Cabergoline

Summary

Cabergoline (CHEMBL1201087) is an approved small-molecule dopamine agonist (ATC G02CB03) targeting HTR1A, DRD1, and DRD2; indicated across 15 conditions including hypothalamic neoplasm and parkinson disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: G02CB03 (+1 more)
• Targets: 15 (HTR1A, DRD1, DRD2…)
• Indications: 15 conditions
• Clinical trials: 60
• Chemistry: 451.6 Da · C26H37N5O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1201087
Name	Cabergoline
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	54746
ChEBI	CHEBI:3286
ATC	G02CB03, N04BC06
Molecular formula	C26H37N5O2
Molecular weight	451.6
InChIKey	KORNTPPJEAJQIU-KJXAQDMKSA-N

SMILES: CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@H]2[C@@H](CC3=CNC4=CC=CC2=C34)N(C1)CC=C

IUPAC name: (6aR,9R,10aR)-N-[3-(dimethylamino)propyl]-N-(ethylcarbamoyl)-7-prop-2-enyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinoline-9-carboxamide

ChEBI definition: An N-acylurea that is (8R)-ergoline-8-carboxamide in which the hydrogen attached to the piperidine nitrogen (position 6) is substituted by an allyl group and the hydrogens attached to the carboxamide nitrogen are substituted by a 3-(dimethylamino)propyl group and an N-ethylcarbamoyl group. A dopamine D2 receptor agonist, cabergoline is used in the management of Parkinson’s disease and of disorders associated with hyperprolactinaemia.

Pharmacological roles (ChEBI): dopamine agonist, antiparkinson drug, antineoplastic agent.

Also known as: Cabaser, Cabergolina, Cabergoline, Dostinex, FCE 21336, FCE-21336, Velactis, CABERGOLINE, cabergoline, SID144206142, SID170464667

Patent coverage: 3,065 distinct patent families (12,778 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 12,729 (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
HTR1A	5-HT1A receptor	Full agonist	7.7	0%	P08908
DRD1	D1 receptor	Full agonist	6.7	0%	P21728
DRD2	D2 receptor	Partial agonist	9.2	0%	P14416
DRD3	D3 receptor	Partial agonist	9.1	0%	P35462
DRD4	D4 receptor	Partial agonist	7.3	0%	P21917
DRD5	D5 receptor	Full agonist	7.7	0%	P21918
ADRA1A	α1A-adrenoceptor	Antagonist	6.5		P35348
ADRA2A	α2A-adrenoceptor	Antagonist	7.9	0.1%	P08913
ADRA2B	α2B-adrenoceptor	Antagonist	7.1	0.2%	P18089
ADRA2C	α2C-adrenoceptor	Antagonist	7.7	0%	P18825
HTR1B	5-HT1B receptor	Full agonist	6.3	0.2%	P28222
HTR1D	5-HT1D receptor	Partial agonist	8.1	0%	P28221
HTR2A	5-HT2A receptor	Full agonist	8.2	0%	P28223
HTR2B	5-HT2B receptor	Full agonist	8.9	0.4%	P41595
HTR2C	5-HT2C receptor	Full agonist	6.2	0%	P28335

Broader ChEMBL bioactivity targets: 18 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Histamine H2 receptor, Alpha-2B adrenergic receptor, D(1A) dopamine receptor, Dopamine receptor, 5-hydroxytryptamine receptor 1A, D(2) dopamine receptor, Acetylcholinesterase.

Bioactivity

ChEMBL activities: 36 potent at pChembl ≥ 5 of 39 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DRD2	9.44	Ki	0.36	nM	CHEMBL_ACT_25917657
DRD2	9.44	Ki	0.36	nM	CHEMBL_ACT_25917756
HTR2B	8.85	Ki	1.4	nM	CHEMBL_ACT_12659679
DRD1	8.85	Ki	1.4	nM	CHEMBL_ACT_25553895
DRD3	8.52	AC50	3	nM	CHEMBL_ACT_25194835
HTR2B	8.49	AC50	3.2	nM	CHEMBL_ACT_25201787
DRD3	8.12	AC50	7.6	nM	CHEMBL_ACT_25193803
HTR2A	8.11	AC50	7.7	nM	CHEMBL_ACT_25173709
HTR1A	8.08	AC50	8.3	nM	CHEMBL_ACT_25165346
HTR2B	8.07	AC50	8.6	nM	CHEMBL_ACT_25164189
HTR2B	7.89	EC50	13	nM	CHEMBL_ACT_12659655
DRD2	7.89	AC50	13	nM	CHEMBL_ACT_25140614
DRD2	7.89	EC50	13	nM	CHEMBL_ACT_25553897
HTR2B	7.83	AC50	14.8	nM	CHEMBL_ACT_25164296
DRD1	7.43	AC50	36.7	nM	CHEMBL_ACT_25180791
HTR2A	7.2	AC50	62.6	nM	CHEMBL_ACT_25226596
HTR1A	7.14	AC50	73	nM	CHEMBL_ACT_25164594
ADRA2A	6.99	AC50	102.7	nM	CHEMBL_ACT_25156751
ADRA1A	6.85	AC50	141.9	nM	CHEMBL_ACT_25208816
HTR1A	6.79	AC50	162.1	nM	CHEMBL_ACT_25217284
HTR2B	6.72	AC50	188.7	nM	CHEMBL_ACT_25228982
ADRA2A	6.54	EC50	285.4	nM	CHEMBL_ACT_25751423
ADRA2C	6.52	AC50	300	nM	CHEMBL_ACT_25148159
ADRA1A	6.22	AC50	598.8	nM	CHEMBL_ACT_25230024
DRD1	6.19	AC50	648.1	nM	CHEMBL_ACT_25115532
ADRA2A	6.14	AC50	715.8	nM	CHEMBL_ACT_25156022
ADRA2A	5.97	AC50	1078	nM	CHEMBL_ACT_25220156
ADRA2B	5.6	AC50	2500	nM	CHEMBL_ACT_25143974
ADRA1A	5.44	AC50	3618	nM	CHEMBL_ACT_25138092
DRD1	5.42	Ki	3800	nM	CHEMBL_ACT_25917635

Target pathways

Aggregated over 15 target gene(s): HTR1A, DRD1, DRD2, DRD3, DRD4, DRD5, ADRA1A, ADRA2A, ADRA2B, ADRA2C, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C.

Top Reactome pathways

24 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	10	ADRA1A, ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
Signaling by GPCR	10	ADRA1A, ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
Class A/1 (Rhodopsin-like receptors)	10	ADRA1A, ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
Amine ligand-binding receptors	10	ADRA1A, ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
GPCR ligand binding	10	ADRA1A, ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
GPCR downstream signalling	9	ADRA1A, ADRA2A, ADRA2B, ADRA2C, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
G alpha (i) signalling events	7	ADRA2A, ADRA2B, ADRA2C, DRD3, DRD4, HTR1B, HTR1D
Serotonin receptors	6	HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
Dopamine receptors	5	DRD1, DRD2, DRD3, DRD4, DRD5
Adrenoceptors	4	ADRA1A, ADRA2A, ADRA2B, ADRA2C
G alpha (q) signalling events	4	ADRA1A, HTR2A, HTR2B, HTR2C
Hemostasis	3	ADRA2A, ADRA2B, ADRA2C
Adrenaline signalling through Alpha-2 adrenergic receptor	3	ADRA2A, ADRA2B, ADRA2C
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
G alpha (12/13) signalling events	1	ADRA1A

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	15
signal transduction	15
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	8
chemical synaptic transmission	8
positive regulation of MAPK cascade	7
intracellular calcium ion homeostasis	7
response to xenobiotic stimulus	6
regulation of vasoconstriction	5
adenylate cyclase-activating G protein-coupled receptor signaling pathway	5
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
positive regulation of ERK1 and ERK2 cascade	5

Indications & clinical

Indications

15 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
hypothalamic neoplasm	4	MONDO:0006799	EFO:1000979
Parkinson disease	4	MONDO:0005180	MONDO:0005180
restless legs syndrome	3	MONDO:0005391	EFO:0004270
diabetes mellitus	3	MONDO:0005015	EFO:0000400
ovarian hyperstimulation syndrome	3	MONDO:0011972	MONDO:0011972
infertility disorder	2	MONDO:0005047	EFO:0000545
cocaine dependence	2	MONDO:0005186	EFO:0002610
endometriosis	2	MONDO:0005133	EFO:0001065
reproductive system disorder	2	MONDO:0005039	EFO:0000512
ACTH-dependent Cushing syndrome	2	MONDO:0020528	EFO:1001110
polycystic ovary syndrome	2	MONDO:0008487	EFO:0000660
obesity disorder	1	MONDO:0011122	EFO:0001073
substance-related disorder	1	MONDO:0002494	MONDO:0002491
breast neoplasm	0	MONDO:0021100	MONDO:0007254

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

Clinical trials

Total trials: 60.

Phase distribution

Phase	Trials
PHASE2	13
Not specified	13
PHASE3	11
PHASE4	10
PHASE2/PHASE3	5
PHASE1	4
PHASE1/PHASE2	2
EARLY_PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06123026	PHASE4	RECRUITING	Pharmacological Inhibition of Lactation After 16 to 20 Week Abortion
NCT07034859	PHASE4	ENROLLING_BY_INVITATION	Cabergoline in the Management of Nonfunctioning Pituitary Adenoma
NCT07603466	PHASE4	ENROLLING_BY_INVITATION	Combination Osilodrostat and Cabergoline in Cushing’s Disease
NCT00153972	PHASE4	COMPLETED	Dopamine Turnover Rate as Surrogate Parameter for Diagnosis of Early Parkinson’s Disease
NCT00174239	PHASE4	TERMINATED	Study Of Cabaser and Sinemet CR For The Treatment Of Nighttime Symptoms Associated With Parkinson’s Disease.
NCT01278342	PHASE4	COMPLETED	Study to Evaluate the Efficacy and Safety of Sandostatin LAR at High Dose or in Combination Either With GH-receptor Antagonist or Dopamine-agonist in Acromegalic Patients
NCT01794793	PHASE4	COMPLETED	Study to Allow Access to Pasireotide for Patients Benefiting From Pasireotide Treatment in Novartis-sponsored Studies
NCT01957839	PHASE4	COMPLETED	Color Doppler Analysıs Of Uterin And Intraovarian Blood Flow Before And After Treatment Wıth Cabergoline In Hyperprolactinemic Patients
NCT03263299	PHASE4	UNKNOWN	Value of Cabergoline and Low Dose Aspirin in Poor Responders Undergoing ICSI-ET With GnRH Agonist Flare-Up-Protocol
NCT04096027	PHASE4	COMPLETED	Cabergoline Before or After Oocyte Collection for Follicular Resolution
NCT02288962	PHASE3	ACTIVE_NOT_RECRUITING	Dopamine Agonist Treatment of Non-functioning Pituitary Adenomas
NCT07124221	PHASE3	RECRUITING	A Phase III Clinical Study of Cabergoline Tablets Compared With Bromocriptine Mesylate Tablets
NCT07463235	PHASE3	RECRUITING	Safety and Potency of a High Cabergoline Dosage in Microprolactinomas
NCT00440258	PHASE3	COMPLETED	Cabergoline Reduces OHSS
NCT00625547	PHASE3	COMPLETED	A Study to Determine the Efficacy and Safety of Cabergoline for the Treatment of Patients With RLS
NCT00627003	PHASE3	COMPLETED	A Study to Evaluate the Efficacy and Safety of Cabergoline Compared With Placebo for the Treatment of RLS
NCT00889525	PHASE3	COMPLETED	Study of Cabergoline in Treatment of Corticotroph Pituitary Tumor
NCT01535859	PHASE3	COMPLETED	Study of Cabergoline for Prevention of Ovarian Hyperstimulation Syndrome (OHSS) in In Vito Fertilization Cycles and Derivation of OHSS Biomarkers
NCT01620138	PHASE2/PHASE3	COMPLETED	Response to Cabergoline and Pasireotide in Non-functioning Pituitary Adenomas and Resistant Prolactinomas
NCT02134249	PHASE2/PHASE3	COMPLETED	Diosmin Versus Cabergoline for Prevention of Ovarian Hyperstimulation Syndrome
NCT02271360	PHASE2/PHASE3	COMPLETED	Calcium Dobesilate Versus Cabergoline for Prevention of Ovarian Hyperstimulation Syndrome
NCT02306564	PHASE2/PHASE3	UNKNOWN	Effect of Cabergoline on Endometrial Vascularity During IntraCytoplasmic Sperm Injection
NCT03271918	PHASE3	COMPLETED	Cabergoline in Nonfunctioning Pituitary Adenomas
NCT03313661	PHASE3	UNKNOWN	Co-administration of Cabergoline and Gliclazide Improve Glycemic Parameters and Lipid Profile in T2DM Patients
NCT03473613	PHASE3	COMPLETED	Cabergoline Versus Calcium Infusion in Ovarian Hyperstimulation Syndrome Prevention
NCT03549741	PHASE2/PHASE3	UNKNOWN	Cabergoline As An Adjuvant To Clomiphene Citrate For Management Of Unexplained Infertility
NCT06909123	PHASE2	NOT_YET_RECRUITING	A Reduced Dose of Cabergoline for Lactation Inhibition After Second-Trimester Abortion or Pregnancy Loss
NCT07043322	PHASE2	RECRUITING	Clinical Study to Evaluate Efficacy of Cabergoline to Coasting in Reducing the Incidence of Ovarian Hyperstimulation Syndrome
NCT07072910	PHASE2	RECRUITING	Cabergoline for Episodic Migraine
NCT07492160	PHASE2	RECRUITING	Efficacy of Cabergoline in Inhibiting Lactation and Alleviating Breast Symptoms
NCT00033111	PHASE2	COMPLETED	A Study of Cabergoline for the Treatment of Cocaine Dependence - 1
NCT01009567	PHASE1/PHASE2	COMPLETED	Compare the Efficacy of Human Albumin With Cabergoline to Prevent Ovarian Hyper Stimulation in Assisted Reproductive Technology (ART) Program
NCT01395602	PHASE1/PHASE2	COMPLETED	Effect of Cabergoline on Weight and Glucose Tolerance
NCT02461875	PHASE2	UNKNOWN	Cabergoline Versus GnRH Antagonist Rescue and Cabergoline in the Prevention of Ovarian Hyperstimulation Syndrome
NCT02542410	PHASE2	COMPLETED	Dopamine Receptor Agonist Therapy for Pain Relief in Women Suffering From Endometriosis: A Pilot Study
NCT02644304	PHASE2	UNKNOWN	Clomiphene Citrate Plus Cabergoline in Treatment of Polycystic Ovary Syndrome
NCT02875587	PHASE2	COMPLETED	Cabergoline Versus Calcium Gluconate Infusion in the Prevention of Ovarian Hyperstimulation Syndrome
NCT03928288	PHASE2	COMPLETED	Cabergoline for the Treatment of Chronic Pain Due to Endometriosis
NCT04701333	PHASE2	COMPLETED	Cabergoline for Lactation Inhibition After Second-Trimester Abortion or Loss
NCT05981742	PHASE2	COMPLETED	Effects of Combined Metformin and Cabergoline in Comparison With Metformin Only Therapy on Ovarian and Hormonal Activities in Iraqi Patients With PCOS

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.

1,075 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
CARIPRAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
RISPERIDONE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
CLOZAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR2A, HTR2B, HTR2C
OLANZAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR2A, HTR2B, HTR2C
TEGASEROD	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C
IMIPRAMINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
NEFAZODONE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
PALIPERIDONE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1B, HTR1D, HTR2A, HTR2C
PRAMIPEXOLE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR2A, HTR2B
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
AMOXAPINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
APOMORPHINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
DOXEPIN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
ERGOTAMINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
HALOPERIDOL	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
KETANSERIN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
LOXAPINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
MIANSERIN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C
PROMAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
SERTINDOLE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR1B, HTR2A, HTR2B, HTR2C
RITANSERIN	ChEMBL	Phase 2	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR2A, HTR2C
DESLORATADINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
Fidaxomicin	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
Propoxyphene	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
Pyrazinamide	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
ASENAPINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
AZELASTINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
BENPERIDOL	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
CARVEDILOL	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
EBASTINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
ILOPERIDONE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
KETOTIFEN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD5, HTR1B, HTR2A, HTR2B, HTR2C
MAPROTILINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
PERGOLIDE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
PIMOZIDE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
PROMETHAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
QUETIAPINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
SILODOSIN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR1B, HTR1D, HTR2B
SUNITINIB	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
THIORIDAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
THIOTHIXENE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
TRAZODONE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
XYLOMETAZOLINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD2, DRD3, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
ZIPRASIDONE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
LISURIDE	ChEMBL	Phase 3	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
YOHIMBINE	ChEMBL	Phase 3	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B
PENFLURIDOL	ChEMBL	Phase 2	ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C
SPIPERONE	ChEMBL	Phase 2	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
ZOTEPINE	ChEMBL	Phase 2	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
Afatinib	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2B, HTR2C
chenodiol	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2B, HTR2C
CISAPRIDE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2B, HTR2C