◎ Sugi Atlas

Atlas / Drug / Ghrelin

Ghrelin

drug
On this page

Also known as Human ghrelinLenomorelin

Summary

Ghrelin (CHEMBL500468) is a phase-3 clinical-stage protein targeting GHSR; indicated across 8 conditions including neoplasm and peripheral arterial disease.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Protein
  • Targets: 1 (GHSR)
  • Indications: 8 conditions
  • Clinical trials: 33
  • Chemistry: 3314.8 Da · C147H245N45O42

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL500468
NameGhrelin
TypeProtein
Max phase3
FDA approvedno
PubChem CID44576256
Molecular formulaC147H245N45O42
Molecular weight3314.8
InChIKeyJSRSZGUKOAXAJV-MXAPAKLGSA-N

SMILES: CCCCCCCC(=O)OC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC3=CN=CN3)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N4CCC[C@H]4C(=O)N5CCC[C@H]5C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)N)C(=O)N6CCC[C@H]6C(=O)O)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)N

IUPAC name: (2S)-1-[(2S)-5-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-1-[(2S)-1-[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]acetyl]amino]-3-octanoyloxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-4-carboxybutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-oxopentanoyl]amino]hexanoyl]amino]propanoyl]amino]-5-oxopentanoyl]amino]-5-oxopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-4-carboxybutanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoyl]pyrrolidine-2-carboxylic acid

Also known as: Ghrelin, Human ghrelin, Lenomorelin, ghrelin, GHRELIN

Patent coverage: 2,175 distinct patent families (4,691 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
GHSRghrelin receptorFull agonist8.10.2%Q92847

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Growth hormone secretagogue receptor type 1.

Bioactivity

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

TargetpChemblTypeValueUnitActivity ID
GHSR9.85IC500.14nMCHEMBL_ACT_1429565
GHSR9.6IC500.25nMCHEMBL_ACT_439602
GHSR9.41IC500.39nMCHEMBL_ACT_1142729
GHSR9.15Ki0.7nMCHEMBL_ACT_12098275
GHSR8.85EC501.4nMCHEMBL_ACT_12098320
GHSR8.85EC501.4nMCHEMBL_ACT_1430778
GHSR8.85EC501.41nMCHEMBL_ACT_2081670
GHSR8.85EC501.4nMCHEMBL_ACT_2163153
GHSR8.85EC501.42nMCHEMBL_ACT_2449145
GHSR8.64IC502.3nMCHEMBL_ACT_15609768
GHSR8.64IC502.29nMCHEMBL_ACT_15609832
GHSR8.01IC509.8nMCHEMBL_ACT_1142728
GHSR7.5EC5032nMCHEMBL_ACT_439603

Target pathways

Aggregated over 1 target gene(s): GHSR.

Top Reactome pathways

2 total, by targets touching each:

PathwayTargetsGenes
Peptide ligand-binding receptors1GHSR
G alpha (q) signalling events1GHSR

Dominant GO biological processes

GO termTargets
G protein-coupled receptor signaling pathway1
spermatogenesis1
learning or memory1
actin polymerization or depolymerization1
adult feeding behavior1
response to hormone1
hormone-mediated signaling pathway1
negative regulation of norepinephrine secretion1
growth hormone secretion1
response to food1
negative regulation of appetite1
positive regulation of appetite1
response to follicle-stimulating hormone1
response to estradiol1
negative regulation of interleukin-1 beta production1

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).

IndicationTrial phaseMONDOEFO
neoplasm3MONDO:0005070MONDO:0004992
peripheral arterial disease2MONDO:0005386EFO:0004265
stroke disorder2MONDO:0005098EFO:0000712
obesity disorder1MONDO:0011122EFO:0001073
major depressive disorder1MONDO:0002009MONDO:0002009
type 2 diabetes mellitus1MONDO:0005148MONDO:0005148

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

Clinical trials

Total trials: 33.

Phase distribution

PhaseTrials
Not specified12
PHASE17
PHASE26
PHASE1/PHASE24
EARLY_PHASE12
PHASE41
PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05560529PHASE4COMPLETEDDialectical Behavioral Therapy As A Therapeutic Tool In Patients With Binge Eating Disorder
NCT00681486PHASE3COMPLETEDGhrelin - A Possible Opportunity to Improve Appetite
NCT00933361PHASE1/PHASE2COMPLETEDIndividual Dose-escalated Bi-daily Subcutaneously (sc) Ghrelin in Cancer Cachexia: a Phase I/II Study
NCT01779024PHASE2COMPLETEDGhrelin for Alcohol Use in Non-Treatment-Seeking Heavy Drinkers
NCT01833078PHASE2COMPLETEDGhrelin Repeated Dose Study
NCT01898611PHASE2COMPLETEDGhrelin Plus Strength Training in Frail Elderly Study
NCT03358355PHASE1/PHASE2COMPLETEDUnacylated Ghrelin to Improve FuncTioning in PAD: The GIFT Trial
NCT04377126PHASE2COMPLETEDUnacylated Ghrelin to Improve Functioning in PAD
NCT04558346PHASE2COMPLETEDGhrelin (OXE–103) for Acute Concussion Management
NCT05277415PHASE1/PHASE2COMPLETEDTranslational and Clinical Aspects of Metabolic, Anabolic and Endothelial Dysfunction in Heart Failure
NCT05318924PHASE1/PHASE2COMPLETEDEffects of Ghrelin Administration on Dopamine and Effort
NCT05726240PHASE2UNKNOWNRCT of Ghrelin in Stroke Patients
NCT00512525PHASE1COMPLETEDGhrelin Decreases Insulin Sensitivity
NCT00771940PHASE1COMPLETEDPeripheral Metabolic Effects of Ghrelin
NCT01474785PHASE1COMPLETEDRYGB and the Gastric Adipose Axis
NCT02272647PHASE1COMPLETEDProgesterone Amplifies Estrogen-stimulated Growth Hormone Secretion in Older Women
NCT02913703PHASE1COMPLETEDPreprandial Ghrelin Effect
NCT02953587PHASE1COMPLETEDEffect of Ghrelin on Glucose Metabolism After Bariatric Surgery
NCT03198143PHASE1WITHDRAWNEffect of Ghrelin on Decision-Making
NCT01595373EARLY_PHASE1COMPLETEDLocal Metabolic Effects of Ghrelin in Skeletal Muscle and Adipose Tissue
NCT02690987EARLY_PHASE1UNKNOWNGut Hormones in Obesity, Nicotine and Alcohol Dependence
NCT00447512Not specifiedCOMPLETEDEffects of Ghrelin on the Sleep-EEG and Nocturnal Secretion of Hormones
NCT00763477Not specifiedUNKNOWNGhrelin in Cystic Fibrosis
NCT00912587Not specifiedCOMPLETEDEffect of Ghrelin on Sympathetic Nervous System
NCT01190085Not specifiedCOMPLETEDEffects of Ghrelin on Alcohol Cue Reactivity and Craving
NCT01209416Not specifiedCOMPLETEDThe Effect of Pharmacological Antilipolysis on the Metabolic Effects of Ghrelin
NCT01531283Not specifiedUNKNOWNDeacylated Ghrelin and Beta Cell Function
NCT01729299Not specifiedUNKNOWNGhrelin Effect on Beta Cell Function in Health and Disease
NCT03264742Not specifiedTERMINATEDGhrelintrial With Patients With Stroke
NCT03772067Not specifiedUNKNOWNInfluence of Dairy Protein Breakfast on Glycemia, Weight Loss and Clock Genes in T2D
NCT04055025Not specifiedCOMPLETEDPhysiological Responses to Laparoscopic Sleeve Gastrectomy: Focusing on Ghrelin
NCT05189353Not specifiedCOMPLETEDThe Importance of Ghrelin for Glucose Metabolism After Sleeve Gastrectomy
NCT06576440Not specifiedCOMPLETEDEffects of Ghrelin Administration on Motivation

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.

168 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
ATAZANAVIRChEMBL + PubChemPhase 4 (approved)GHSR
CINACALCETChEMBL + PubChemPhase 4 (approved)GHSR
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)GHSR
DIHYDROERGOTAMINEChEMBL + PubChemPhase 4 (approved)GHSR
LINAGLIPTINChEMBL + PubChemPhase 4 (approved)GHSR
TEGASERODChEMBL + PubChemPhase 4 (approved)GHSR
AMIODARONEChEMBLPhase 4 (approved)GHSR
ARIPIPRAZOLEChEMBLPhase 4 (approved)GHSR
ASENAPINEChEMBLPhase 4 (approved)GHSR
ASTEMIZOLEChEMBLPhase 4 (approved)GHSR
ATRACURIUMChEMBLPhase 4 (approved)GHSR
AZELASTINEChEMBLPhase 4 (approved)GHSR
BAZEDOXIFENEChEMBLPhase 4 (approved)GHSR
BENFLUOREXChEMBLPhase 4 (approved)GHSR
BENPERIDOLChEMBLPhase 4 (approved)GHSR
BEPRIDILChEMBLPhase 4 (approved)GHSR
BICALUTAMIDEChEMBLPhase 4 (approved)GHSR
BOSUTINIBChEMBLPhase 4 (approved)GHSR
BROMOCRIPTINEChEMBLPhase 4 (approved)GHSR
BROMPERIDOLChEMBLPhase 4 (approved)GHSR
BUCLIZINEChEMBLPhase 4 (approved)GHSR
CARVEDILOLChEMBLPhase 4 (approved)GHSR
CHLORHEXIDINEChEMBLPhase 4 (approved)GHSR
CHLORPROMAZINEChEMBLPhase 4 (approved)GHSR
CHLORPROTHIXENEChEMBLPhase 4 (approved)GHSR
CLEMASTINEChEMBLPhase 4 (approved)GHSR
CLOFAZIMINEChEMBLPhase 4 (approved)GHSR
CLOMIPRAMINEChEMBLPhase 4 (approved)GHSR
DARIFENACINChEMBLPhase 4 (approved)GHSR
DAUNORUBICINChEMBLPhase 4 (approved)GHSR
DESERPIDINEChEMBLPhase 4 (approved)GHSR
DESIPRAMINEChEMBLPhase 4 (approved)GHSR
DIBUCAINEChEMBLPhase 4 (approved)GHSR
DICYCLOMINEChEMBLPhase 4 (approved)GHSR
DIETHYLSTILBESTROLChEMBLPhase 4 (approved)GHSR
DILTIAZEMChEMBLPhase 4 (approved)GHSR
DOMPERIDONEChEMBLPhase 4 (approved)GHSR
DULOXETINEChEMBLPhase 4 (approved)GHSR
EBASTINEChEMBLPhase 4 (approved)GHSR
FEDRATINIBChEMBLPhase 4 (approved)GHSR
FENTANYLChEMBLPhase 4 (approved)GHSR
FLUNITRAZEPAMChEMBLPhase 4 (approved)GHSR
FLURAZEPAMChEMBLPhase 4 (approved)GHSR
FLUSPIRILENEChEMBLPhase 4 (approved)GHSR
HALOPERIDOLChEMBLPhase 4 (approved)GHSR
IDARUBICINChEMBLPhase 4 (approved)GHSR
INDOCYANINE GREEN ACID FORMChEMBLPhase 4 (approved)GHSR
LANSOPRAZOLEChEMBLPhase 4 (approved)GHSR
LASOFOXIFENEChEMBLPhase 4 (approved)GHSR
LIOTHYRONINEChEMBLPhase 4 (approved)GHSR
LOFEPRAMINEChEMBLPhase 4 (approved)GHSR
MACIMORELINChEMBLPhase 4 (approved)GHSR
MECLIZINEChEMBLPhase 4 (approved)GHSR
MEFLOQUINEChEMBLPhase 4 (approved)GHSR
NAFARELINChEMBLPhase 4 (approved)GHSR
NEBIVOLOLChEMBLPhase 4 (approved)GHSR
NERATINIBChEMBLPhase 4 (approved)GHSR
NIMESULIDEChEMBLPhase 4 (approved)GHSR
NITAZOXANIDEChEMBLPhase 4 (approved)GHSR
NOSCAPINEChEMBLPhase 4 (approved)GHSR

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
v1.1.2
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