Tolterodine

Summary

Tolterodine (CHEMBL1382) is an approved small-molecule muscarinic antagonist (ATC G04BD07) targeting CHRM1, CHRM2, and CHRM3; indicated across 8 conditions including overactive bladder and pelvic organ prolapse.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: G04BD07
• Targets: 5 (CHRM1, CHRM2, CHRM3…)
• Indications: 8 conditions
• Clinical trials: 47
• Chemistry: 325.5 Da · C22H31NO

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1382
Name	Tolterodine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	443879
ChEBI	CHEBI:9622
ATC	G04BD07
Molecular formula	C22H31NO
Molecular weight	325.5
InChIKey	OOGJQPCLVADCPB-HXUWFJFHSA-N

SMILES: CC1=CC(=C(C=C1)O)[C@H](CCN(C(C)C)C(C)C)C2=CC=CC=C2

IUPAC name: 2-[(1R)-3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-methylphenol

Pharmacological roles (ChEBI): muscarinic antagonist, muscle relaxant, antispasmodic drug.

Also known as: Blerone xl, Detrusitol, Detrusitol xl, Efflosomyl xl, Inconex xl, KABI 2234, KABI-2234, Mariosea xl, Neditol xl, Preblacon xl, Santizor xl, Tolterodina

Parent form; salt/anhydrous children: CHEMBL1200871, CHEMBL1722209

Patent coverage: 3,589 distinct patent families (13,460 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 13,422 (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
CHRM1	M1 receptor	Antagonist	8.5	0.2%	P11229
CHRM2	M2 receptor	Inverse agonist	8.5	0%	P08172
CHRM3	M3 receptor	Antagonist	8.5	0%	P20309
CHRM4	M4 receptor	Antagonist	8.4	1.6%	P08173
CHRM5	M5 receptor	Antagonist	8.8	0%	P08912

Broader ChEMBL bioactivity targets: 29 (assay-derived). Sample: Microtubule-associated protein tau, Nuclear receptor ROR-gamma, Prelamin-A/C, Inositol monophosphatase 1, Muscarinic acetylcholine receptor M4, Muscarinic acetylcholine receptor, Voltage-dependent L-type calcium channel subunit alpha-1C, Histamine H2 receptor, A-type voltage-gated potassium channel KCND3, Sodium channel protein type 5 subunit alpha, Muscarinic acetylcholine receptor M5, Estrogen receptor, Muscarinic acetylcholine receptor M2, Muscarinic acetylcholine receptor M1, Prostaglandin G/H synthase 1, Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK), 5-hydroxytryptamine receptor 2A, Sodium-dependent serotonin transporter, Alpha-1A adrenergic receptor, Histamine H1 receptor.

Bioactivity

ChEMBL activities: 41 potent at pChembl ≥ 5 of 51 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P08482	8.85	Ki	1.4	nM	CHEMBL_ACT_18475893
CHRM1	8.85	Ki	1.4	nM	CHEMBL_ACT_2090898
P08911	8.66	Ki	2.2	nM	CHEMBL_ACT_18475901
CHRM5	8.66	Ki	2.2	nM	CHEMBL_ACT_2090902
P10980	8.57	Ki	2.7	nM	CHEMBL_ACT_18475895
CHRM2	8.57	Ki	2.7	nM	CHEMBL_ACT_2090899
P08485	8.51	Ki	3.1	nM	CHEMBL_ACT_18475899
CHRM4	8.51	Ki	3.1	nM	CHEMBL_ACT_2090901
CHRM3	8.49	Ki	3.2	nM	CHEMBL_ACT_1666531
P08483	8.44	Ki	3.6	nM	CHEMBL_ACT_18475897
CHRM3	8.44	Ki	3.6	nM	CHEMBL_ACT_2090900
CHRM3	8.44	Ki	3.6	nM	CHEMBL_ACT_6185871
CHRM3	8.44	Ki	3.6	nM	CHEMBL_ACT_6376071
CHRM2	8.4	Ki	4	nM	CHEMBL_ACT_1666567
CHRM1	8.29	AC50	5.1	nM	CHEMBL_ACT_25135641
P08482	8.2	IC50	6.31	nM	CHEMBL_ACT_18475903
CHRM5	8.19	AC50	6.5	nM	CHEMBL_ACT_25137449
P10980	8.16	Ki	6.91	nM	CHEMBL_ACT_1518809
P08483	8.15	Ki	7.07	nM	CHEMBL_ACT_1518808
CHRM2	8.07	AC50	8.6	nM	CHEMBL_ACT_25196389
CHRM2	8.05	AC50	8.9	nM	CHEMBL_ACT_25195991
CHRM2	7.97	AC50	10.7	nM	CHEMBL_ACT_25195315
KCNH2	7.9	IC50	12.59	nM	CHEMBL_ACT_15258102
CHRM2	7.8	Kd	15.85	nM	CHEMBL_ACT_1666602
KCNH2	7.77	IC50	16.98	nM	CHEMBL_ACT_1523561
CHRM3	7.71	AC50	19.4	nM	CHEMBL_ACT_25136869
CHRM1	7.69	AC50	20.6	nM	CHEMBL_ACT_25210424
CHRM2	7.63	AC50	23.2	nM	CHEMBL_ACT_25213913
KCNH2	7.52	AC50	30	nM	CHEMBL_ACT_25118122
KCNH2	6.9	IC50	125.9	nM	CHEMBL_ACT_15258042
O35505	6.84	IC50	143	nM	CHEMBL_ACT_15373301
KCNH2	6.8	IC50	158.5	nM	CHEMBL_ACT_15258068
ADRA1A	5.56	AC50	2744	nM	CHEMBL_ACT_25138047
HRH2	5.5	AC50	3196	nM	CHEMBL_ACT_25114490
HRH1	5.39	AC50	4062	nM	CHEMBL_ACT_25212697
MAPT	5.3	Potency	5012	nM	CHEMBL_ACT_4506747
P51450	5.25	Potency	5623	nM	CHEMBL_ACT_4766701
SCN5A	5.2	IC50	6310	nM	CHEMBL_ACT_15258196
OPRK1	5.17	AC50	6711	nM	CHEMBL_ACT_25129600
HTR2A	5.05	AC50	8838	nM	CHEMBL_ACT_25173681
SCN5A	5.04	AC50	9100	nM	CHEMBL_ACT_25158947

Target pathways

Aggregated over 5 target gene(s): CHRM1, CHRM2, CHRM3, CHRM4, CHRM5.

Top Reactome pathways

17 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	3	CHRM1, CHRM3, CHRM5
G alpha (i) signalling events	2	CHRM2, CHRM4
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

Dominant GO biological processes

GO term	Targets
signal transduction	5
G protein-coupled receptor signaling pathway	5
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	5
G protein-coupled acetylcholine receptor signaling pathway	5
chemical synaptic transmission	5
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathway	3
nervous system development	3
acetylcholine receptor signaling pathway	3
regulation of locomotion	2
saliva secretion	2
regulation of smooth muscle contraction	2
phospholipase C-activating G protein-coupled receptor signaling pathway	1
neuromuscular synaptic transmission	1
positive regulation of monoatomic ion transport	1

Indications & clinical

Indications

4 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
overactive bladder	3	MONDO:0006624	EFO:1000781
pelvic organ prolapse	3	MONDO:0000082	EFO:0004710
nephrolithiasis	2	MONDO:0008171	EFO:0004253
neuralgia	1	MONDO:0021667	EFO:0005762

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

Clinical trials

Total trials: 47.

Phase distribution

Phase	Trials
PHASE4	13
PHASE3	11
PHASE2	8
Not specified	7
PHASE1	4
PHASE2/PHASE3	3
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00313924	PHASE4	UNKNOWN	Assessing the OAB-8 Questionnaire as a Tool to Measure Treatment Outcome
NCT00323635	PHASE4	TERMINATED	A Comparison of Tolterodine and Placebo Treatments on Nocturnal Frequency and Sleep Quality in Women After Menopause.
NCT00413790	PHASE4	COMPLETED	Pharmacologic Effects of Darifenacin and Tolterodine on Cardiovascular Parameters in Healthy Subjects
NCT00448175	PHASE4	COMPLETED	Overactive Bladder Innovative Therapy Trial (OrBIT)
NCT00523068	PHASE4	WITHDRAWN	Pharmacological vs Surgical Treatment for Mixed Incontinence
NCT00730535	PHASE4	COMPLETED	Exploring Predictors of Symptoms Relapse After Discontinuation of Treatment in Overactive Bladder (OAB) Patients
NCT01964183	PHASE4	COMPLETED	Post-marketing Study to Evaluate the Effect of Mirabegron on the Plasma Concentration of Tolterodine
NCT02256943	PHASE4	COMPLETED	Genetic Determinants of Amitriptyline Efficiency for Pain Treatment
NCT02256956	PHASE4	COMPLETED	Genetic Determinants of Amitriptyline Efficiency for Pain Treatment - Part II
NCT02294396	PHASE4	COMPLETED	Postmarketing Study to Evaluate add-on Therapy With Anticholinergics in Patients With Overactive Bladder (OAB) on Mirabegron.
NCT04090190	PHASE4	COMPLETED	Inflammation in Women With Urgency Urinary Incontinence Treated With Anticholinergics
NCT04909255	PHASE4	UNKNOWN	Beta-3 Agonist and Anti-muscarinic Agent for Sjogren’s Syndrome With Overactive Bladder
NCT05946902	PHASE4	UNKNOWN	Comparisons of the Impact of Monotherapy With Mirabegron or Tolterodine Versus Combined Treatment With Mirabegron and Tolterodine on Autonomic Function and Bladder Blow Flow in Women With Overactive Bladder Syndrome: a Randomized Controlled Study
NCT07114640	PHASE3	NOT_YET_RECRUITING	The Effect of Nighttime Mirabegron, Solifenacin, Tolterodine, or Oxybutynin on Nocturia, Sexual Function, Autonomic Function, and Lower Urinary Tract Blood Flow Perfusion in Women With Overactive Bladder Syndrome: Randomized Controlled Trial
NCT00368706	PHASE3	COMPLETED	A Double-Blind, Paralleled Study Comparing Efficacy/Safety of Solifenacin to Tolterodine in Overactive Bladder Patients
NCT00648310	PHASE2/PHASE3	COMPLETED	Topical Oestrogens and Antimuscarinics In The Treatment Of Detrusor Overactivity
NCT00688688	PHASE3	COMPLETED	Study to Test the Long Term Safety and Efficacy of the Beta-3 Agonist Mirabegron (YM178) in Patients With Symptoms of Overactive Bladder
NCT00689104	PHASE3	COMPLETED	Study to Assess the Efficacy and Safety of the Beta-3 Agonist Mirabegron (YM178) in Patients With Symptoms of Overactive Bladder
NCT00802373	PHASE3	COMPLETED	Solifenacin Succinate Versus Tolterodine 4mg Once Daily
NCT00966004	PHASE3	COMPLETED	A Study to Evaluate Safety and Efficacy of YM178 in Patients With Overactive Bladder
NCT01004315	PHASE3	COMPLETED	A Confirmatory Study of KUC-7483 in Patients With Overactive Bladder
NCT01011036	PHASE3	COMPLETED	Effects of GABA-a-Agonists on Pain Mechanisms: An Experimental Study in Healthy Volunteers
NCT01175382	PHASE2/PHASE3	COMPLETED	Combined Behavioral and Drug Treatment of Overactive Bladder in Men
NCT01179828	PHASE3	COMPLETED	Linking Altered Central Pain Processing and Genetic Polymorphism to Drug Efficacy in Chronic Low Back Pain (Predictio)
NCT01530243	PHASE2/PHASE3	COMPLETED	The Effect of Terazosin and Tolterodine on Ureteral Stent Related Symptoms
NCT02599311	PHASE3	UNKNOWN	the Indications and Clinical Efficacy of Pelvic Organ Prolapse Surgery
NCT03492281	PHASE3	COMPLETED	A Study to Examine the Safety and Efficacy of a New Drug in Patients With Symptoms of Overactive Bladder (OAB)
NCT00174798	PHASE2	COMPLETED	MILADY: A Randomized, Placebo-controlled Safety and Efficacy Trial of SSR240600C in Treatment of Overactive Bladder or Urge Urinary Incontinence.
NCT00332137	PHASE2	COMPLETED	Effects of Tolterodine, a Non-Specific Muscarinic Antagonist, on Gastrointestinal Transit in Healthy Subjects
NCT00439192	PHASE2	TERMINATED	ELB245 for 12 Weeks Versus 4mg Tolterodine in Patients With Incontinent Overactive Bladder (OAB)
NCT00564226	PHASE2	COMPLETED	SSR240600C Treatment in Women With Overactive Bladder
NCT00746681	PHASE2	COMPLETED	Investigation of Tolterodine, Pregabalin and a Tolterodine - Pregabalin Combination for the Treatment of Overactive Bladder
NCT00876421	PHASE2	COMPLETED	Study of ONO-8539 in Patients With Overactive Bladder
NCT01291316	PHASE1/PHASE2	COMPLETED	GABAergic Modulation in Pain Transmission in Human: Effect of the GABAA Agonist Clobazam on Peripheral and Central Sensitisation
NCT01356355	PHASE2	COMPLETED	Study of Herbmed Plus in Ureteral Stent Discomfort
NCT01604928	PHASE2	COMPLETED	Study to Test the Efficacy and Safety of YM178 in Subjects With Symptoms of Overactive Bladder
NCT00481728	PHASE1	COMPLETED	Evaluation of the Link Between Bladder Sensation and Changes in Skin Electrical Conductance and Heart Rate.
NCT00703703	PHASE1	COMPLETED	Pharmacologic Effects of Darifenacin and Tolterodine on Cardiovascular Parameters in Healthy Subjects
NCT01036035	PHASE1	COMPLETED	Effects of Novel Combinations of Tolterodine/Pilocarpine on Pharmacokinetics (PK) and Pharmacodynamics (PD) of Tolterodine in Healthy Subjects
NCT01181505	PHASE1	COMPLETED	STUDY The Effect of HNF-4A G60D Variant on the In VIVO CYP2D6 Activity By Tolterodine Pharmacokinetic Study
NCT07046156	Not specified	ACTIVE_NOT_RECRUITING	Treatment of Overactive Bladder With Anticholinergic Agents
NCT00090584	Not specified	COMPLETED	Behavior Enhances Drug Reduction of Incontinence (BE-DRI)
NCT00498888	Not specified	COMPLETED	The Long Term Outcomes of Rehabilitation and Drug Treatment for in Urgency Urinary Incontinence
NCT00913315	Not specified	UNKNOWN	Efficacy Study of Tamsulosin and Tolterodine Treatment for Chronic Prostatitis
NCT01503580	Not specified	COMPLETED	Studies of Psychiatric Predisposing Factors, Treatment-related Cardiovascular Effects, and Prognostic Factors Associated With Antimuscarinic Drug (Tolterodine) for Female Overactive Bladder Syndrome
NCT03572231	Not specified	COMPLETED	A Registry Study of Patients Initiating a Course of Drug Therapy for Overactive Bladder in Taiwan, Korea and China
NCT03602508	Not specified	COMPLETED	Treatment Persistence Among Patients With Overactive Bladder: A Retrospective Secondary Data Analysis in Asia Oceania

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.

576 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
CLOZAPINE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
GENTIAN VIOLET	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
Mavorixafor	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
OLANZAPINE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
ACETYLCHOLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
AMIODARONE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
AMOXAPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
ATROPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
BENZTROPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
BETHANECHOL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CARBACHOL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CARBAMOYLCHOLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CHLOROQUINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CINNARIZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CLEMASTINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CLIDINIUM	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CYCLIZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DARIFENACIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DESLORATADINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DEXCHLORPHENIRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DICYCLOMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DIMENHYDRINATE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DIPHENHYDRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DIPHENIDOL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DOXEPIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
EBASTINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
GLYCOPYRRONIUM BROMIDE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
HALOPERIDOL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
HOMATROPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
HYDROXYCHLOROQUINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
IMIPRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
IPRATROPIUM	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
KETOTIFEN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
LOXAPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
MAPROTILINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
MEPAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
METHSCOPOLAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
METHSCOPOLAMINE BROMIDE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
MIANSERIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
NORTRIPTYLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
ORPHENADRINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
OXYBUTYNIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
PAROXETINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
PERHEXILINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
PILOCARPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
PIRENZEPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
PROMAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
PROMETHAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
QUETIAPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
QUINACRINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
RISPERIDONE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
SCOPOLAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
SERTRALINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
SOLIFENACIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
SULOCTIDIL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
TAMOXIFEN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
TERCONAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
THIORIDAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
TIOTROPIUM BROMIDE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
TRIHEXYPHENIDYL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
TROPICAMIDE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
TROSPIUM CHLORIDE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
XANOMELINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DIMETHINDENE	ChEMBL	Phase 3	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
ENCLOMIPHENE	ChEMBL	Phase 3	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
ABAPERIDONE	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
APROFENE	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
BENZETHONIUM CHLORIDE	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
FLUNARIZINE	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
PF-03635659	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
SABCOMELINE	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
TALSACLIDINE	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
BETAMETHASONE PHOSPHORIC ACID	ChEMBL	Phase 4 (approved)	CHRM1, CHRM3, CHRM4, CHRM5
BIPERIDEN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
CARIPRAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM4, CHRM5
CEVIMELINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
ECONAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
FLUOXETINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM5
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
MICONAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
OXYMETAZOLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM4, CHRM5
SULCONAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM3, CHRM4, CHRM5
BLARCAMESINE	ChEMBL	Phase 3	CHRM1, CHRM2, CHRM3, CHRM4
METHYLBENACTYZIUM BROMIDE	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, CHRM4
OTENZEPAD	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, CHRM4
ZOTEPINE	ChEMBL	Phase 2	CHRM1, CHRM2, CHRM3, CHRM4
Afatinib	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3
chenodiol	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3
LINAGLIPTIN	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3
Propoxyphene	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3
ACETYLCHOLINE CHLORIDE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM3, CHRM5
AMBENONIUM	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3