KISSPEPTIN-10

Summary

Kisspeptin-10 (CHEMBL376756) is a phase-3 clinical-stage protein targeting KISS1R; indicated across 6 conditions including infertility disorder and hypogonadism.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Protein
• Targets: 1 (KISS1R)
• Indications: 6 conditions
• Clinical trials: 3
• Chemistry: 1302.4 Da · C63H83N17O14

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL376756
Name	KISSPEPTIN-10
Type	Protein
Max phase	3
FDA approved	no
PubChem CID	25240297
Molecular formula	C63H83N17O14
Molecular weight	1302.4
InChIKey	RITKWYDZSSQNJI-INXYWQKQSA-N

SMILES: CC(C)C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N)NC(=O)CNC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CC3=CNC4=CC=CC=C43)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CC5=CC=C(C=C5)O)N

IUPAC name: (2S)-N-[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide

Also known as: Kisspeptin-10, Kisspeptin-10 (human), YNWNSFGLRF, kisspeptin-10, KISSPEPTIN-10, Metastin

Patent coverage: 451 distinct patent families (982 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 898 (91%) of the total. 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
KISS1R	kisspeptin receptor	Full agonist	10.4	0.2%	Q969F8

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: KiSS-1 receptor, KiSS-1 receptor, Neuropeptide FF receptor 1, Neuropeptide FF receptor 2.

Bioactivity

ChEMBL activities: 22 potent at pChembl ≥ 5 of 22 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
KISS1R	10.46	Ki	0.04	nM	CHEMBL_ACT_14997246
KISS1R	10.41	Ki	0.04	nM	CHEMBL_ACT_13825109
KISS1R	10.31	EC50	0.05	nM	CHEMBL_ACT_12059909
Q924U1	10.24	Ki	0.06	nM	CHEMBL_ACT_13825078
KISS1R	10.21	Ki	0.06	nM	CHEMBL_ACT_24397216
KISS1R	10.19	EC50	0.07	nM	CHEMBL_ACT_12064712
KISS1R	10.15	IC50	0.07	nM	CHEMBL_ACT_2383610
KISS1R	10.09	IC50	0.08	nM	CHEMBL_ACT_12059910
Q924U1	10.06	Ki	0.09	nM	CHEMBL_ACT_14997272
KISS1R	10.06	EC50	0.09	nM	CHEMBL_ACT_18955180
Q924U1	9.96	IC50	0.11	nM	CHEMBL_ACT_12059911
KISS1R	9.92	IC50	0.12	nM	CHEMBL_ACT_5208129
KISS1R	9.62	EC50	0.24	nM	CHEMBL_ACT_2383586
KISS1R	9.02	EC50	0.96	nM	CHEMBL_ACT_14997208
KISS1R	9.02	EC50	0.96	nM	CHEMBL_ACT_16754365
KISS1R	8.89	Ki	1.3	nM	CHEMBL_ACT_1816617
Q924U1	8.38	EC50	4.2	nM	CHEMBL_ACT_14997220
Q924U1	8.38	EC50	4.2	nM	CHEMBL_ACT_16754401
NPFFR1	8.33	IC50	4.7	nM	CHEMBL_ACT_5208135
KISS1R	7.76	EC50	17.3	nM	CHEMBL_ACT_1816618
NPFFR2	7.12	IC50	76	nM	CHEMBL_ACT_5208139
KISS1R	5.07	IC50	8510	nM	CHEMBL_ACT_13825019

Target pathways

Aggregated over 1 target gene(s): KISS1R.

Top Reactome pathways

7 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	1	KISS1R
Signaling by GPCR	1	KISS1R
Class A/1 (Rhodopsin-like receptors)	1	KISS1R
Peptide ligand-binding receptors	1	KISS1R
GPCR downstream signalling	1	KISS1R
G alpha (q) signalling events	1	KISS1R
GPCR ligand binding	1	KISS1R

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	1
neuropeptide signaling pathway	1
positive regulation of hormone secretion	1
signal transduction	1

Indications & clinical

Indications

6 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	3	MONDO:0005047	EFO:0000545
hypogonadism	2	MONDO:0002146	MONDO:0018555
metabolic disease	1	MONDO:0005066	EFO:0000589
reproductive system disorder	1	MONDO:0005039	EFO:0000512
polycystic ovary syndrome	1	MONDO:0008487	EFO:0000660

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
PHASE1	2
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03771326	PHASE3	COMPLETED	KP-10 and Insulin Secretion in Men
NCT04532801	PHASE1	WITHDRAWN	Evaluation of Kisspeptin Glucose-Stimulated Insulin Secretion With Physiologic Mixed Meal Tolerance
NCT05456854	PHASE1	WITHDRAWN	Evaluation of Kisspeptin Stimulated Insulin Secretion With Hyperglycemic Clamp

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.

3 molecules share ≥1 primary target. Top 3 by shared-target count:

Molecule	Source	Status	Shared targets
BENZETHONIUM CHLORIDE	ChEMBL + PubChem	Phase 2 (approved)	KISS1R
TAK-448	ChEMBL	Phase 2	KISS1R
Naloxone	PubChem	Approved	KISS1R