Amitriptyline

Summary

Amitriptyline (CHEMBL629) is an approved small-molecule adrenergic uptake inhibitor (ATC N06AA09) targeting HTR6, HTR7, and CHRM1; indicated across 24 conditions including depressive disorder and insomnia.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N06AA09
• Targets: 16 (HTR6, HTR7, CHRM1…)
• Indications: 24 conditions
• Clinical trials: 79
• Chemistry: 277.4 Da · C20H23N

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL629
Name	Amitriptyline
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	2160
ChEBI	CHEBI:2666
ATC	N06AA09
Molecular formula	C20H23N
Molecular weight	277.4
InChIKey	KRMDCWKBEZIMAB-UHFFFAOYSA-N

SMILES: CN(C)CCC=C1C2=CC=CC=C2CCC3=CC=CC=C31

IUPAC name: N,N-dimethyl-3-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,11,13-hexaenylidene)propan-1-amine

ChEBI definition: An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(dimethylamino)propylidene group at position 5.

Pharmacological roles (ChEBI): adrenergic uptake inhibitor, antidepressant, tropomyosin-related kinase B receptor agonist.

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

Also known as: Amitriptilina, Amitriptyline, Damitriptyline, Flavyl, Laroxyl, Proheptadiene, Seroten, Triptanol, amitriptyline, SID11110782, SID11110783, SID90340850

Parent form; salt/anhydrous children: CHEMBL1200964

Patent coverage: 14,646 distinct patent families (52,595 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 52,367 (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	Antagonist	7.2	0.2%	P50406
HTR7	5-HT7 receptor	Antagonist	6.4	0.8%	P34969
CHRM1	M1 receptor	Antagonist	7.83	0.2%	P11229
CHRM2	M2 receptor	Antagonist	7.93	0%	P08172
CHRM3	M3 receptor	Antagonist	7.89	0%	P20309
CHRM4	M4 receptor	Antagonist	8.14	1.6%	P08173
CHRM5	M5 receptor	Antagonist	7.8	0%	P08912
ADRA1A	α1A-adrenoceptor	Antagonist	8.2		P35348
HRH1	H1 receptor	Antagonist	9.3	0%	P35367
LPAR1	LPA1 receptor	Antagonist	6.22	1.9%	Q92633
KCNJ6	Kir3.2	Antagonist	4	0.1%	P48051
KCNJ5	Kir3.4	Antagonist	3.6	0%	P48544
HTR2A	5-HT2A receptor	Antagonist	7.96	0%	P28223
HTR2C	5-HT2C receptor	Antagonist	8.1	0%	P28335
SLC6A2	NET	Inhibition	6.48	0.4%	P23975
SLC6A4	SERT	Inhibition	6.85	0.7%	P31645

Broader ChEMBL bioactivity targets: 65 (assay-derived). Sample: Muscarinic acetylcholine receptor M4, 5-hydroxytryptamine receptor 2B, D(1B) dopamine receptor, Alpha-2A adrenergic receptor, 5-hydroxytryptamine receptor 3A, Muscarinic acetylcholine receptor, Alpha-2C adrenergic receptor, Voltage-dependent L-type calcium channel subunit alpha-1C, Histamine H2 receptor, Alpha-2B adrenergic receptor.

Bioactivity

ChEMBL activities: 144 potent at pChembl ≥ 5 of 171 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P43140	10.7	IC50	0.02	nM	CHEMBL_ACT_782754
P31390	10.7	IC50	0.02	nM	CHEMBL_ACT_782755
HRH1	9.26	Ki	0.56	nM	CHEMBL_ACT_7637819
CHRM4	9.13	Ki	0.74	nM	CHEMBL_ACT_7639165
SLC6A4	9.05	Ki	0.88	nM	CHEMBL_ACT_7639253
HRH1	8.95	Ki	1.12	nM	CHEMBL_ACT_2600992
SLC6A4	8.78	IC50	1.66	nM	CHEMBL_ACT_7639252
CHRM1	8.56	Ki	2.72	nM	CHEMBL_ACT_7639159
HTR2C	8.5	Ki	3.17	nM	CHEMBL_ACT_7639245
ADRA2B	8.43	Ki	3.69	nM	CHEMBL_ACT_7637719
SLC6A4	8.37	Ki	4.3	nM	CHEMBL_ACT_13876506
HTR2A	8.36	Ki	4.37	nM	CHEMBL_ACT_7639241
HRH1	8.32	IC50	4.78	nM	CHEMBL_ACT_7637818
CHRM4	8.28	IC50	5.3	nM	CHEMBL_ACT_7639164
SLC6A4	8.27	Ki	5.4	nM	CHEMBL_ACT_19405243
CHRM3	8.27	Ki	5.44	nM	CHEMBL_ACT_7639163
P43140	8.25	Ki	5.6	nM	CHEMBL_ACT_7637711
CHRM5	8.24	Ki	5.76	nM	CHEMBL_ACT_7639167
HTR2C	8.22	IC50	6.05	nM	CHEMBL_ACT_7639244
SLC6A4	8.12	AC50	7.6	nM	CHEMBL_ACT_25151028
CHRM5	8.1	IC50	8.02	nM	CHEMBL_ACT_7639166
ADRA2B	8.09	IC50	8.08	nM	CHEMBL_ACT_7637718
ADRA2C	8.07	Ki	8.6	nM	CHEMBL_ACT_7637721
SLC6A4	8.04	Ki	9.2	nM	CHEMBL_ACT_24507966
SLC6A4	8.02	Ki	9.55	nM	CHEMBL_ACT_13876472
SLC6A4	8.02	AC50	9.5	nM	CHEMBL_ACT_25149825
CHRM1	7.96	IC50	11	nM	CHEMBL_ACT_7639158
HRH1	7.89	AC50	13	nM	CHEMBL_ACT_25211982
P43140	7.85	IC50	14	nM	CHEMBL_ACT_7637710
HTR2A	7.82	IC50	15	nM	CHEMBL_ACT_7639240

Target pathways

Aggregated over 16 target gene(s): HTR6, HTR7, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, ADRA1A, HRH1, LPAR1, KCNJ6, KCNJ5, HTR2A, HTR2C, SLC6A2, SLC6A4.

Top Reactome pathways

45 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	11	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2C, HTR6, HTR7, LPAR1
Signaling by GPCR	11	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2C, HTR6, HTR7, LPAR1
Class A/1 (Rhodopsin-like receptors)	11	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2C, HTR6, HTR7, LPAR1
GPCR downstream signalling	11	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2C, HTR6, HTR7, LPAR1
GPCR ligand binding	11	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2C, HTR6, HTR7, LPAR1
Amine ligand-binding receptors	10	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2C, HTR6, HTR7
G alpha (q) signalling events	8	ADRA1A, CHRM1, CHRM3, CHRM5, HRH1, HTR2A, HTR2C, LPAR1
Muscarinic acetylcholine receptors	5	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
Serotonin receptors	4	HTR2A, HTR2C, HTR6, HTR7
Transmission across Chemical Synapses	3	KCNJ5, KCNJ6, SLC6A4
Neuronal System	3	KCNJ5, KCNJ6, SLC6A4
G alpha (i) signalling events	3	CHRM2, CHRM4, LPAR1
Neurotransmitter receptors and postsynaptic signal transmission	2	KCNJ5, KCNJ6
Activation of G protein gated Potassium channels	2	KCNJ5, KCNJ6
G protein gated Potassium channels	2	KCNJ5, KCNJ6
Inwardly rectifying K+ channels	2	KCNJ5, KCNJ6
Potassium Channels	2	KCNJ5, KCNJ6
G alpha (s) signalling events	2	HTR6, HTR7
SLC-mediated transport of neurotransmitters	2	SLC6A2, SLC6A4
GABA receptor activation	2	KCNJ5, KCNJ6
GABA B receptor activation	2	KCNJ5, KCNJ6
Activation of GABAB receptors	2	KCNJ5, KCNJ6
Inhibition of voltage gated Ca2+ channels via Gbeta/gamma subunits	2	KCNJ5, KCNJ6
Neurotransmitter clearance	1	SLC6A4
Metabolism	1	CHRM3
Integration of energy metabolism	1	CHRM3
Disease	1	SLC6A2
Membrane Trafficking	1	CHRM2
Serotonin clearance from the synaptic cleft	1	SLC6A4
Transport of small molecules	1	SLC6A2

Dominant GO biological processes

GO term	Targets
signal transduction	12
G protein-coupled receptor signaling pathway	12
chemical synaptic transmission	11
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	10
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	5
phospholipase C-activating G protein-coupled receptor signaling pathway	5
G protein-coupled acetylcholine receptor signaling pathway	5
G protein-coupled serotonin receptor signaling pathway	4
response to xenobiotic stimulus	4
smooth muscle contraction	3
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathway	3
nervous system development	3
acetylcholine receptor signaling pathway	3
positive regulation of cytosolic calcium ion concentration	3
positive regulation of vasoconstriction	3

Indications & clinical

Indications

24 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
depressive disorder	4	MONDO:0002050	MONDO:0002009
insomnia	3	MONDO:0013600	EFO:0004698
anxiety	3	MONDO:0011918	EFO:0005230
fibromyalgia	3	MONDO:0005546	EFO:0005687
neuralgia	3	MONDO:0021667	EFO:0005762
dementia	3	MONDO:0001627	HP:0000726
interstitial cystitis	3	MONDO:0018301	EFO:0008507
migraine disorder	3	MONDO:0005277	MONDO:0005277
major depressive disorder	3	MONDO:0002009	EFO:0003761
diabetes mellitus	2	MONDO:0005015	EFO:0000400
reproductive system disorder	2	MONDO:0005039	EFO:0000512
peripheral nervous system disorder	2	MONDO:0003620	EFO:0004149
biliary dyskinesia	2	MONDO:0005667	EFO:0007169
frozen shoulder	2	MONDO:0006763	EFO:1000941
interstitial lung disease	2	MONDO:0015925	EFO:0004244
peripheral neuropathy	2	MONDO:0005244	EFO:0003100
inflammatory bowel disease	2	MONDO:0005265	EFO:0003767
rosacea	2	MONDO:0006604	EFO:1000760

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

Clinical trials

Total trials: 79.

Phase distribution

Phase	Trials
PHASE3	17
PHASE2	17
Not specified	17
PHASE4	16
PHASE2/PHASE3	7
PHASE1	3
PHASE1/PHASE2	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06499116	PHASE4	NOT_YET_RECRUITING	Comparison of the Effectiveness of First-line Preventive Treatment of Migraine in Primary Care
NCT00000428	PHASE4	COMPLETED	Combining N-of-1 Trials to Assess Fibromyalgia Treatments
NCT00006427	PHASE4	COMPLETED	Chronic Pain After Amputation
NCT00006428	PHASE4	COMPLETED	Chronic Pain in Spinal Cord Injury
NCT00189059	PHASE4	TERMINATED	Effects of Amitriptyline for the Treatment of Pain on Driving Performance and Cognition.
NCT00564525	PHASE4	COMPLETED	Study of Medication for Functional Abdominal Pain in Children
NCT00766350	PHASE4	COMPLETED	Comparative Efficacy and Tolerability of Quetiapine XR and Amitriptyline in the Treatment of Fibromyalgia
NCT00862095	PHASE4	TERMINATED	Medical Therapies for Chronic Post-Traumatic Headaches
NCT01869907	PHASE4	COMPLETED	Effect of Minocycline on Pain Caused by Nerve Damage
NCT02090998	PHASE4	TERMINATED	Sphenopalatine Ganglion Nerve Block vs. Elavil for Treatment of Transformed Migraines
NCT02190526	PHASE4	WITHDRAWN	Effects of Mesalamine and Amitriptyline on Irritable Bowel Syndrome
NCT02237937	PHASE4	UNKNOWN	Optimizing Antidepressant Treatment by Genotype-dependent Adjustment of Medication According to the ABCB1 Gene
NCT02256943	PHASE4	COMPLETED	Genetic Determinants of Amitriptyline Efficiency for Pain Treatment
NCT02256956	PHASE4	COMPLETED	Genetic Determinants of Amitriptyline Efficiency for Pain Treatment - Part II
NCT02339662	PHASE4	UNKNOWN	Prospective, Cross Over Gabapentin vs Amitriptyline Study on Patients Suffering From Masticatory Muscle Pain
NCT05867550	PHASE4	COMPLETED	To Compare the Efficacy of Drugs in Combination for Treating Irritable Bowel Syndrome Associated With Diarrhea
NCT00124306	PHASE3	COMPLETED	Efficacy of Amitriptyline for Painful Bladder Syndrome (PBS)
NCT00248651	PHASE2/PHASE3	COMPLETED	Functional Dyspepsia Treatment Trial
NCT00312260	PHASE3	COMPLETED	Comparing Gabapentin and Amitriptyline for the Treatment of Neuropathic Pain in Children and Adolescents
NCT00351910	PHASE3	COMPLETED	Efficacy of Seroquel SR in Combination With an Antidepressant in Treatment of Major Depressive Disorder
NCT00370656	PHASE2/PHASE3	COMPLETED	Effects of Pregabalin, Duloxetine & Amitriptyline on Pain & Sleep
NCT00389038	PHASE3	UNKNOWN	Pediatric Chronic Headache Trial
NCT00516503	PHASE3	COMPLETED	Baclofen-Amitriptyline Hydrochloride-Ketamine Gel in Treating Peripheral Neuropathy Caused by Chemotherapy in Patients With Cancer
NCT00740571	PHASE3	UNKNOWN	Amitriptyline or Pregabalin to Treat Neuropathic Pain in Incurable Cancer
NCT00798083	PHASE3	COMPLETED	Neuropathic Pain Caused by Radiation Therapy
NCT01049347	PHASE3	COMPLETED	Amitriptyline and Paroxetine Treatment of Major Depression
NCT01357031	PHASE3	COMPLETED	Study With Amitriptylin to Evaluate the Efficacy of Melatonin in Treatment of Migraine
NCT01581281	PHASE3	TERMINATED	The Childhood and Adolescent Migraine Prevention Study
NCT02041455	PHASE2/PHASE3	UNKNOWN	Immune-Pineal Axis Function in Fibromyalgia
NCT02099006	PHASE2/PHASE3	COMPLETED	Novel Topical Therapies for the Treatment of Genital Pain
NCT02139098	PHASE3	TERMINATED	Alternative Dosing Regimens in the Pharmacotherapy of Insomnia
NCT02374567	PHASE3	TERMINATED	Pharmacovigilance in Gerontopsychiatric Patients
NCT02434523	PHASE2/PHASE3	TERMINATED	Trial of the Treatment of Chronic Laryngitis With Amitryptiline
NCT02552225	PHASE2/PHASE3	TERMINATED	Treatment of Chronic Laryngitis With Amitriptyline
NCT02871661	PHASE3	UNKNOWN	Physical Therapy as Adjuvant Treatment of Vulvodynia: a Randomized Controled Trial
NCT03324035	PHASE3	UNKNOWN	Treatment of Neuropathic Pain in Leprosy
NCT03587025	PHASE3	COMPLETED	Preemptive Analgesia With Amitryptyline for Prevention of Pain in Women After Hysterectomy
NCT04725383	PHASE3	TERMINATED	Amitriptyline for Repetitive Behaviors in Autism Spectrum Disorders
NCT04777838	PHASE2/PHASE3	UNKNOWN	Myofascial Pain Patients’ Response to the Administration of Low Doses of Amitriptyline and Citalopram Compared With the Use of Bite Splint
NCT05658874	PHASE3	TERMINATED	A Multidisciplinary, Multimodal Bundled Care Approach to Chronic Pelvic Pain

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (3) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of DPWG Guideline for amitriptyline and CYP2D6	DPWG	CYP2D6	yes	yes
Annotation of CPIC Guideline for amitriptyline and CYP2C19, CYP2D6	CPIC	CYP2C19;CYP2D6	yes	yes
Annotation of DPWG Guideline for amitriptyline and CYP2C19	DPWG	CYP2C19

PharmGKB also curates 15 clinical and 76 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

1,103 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
IMIPRAMINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7, KCNJ5, SLC6A2, SLC6A4
CLOZAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
AMOXAPINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
DOXEPIN	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
HALOPERIDOL	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
LOXAPINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
MIANSERIN	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
PROMAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
RISPERIDONE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
THIORIDAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
DESLORATADINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
OLANZAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A4
AMIODARONE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
BENZTROPINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
CLEMASTINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
DIPHENHYDRAMINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
EBASTINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
MEPAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
NORTRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
ORPHENADRINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
PROMETHAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
Pyrazinamide	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
CARIPRAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A4
FLUOXETINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM5, HRH1, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
KETOTIFEN	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7
MAPROTILINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, SLC6A2
QUETIAPINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6, HTR7
SERTRALINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, SLC6A2, SLC6A4
FLUNARIZINE	ChEMBL	Phase 2	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, SLC6A2, SLC6A4
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
AZELASTINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
CINNARIZINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, SLC6A2, SLC6A4
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, HRH1, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
DEXCHLORPHENIRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, SLC6A2, SLC6A4
PAROXETINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR6, SLC6A2, SLC6A4
SUNITINIB	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, HRH1, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
TAMOXIFEN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
TERCONAZOLE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2C, SLC6A2, SLC6A4
ZIPRASIDONE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
ENCLOMIPHENE	ChEMBL	Phase 3	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, HTR2C, HTR6, SLC6A2, SLC6A4
METERGOLINE	ChEMBL	Phase 2	ADRA1A, CHRM1, CHRM2, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
NIGULDIPINE	ChEMBL	Phase 2	ADRA1A, CHRM2, CHRM3, CHRM5, HRH1, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
ZOTEPINE	ChEMBL	Phase 2	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, HRH1, HTR2A, HTR2C, SLC6A2, SLC6A4
ACLIDINIUM BROMIDE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
Afatinib	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, HRH1, HTR2A, HTR2C, SLC6A2, SLC6A4
chenodiol	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, HRH1, HTR2A, HTR2C, SLC6A2, SLC6A4
GENTIAN VIOLET	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR2A, SLC6A2, SLC6A4
Propoxyphene	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, HRH1, HTR2A, HTR2C, SLC6A2, SLC6A4
Tadalafil	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, HRH1, HTR2A, HTR2C, SLC6A2, SLC6A4
CINACALCET	ChEMBL	Phase 4 (approved)	CHRM1, CHRM3, HRH1, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
CYCLOBENZAPRINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, HRH1, HTR2A, HTR2C, SLC6A2, SLC6A4
DESIPRAMINE	ChEMBL	Phase 4 (approved)	ADRA1A, CHRM1, CHRM2, CHRM3, HRH1, HTR2A, HTR2C, SLC6A2, SLC6A4
DICYCLOMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, HTR2A, HTR2C, HTR6