Clozapine

Summary

Clozapine (CHEMBL42) is an approved small-molecule serotonergic antagonist (ATC N05AH02) targeting HTR5A, HTR6, and HTR7; indicated across 9 conditions including psychotic disorder and schizoaffective disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N05AH02
• Targets: 24 (HTR5A, HTR6, HTR7…)
• Indications: 9 conditions
• Clinical trials: 62
• Chemistry: 326.8 Da · C18H19ClN4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL42
Name	Clozapine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	135398737
ChEBI	CHEBI:3766
ATC	N05AH02
Molecular formula	C18H19ClN4
Molecular weight	326.8
InChIKey	QZUDBNBUXVUHMW-UHFFFAOYSA-N

SMILES: CN1CCN(CC1)C2=NC3=C(C=CC(=C3)Cl)NC4=CC=CC=C42

IUPAC name: 3-chloro-6-(4-methylpiperazin-1-yl)-11H-benzo[b][1,4]benzodiazepine

ChEBI definition: A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.

Pharmacological roles (ChEBI): serotonergic antagonist, dopaminergic antagonist, adrenergic antagonist, histamine antagonist, muscarinic antagonist, second generation antipsychotic, GABA antagonist, EC 3.4.21.26 (prolyl oligopeptidase) inhibitor.

Other ChEBI roles (chemical / environmental): xenobiotic, environmental contaminant.

Also known as: Clozapina, Clozapine, Clozapine (caraco), Clozapine (clozaril), Clozapine (fazaclo), Clozapine (ivax), Clozapine (mylan), Clozapine (teva), Clozapine (udl), Clozapine (versacloz), Clozapine resolution mixture, Clozaril

Parent form; salt/anhydrous children: CHEMBL538973

Patent coverage: 10,109 distinct patent families (37,581 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 37,406 (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
HTR5A	5-HT5A receptor	Antagonist	6.5	0%	P47898
HTR6	5-HT6 receptor	Inverse agonist	8.1	0.2%	P50406
HTR7	5-HT7 receptor	Inverse agonist	7.8	0.8%	P34969
CHRM1	M1 receptor	Positive	7.9	0.2%	P11229
HTR1A	5-HT1A receptor	Full agonist	6.9	0%	P08908
DRD1	D1 receptor	Antagonist	6.9	0%	P21728
DRD2	D2 receptor	Antagonist	6.9	0%	P14416
DRD3	D3 receptor	Antagonist	6.3	0%	P35462
DRD4	D4 receptor	Antagonist	7.5	0%	P21917
DRD5	D5 receptor	Antagonist	6.6	0%	P21918
ADRA1A	α1A-adrenoceptor	Antagonist	8.3		P35348
ADRA1B	α1B-adrenoceptor	Antagonist	8.2	0%	P35368
ADRA1D	α1D-adrenoceptor	Antagonist	7.7	0.2%	P25100
HRH1	H1 receptor	Antagonist	9.6	0%	P35367
HRH3	H3 receptor	Antagonist	5.8	0.5%	Q9Y5N1
HRH4	H4 receptor	Antagonist	6.7	0%	Q9H3N8
HTR1B	5-HT1B receptor	Full agonist	6.2	0.2%	P28222
HTR1D	5-HT1D receptor	Full agonist	6.4	0%	P28221
KCNJ6	Kir3.2	Antagonist	3.8	0.1%	P48051
HTR1E	5-ht1e receptor	Full agonist	6.4	0%	P28566
HTR1F	5-HT1F receptor	Full agonist	6.9	0.1%	P30939
HTR2A	5-HT2A receptor	Inverse agonist	9	0%	P28223
HTR2B	5-HT2B receptor	Antagonist	8.8	0.4%	P41595
HTR2C	5-HT2C receptor	Inverse agonist	8.7	0%	P28335

Broader ChEMBL bioactivity targets: 118 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Microtubule-associated protein tau, Nuclear receptor ROR-gamma, Survival motor neuron protein, Prelamin-A/C, RecQ-like DNA helicase BLM, Inositol monophosphatase 1, Peripheral myelin protein 22, Muscarinic acetylcholine receptor M4, 5-hydroxytryptamine receptor 2B.

Bioactivity

ChEMBL activities: 853 potent at pChembl ≥ 5 of 899 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HRH1	9.4	EC50	0.4	nM	CHEMBL_ACT_16879837
HRH1	9.24	Ki	0.57	nM	CHEMBL_ACT_7706180
P14842	9.16	Kd	0.69	nM	CHEMBL_ACT_223349
CHRM1	9.01	Ki	0.98	nM	CHEMBL_ACT_701862
HRH1	9	Ki	1	nM	CHEMBL_ACT_14583576
HRH1	9	Ki	1	nM	CHEMBL_ACT_16334547
HRH1	8.96	Ki	1.1	nM	CHEMBL_ACT_1518211
ADRA2C	8.94	Ki	1.14	nM	CHEMBL_ACT_7704046
HTR2A	8.92	Ki	1.2	nM	CHEMBL_ACT_7706290
P15823	8.85	Ki	1.4	nM	CHEMBL_ACT_1119261
HTR2A	8.85	Ki	1.4	nM	CHEMBL_ACT_22411680
P15823	8.85	Ki	1.4	nM	CHEMBL_ACT_467894
P15823	8.85	Ki	1.4	nM	CHEMBL_ACT_757082
P14842	8.8	Ki	1.58	nM	CHEMBL_ACT_1143925
CHRM1	8.74	Ki	1.8	nM	CHEMBL_ACT_2556814
HRH1	8.74	Ki	1.8	nM	CHEMBL_ACT_2577135
P08909	8.74	Ki	1.8	nM	CHEMBL_ACT_340352
CHRM1	8.74	Ki	1.8	nM	CHEMBL_ACT_7998791
HRH1	8.74	Ki	1.8	nM	CHEMBL_ACT_7998796
HRH1	8.68	Ki	2.1	nM	CHEMBL_ACT_446879
P08482	8.68	Ki	2.1	nM	CHEMBL_ACT_791902
HRH1	8.62	Ki	2.38	nM	CHEMBL_ACT_2601002
P14842	8.62	Kd	2.4	nM	CHEMBL_ACT_526385
CHRM1	8.61	Ki	2.47	nM	CHEMBL_ACT_7706208
HTR2A	8.57	Ki	2.69	nM	CHEMBL_ACT_1443930
HTR2C	8.54	Ki	2.88	nM	CHEMBL_ACT_12606988
HTR2C	8.54	Ki	2.88	nM	CHEMBL_ACT_1443931
ADRA2C	8.54	Ki	2.9	nM	CHEMBL_ACT_1518198
P31390	8.54	Ki	2.9	nM	CHEMBL_ACT_760628
HTR2A	8.52	Ki	3	nM	CHEMBL_ACT_20691136

Target pathways

Aggregated over 24 target gene(s): HTR5A, HTR6, HTR7, CHRM1, HTR1A, DRD1, DRD2, DRD3, DRD4, DRD5, ADRA1A, ADRA1B, ADRA1D, HRH1, HRH3, HRH4, HTR1B, HTR1D, KCNJ6, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C.

Top Reactome pathways

27 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	15	ADRA1A, ADRA1B, ADRA1D, CHRM1, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
Signaling by GPCR	15	ADRA1A, ADRA1B, ADRA1D, CHRM1, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
Class A/1 (Rhodopsin-like receptors)	15	ADRA1A, ADRA1B, ADRA1D, CHRM1, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
Amine ligand-binding receptors	15	ADRA1A, ADRA1B, ADRA1D, CHRM1, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
GPCR ligand binding	15	ADRA1A, ADRA1B, ADRA1D, CHRM1, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
GPCR downstream signalling	14	ADRA1A, ADRA1B, ADRA1D, CHRM1, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
Serotonin receptors	11	HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
G alpha (q) signalling events	8	ADRA1A, ADRA1B, ADRA1D, CHRM1, HRH1, HTR2A, HTR2B, HTR2C
G alpha (i) signalling events	8	DRD3, DRD4, HRH4, HTR1B, HTR1D, HTR1E, HTR1F, HTR5A
Dopamine receptors	5	DRD1, DRD2, DRD3, DRD4, DRD5
G alpha (s) signalling events	4	DRD1, DRD5, HTR6, HTR7
Histamine receptors	3	HRH1, HRH3, HRH4
Adrenoceptors	3	ADRA1A, ADRA1B, ADRA1D
G alpha (12/13) signalling events	3	ADRA1A, ADRA1B, ADRA1D
Neurotransmitter receptors and postsynaptic signal transmission	1	KCNJ6
Transmission across Chemical Synapses	1	KCNJ6
Neuronal System	1	KCNJ6
Activation of G protein gated Potassium channels	1	KCNJ6
G protein gated Potassium channels	1	KCNJ6
Inwardly rectifying K+ channels	1	KCNJ6
Potassium Channels	1	KCNJ6
Muscarinic acetylcholine receptors	1	CHRM1
RHOBTB3 ATPase cycle	1	HTR7
GABA receptor activation	1	KCNJ6
GABA B receptor activation	1	KCNJ6
Activation of GABAB receptors	1	KCNJ6
Inhibition of voltage gated Ca2+ channels via Gbeta/gamma subunits	1	KCNJ6

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	23
signal transduction	23
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	17
chemical synaptic transmission	17
adenylate cyclase-activating G protein-coupled receptor signaling pathway	8
G protein-coupled serotonin receptor signaling pathway	8
phospholipase C-activating G protein-coupled receptor signaling pathway	7
intracellular calcium ion homeostasis	7
adenylate cyclase-inhibiting serotonin receptor signaling pathway	6
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	6
response to xenobiotic stimulus	6
positive regulation of MAPK cascade	6
behavioral response to cocaine	5
phospholipase C-activating dopamine receptor signaling pathway	5
adenylate cyclase-activating adrenergic receptor signaling pathway	5

Indications & clinical

Indications

9 indications (3 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
schizoaffective disorder	4	MONDO:0005487	EFO:0005411
anxiety	3	MONDO:0011918	EFO:0005230
dementia	3	MONDO:0001627	HP:0000726
developmental disability	3	MONDO:0005287	EFO:0003852
depressive disorder	3	MONDO:0002050	MONDO:0002050
intellectual disability	3	MONDO:0001071	HP:0001249
bipolar disorder	3	MONDO:0004985	MONDO:0004985

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

Clinical trials

Total trials: 62.

Phase distribution

Phase	Trials
PHASE4	29
Not specified	17
PHASE3	9
PHASE2	3
PHASE1	2
PHASE1/PHASE2	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02639702	PHASE4	RECRUITING	Switching From Twice-Daily to Once-Daily Clozapine Dosing in Schizophrenia
NCT04580134	PHASE4	RECRUITING	CLOZAPINE Response in Biotype-1
NCT05208190	PHASE4	RECRUITING	Clozapine for the Prevention of Violence in Schizophrenia: a Randomized Clinical Trial
NCT05316883	PHASE4	RECRUITING	Biomarkers in Clozapine-responding Schizophrenia
NCT05958875	PHASE4	RECRUITING	The Effect of a Six Week Intensified Pharmacological Treatment for Schizophrenia Compared to Treatment as Usual in Subjects Who Had a First-time Treatment Failure on Their First-line Treatment.
NCT06969755	PHASE4	RECRUITING	Biomarkers to Enhance Early Schizophrenia Treatment
NCT00001656	PHASE4	COMPLETED	Comparison of Clozapine vs Olanzapine in Childhood-Onset Psychotic Disorders
NCT00014001	PHASE4	COMPLETED	CATIE- Schizophrenia Trial
NCT00031317	PHASE4	COMPLETED	Evaluation of Clonazepam and Paroxetine for Panic Disorder With Depression
NCT00048828	PHASE4	COMPLETED	Treating Drug-Resistant Childhood Schizophrenia
NCT00169039	PHASE4	TERMINATED	Clozapine Versus Chlorpromazine for Treatment-Unresponsive Schizophrenia
NCT00169065	PHASE4	COMPLETED	Effectiveness of Clozapine Versus Olanzapine for Treatment-resistant Schizophrenia
NCT00169091	PHASE4	TERMINATED	Clozapine Versus Haloperidol for Treating the First Episode of Schizophrenia
NCT00498550	PHASE4	COMPLETED	Treatment of Schizophrenia and Comorbid Cannabis Use Disorder: Comparing Clozapine to Treatment-as-Usual
NCT00501618	PHASE4	COMPLETED	Equivalence of Generic Clozapine to Orally Dissolving Clozapine in Schizophrenia or Schizoaffective Disorder
NCT00654576	PHASE4	COMPLETED	Effectiveness of Antipsychotic Combination With Psychosocial Intervention on Outcome of Patients With Schizophrenia
NCT00981526	PHASE4	COMPLETED	Telmisartan as an Adjunctive Treatment for Metabolic Problems in Patients With Schizophrenia
NCT01279213	PHASE4	COMPLETED	Clozapine/Paliperidone Versus Clozapine/Placebo in Resistant Schizophrenia
NCT01639872	PHASE4	COMPLETED	Clozapine for Cannabis Use in Schizophrenia
NCT01663077	PHASE4	COMPLETED	Clozapine Plasma Levels and the Relationship to the Genetic Polymorphism in Shizophrenic Patients
NCT02286206	PHASE4	WITHDRAWN	Study of the Effect of Dosing on Clozapine Levels
NCT02562287	PHASE4	UNKNOWN	Clozapine Versus Other Atypical Antipsychotics for Bipolar Disorder
NCT02625103	PHASE4	COMPLETED	The Significance of Deviation in Time From the 12-hour Standard Serum-clozapine Monitoring.
NCT02640300	PHASE4	COMPLETED	Switching Antipsychotics: Abrupt Discontinuation Versus Overlap
NCT02751307	PHASE4	COMPLETED	Adjunctive Low-dose Metformin in Patients With Schizophrenia and Metabolic Abnormalities
NCT03772951	PHASE4	COMPLETED	The Efficacy of Computerized Cognitive Remediation Therapy for Chronic Schizophrenia
NCT03807882	PHASE4	COMPLETED	Comparison of Maintenance ECT Versus Clozapine in Treatment-resistant Schizophrenia
NCT03857581	PHASE4	UNKNOWN	Clozapine Versus Olanzapine as Treatment for Comorbid Psychotic Disorder and Substance Use Disorder
NCT05741502	PHASE4	TERMINATED	An Exploratory Analysis of Immune and Inflammatory Response Associated With Clozapine
NCT05603104	PHASE3	RECRUITING	Intensified Pharmacological Treatment for Schizophrenia, Major Depressive Disorder and Bipolar Depression After a First-time Treatment Failure
NCT00000372	PHASE3	WITHDRAWN	Glycine and D-Cycloserine in Schizophrenia
NCT00036582	PHASE3	COMPLETED	Clozapine vs. Placebo in Treatment-Refractory Bipolar Disorder in Children and Adolescents
NCT00065273	PHASE3	COMPLETED	Atypical Neuroleptic Drugs in People With Mental Retardation/Developmental Delay
NCT00189995	PHASE3	WITHDRAWN	Clozapine IM and Aggression in Schizophrenic Patients
NCT00250575	PHASE3	COMPLETED	A Study to Evaluate the Safety and Efficacy of Clozapine in Patients With Treatment-resistant Schizophrenia
NCT00649844	PHASE3	COMPLETED	A Study Comparing the Efficacy and Tolerability of Ziprasidone vs. Clozapine for the Treatment of Schizophrenia in Patients Who Continue to Have Symptoms on or Cannot Tolerate Other Antipsychotic Drugs
NCT02374567	PHASE3	TERMINATED	Pharmacovigilance in Gerontopsychiatric Patients
NCT04528095	PHASE3	UNKNOWN	SMART Design to Compare Antipsychotic Treatments in Treatment-Resistant Schizophrenia
NCT00029458	PHASE2	COMPLETED	Clozapine for Treatment-Resistant Mania
NCT00042224	PHASE1/PHASE2	COMPLETED	Electroconvulsive Therapy in Clozapine Refractory Schizophrenia

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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.

1,160 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, CHRM1, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HRH3, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
RISPERIDONE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HRH3, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
BREXPIPRAZOLE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HRH3, HTR1A, HTR1B, HTR1D, HTR1E, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
OLANZAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HTR1A, HTR1B, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HRH3, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
IMIPRAMINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
CARIPRAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
HALOPERIDOL	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HTR1A, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
QUETIAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, HRH1, HTR1A, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
TEGASEROD	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, DRD1, DRD2, DRD3, DRD4, DRD5, HRH3, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, HRH1, HRH3, HRH4, HTR1A, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
AZELASTINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, CHRM1, DRD1, DRD2, DRD3, HRH1, HRH3, HTR1B, HTR1D, HTR1E, HTR2A, HTR2B, HTR2C, HTR6, HTR7
NEFAZODONE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, DRD1, DRD2, DRD3, DRD4, HRH1, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
AMOXAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HTR1A, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
CHLORPROMAZINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HTR1A, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
Cyproheptadine	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, HRH1, HTR1A, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
DOXEPIN	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HTR1A, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
LOXAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HRH4, HTR1A, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
Pramipexole	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1D, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HRH4, HTR1A, HTR1B, HTR1E, HTR2A, HTR2B, HTR5A, HTR7
ZIPRASIDONE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, HRH1, HTR1A, HTR1E, HTR2A, HTR2B, HTR2C, HTR6, HTR7
PROMAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HTR1A, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
RITANSERIN	ChEMBL	Phase 2	ADRA1A, ADRA1B, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HTR1A, HTR1B, HTR1E, HTR2A, HTR2C, HTR5A, HTR6, HTR7
ERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1D, DRD1, DRD2, DRD3, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR5A, HTR6
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HRH3, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
KETANSERIN	ChEMBL	Phase 4 (approved)	ADRA1A, DRD1, DRD2, DRD3, DRD4, HRH1, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
KETOTIFEN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD5, HRH1, HRH4, HTR1B, HTR2A, HTR2B, HTR2C, HTR6, HTR7
MIANSERIN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, HRH1, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
SERTINDOLE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, HRH1, HTR1A, HTR1B, HTR2A, HTR2B, HTR2C, HTR6
NIGULDIPINE	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA1D, DRD1, DRD2, DRD3, DRD5, HRH1, HRH3, HTR1A, HTR1B, HTR2C, HTR5A, HTR6, HTR7
PENFLURIDOL	ChEMBL	Phase 2	ADRA1D, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
SPIPERONE	ChEMBL	Phase 2	ADRA1A, ADRA1B, DRD1, DRD2, DRD3, DRD4, HRH1, HRH3, HTR1A, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
ASENAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, DRD1, DRD2, DRD3, DRD4, HRH1, HTR1A, HTR1E, HTR2A, HTR2B, HTR2C, HTR6
PIMOZIDE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, DRD1, DRD2, DRD3, DRD4, HRH1, HRH3, HRH4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
Pyrazinamide	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, DRD1, DRD2, DRD3, DRD4, HRH1, HRH3, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
EBASTINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, HRH1, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
SUNITINIB	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, DRD1, DRD2, DRD3, DRD4, HRH1, HRH3, HTR1A, HTR2A, HTR2B, HTR2C, HTR5A, HTR6
THIORIDAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, HRH1, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
YOHIMBINE	ChEMBL + PubChem	Phase 3 (approved)	ADRA1A, ADRA1B, ADRA1D, DRD1, DRD2, DRD3, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR6
LATREPIRDINE	ChEMBL	Phase 3	ADRA1A, ADRA1B, ADRA1D, DRD2, DRD3, HRH1, HTR1D, HTR1E, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
LYSERGIDE	ChEMBL	Phase 2	DRD2, DRD3, DRD4, DRD5, HRH1, HTR1A, HTR1D, HTR1E, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
METERGOLINE	ChEMBL	Phase 2	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, HRH1, HRH3, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
ZOTEPINE	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, HRH1, HRH3, HTR1A, HTR2A, HTR2B, HTR2C
DESLORATADINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, DRD1, DRD2, DRD3, DRD4, HRH1, HRH4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
CINACALCET	ChEMBL	Phase 4 (approved)	ADRA1B, CHRM1, DRD2, DRD3, HRH1, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
CLEMASTINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, HRH1, HRH3, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, HRH1, HRH3, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
MAPROTILINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD5, HRH1, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, HRH1, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
PROMETHAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1D, CHRM1, DRD1, DRD2, DRD3, DRD4, HRH1, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
SILODOSIN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, DRD1, DRD2, DRD3, DRD4, HRH1, HTR1A, HTR1B, HTR1D, HTR2B, HTR7
TERFENADINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, CHRM1, DRD1, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
VILAZODONE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, DRD2, DRD3, DRD4, HRH1, HTR1A, HTR1B, HTR1D, HTR2B, HTR6, HTR7
XYLOMETAZOLINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D, CHRM1, DRD2, DRD3, HRH3, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
SEROTONIN	ChEMBL + PubChem	Phase 3 (approved)	DRD1, DRD3, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR5A, HTR6, HTR7
PIZOTYLINE	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA1D, CHRM1, DRD1, DRD2, DRD3, HRH1, HTR1A, HTR2A, HTR2B, HTR2C, HTR7
SPIRAMIDE	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA1D, DRD2, DRD3, DRD4, HRH1, HTR1A, HTR1D, HTR2A, HTR2B, HTR6, HTR7
Fidaxomicin	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, DRD1, DRD2, DRD3, DRD4, HRH1, HRH3, HTR1A, HTR2A, HTR2B, HTR2C
METHYLERGONOVINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, DRD1, DRD2, DRD3, HRH1, HTR1A, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6
PALIPERIDONE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HTR1B, HTR1D, HTR2A, HTR2C, HTR7