◎ Sugi Atlas

Atlas / Drug / (D)-Serine

(D)-Serine

drug
On this page

Also known as D-serineSID26753645SID50106988SID90341480SID26753646SID144204821

Summary

(D)-Serine (CHEMBL285123) is a phase-3 clinical-stage small-molecule NMDA receptor agonist targeting GRIN1, GRIN2A, and GRIN2B; indicated across 3 conditions including schizoaffective disorder and cocaine dependence.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 5 (GRIN1, GRIN2A, GRIN2B…)
  • Indications: 3 conditions
  • Clinical trials: 26
  • Chemistry: 105.09 Da · C3H7NO3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL285123
Name(D)-Serine
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID71077
ChEBICHEBI:16523
Molecular formulaC3H7NO3
Molecular weight105.09
InChIKeyMTCFGRXMJLQNBG-UWTATZPHSA-N

SMILES: C([C@H](C(=O)O)N)O

IUPAC name: (2R)-2-amino-3-hydroxypropanoic acid

ChEBI definition: The R-enantiomer of serine.

Pharmacological roles (ChEBI): NMDA receptor agonist.

Other ChEBI roles (chemical / environmental): human metabolite, Escherichia coli metabolite.

Also known as: (d)-serine, D-serine, D-Serine, SID26753645, SID50106988, SID90341480, SID26753646, SID144204821, (D)-serine, (D)-SERINE, D-SERINE

Parent form; salt/anhydrous children: CHEMBL4650463

Patent coverage: 4,483 distinct patent families (13,551 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
GRIN1GluN1Agonist0.1%Q05586
GRIN2AGluN2AAgonist0.4%Q12879
GRIN2BGluN2BAgonist0%Q13224
GRIN2CGluN2CAgonist0.2%Q14957
GRIN2DGluN2DAgonist0.2%O15399

Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: Prelamin-A/C, RecQ-like DNA helicase BLM, Glutamate NMDA receptor, Glutamate NMDA receptor; Grin1/Grin2b, Glutamate NMDA receptor; Grin1/Grin2a, Glutamate NMDA receptor; Grin1/Grin2c, Ionotropic glutamate receptor NMDA 1/2D, Glutamate receptor ionotropic, NMDA 1, Asc-type amino acid transporter 1.

Bioactivity

ChEMBL activities: 16 potent at pChembl ≥ 5 of 17 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
BLM8.6Potency2.5nMCHEMBL_ACT_4745850
BLM8.6Potency2.5nMCHEMBL_ACT_4917938
P354396.82EC50150nMCHEMBL_ACT_24390742
P354396.8EC50160nMCHEMBL_ACT_430452
P354396.77EC50170nMCHEMBL_ACT_29223729
P354396.72EC50190nMCHEMBL_ACT_24390725
P354396.7EC50200nMCHEMBL_ACT_426896
P354396.68EC50210nMCHEMBL_ACT_29223713
P354396.52IC50300nMCHEMBL_ACT_426895
P354396.5Ki316.2nMCHEMBL_ACT_2710062
P354396.21EC50620nMCHEMBL_ACT_24390715
P354396.17EC50670nMCHEMBL_ACT_29223697
P354396.17IC50670nMCHEMBL_ACT_430451
P354396EC501000nMCHEMBL_ACT_24390705
P354395.95EC501130nMCHEMBL_ACT_29223645
P631165.03IC509400nMCHEMBL_ACT_17949456

Target pathways

Aggregated over 5 target gene(s): GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D.

Top Reactome pathways

11 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
Activated NTRK2 signals through FYN1GRIN2B

Dominant GO biological processes

GO termTargets
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 transport5
monoatomic ion transmembrane transport5
regulation of membrane potential4
calcium-mediated signaling4

Indications & clinical

Indications

2 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)PhaseMONDOEFO
schizoaffective disorder3MONDO:0005487EFO:0005411
cocaine dependence2MONDO:0005186EFO:0002610

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

Clinical trials

Total trials: 26.

Phase distribution

PhaseTrials
PHASE211
Not specified5
PHASE33
PHASE13
PHASE42
PHASE1/PHASE22

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00215904PHASE4COMPLETEDD-serine Adjuvant Treatment for Parkinson’s Disease
NCT01018056PHASE4COMPLETEDDeveloping New Treatments for Tourette Syndrome: Therapeutic Trials With Modulators of Glutamatergic Neurotransmission
NCT07263022PHASE3NOT_YET_RECRUITINGCognitive Strategies in Early Psychosis 2
NCT00237809PHASE3COMPLETEDD-Serine Treatment of Negative Symptoms and Cognitive Deficits in Schizophrenia
NCT00237848PHASE3COMPLETEDD-Serine for Enhancing Cognitive Retraining for the Treatment of Schizophrenia
NCT07312110PHASE2RECRUITINGD-SPARK: A Clinical Trial of D-Serine for Modifying Parkinson’s Disease Progression
NCT00138775PHASE2UNKNOWNIsrael Multicenter D-Serine Study (IMSER) for the Treatment of Schizophrenia
NCT00215878PHASE2COMPLETEDD-serine for Posttraumatic Stress Disorder Treatment
NCT00322023PHASE2COMPLETEDSafety and Effectiveness of D-serine in Schizophrenia
NCT00491569PHASE2COMPLETEDSarcosine or D-Serine Add-on Treatment for Chronic Schizophrenia
NCT00816894PHASE2COMPLETEDD-serine Monotherapy for Schizophrenia
NCT00826202PHASE2COMPLETEDD-serine for the Schizophrenia Prodrome
NCT01459029PHASE2UNKNOWNHigh Dose D-Serine as Adjuvant Treatment for Recent Onset Schizophrenia
NCT01474395PHASE2UNKNOWNN-methyl-D-aspartic Acid (NMDA) and Cognitive Remediation in Schizophrenia
NCT01715051PHASE2WITHDRAWND-Serine for Cocaine Dependence Pilot
NCT02156908PHASE2COMPLETEDD-serine and Cognitive Remediation in Schizophrenia
NCT03711500PHASE1/PHASE2COMPLETEDD-serine Augmentation of Neuroplasticity
NCT05046353PHASE1/PHASE2SUSPENDEDD-serine AudRem: R33 Phase
NCT06876129PHASE1RECRUITINGPharmacologic Augmentation of TMS for Depression With D-serine
NCT07079930PHASE1RECRUITINGSafety and Psychological Effects of Psilocybin and D-Serine Formulation in Healthy Volunteers
NCT03778320PHASE1COMPLETEDA Study to Compare the Safety, Tolerability, and Pharmacokinetics of CTP-692 Versus D-serine in Healthy Volunteers
NCT01804920Not specifiedUNKNOWND-Serine Treatment For Tardive Dyskinesia
NCT02051426Not specifiedCOMPLETEDBehavioral and Cognitive Effects of the N-methyl-D-aspartate Receptor (NMDAR) Co-agonist D-serine in Healthy Humans
NCT03702933Not specifiedUNKNOWND-serine in Schizophrenia
NCT04140773Not specifiedTERMINATEDThe Effect of D-serine as add-on Therapy in Recent-onset Psychosis
NCT04721249Not specifiedCOMPLETEDD-serine Supplementation for 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.

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

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.4
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot