Dothiepin

drug

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Also known as DosulepinDosulepinaDosulepineDothirpinSID11112454

Summary

Dothiepin (CHEMBL1492500) is an approved small molecule (ATC N06AA16) targeting CHRM1, CHRM2, and CHRM3; indicated across 1 condition including depressive disorder.

At a glance

Status: Approved (max clinical phase 4)
Modality: Small molecule
ATC class: N06AA16
Targets: 8 (CHRM1, CHRM2, CHRM3…)
Indications: 1 condition
Clinical trials: 2
Chemistry: 295.4 Da · C19H21NS

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1492500
Name	Dothiepin
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	5284550
ChEBI	CHEBI:36803
ATC	N06AA16
Molecular formula	C19H21NS
Molecular weight	295.4
InChIKey	PHTUQLWOUWZIMZ-GZTJUZNOSA-N

SMILES: CN(C)CC/C=C/1\C2=CC=CC=C2CSC3=CC=CC=C31

IUPAC name: (3E)-3-(6H-benzo[c][1]benzothiepin-11-ylidene)-N,N-dimethylpropan-1-amine

Also known as: Dosulepin, Dosulepina, Dosulepine, Dothiepin, Dothirpin, SID11112454, DOSULEPINE, DOTHIEPIN, dosulepin, DOSULEPIN

Parent form; salt/anhydrous children: CHEMBL1711280

Patent coverage: 13 distinct patent families (24 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 19 (79%) 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

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
CHRM1	M₁ receptor	Antagonist	7.74	0.2%	P11229
CHRM2	M₂ receptor	Antagonist	6.96	0%	P08172
CHRM3	M₃ receptor	Antagonist	7.42	0%	P20309
CHRM4	M₄ receptor	Antagonist	7.21	1.6%	P08173
CHRM5	M₅ receptor	Antagonist	7.04	0%	P08912
HRH1	H₁ receptor	Antagonist	8.4	0%	P35367
SLC6A2	NET	Inhibition	7.34	0.4%	P23975
SLC6A4	SERT	Inhibition	8.07	0.7%	P31645

Broader ChEMBL bioactivity targets: 23 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, Muscarinic acetylcholine receptor M2, Muscarinic acetylcholine receptor M1, D(2) dopamine receptor, Sodium-dependent noradrenaline transporter, 5-hydroxytryptamine receptor 2A, 5-hydroxytryptamine receptor 2C, Sodium-dependent serotonin transporter, Alpha-1A adrenergic receptor, Histamine H1 receptor, D(3) dopamine receptor, Kappa-type opioid receptor, Sodium-dependent dopamine transporter, Voltage-gated inwardly rectifying potassium channel KCNH2, Muscarinic acetylcholine receptor M3, Histamine H3 receptor, Cytochrome P450 2D6.

Bioactivity

ChEMBL activities: 19 potent at pChembl ≥ 5 of 25 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SLC6A4	8	AC50	9.9	nM	CHEMBL_ACT_25149828
HRH1	7.72	AC50	19	nM	CHEMBL_ACT_25211985
CHRM3	6.38	AC50	420	nM	CHEMBL_ACT_25136190
CHRM1	6.17	AC50	670	nM	CHEMBL_ACT_25134924
SLC6A2	6.1	AC50	800	nM	CHEMBL_ACT_25144492
ADRA1A	6.06	AC50	870	nM	CHEMBL_ACT_25217708
ALDH1A1	5.9	Potency	1259	nM	CHEMBL_ACT_4186931
ADRA2B	5.89	AC50	1300	nM	CHEMBL_ACT_25143187
CHRM2	5.85	AC50	1400	nM	CHEMBL_ACT_25213242
KCNH2	5.82	AC50	1500	nM	CHEMBL_ACT_25117081
HTR2C	5.8	AC50	1600	nM	CHEMBL_ACT_25131295
OPRK1	5.57	AC50	2700	nM	CHEMBL_ACT_25128957
DRD3	5.52	AC50	3000	nM	CHEMBL_ACT_25193013
ADRA1A	5.5	AC50	3200	nM	CHEMBL_ACT_25137624
HTR2B	5.44	AC50	3600	nM	CHEMBL_ACT_25227033
HTR2A	5.32	AC50	4800	nM	CHEMBL_ACT_25224692
CYP2D6	5.1	Potency	7943	nM	CHEMBL_ACT_4949782
CYP2D6	5.1	AC50	7943	nM	CHEMBL_ACT_5988705
ADRA2C	5.01	AC50	9800	nM	CHEMBL_ACT_25147350

Target pathways

Aggregated over 8 target gene(s): CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4.

Top Reactome pathways

30 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	5	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
Signaling by GPCR	5	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
Class A/1 (Rhodopsin-like receptors)	5	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
Amine ligand-binding receptors	5	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
GPCR downstream signalling	5	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
Muscarinic acetylcholine receptors	5	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
GPCR ligand binding	5	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
G alpha (q) signalling events	4	CHRM1, CHRM3, CHRM5, HRH1
G alpha (i) signalling events	2	CHRM2, CHRM4
SLC-mediated transport of neurotransmitters	2	SLC6A2, SLC6A4
Neurotransmitter clearance	1	SLC6A4
Transmission across Chemical Synapses	1	SLC6A4
Neuronal System	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
Histamine receptors	1	HRH1
Acetylcholine regulates insulin secretion	1	CHRM3
Regulation of insulin secretion	1	CHRM3
R-HSA-425366	1	SLC6A2
SLC-mediated transmembrane transport	1	SLC6A2
SLC transporter disorders	1	SLC6A2
Defective SLC6A2 causes orthostatic intolerance (OI)	1	SLC6A2
Disorders of transmembrane transporters	1	SLC6A2
Vesicle-mediated transport	1	CHRM2
Cargo recognition for clathrin-mediated endocytosis	1	CHRM2
Clathrin-mediated endocytosis	1	CHRM2

Dominant GO biological processes

GO term	Targets
chemical synaptic transmission	7
signal transduction	6
G protein-coupled receptor signaling pathway	6
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	6
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	5
G protein-coupled acetylcholine receptor signaling pathway	5
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathway	3
nervous system development	3
acetylcholine receptor signaling pathway	3
phospholipase C-activating G protein-coupled receptor signaling pathway	2
regulation of locomotion	2
saliva secretion	2
regulation of smooth muscle contraction	2
memory	2
neurotransmitter transport	2

Indications & clinical

Indications

1 approved indication. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

Indication	Phase	MONDO	EFO
depressive disorder	4	MONDO:0002050	MONDO:0002009

Clinical trials

Total trials: 2.

Phase distribution

Phase	Trials
PHASE4	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06803485	PHASE4	RECRUITING	Effect of Venlafaxine Versus Dosulepin in Pain Predominant Somatic Symptom Disorder
NCT03126188	Not specified	COMPLETED	Study of the Effect of Antidepressant Drugs on Neurotrophic Factors in Patients With Depression

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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.

895 molecules share ≥1 primary target. Top 100 by shared-target count:

Molecule	Source	Status	Shared targets
ACLIDINIUM BROMIDE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
AMITRIPTYLINE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
CLOZAPINE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
DESLORATADINE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
AMIODARONE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
AMOXAPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
BENZTROPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
CINNARIZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
CLEMASTINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
DEXCHLORPHENIRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
DIPHENHYDRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
DOXEPIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
EBASTINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
HALOPERIDOL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
IMIPRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
LOXAPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
MEPAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
MIANSERIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
NORTRIPTYLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
ORPHENADRINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
PROMAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
PROMETHAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
RISPERIDONE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
SERTRALINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
SULOCTIDIL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
THIORIDAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
DIMETHINDENE	ChEMBL	Phase 3	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
FLUNARIZINE	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
GENTIAN VIOLET	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, SLC6A2, SLC6A4
OLANZAPINE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A4
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, HRH1, SLC6A2, SLC6A4
DIMENHYDRINATE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2
FLUOXETINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM5, HRH1, SLC6A2, SLC6A4
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, HRH1, SLC6A2, SLC6A4
MAPROTILINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2
PAROXETINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, SLC6A2, SLC6A4
PERHEXILINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, SLC6A2, SLC6A4
TAMOXIFEN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, SLC6A2, SLC6A4
TERCONAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, SLC6A2, SLC6A4
TOLTERODINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A4
XANOMELINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, SLC6A2, SLC6A4
ENCLOMIPHENE	ChEMBL	Phase 3	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, SLC6A2, SLC6A4
BENZETHONIUM CHLORIDE	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, SLC6A2, SLC6A4
ZOTEPINE	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, CHRM4, HRH1, SLC6A2, SLC6A4
Afatinib	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
chenodiol	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
Dihydroergotamine	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
LINAGLIPTIN	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
Propoxyphene	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
Tadalafil	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
CARIPRAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM4, CHRM5, HRH1, SLC6A4
CHLORPHENIRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM5, HRH1, SLC6A2, SLC6A4
CLIDINIUM	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, SLC6A4
CYCLIZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1
CYCLOBENZAPRINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
DARIFENACIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, SLC6A4
DESIPRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
DICYCLOMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1
ECONAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, SLC6A2, SLC6A4
GLYCOPYRRONIUM BROMIDE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1
KETOTIFEN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1
LASOFOXIFENE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
METHAPYRILENE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM5, HRH1, SLC6A2, SLC6A4
MICONAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, SLC6A2, SLC6A4
NEFOPAM	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
OXYBUTYNIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, SLC6A2
PIPERACETAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
QUETIAPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1
QUINACRINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, SLC6A2
SULCONAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM3, CHRM4, CHRM5, SLC6A2, SLC6A4
SUNITINIB	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
THIOTEPA	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
TIOTROPIUM BROMIDE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1
MELITRACEN	ChEMBL	Phase 3	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
OTILONIUM BROMIDE	ChEMBL	Phase 3	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
BENZETHONIUM	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
CLOTHIAPINE	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
DOMIPHEN	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
MEQUITAZINE	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
NIGULDIPINE	ChEMBL	Phase 2	CHRM2, CHRM3, CHRM5, HRH1, SLC6A2, SLC6A4
OXATOMIDE	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
THIOPROPERAZINE	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
Apixaban	PubChem	Approved	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
Binimetinib	PubChem	Approved	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
Bosentan	PubChem	Approved	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
Fulvestrant	PubChem	Approved	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
Imipenem	PubChem	Approved	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
Pyrazinamide	PubChem	Approved	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
Tafamidis	PubChem	Approved	CHRM1, CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
Tiotropium Bromide Monohydrate	PubChem	Approved	CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
Mavorixafor	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
OLODATEROL	ChEMBL + PubChem	Phase 4 (approved)	CHRM2, CHRM3, HRH1, SLC6A2, SLC6A4
ACETYLCHOLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
AMBENONIUM	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, SLC6A2, SLC6A4
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, HRH1, SLC6A2, SLC6A4

Genes: CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HRH1, SLC6A2, SLC6A4
Indicated for: depressive disorder
Drugs: Aclidinium Bromide, Amitriptyline, Clozapine, Desloratadine, Amiodarone, Amoxapine, Astemizole, Benztropine, Chlorpromazine, Cinnarizine, Clemastine, Clomipramine, Cyproheptadine, Dexchlorpheniramine, Diphenhydramine, Doxepin, Ebastine, Haloperidol, Imipramine, Loxapine, Mepazine, Mianserin, Nortriptyline, Orphenadrine, Prochlorperazine, Promazine, Promethazine, Risperidone, Sertraline, Suloctidil, Thioridazine, Dimethindene, Olanzapine, Clotrimazole, Dimenhydrinate, Fluoxetine, Fluphenazine, Maprotiline, Paroxetine, Perhexiline, Tamoxifen, Terconazole, Tolterodine, Xanomeline, Enclomiphene, Afatinib, chenodiol, Dihydroergotamine, Linagliptin, Propoxyphene, Tadalafil, Cariprazine, Clidinium, Cyclizine, Cyclobenzaprine, Darifenacin, Desipramine, Dicyclomine, Econazole, Glycopyrronium Bromide, Ketotifen, Lasofoxifene, Methapyrilene, Miconazole, Nefopam, Oxybutynin, Piperacetazine, Quetiapine, Quinacrine, Sulconazole, Sunitinib, Thiotepa, Tiotropium Bromide, Melitracen, Otilonium Bromide, Apixaban, Binimetinib, Bosentan, Fulvestrant, Imipenem, Pyrazinamide, Tafamidis, Mavorixafor, Olodaterol, Acetylcholine, Ambenonium, Aripiprazole

Summary

Identifiers

Drug identity and classification

Targets

Targets

Bioactivity

Target pathways

Top Reactome pathways

Dominant GO biological processes

Indications & clinical

Indications

Clinical trials

Phase distribution

Top trials by phase / activity

Clinical evidence (CIViC)

Pharmacology

Pharmacogenomics

Related molecules

Related molecules

Related Atlas pages