Serine

Summary

Serine (CHEMBL11298) is a phase-3 clinical-stage small molecule targeting GPRC6A; indicated across 8 conditions including post-traumatic stress disorder and exocrine pancreatic carcinoma.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (GPRC6A)
• Indications: 8 conditions
• Clinical trials: 14
• Chemistry: 105.09 Da · C3H7NO3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL11298
Name	Serine
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	5951
ChEBI	CHEBI:17115
Molecular formula	C3H7NO3
Molecular weight	105.09
InChIKey	MTCFGRXMJLQNBG-REOHCLBHSA-N

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

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

ChEBI definition: The L-enantiomer of serine.

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

Also known as: L-(-)-serine, L-serine, NSC-118365, Serina, Serine, L-Serine, SID11111802, SID11113417, SID11113418, SERINE, serine, (L)-Serine

Patent coverage: 209,191 distinct patent families (684,216 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).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
GPRC6A	GPRC6	Full agonist	3.2	0%	Q5T6X5

Broader ChEMBL bioactivity targets: 10 (assay-derived). Sample: Lysine-specific demethylase 4E, 4’-phosphopantetheinyl transferase ffp, Acetylcholinesterase, Muscarinic acetylcholine receptor M1, Glutathione hydrolase 1 proenzyme, Cytochrome P450 1A2, Acetylcholinesterase, Asc-type amino acid transporter 1, Lethal factor, Cholinesterase.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 13 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P08482	7.95	Potency	11.2	nM	CHEMBL_ACT_4811431
O42275	7.82	IC50	15	nM	CHEMBL_ACT_15637807
P81908	7.8	IC50	16	nM	CHEMBL_ACT_15637804
P15917	6	Potency	1000	nM	CHEMBL_ACT_4633741
P63116	5.02	IC50	9600	nM	CHEMBL_ACT_17949457

Target pathways

Aggregated over 1 target gene(s): GPRC6A.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
G alpha (q) signalling events	1	GPRC6A
Class C/3 (Metabotropic glutamate/pheromone receptors)	1	GPRC6A

Dominant GO biological processes

GO term	Targets
adenylate cyclase-activating G protein-coupled receptor signaling pathway	1
calcium-mediated signaling	1
positive regulation of insulin secretion involved in cellular response to glucose stimulus	1
response to amino acid	1
regulation of testosterone biosynthetic process	1
signal transduction	1
G protein-coupled receptor signaling pathway	1

Indications & clinical

Indications

8 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).

Indication	Trial phase	MONDO	EFO
post-traumatic stress disorder	2	MONDO:0005146	EFO:0001358
exocrine pancreatic carcinoma	2	MONDO:0005192	EFO:0002618
schizoaffective disorder	2	MONDO:0005487	EFO:0005411
Alzheimer disease	2	MONDO:0004975	MONDO:0004975
amyotrophic lateral sclerosis	2	MONDO:0004976	MONDO:0004976
hereditary sensory and autonomic neuropathy	2	MONDO:0015364	MONDO:0018213
mental disorder	2	MONDO:0005084	EFO:0000677

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

Clinical trials

Total trials: 14.

Phase distribution

Phase	Trials
PHASE2	5
Not specified	4
PHASE1/PHASE2	3
PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07342439	PHASE3	NOT_YET_RECRUITING	Study of Serine Supplementation to Protect Vision in MacTel
NCT07377032	PHASE3	RECRUITING	TAP-GRIN: Interventional Study on Patients With GRIN-related Neurodevelopmental Disorders
NCT00243308	PHASE2	TERMINATED	Serp-1 for the Treatment of Acute Coronary Syndrome
NCT01733407	PHASE1/PHASE2	COMPLETED	L-Serine Supplementation in Hereditary Sensory Neuropathy Type 1
NCT01835782	PHASE1/PHASE2	UNKNOWN	Determining the Safety of L-serine in ALS
NCT02599038	PHASE1/PHASE2	COMPLETED	Serine Supplementation for Obese Subjects With Fatty Liver Disease
NCT03062449	PHASE2	TERMINATED	Phase IIa L-serine Trial for eAD
NCT03580616	PHASE2	TERMINATED	Tolerability and Efficacy of L-Serine in Patients With Amyotrophic Lateral Sclerosis (ALS)
NCT04907084	PHASE2	UNKNOWN	Serine and Fenofibrate Study in Patients With MacTel Type 2
NCT06113055	PHASE2	UNKNOWN	Hereditary Sensory Neuropathy Serine Trial
NCT07466290	Not specified	RECRUITING	L-serine and Strength Training in the Elderly
NCT07497347	Not specified	RECRUITING	Effects of Specific Amino Acid Supplementation and Lifestyle Factors on Brain Ageing
NCT02528994	Not specified	WITHDRAWN	Short Term Dietary Serine Supplementation and Circulating Serine Levels
NCT04646447	Not specified	UNKNOWN	Tolerability and Efficacy of L-Serine in Patients With GRIN-related Encephalopathy

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).