Nafarelin

Summary

Nafarelin (CHEMBL1201309) is an approved protein (ATC H01CA02) targeting GNRHR; indicated across 3 conditions including infertility disorder and endometriosis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• ATC class: H01CA02
• Targets: 1 (GNRHR)
• Indications: 3 conditions
• Clinical trials: 3
• Chemistry: 1322.5 Da · C66H83N17O13

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1201309
Name	Nafarelin
Type	Protein
Max phase	4
FDA approved	no
PubChem CID	49800011
ATC	H01CA02
Molecular formula	C66H83N17O13
Molecular weight	1322.5
InChIKey	PPXLVGBVOZLEIW-ITQXDASVSA-N

SMILES: CC(C)C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N)NC(=O)[C@@H](CC2=CC=CC3=CC=CC=C32)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CNC6=CC=CC=C65)NC(=O)[C@H](CC7=CN=CN7)NC(=O)[C@@H]8CCC(=O)N8

IUPAC name: (2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[(2-amino-2-oxoethyl)carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-naphthalen-1-yl-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide

Also known as: Lhrh, 6(d-nal(2)), Nafarelin, Nafarelina, Nafareline, NAFARELIN, nafarelin

Parent form; salt/anhydrous children: CHEMBL1200671

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
GNRHR	GnRH1 receptor	Full agonist		0.1%	P30968

Broader ChEMBL bioactivity targets: 8 (assay-derived). Sample: Motilin receptor, D(3) dopamine receptor, Kappa-type opioid receptor, Melanocortin receptor 4, 3’,5’-cyclic-AMP phosphodiesterase 4D, Nuclear receptor subfamily 1 group I member 2, Growth hormone secretagogue receptor type 1, Melanocortin receptor 3.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 8 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
MC4R	5.76	AC50	1750	nM	CHEMBL_ACT_25184447
MC3R	5.56	AC50	2730	nM	CHEMBL_ACT_25183453
GHSR	5.41	AC50	3910	nM	CHEMBL_ACT_25172808
MLNR	5.21	AC50	6190	nM	CHEMBL_ACT_25189240
NR1I2	5.04	AC50	9060	nM	CHEMBL_ACT_25188213

Target pathways

Aggregated over 1 target gene(s): GNRHR.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
Hormone ligand-binding receptors	1	GNRHR
G alpha (q) signalling events	1	GNRHR

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	1
gonadotropin secretion	1
cellular response to hormone stimulus	1
signal transduction	1
cellular response to gonadotropin-releasing hormone	1

Indications & clinical

Indications

3 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
infertility disorder	2	MONDO:0005047	EFO:0000545
endometriosis	1	MONDO:0005133	EFO:0001065

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

Clinical trials

Total trials: 3.

Phase distribution

Phase	Trials
PHASE4	2
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06763926	PHASE4	NOT_YET_RECRUITING	Intranasal Nafarelin For Triggering Oocyte Maturation
NCT00843570	PHASE4	COMPLETED	Natural Versus HRT Cycles in Frozen Embryo Replacement Treatment
NCT00034047	PHASE1/PHASE2	COMPLETED	Endometriosis : Traditional Medicine vs Hormone Therapy

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

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.

14 molecules share ≥1 primary target. Top 14 by shared-target count:

Molecule	Source	Status	Shared targets
CETRORELIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
DEGARELIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
ELAGOLIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
GANIRELIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
RELUGOLIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
ABARELIX	ChEMBL	Phase 4 (approved)	GNRHR
GONADORELIN	ChEMBL	Phase 4 (approved)	GNRHR
LEUPROLIDE	ChEMBL	Phase 4 (approved)	GNRHR
LINZAGOLIX	ChEMBL	Phase 4 (approved)	GNRHR
ACYLINE	ChEMBL	Phase 2	GNRHR
SUFUGOLIX	ChEMBL	Phase 2	GNRHR
Belzutifan	PubChem	Approved	GNRHR
Deslorelin	PubChem	Approved	GNRHR
Triptorelin	PubChem	Approved	GNRHR