Glycine

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Also known as FEMA NO. 3287GlicinaGlycolixirNSC-25936Amino-acetic acidAmino-acetic acid (Glycine)glyAmino acidSID11113413L-GlycineSID170466831SID144207124AZD4282

Summary

Glycine (CHEMBL773) is an approved small-molecule hepatoprotective agent (ATC B05CX03) targeting SLC38A4, GRIN1, and GRIN2A; indicated across 17 conditions including diarrheal disease and hypertensive disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: B05CX03
  • Targets: 6 (SLC38A4, GRIN1, GRIN2A…)
  • Indications: 17 conditions
  • Clinical trials: 47
  • Chemistry: 75.07 Da · C2H5NO2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL773
NameGlycine
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID750
ChEBICHEBI:15428
ATCB05CX03
Molecular formulaC2H5NO2
Molecular weight75.07
InChIKeyDHMQDGOQFOQNFH-UHFFFAOYSA-N

SMILES: C(C(=O)O)N

IUPAC name: 2-aminoacetic acid

ChEBI definition: The simplest (and the only achiral) proteinogenic amino acid, with a hydrogen atom as its side chain.

Pharmacological roles (ChEBI): neurotransmitter, nutraceutical, hepatoprotective agent, EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor, NMDA receptor agonist, micronutrient.

Other ChEBI roles (chemical / environmental): fundamental metabolite.

Also known as: FEMA NO. 3287, Glicina, Glycine, Glycolixir, NSC-25936, Amino-acetic acid, Amino-acetic acid (Glycine), glycine, gly, Amino acid, GLYCINE, SID11113413

Parent form; salt/anhydrous children: CHEMBL3707233

Patent coverage: 428,855 distinct patent families (1,220,071 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).

GeneTargetActionpAffinityCancer dependencyUniProt
SLC38A4sodium-coupled neutral amino acid transporter 40%Q969I6
GRIN1GluN1Full agonist0.1%Q05586
GRIN2AGluN2AAgonist0.4%Q12879
GRIN2BGluN2BAgonist0%Q13224
GRIN2CGluN2CAgonist0.2%Q14957
GRIN2DGluN2DAgonist0.2%O15399

Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: Glutamate NMDA receptor, Glutamate NMDA receptor; Grin1/Grin2b, Glutamate NMDA receptor; Grin1/Grin2a, Glutamate NMDA receptor; Grin1/Grin2c, Sodium- and chloride-dependent glycine transporter 1, Ionotropic glutamate receptor NMDA 1/2D, Glutamate receptor ionotropic, NMDA 1, Olfactory receptor 51E2, Glycine receptor subunit alpha-1.

Bioactivity

ChEMBL activities: 18 potent at pChembl ≥ 5 of 21 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
OR51E27.24EC5058nMCHEMBL_ACT_19491366
P354397.17EC5068nMCHEMBL_ACT_396210
P354397.07IC5086nMCHEMBL_ACT_819738
P354397.04EC5091nMCHEMBL_ACT_24390740
P354396.9Ki125.9nMCHEMBL_ACT_2710065
P354396.89EC50130nMCHEMBL_ACT_29223728
P354396.77Ki170nMCHEMBL_ACT_162086
P354396.7IC50200nMCHEMBL_ACT_414162
P354396.7EC50200nMCHEMBL_ACT_414163
P354396.68EC50210nMCHEMBL_ACT_24390726
P354396.62EC50240nMCHEMBL_ACT_24390714
P354396.6IC50250nMCHEMBL_ACT_396209
P354396.52EC50300nMCHEMBL_ACT_29223712
P354396.44EC50360nMCHEMBL_ACT_29223696
P354396.16IC50690nMCHEMBL_ACT_113750
P354396EC50990nMCHEMBL_ACT_24390704
P354396EC501000nMCHEMBL_ACT_29223644
P354395.21IC506200nMCHEMBL_ACT_1227955

Target pathways

Aggregated over 6 target gene(s): SLC38A4, GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D.

Top Reactome pathways

15 total, by targets touching each:

PathwayTargetsGenes
Unblocking of NMDA receptors, glutamate binding and activation5GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
Neurexins and neuroligins5GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
Synaptic adhesion-like molecules5GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
Assembly and cell surface presentation of NMDA receptors5GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
Negative regulation of NMDA receptor-mediated neuronal transmission5GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
Long-term potentiation5GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
Ras activation upon Ca2+ influx through NMDA receptor3GRIN1, GRIN2B, GRIN2D
RAF/MAP kinase cascade3GRIN1, GRIN2B, GRIN2D
EPHB-mediated forward signaling2GRIN1, GRIN2B
MECP2 regulates neuronal receptors and channels2GRIN2A, GRIN2B
Amino acid transport across the plasma membrane1SLC38A4
Transport of small molecules1SLC38A4
R-HSA-4253931SLC38A4
SLC-mediated transmembrane transport1SLC38A4
Activated NTRK2 signals through FYN1GRIN2B

Dominant GO biological processes

GO termTargets
monoatomic ion transport6
brain development5
ionotropic glutamate receptor signaling pathway5
regulation of synaptic plasticity5
regulation of neuronal synaptic plasticity5
positive regulation of synaptic transmission, glutamatergic5
excitatory postsynaptic potential5
calcium ion transmembrane import into cytosol5
monoatomic cation transmembrane transport5
excitatory chemical synaptic transmission5
regulation of monoatomic cation transmembrane transport5
positive regulation of excitatory postsynaptic potential5
monoatomic ion transmembrane transport5
regulation of membrane potential4
calcium-mediated signaling4

Indications & clinical

Indications

17 indications (0 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).

IndicationTrial phaseMONDOEFO
diarrheal disease3MONDO:0001673MONDO:0001673
hypertensive disorder2MONDO:0005044EFO:0000537
obsessive-compulsive disorder2MONDO:0008114EFO:0004242
schizoaffective disorder2MONDO:0005487EFO:0005411
asthma2MONDO:0004979MONDO:0004979
cystic fibrosis2MONDO:0009061MONDO:0009061
bipolar disorder2MONDO:0004985MONDO:0004985
mental disorder2MONDO:0005084EFO:0000677
respiratory system disorder2MONDO:0005087EFO:0000684
herpes simplex infectious disease2MONDO:0004609EFO:1002022
herpes labialis2MONDO:0043653MONDO:0043653
HIV infectious disease1MONDO:0005109EFO:0000764
severe acute respiratory syndrome0MONDO:0005091MONDO:0100096
Alzheimer disease0MONDO:0004975MONDO:0004975

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

Clinical trials

Total trials: 47.

Phase distribution

PhaseTrials
Not specified16
PHASE29
PHASE45
PHASE35
PHASE14
EARLY_PHASE14
PHASE2/PHASE33
PHASE1/PHASE21

Top trials by phase / activity

NCTPhaseStatusTitle
NCT06597201PHASE4RECRUITINGEvaluate the Efficacy and Safety of Amino Acid (15) Peritoneal Dialysis Solution in Peritoneal Dialysis Patients with Malnutrition.
NCT07370441PHASE4ENROLLING_BY_INVITATIONAmino Acid (15) Peritoneal Dialysis Solution for Nutritional Improvement in Peritoneal Dialysis Patients
NCT07575984PHASE4RECRUITINGMexidol® Safety and Efficacy in Treatment of Hyperacute and Acute Ischemic Stroke
NCT02926235PHASE4TERMINATEDTrial of Essential Amino Acid Supplementation in Protein Deficient Patients Following Total Knee Arthroplasty
NCT05877989PHASE4COMPLETEDEvaluation of Effectiveness of Combining High Protein Intake With Early Physical Exercise During Critical Illness
NCT00000372PHASE3WITHDRAWNGlycine and D-Cycloserine in Schizophrenia
NCT00133406PHASE3UNKNOWNLong-term Impact and Intervention for Diarrhea in Brazil
NCT00133562PHASE3WITHDRAWNHIAS II - Study of Nutritional Supplementation in Hospitalized Children With Persistent Diarrhea or Malnutrition
NCT00222235PHASE2/PHASE3COMPLETEDAdjunctive Treatment for Decreasing Symptoms of Schizophrenia
NCT00291226PHASE2/PHASE3COMPLETEDGlycine vs Placebo for the Schizophrenia Prodrome
NCT00338221PHASE3WITHDRAWNClinical Trial of Alanyl-Glutamine or Glycine in Children With Persistent Diarrhea or Malnutrition
NCT00762450PHASE3COMPLETEDEffect on Bacterial Glycolytic Acid Formation on Plaque
NCT03850314PHASE2/PHASE3UNKNOWNThe Effects of Glycine on Atherosclerosis and Metabolic Syndrome-related Parameters.
NCT04738422PHASE2ENROLLING_BY_INVITATIONDetermining Airway pH by Compartmental Exhaled Nitric Oxide Levels During Alkaline Buffer Challenge
NCT00005658PHASE2COMPLETEDGlycine to Treat Psychotic Disorders in Children
NCT00268749PHASE2COMPLETEDGlycine Treatment of Prodromal Symptoms
NCT00313807PHASE2WITHDRAWNStudy of Intravenous Amino Acid Infusion to Prevent Contrast Dye Mediated Renal Damage
NCT00338598PHASE2COMPLETEDFacilitation of NMDA Receptor Function in Patients With Schizophrenia and Co-morbid Alcoholism
NCT00913692PHASE2TERMINATEDA Randomized Double-Blind Control-Comparison Crossover Trial of Oral Glutamine to Suppress Frequently Recurrent Herpes Labialis
NCT01031927PHASE2COMPLETEDN-methyl Glycine (Sarcosine) for the Treatment of Obsessive Compulsive Disorder (OCD)
NCT01417481PHASE2TERMINATEDEffect of Glycine in Cystic Fibrosis
NCT01720316PHASE2COMPLETEDNeurobiology of a Mutation in Glycine Metabolism in Psychotic Disorders
NCT03617718PHASE1/PHASE2COMPLETEDProject 2 Airway Potential Hydrogen (pH) in Asthma
NCT00575848PHASE1TERMINATEDStudy of the Effects of Glycine on Symptoms and Memory in Patients With Schizophrenia
NCT00929370PHASE1TERMINATEDA Repeat Dose Study With GSK1018921 to Assess Safety, Tolerability, Pharmacokinetics, Pharmacodynamics in Healthy Volunteers and Patients With Schizophrenia and to Evaluate Its Effect on PK of Midazolam.
NCT01355198PHASE1COMPLETEDRole of HIV on Glutathione Synthesis and Oxidative Stress
NCT02348762PHASE1COMPLETEDEnergetics and Function in Older Humans
NCT03493178EARLY_PHASE1ACTIVE_NOT_RECRUITINGGlutathione in Mild Cognitive Impairment
NCT04740580EARLY_PHASE1RECRUITINGGlutathione, Brain Metabolism and Inflammation in Alzheimer’s Disease
NCT01870193EARLY_PHASE1COMPLETEDGlutathione and Fuel Oxidation in Aging
NCT04703036EARLY_PHASE1TERMINATEDGlutathione, Oxidative Stress and Mitochondrial Function in COVID-19
NCT06959251Not specifiedRECRUITINGGlycine and Magnesium+Thiamine for the Treatment of Primary Ciliary Dyskinesia
NCT07285135Not specifiedNOT_YET_RECRUITINGDietary Glycine Supplementation in Metabolic Dysfunction-associated Steatotic Liver Disease
NCT07556029Not specifiedNOT_YET_RECRUITINGOptimal Protein Intake to Maximize Whole-Body Protein Balance in Healthy Adults
NCT00405535Not specifiedCOMPLETEDAdjunctive Glycine for Obsessive Compulsive Disorder
NCT01610011Not specifiedCOMPLETEDAcute Glycine Pharmacodynamic Study
NCT02149953Not specifiedCOMPLETEDDetermination of Glycine Requirement in Pregnancy
NCT02235194Not specifiedCOMPLETEDEffects of an Amino Acid and Chromium-picolinate Containing Drink on Glucose Metabolism
NCT02315391Not specifiedCOMPLETEDProtein Nutrition for Muscle Hypertrophy in Older Adults
NCT02655276Not specifiedCOMPLETEDSublingual Glycine vs. Placebo on Attentional Difficulties and Hyperactivity in Prepuberal Children

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.

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.

41 molecules share ≥1 primary target. Top 41 by shared-target count:

MoleculeSourceStatusShared targets
AMANTADINEChEMBL + PubChemPhase 4 (approved)GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
CHLORPROMAZINEChEMBL + PubChemPhase 4 (approved)GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
DEXTROMETHORPHANChEMBL + PubChemPhase 4 (approved)GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
KETAMINEChEMBL + PubChemPhase 4 (approved)GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
LEVORPHANOLChEMBL + PubChemPhase 4 (approved)GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
MEMANTINEChEMBL + PubChemPhase 4 (approved)GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
ORPHENADRINEChEMBL + PubChemPhase 4 (approved)GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
CYCLOSERINEChEMBLPhase 4 (approved)GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
PROCYCLIDINEChEMBLPhase 4 (approved)GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
GLUTAMIC ACIDChEMBL + PubChemPhase 3 (approved)GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
DALZANEMDORChEMBLPhase 3GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
ESMETHADONEChEMBLPhase 3GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
ALPHAMETHADOLChEMBLPhase 2GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
BUDIPINEChEMBLPhase 2GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
DEXTRORPHANChEMBLPhase 2GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
DIZOCILPINEChEMBLPhase 2GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
IFENPRODILChEMBLPhase 2GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
LANICEMINEChEMBLPhase 2GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
LEVOMETHADONEChEMBLPhase 2GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
LICOSTINELChEMBLPhase 2GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
PERZINFOTELChEMBLPhase 2GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
PHENCYCLIDINEChEMBLPhase 2GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
RACEMETHORPHANChEMBLPhase 2GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
RADIPRODILChEMBLPhase 2GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
SELFOTELChEMBLPhase 2GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
TEZAMPANELChEMBLPhase 2GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
TRAXOPRODILChEMBLPhase 2GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
BETAMETHADOLChEMBLPhase 2GRIN1, GRIN2A, GRIN2C, GRIN2D
TACRINEChEMBLPhase 4 (approved)GRIN1, GRIN2A, GRIN2B
LATREPIRDINEChEMBLPhase 3GRIN1, GRIN2A, GRIN2B
ESKETAMINEChEMBL + PubChemPhase 4 (approved)GRIN1, GRIN2A
PENTAMIDINEChEMBLPhase 4 (approved)GRIN1, GRIN2A
DEXOXADROLChEMBLPhase 2GRIN1, GRIN2A
DIMEMORFANChEMBLPhase 2GRIN1, GRIN2A
ELIPRODILChEMBLPhase 2GRIN1, GRIN2B
ETOXADROLChEMBLPhase 2GRIN1, GRIN2A
ONFASPRODILChEMBLPhase 2GRIN1, GRIN2B
ZELQUISTINELChEMBLPhase 2GRIN2B, GRIN2C
NimodipinePubChemApprovedGRIN2C, GRIN2D
HALOPERIDOLChEMBLPhase 4 (approved)GRIN2B
EVT-101 FREE BASEChEMBLPhase 2GRIN2B