Choline

Summary

Choline (CHEMBL920) is an approved small-molecule neurotransmitter.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Clinical trials: 29
• Chemistry: 104.17 Da · C5H14NO+

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL920
Name	Choline
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	305
ChEBI	CHEBI:15354
Molecular formula	C5H14NO+
Molecular weight	104.17
InChIKey	OEYIOHPDSNJKLS-UHFFFAOYSA-N

SMILES: C[N+](C)(C)CCO

IUPAC name: 2-hydroxyethyl(trimethyl)azanium

ChEBI definition: A choline that is the parent compound of the cholines class, consisting of ethanolamine having three methyl substituents attached to the amino function.

Pharmacological roles (ChEBI): neurotransmitter, nutrient, allergen.

Other ChEBI roles (chemical / environmental): human metabolite, plant metabolite, Daphnia magna metabolite, Saccharomyces cerevisiae metabolite, Escherichia coli metabolite, mouse metabolite.

Also known as: choline, N, N-trimethylethanaminium, Choline, SID11110922, SID90340588

Parent form; salt/anhydrous children: CHEMBL282468, CHEMBL2095207, CHEMBL4297301

Patent coverage: 93,202 distinct patent families (260,153 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

Broader ChEMBL bioactivity targets: 10 (assay-derived). Sample: Neuronal acetylcholine receptor; alpha3/beta2, Neuronal acetylcholine receptor; alpha2/beta2, Neuronal acetylcholine receptor; alpha3/beta4, Neuronal acetylcholine receptor; alpha4/beta4, Neuronal acetylcholine receptor; alpha4/beta2, Solute carrier family 22 member 1, Neuronal acetylcholine receptor, Muscarinic acetylcholine receptor M1, High affinity choline transporter 1, Sodium- and chloride-dependent creatine transporter 1.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
Q8BGY9	5.8	IC50	1600	nM	CHEMBL_ACT_636192

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

0 indications (0 at ChEMBL trial phase 4).

Clinical trials

Total trials: 29.

Phase distribution

Phase	Trials
Not specified	16
PHASE4	4
PHASE1	4
PHASE2	3
PHASE3	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00720343	PHASE4	COMPLETED	Effect of Oral Choline Supplementation on Postoperative Pain
NCT01098383	PHASE4	UNKNOWN	Treatment With Acetyl-Choline Esterase Inhibitors in Children With Autism Spectrum Disorders
NCT02669641	PHASE4	UNKNOWN	Complex Imaging Assessment of Steatosis
NCT06772727	PHASE4	COMPLETED	Lidocaine-based Versus Opioid-based Induction of Anesthesia in Emergency Laparotomy
NCT02371993	PHASE3	COMPLETED	Asthma in the Elderly: A Study of Choline Supplementation
NCT05076682	PHASE2	RECRUITING	Reverse Triple Negative Immune Resistant Breast Cancer
NCT01132599	PHASE2	WITHDRAWN	Comparing PET-CT Using C-11 Choline and 18F-Fluoromethylcholine in Patients With Metastatic Prostate Cancer
NCT01911299	PHASE2	COMPLETED	Choline Supplementation in Children With Fetal Alcohol Spectrum Disorders
NCT06379971	PHASE1	RECRUITING	Maternal Choline Supplementation and Cannabis Use During Pregnancy: Impact on Early Brain Development
NCT00332124	PHASE1	COMPLETED	Safety and Effectiveness of Taking Choline Supplements During Pregnancy for Improving Infant Brain Development
NCT03028857	PHASE1	COMPLETED	Choline Supplementation During Pregnancy: Impact on Attention and Social Withdrawal
NCT05880849	PHASE1	COMPLETED	Choline Effects - Pre-symptomatic AD
NCT01731236	EARLY_PHASE1	ACTIVE_NOT_RECRUITING	CARNIVAL Study: Gut Flora Dependent Metabolism of Dietary CARNItine and Phosphatidylcholine and cardioVAscuLar Disease
NCT00686361	Not specified	COMPLETED	Choline Nutrition in Children With Cystic Fibrosis (CF)
NCT01672359	Not specified	COMPLETED	Evaluating Whole Foods Supplementation on Cognition
NCT01722448	Not specified	COMPLETED	Nutritional Prevention of Exertional Muscle Dysfunction
NCT02509728	Not specified	COMPLETED	Metabolic Effects of Choline and Docosahexaenoic Acid Supplementation in Preterm Infants
NCT02852122	Not specified	COMPLETED	The Role of C-11 Choline PET in Patients With Prostate Cancer
NCT03142763	Not specified	COMPLETED	Assessment of TMAO Formation With Egg Intake Versus Choline Supplement in a Healthy Population
NCT03194659	Not specified	UNKNOWN	Synergy Between Choline and DHA
NCT03327805	Not specified	COMPLETED	Short Term Choline and Cardiovascular Health
NCT03646175	Not specified	COMPLETED	Choline Supplementation and Cardiovascular Health
NCT03938662	Not specified	UNKNOWN	S-adenosylmethionine Plus Choline in Treatment of Patients With Alcoholic Liver Disease
NCT04255368	Not specified	COMPLETED	Choline Source, Gut Microbiota and Trimethylamine-N-oxide Response
NCT04302168	Not specified	COMPLETED	Choline Supplementation on Fetal Growth in Gestational Diabetes Mellitus
NCT04764162	Not specified	COMPLETED	Choline and Cardiometabolic Health
NCT05052515	Not specified	COMPLETED	The Effects of Dihydromiricetin on MASLD
NCT06924541	Not specified	COMPLETED	Choline Dose Ranging in Postmenopausal Women
NCT07264257	Not specified	COMPLETED	Choline and Brain Functioning in Postmenopausal Women

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

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).