Xanomeline

Summary

Xanomeline (CHEMBL21536) is an approved small-molecule muscarinic agonist targeting HTR6, HTR7, and CHRM1; indicated across 1 condition.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Targets: 15 (HTR6, HTR7, CHRM1…)
• Indications: 1 condition
• Clinical trials: 22
• Chemistry: 281.42 Da · C14H23N3OS

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL21536
Name	Xanomeline
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	60809
ChEBI	CHEBI:10056
Molecular formula	C14H23N3OS
Molecular weight	281.42
InChIKey	JOLJIIDDOBNFHW-UHFFFAOYSA-N

SMILES: CCCCCCOC1=NSN=C1C2=CCCN(C2)C

IUPAC name: 3-hexoxy-4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazole

Pharmacological roles (ChEBI): muscarinic agonist, serotonergic agonist.

Also known as: LY-246708, LY-246708 FREE BASE, LY246708, Xanomelina, Xanomeline, XANOMELINE, xanomeline

Parent form; salt/anhydrous children: CHEMBL73149, CHEMBL2336050

Patent coverage: 929 distinct patent families (3,299 SureChEMBL compound mentions), from 1 matched compound structure(s). 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	5.9	0.2%	P50406
HTR7	5-HT7 receptor	Full agonist	6.9	0.8%	P34969
CHRM1	M1 receptor	Partial agonist	7.9	0.2%	P11229
CHRM2	M2 receptor	Full agonist	7.4	0%	P08172
CHRM3	M3 receptor	Partial agonist	7.4	0%	P20309
CHRM4	M4 receptor	Partial agonist	7.7	1.6%	P08173
CHRM5	M5 receptor	Partial agonist	7.4	0%	P08912
HTR1A	5-HT1A receptor	Full agonist	7.2	0%	P08908
HTR1B	5-HT1B receptor	Full agonist	7.3	0.2%	P28222
HTR1D	5-HT1D receptor	Full agonist	8.2	0%	P28221
HTR1E	5-ht1e receptor	Full agonist	5.6	0%	P28566
HTR1F	5-HT1F receptor	Full agonist	6.5	0.1%	P30939
HTR2A	5-HT2A receptor	Antagonist	6.9	0%	P28223
HTR2B	5-HT2B receptor	Antagonist	7.7	0.4%	P41595
HTR2C	5-HT2C receptor	Antagonist	7.4	0%	P28335

Broader ChEMBL bioactivity targets: 28 (assay-derived). Sample: Muscarinic acetylcholine receptor M4, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Muscarinic acetylcholine receptor, Voltage-dependent L-type calcium channel subunit alpha-1C, Amine oxidase [flavin-containing] A, Sodium channel protein type 5 subunit alpha, Muscarinic acetylcholine receptor M5, D(1A) dopamine receptor, Muscarinic acetylcholine receptor M2.

Bioactivity

ChEMBL activities: 108 potent at pChembl ≥ 5 of 117 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CHRM1	8.8	EC50	1.6	nM	CHEMBL_ACT_3439266
P08482	8.7	IC50	2	nM	CHEMBL_ACT_1058442
P08482	8.7	IC50	2	nM	CHEMBL_ACT_131468
P08482	8.3	IC50	5	nM	CHEMBL_ACT_1058443
P08482	8.3	IC50	5	nM	CHEMBL_ACT_131469
CHRM4	8.22	EC50	6	nM	CHEMBL_ACT_18852468
CHRM4	8.21	EC50	6.2	nM	CHEMBL_ACT_3430216
CHRM1	8.17	AC50	6.7	nM	CHEMBL_ACT_25209756
P08482	8.15	IC50	7	nM	CHEMBL_ACT_558418
P08482	8.15	IC50	7	nM	CHEMBL_ACT_895990
P08482	8.15	IC50	7	nM	CHEMBL_ACT_984501
CHRM3	8.11	Ki	7.76	nM	CHEMBL_ACT_15082784
CHRM1	8.1	Ki	7.94	nM	CHEMBL_ACT_15082752
CHRM1	8.1	Ki	7.94	nM	CHEMBL_ACT_2140356
CHRM2	8.09	Ki	8.13	nM	CHEMBL_ACT_15082768
CHRM5	8.03	Ki	9.33	nM	CHEMBL_ACT_15087301
P08482	8.01	IC50	9.7	nM	CHEMBL_ACT_549852
P08482	8.01	IC50	9.7	nM	CHEMBL_ACT_895989
P08482	8.01	IC50	9.7	nM	CHEMBL_ACT_984500
CHRM1	8	EC50	10	nM	CHEMBL_ACT_405935
P08482	8	IC50	10	nM	CHEMBL_ACT_558419
CHRM4	7.95	Ki	11.22	nM	CHEMBL_ACT_15087285
CHRM2	7.93	Ki	11.75	nM	CHEMBL_ACT_2140380
CHRM2	7.9	IC50	12.59	nM	CHEMBL_ACT_405938
CHRM3	7.89	Ki	13	nM	CHEMBL_ACT_3430243
CHRM1	7.88	EC50	13.18	nM	CHEMBL_ACT_15087354
CHRM5	7.82	Ki	15.14	nM	CHEMBL_ACT_2140400
P10980	7.8	IC50	16	nM	CHEMBL_ACT_1094702
CHRM1	7.8	EC50	15.85	nM	CHEMBL_ACT_15087317
CHRM4	7.79	EC50	16.22	nM	CHEMBL_ACT_15087465

Target pathways

Aggregated over 15 target gene(s): HTR6, HTR7, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C.

Top Reactome pathways

20 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	15	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
Signaling by GPCR	15	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
Class A/1 (Rhodopsin-like receptors)	15	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
Amine ligand-binding receptors	15	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
GPCR ligand binding	15	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
GPCR downstream signalling	14	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
Serotonin receptors	10	HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
G alpha (q) signalling events	6	CHRM1, CHRM3, CHRM5, HTR2A, HTR2B, HTR2C
G alpha (i) signalling events	6	CHRM2, CHRM4, HTR1B, HTR1D, HTR1E, HTR1F
Muscarinic acetylcholine receptors	5	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
G alpha (s) signalling events	2	HTR6, HTR7
Metabolism	1	CHRM3
Integration of energy metabolism	1	CHRM3
Membrane Trafficking	1	CHRM2
Acetylcholine regulates insulin secretion	1	CHRM3
Regulation of insulin secretion	1	CHRM3
Vesicle-mediated transport	1	CHRM2
Cargo recognition for clathrin-mediated endocytosis	1	CHRM2
Clathrin-mediated endocytosis	1	CHRM2
RHOBTB3 ATPase cycle	1	HTR7

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	15
chemical synaptic transmission	15
signal transduction	15
G protein-coupled receptor signaling pathway	15
G protein-coupled serotonin receptor signaling pathway	6
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	5
G protein-coupled acetylcholine receptor signaling pathway	5
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	5
adenylate cyclase-inhibiting serotonin receptor signaling pathway	5
smooth muscle contraction	4
vasoconstriction	4
serotonin receptor signaling pathway	4
regulation of behavior	4
adenylate cyclase-activating G protein-coupled receptor signaling pathway	4
phospholipase C-activating serotonin receptor signaling pathway	4

Indications & clinical

Indications

1 indication (0 at ChEMBL trial phase 4).

The 1 indication record carries no mapped disease name (EFO/MeSH-only); none shown.

Clinical trials

Total trials: 22.

Phase distribution

Phase	Trials
PHASE3	12
PHASE4	4
PHASE1	3
PHASE2	1
PHASE1/PHASE2	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06923891	PHASE4	NOT_YET_RECRUITING	An Open-Label Study to Evaluate the Efficacy and Tolerability of Xanomeline/Trospium In First Episode/Early Phase Schizophrenia Patients
NCT06924255	PHASE4	NOT_YET_RECRUITING	An 8-week Open-label Study of an Accelerated and Slower Switching to Xanomeline/Trospium Following Atypical Antipsychotic Treatment in Participants With Schizophrenia
NCT07221877	PHASE4	RECRUITING	A Study to Evaluate the Effect of KarXT on Urological Safety
NCT07257120	PHASE4	RECRUITING	KarXT Concentrations in the Breast Milk and Plasma of Lactating Females
NCT05304767	PHASE3	RECRUITING	An Extension Study to Assess Long-Term Safety and Tolerability of Adjunctive KarXT in Subjects With Inadequately Controlled Symptoms of Schizophrenia
NCT07011732	PHASE3	RECRUITING	A Phase 3 Study to Evaluate the Safety and Efficacy of KarXT + KarX-EC for the Treatment of Agitation Associated With Alzheimer’s Disease (ADAGIO-1)
NCT07011745	PHASE3	RECRUITING	A Phase 3 Study to Evaluate the Safety and Efficacy of KarXT + KarX-EC for the Treatment of Agitation Associated With Alzheimer’s Disease (ADAGIO-2)
NCT07084831	PHASE3	NOT_YET_RECRUITING	A Study Evaluating the Efficacy of Xanomeline/Trospium (XT) on Cognitive Impairment After 24 and 52 Weeks of Treatment in Adult Participants With Schizophrenia
NCT07140913	PHASE3	RECRUITING	A Study to Evaluate the Efficacy and Safety of Adjunctive KarXT for the Treatment of Mania, With or Without Mixed Features, in Participants With Bipolar-I Disorder Taking Lithium, Valproate, or Lamotrigine
NCT04659161	PHASE3	COMPLETED	A Study to Assess Efficacy and Safety of KarXT in Acutely Psychotic Hospitalized Adult Patients With Schizophrenia (EMERGENT-2)
NCT04659174	PHASE3	COMPLETED	An Extension Study to Assess Long-term Safety, Tolerability, and Efficacy of KarXT in Adult Patients With Schizophrenia (EMERGENT-4)
NCT04738123	PHASE3	COMPLETED	A Study to Assess Efficacy and Safety of KarXT in Acutely Psychotic Hospitalized Adult Patients With Schizophrenia (EMERGENT-3)
NCT04820309	PHASE3	COMPLETED	An Open-label Study to Assess the Long-term Safety, Tolerability, and Efficacy of KarXT in Adult Patients With Schizophrenia (EMERGENT-5)
NCT05145413	PHASE3	COMPLETED	A Study to Assess Efficacy and Safety of Adjunctive KarXT in Subjects With Inadequately Controlled Symptoms of Schizophrenia
NCT05643170	PHASE3	TERMINATED	An Open-label Study to Assess the Long-term Safety, Tolerability, Effectiveness, and Durability of Effect of KarXT in Patients With DSM-5 Diagnosis of Schizophrenia
NCT05919823	PHASE3	COMPLETED	A Study to Assess the Efficacy and Safety of KarXT in Acutely Psychotic Hospitalized Chinese Adult Subjects With DSM-5 Schizophrenia
NCT07423546	PHASE1/PHASE2	NOT_YET_RECRUITING	A PET/MRI Study of Cobenfy on Dopamine Transmission in Schizophrenia
NCT03697252	PHASE2	COMPLETED	A Study to Assess Safety and Efficacy of KarXT in Adult Patients With Schizophrenia
NCT07063342	PHASE1	RECRUITING	A Study to Evaluate Novel KarX and KarT Prototypes Versus the KarXT and KarX-EC Reference Following Single Doses, and to Explore the Effect of Food After Multiple Doses of Selected Prototypes in Healthy Adult Participants
NCT07204418	PHASE1	RECRUITING	A Study to Evaluate the Effects of CYP2D6 Phenotypes on the Pharmacokinetics of Xanomeline Following KarXT Administration in Healthy Adult Participants
NCT06729970	PHASE1	COMPLETED	A Study to Evaluate the Effects of Lithium, Valproic Acid, and Lamotrigine on the Pharmacokinetics of KarXT and Effects of KarXT on the Pharmacokinetics of Lithium, Valproic Acid, and Lamotrigine in Healthy Participants
NCT07379827	Not specified	RECRUITING	Effectiveness and Adverse-effect Switch Evaluation of Xanomeline and Trospium Chloride (KarXT)

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.

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

Molecule	Source	Status	Shared targets
IMIPRAMINE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
RISPERIDONE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
CLOZAPINE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR1B, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
OLANZAPINE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR1B, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
CYPROHEPTADINE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
QUETIAPINE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
CARIPRAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM4, CHRM5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
MIANSERIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
AMOXAPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
DOXEPIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
HALOPERIDOL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
KETOTIFEN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1B, HTR2A, HTR2B, HTR2C, HTR6, HTR7
LOXAPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
OXYMETAZOLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM4, CHRM5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6
PROMAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
THIORIDAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
AZELASTINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, HTR1B, HTR1D, HTR1E, HTR2A, HTR2B, HTR2C, HTR6, HTR7
CLEMASTINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
DESLORATADINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
EBASTINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
MAPROTILINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
NORTRIPTYLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
PROMETHAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6
SEROTONIN	ChEMBL + PubChem	Phase 3 (approved)	HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
MEBUFOTENIN	ChEMBL	Phase 2	HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
BREXPIPRAZOLE	ChEMBL + PubChem	Phase 4 (approved)	HTR1A, HTR1B, HTR1D, HTR1E, HTR2A, HTR2B, HTR2C, HTR6, HTR7
ERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6
SUMATRIPTAN	ChEMBL + PubChem	Phase 4 (approved)	HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR7
ZIPRASIDONE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, HTR1A, HTR1E, HTR2A, HTR2B, HTR2C, HTR6, HTR7
AMIODARONE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2B, HTR2C, HTR6
BENZTROPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2B, HTR2C, HTR6
CINACALCET	ChEMBL	Phase 4 (approved)	CHRM1, CHRM3, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
DICYCLOMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2B, HTR2C, HTR6
DIPHENHYDRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2B, HTR2C, HTR6
MEPAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2B, HTR2C, HTR6
NEFAZODONE	ChEMBL	Phase 4 (approved)	CHRM2, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
ORPHENADRINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2B, HTR2C, HTR6
PAROXETINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR6
SERTRALINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C
TAMOXIFEN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2B, HTR2C, HTR6
XYLOMETAZOLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
ENCLOMIPHENE	ChEMBL	Phase 3	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2B, HTR2C, HTR6
FLUNARIZINE	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B, HTR2C
PSILOCIN	ChEMBL	Phase 2	HTR1A, HTR1B, HTR1D, HTR1E, HTR2A, HTR2B, HTR2C, HTR6, HTR7
Pyrazinamide	PubChem	Approved	CHRM1, CHRM2, CHRM3, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7
GENTIAN VIOLET	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B
PRAMIPEXOLE	ChEMBL + PubChem	Phase 4 (approved)	CHRM4, CHRM5, HTR1A, HTR1B, HTR1E, HTR2A, HTR2B, HTR7
RIZATRIPTAN	ChEMBL + PubChem	Phase 4 (approved)	HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C
SORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	HTR1A, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
CINNARIZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR2A, HTR2B
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, HTR2A, HTR2B, HTR2C, HTR6
CYCLIZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2B, HTR2C