signaling pathway	5
behavioral response to cocaine	5
phospholipase C-activating dopamine receptor signaling pathway	5
synaptic transmission, dopaminergic	5
response to cocaine	5
behavioral fear response	4
serotonin receptor signaling pathway	4
positive regulation of cell population proliferation	4

Indications & clinical

Indications

5 indications (2 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
erectile dysfunction	4	MONDO:0005362	EFO:0004234
Parkinson disease	4	MONDO:0005180	MONDO:0005180
brain injury	2	MONDO:0043510	MONDO:0043510
alcohol abuse	2	MONDO:0002046	MONDO:0007079

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

Clinical trials

Total trials: 32.

Phase distribution

Phase	Trials
PHASE2	13
PHASE3	8
PHASE4	4
Not specified	4
PHASE2/PHASE3	2
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02688465	PHASE4	TERMINATED	Effect of an Apomorphine Pump on the Quality of Sleep in Parkinson’s Disease Patients (POMPRENELLE).
NCT02940912	PHASE4	COMPLETED	Effect of Continuous Apomorphine During the Night on Sleep Disorders in Insomniac Patients With Parkinson’s Disease
NCT02969629	PHASE4	COMPLETED	The Effects of Apomorphine on Experimental and Clinical Pain in Patients With Chronic Radicular Pain
NCT04887467	PHASE4	COMPLETED	Monocentric, Prospective Study to Assess the Pharmacokinetic Profile of Continuous and Diurnal Subcutaneous Apomorphine Infusion in Patients With Parkinson’s Disease
NCT02339064	PHASE3	ACTIVE_NOT_RECRUITING	Infusion of Apomorphine: Long-term Safety Study
NCT05213169	PHASE2/PHASE3	RECRUITING	Apomorphine in Severe Brain-injured Patients
NCT00142545	PHASE3	COMPLETED	Long Term Safety and Efficacy of SC Apomorphine in Treatment of Off Episodes in Late-Stage Parkinson’s Disease
NCT00145171	PHASE3	COMPLETED	A Sub-Study With Patients in APO401 to Evaluate Adverse Events During Dose Introduction in Apomorphine-naïve Patients.
NCT00200512	PHASE2/PHASE3	COMPLETED	Continued Efficacy of Apomorphine After Previous Exposure of at Least Three Months
NCT00200525	PHASE3	COMPLETED	Continued Efficacy and Safety of Apomorphine in Patients With Late-Stage Parkinsons Disease
NCT02469090	PHASE3	COMPLETED	Efficacy, Safety and Tolerability Study of APL-130277 for the Acute Treatment of OFF Episodes in Patients With Parkinson’s Disease
NCT02542696	PHASE3	COMPLETED	Open-Label Phase 3 Study to Examine the Long-Term Safety, Tolerability and Efficacy of APL-130277 for the Acute Treatment of OFF Episodes in Patients With Parkinson’s Disease
NCT02864004	PHASE3	UNKNOWN	Apomorphine Pump in Early Stage of Parkinson’s Disease (EARLY-PUMP)
NCT03391882	PHASE3	COMPLETED	A Study of an Investigational Drug to See How it Affects the People With Parkinson’s Disease Complicated by Motor Fluctuations (OFF Episodes) Compared to an Approved Drug Used to Treat People With Parkinson’s Disease Complicated by Motor Fluctuations (OFF Episodes)
NCT00437177	PHASE2	UNKNOWN	Relationship Between D2 Receptors SPECT and the Apomorphine Test in Patients With OH Dependence (ALC-DRD2-APO)
NCT00472355	PHASE2	WITHDRAWN	Low Dose Apomorphine and Parkinsonism
NCT00758368	PHASE2	WITHDRAWN	Comparison of Continuous and Pulsatile Apomorphine in Parkinson’s Disease
NCT00761228	PHASE2	SUSPENDED	Efficacy Study of NH001 in Vegetative State & Minimally Conscious State Following a Traumatic Brain Injury
NCT01683292	PHASE2	COMPLETED	Single-Centre Study of VR040(Inhaled Apomorphine) in Idiopathic Parkinson’s Disease
NCT01693081	PHASE2	COMPLETED	Phase IIa Multicentre Study Investigating of VR040 in Parkinson’s Disease
NCT02228590	PHASE2	COMPLETED	A Study to Examine APL-130277 in Patients With Parkinson’s Disease
NCT02230930	PHASE2	TERMINATED	Treatment of Apomorphine-induced Skin Reactions: a Pilot Study
NCT02702076	PHASE2	UNKNOWN	Apomorphine in Parkinson’s Disease Patients With Visual Hallucinations
NCT03187301	PHASE2	COMPLETED	A Cardiac Safety Study of an Investigational Drug to See How if Affects the Heart in People With Parkinson’s Disease Complicated by Motor Fluctuations OFF Episodes
NCT03292016	PHASE2	COMPLETED	A Study That Compares the Extent to Which Apomorphine Becomes Available in the Body After Taking Either an Investigational Drug Containing Apomorphine or Apomorphine That is Injected Under the Skin in People With PD Complicated by OFF Episodes
NCT03623828	PHASE2	UNKNOWN	Treating Severe Brain-injured Patients With Apomorphine
NCT05979415	PHASE2	TERMINATED	Study to Evaluate the Efficacy and Safety of Staccato Apomorphine (AZ-009) in Patients With Parkinson’s Disease Experiencing OFF Episodes
NCT01744964	EARLY_PHASE1	COMPLETED	Apomorphine Effects on Experimental Pain
NCT00524914	Not specified	COMPLETED	Apomorphine Effect on Nociceptive Perception in Parkinson’s: a Clinical and Imaging Study
NCT03693872	Not specified	COMPLETED	Evaluation of the Nonmotor Symptomatology of Parkinsonian Patients Treated With Two Strategies Related to Apomorphine Pump Therapy in French Hospitals
NCT04786158	Not specified	COMPLETED	Subcutaneous Apomorphine in the Treatment of Progressive Supranuclear Palsy and Cortico Basal Degeneration (APOPARKA)
NCT05331573	Not specified	UNKNOWN	Parkinsonian Patients Treated With Apomorphine Pump: Observatory of Skin Lesions

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

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.

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

Molecule	Source	Status	Shared targets
CLOZAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
OLANZAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
TEGASEROD	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
AMOXAPINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
CARIPRAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
DOXEPIN	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
HALOPERIDOL	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
LOXAPINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
PROMAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
RISPERIDONE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
DESLORATADINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
Fidaxomicin	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
PRAMIPEXOLE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B
Propoxyphene	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
ASENAPINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
BENPERIDOL	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
CABERGOLINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B
CARVEDILOL	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
EBASTINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
ILOPERIDONE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
IMIPRAMINE	ChEMBL	Phase 4 (approved)	ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
MAPROTILINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
MIANSERIN	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
NEFAZODONE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
PERGOLIDE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
PIMOZIDE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
PROMETHAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
QUETIAPINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
SERTINDOLE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
SUNITINIB	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
THIORIDAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
THIOTHIXENE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
TRAZODONE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
ZIPRASIDONE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
LISURIDE	ChEMBL	Phase 3	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
PENFLURIDOL	ChEMBL	Phase 2	ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
RITANSERIN	ChEMBL	Phase 2	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2C
SPIPERONE	ChEMBL	Phase 2	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
ZOTEPINE	ChEMBL	Phase 2	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
Pyrazinamide	PubChem	Approved	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
Afatinib	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2B, HTR2C
chenodiol	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2B, HTR2C
PALIPERIDONE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR2A, HTR2C
CISAPRIDE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2B, HTR2C
CLEMASTINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2B, HTR2C
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2B, HTR2C
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR2A, HTR2B, HTR2C
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2B, HTR2C
ECONAZOLE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR2A, HTR2B, HTR2C
ERGOTAMINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2B, HTR2C
IPRINDOLE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C