Bromocriptine

Summary

Bromocriptine (CHEMBL493) is an approved small-molecule antiparkinson drug (ATC G02CB01) targeting HTR6, HTR7, and HTR1A; indicated across 9 conditions including parkinson disease and peripartum cardiomyopathy.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: G02CB01 (+1 more)
• Targets: 16 (HTR6, HTR7, HTR1A…)
• Indications: 9 conditions
• Clinical trials: 28
• Chemistry: 654.6 Da · C32H40BrN5O5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL493
Name	Bromocriptine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	31101
ChEBI	CHEBI:3181
ATC	G02CB01, N04BC01
Molecular formula	C32H40BrN5O5
Molecular weight	654.6
InChIKey	OZVBMTJYIDMWIL-AYFBDAFISA-N

SMILES: CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]3(N1C(=O)[C@](O3)(C(C)C)NC(=O)[C@H]4CN([C@@H]5CC6=C(NC7=CC=CC(=C67)C5=C4)Br)C)O

IUPAC name: (6aR,9R)-5-bromo-N-[(1S,2S,4R,7S)-2-hydroxy-7-(2-methylpropyl)-5,8-dioxo-4-propan-2-yl-3-oxa-6,9-diazatricyclo[7.3.0.02,6]dodecan-4-yl]-7-methyl-6,6a,8,9-tetrahydro-4H-indolo[4,3-fg]quinoline-9-carboxamide

Pharmacological roles (ChEBI): antiparkinson drug, hormone antagonist, dopamine agonist, antidyskinesia agent.

Also known as: Bromergocryptine, Bromocriptina, Bromocriptine, CB-154, Parlodel, bromocriptine, Bromocriptin, SID26751716, SID26755307, SID90340796, BROMOCRIPTINE, SID144204458

Parent form; salt/anhydrous children: CHEMBL1200503, CHEMBL1255752

Patent coverage: 10,648 distinct patent families (43,885 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 43,832 (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	Full agonist	7.5	0.2%	P50406
HTR7	5-HT7 receptor	Full agonist	8	0.8%	P34969
HTR1A	5-HT1A receptor	Partial agonist	7.9	0%	P08908
DRD1	D1 receptor	Partial agonist	6.2	0%	P21728
DRD2	D2 receptor	Full agonist	8.3	0%	P14416
DRD3	D3 receptor	Partial agonist	8.2	0%	P35462
DRD4	D4 receptor	Antagonist	6.4	0%	P21917
DRD5	D5 receptor	Full agonist	6.3	0%	P21918
ADRA2A	α2A-adrenoceptor	Antagonist	8.3	0.1%	P08913
ADRA2B	α2B-adrenoceptor	Antagonist	7.5	0.2%	P18089
ADRA2C	α2C-adrenoceptor	Antagonist	7.6	0%	P18825
HTR1B	5-HT1B receptor	Partial agonist	6.5	0.2%	P28222
HTR1D	5-HT1D receptor	Partial agonist	8	0%	P28221
HTR2A	5-HT2A receptor	Partial agonist	7	0%	P28223
HTR2B	5-HT2B receptor	Antagonist	7.3	0.4%	P41595
HTR2C	5-HT2C receptor	Partial agonist	6.1	0%	P28335

Broader ChEMBL bioactivity targets: 51 (assay-derived). Sample: Microtubule-associated protein tau, Nuclear receptor ROR-gamma, Survival motor neuron protein, Prelamin-A/C, 4’-phosphopantetheinyl transferase ffp, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Histamine H2 receptor, Alpha-2B adrenergic receptor.

Bioactivity

ChEMBL activities: 103 potent at pChembl ≥ 5 of 122 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DRD3	9.7	Ki	0.2	nM	CHEMBL_ACT_7613898
DRD2	9.3	EC50	0.5	nM	CHEMBL_ACT_16879807
DRD2	9.28	Ki	0.53	nM	CHEMBL_ACT_7613896
DRD3	9.22	IC50	0.6	nM	CHEMBL_ACT_7613897
DRD2	9.21	Ki	0.62	nM	CHEMBL_ACT_25553903
DRD2	8.8	IC50	1.58	nM	CHEMBL_ACT_7613895
HTR2A	8.75	EC50	1.78	nM	CHEMBL_ACT_16879799
P15823	8.71	Ki	1.96	nM	CHEMBL_ACT_7612477
P43140	8.55	Ki	2.82	nM	CHEMBL_ACT_7612475
HTR1A	8.52	AC50	3	nM	CHEMBL_ACT_25165542
P19327	8.49	Ki	3.22	nM	CHEMBL_ACT_7615376
P15823	8.45	IC50	3.55	nM	CHEMBL_ACT_7612476
P61169	8.4	Kd	4	nM	CHEMBL_ACT_189683
HTR2B	8.28	Ki	5.29	nM	CHEMBL_ACT_7615382
ADRA2A	8.26	Ki	5.53	nM	CHEMBL_ACT_7612481
P19327	8.25	IC50	5.63	nM	CHEMBL_ACT_7615375
P43140	8.16	IC50	6.96	nM	CHEMBL_ACT_7612474
P61169	8.1	Kd	8	nM	CHEMBL_ACT_189680
P61169	8.1	Kd	8	nM	CHEMBL_ACT_189681
HTR2B	8.08	IC50	8.32	nM	CHEMBL_ACT_7615381
DRD2	8	Ki	10	nM	CHEMBL_ACT_128951
DRD2	8	Ki	10	nM	CHEMBL_ACT_25917654
HTR2A	8	Ki	10	nM	CHEMBL_ACT_7615380
HTR6	8	Ki	10	nM	CHEMBL_ACT_7615390
DRD2	7.83	Ki	14.79	nM	CHEMBL_ACT_14723107
DRD2	7.82	Ki	15	nM	CHEMBL_ACT_14723045
ADRA1D	7.82	Ki	15	nM	CHEMBL_ACT_7612479
ADRA2A	7.82	IC50	15	nM	CHEMBL_ACT_7612480
ADRA2B	7.8	Ki	16	nM	CHEMBL_ACT_7612483
P61169	7.77	Kd	17	nM	CHEMBL_ACT_189682

Target pathways

Aggregated over 16 target gene(s): HTR6, HTR7, HTR1A, DRD1, DRD2, DRD3, DRD4, DRD5, ADRA2A, ADRA2B, ADRA2C, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C.

Top Reactome pathways

24 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	11	ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
Signaling by GPCR	11	ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
Class A/1 (Rhodopsin-like receptors)	11	ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
Amine ligand-binding receptors	11	ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
GPCR ligand binding	11	ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
GPCR downstream signalling	10	ADRA2A, ADRA2B, ADRA2C, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
Serotonin receptors	8	HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
G alpha (i) signalling events	7	ADRA2A, ADRA2B, ADRA2C, DRD3, DRD4, HTR1B, HTR1D
Dopamine receptors	5	DRD1, DRD2, DRD3, DRD4, DRD5
G alpha (s) signalling events	4	DRD1, DRD5, HTR6, HTR7
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
Regulation of insulin secretion	2	ADRA2A, ADRA2C
Surfactant metabolism	2	ADRA2A, ADRA2C
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
G protein-coupled serotonin receptor signaling pathway	7
intracellular calcium ion homeostasis	7
positive regulation of MAPK cascade	6
adenylate cyclase-activating G protein-coupled receptor signaling pathway	5
response to xenobiotic stimulus	5
behavioral response to cocaine	5
phospholipase C-activating dopamine receptor signaling pathway	5
synaptic transmission, dopaminergic	5
response to cocaine	5
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	4
vasoconstriction	4

Indications & clinical

Indications

9 indications (1 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
Parkinson disease	4	MONDO:0005180	MONDO:0005180
peripartum cardiomyopathy	3	MONDO:0018920	EFO:0002628
obesity disorder	2	MONDO:0011122	EFO:0001073
type 1 diabetes mellitus	2	MONDO:0005147	MONDO:0005147
ovarian hyperstimulation syndrome	2	MONDO:0011972	MONDO:0011972
intellectual disability	2	MONDO:0001071	HP:0001249
adenomyosis	1	MONDO:0010888	EFO:1001757
Alzheimer disease	1	MONDO:0004975	MONDO:0004975
anorexia nervosa	0	MONDO:0005351	MONDO:0005351

Clinical trials

Total trials: 28.

Phase distribution

Phase	Trials
PHASE4	6
PHASE2	6
Not specified	6
PHASE3	5
PHASE1/PHASE2	2
PHASE2/PHASE3	1
PHASE1	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03575000	PHASE4	NOT_YET_RECRUITING	Bromocriptine for Patients With Schizophrenia and Prediabetes
NCT05180773	PHASE4	RECRUITING	Impact of Bromocriptine on Clinical Outcomes for Peripartum Cardiomyopathy
NCT00451672	PHASE4	UNKNOWN	The Therapeutic Effect of Bromocriptin in Patients With Primary Aldosteronism
NCT01673724	PHASE4	COMPLETED	Pramipexole and Bromocriptine on Nonmotor Symptoms of Early Parkinson’s Disease
NCT02233023	PHASE4	COMPLETED	Ophthalmologic Safety of Long Term Treatment With Pramipexole Compared to Bromocriptine or Other Dopamine Agonists in Patients With Parkinson’s Disease
NCT02929485	PHASE4	WITHDRAWN	Dopaminergic Modulation of Frontostriatal Function With a Dopamine Agonist and COMT Inhibitor
NCT00240409	PHASE3	COMPLETED	Randomized Single-blind Placebo Controlled Comparative Trial of Pramipexole and Bromocriptine in Parkinson’s Disease
NCT00315081	PHASE3	UNKNOWN	Risperidone-Induced Hyperprolactinemia Treated With Bromocriptine
NCT02133755	PHASE3	UNKNOWN	Effect of Bromocriptine on Insulin Resistance in Polycystic Ovarian Syndrome - A Pilot Study
NCT02172573	PHASE3	COMPLETED	Safety and Efficacy of Pramipexole and Bromocriptine Combined With L-dopa in Parkinson’s Disease
NCT02590601	PHASE3	WITHDRAWN	Bromocriptine in the Treatment of Peripartum Cardiomyopathy
NCT04181385	PHASE2/PHASE3	UNKNOWN	Acute Olanzapine and Lipid Response
NCT00004300	PHASE2	SUSPENDED	Phase II Study of Stereotypes and Mental Retardation: Neurobiological Basis
NCT00998556	PHASE2	COMPLETED	Effect of Bromocriptine on Left Ventricular Function in Women With Peripartum Cardiomyopathy
NCT02544321	PHASE2	COMPLETED	Bromocriptine Quick Release (BCQR) as Adjunct Therapy in Type 1 Diabetes
NCT02846493	PHASE2	UNKNOWN	Efficacy and Safety of Dexamethasone Prevention for Patients of Ovarian Hyperstimulation Syndrome
NCT03384524	PHASE1/PHASE2	WITHDRAWN	Evaluation of Bromocriptine, Metoprolol and Tamsulosin in Eyes With Non-Central DME
NCT03496545	PHASE1/PHASE2	COMPLETED	Efficacy of Bromocriptine For Fever Reduction in Acute Neurologic Injury
NCT03525002	PHASE2	COMPLETED	Dopamine Action on Metabolism in Relation to Genotype
NCT04351126	PHASE2	COMPLETED	Management of Ovarian Hyperstimulation Syndrome as a State of Defective Mineralocorticoid Response
NCT01821001	PHASE1	COMPLETED	Vaginal Bromocriptine for Treatment of Adenomyosis
NCT04128683	EARLY_PHASE1	COMPLETED	Dopamine Receptor Contributions to Prediction Error and Reversal Learning in Anorexia Nervosa
NCT06556186	Not specified	NOT_YET_RECRUITING	Surgical and Pharmacological Efficacy of Knosp Grade 0-2 Prolactinoma
NCT01893450	Not specified	TERMINATED	Bromocriptine and Pentoxifylline in Ophthalmopathy Autoimmune Treatment
NCT02265484	Not specified	COMPLETED	To Study the Efficacy of Bromocriptine in Patients With Hepatic/Cirrhosis Related Parkinsonism
NCT02428933	Not specified	COMPLETED	Dopaminergic Effects on Brown Adipose Tissue
NCT02428946	Not specified	COMPLETED	Bromocriptine and Insulin Sensitivity
NCT04038749	Not specified	UNKNOWN	Satisfaction of Patients With the Chosen Method of Inhibition of Lactation

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.

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

Molecule	Source	Status	Shared targets
BREXPIPRAZOLE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
CARIPRAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
RISPERIDONE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
CLOZAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR2A, HTR2B, HTR2C, HTR6, HTR7
OLANZAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR2A, HTR2B, HTR2C, HTR6, HTR7
TEGASEROD	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
IMIPRAMINE	ChEMBL	Phase 4 (approved)	ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
NEFAZODONE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
AMOXAPINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
DOXEPIN	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
HALOPERIDOL	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
KETANSERIN	ChEMBL	Phase 4 (approved)	ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
LOXAPINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
MIANSERIN	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
PROMAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
PENFLURIDOL	ChEMBL	Phase 2	ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
RITANSERIN	ChEMBL	Phase 2	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR2A, HTR2C, HTR6, HTR7
PALIPERIDONE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1B, HTR1D, HTR2A, HTR2C, HTR7
PRAMIPEXOLE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR2A, HTR2B, HTR7
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
AZELASTINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
CARVEDILOL	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
ERGOTAMINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6
KETOTIFEN	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD5, HTR1B, HTR2A, HTR2B, HTR2C, HTR6, HTR7
QUETIAPINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
SERTINDOLE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR1B, HTR2A, HTR2B, HTR2C, HTR6
THIORIDAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
THIOTHIXENE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
ZIPRASIDONE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
SPIPERONE	ChEMBL	Phase 2	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
Pyrazinamide	PubChem	Approved	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
DESLORATADINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
APOMORPHINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C
ASENAPINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
EBASTINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
ILOPERIDONE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
MAPROTILINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
METHYSERGIDE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
PERGOLIDE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
PIMOZIDE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
PROMETHAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
SILODOSIN	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR1B, HTR1D, HTR2B, HTR7
SUNITINIB	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
VILAZODONE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD2, DRD3, DRD4, HTR1A, HTR1B, HTR1D, HTR2B, HTR6, HTR7
LISURIDE	ChEMBL	Phase 3	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
YOHIMBINE	ChEMBL	Phase 3	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR6
METERGOLINE	ChEMBL	Phase 2	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
NIGULDIPINE	ChEMBL	Phase 2	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD5, HTR1A, HTR1B, HTR2C, HTR6, HTR7
SPIRAMIDE	ChEMBL	Phase 2	ADRA2A, ADRA2B, ADRA2C, DRD2, DRD3, DRD4, HTR1A, HTR1D, HTR2A, HTR2B, HTR6, HTR7
CINACALCET	ChEMBL + PubChem	Phase 4 (approved)	ADRA2B, ADRA2C, DRD2, DRD3, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
Fidaxomicin	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C
Propoxyphene	ChEMBL + PubChem	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