Selatogrel

Summary

Selatogrel (CHEMBL4297589) is a phase-3 clinical-stage small molecule targeting P2RY12; indicated across 3 conditions including acute myocardial infarction and coronary artery disorder.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (P2RY12)
• Indications: 3 conditions
• Clinical trials: 10
• Chemistry: 618.6 Da · C28H39N6O8P

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4297589
Name	Selatogrel
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	59534142
Molecular formula	C28H39N6O8P
Molecular weight	618.6
InChIKey	FYXHWMQPCJOJCH-GMAHTHKFSA-N

SMILES: CCCCOC(=O)N1CCN(CC1)C(=O)[C@H](CP(=O)(O)O)NC(=O)C2=CC(=NC(=N2)C3=CC=CC=C3)N4CC[C@@H](C4)OC

IUPAC name: [(2R)-3-(4-butoxycarbonylpiperazin-1-yl)-2-[[6-[(3S)-3-methoxypyrrolidin-1-yl]-2-phenylpyrimidine-4-carbonyl]amino]-3-oxopropyl]phosphonic acid

Also known as: Act-246475, ACT-246475, Selatogrel, SELATOGREL

Patent coverage: 15 distinct patent families (53 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 43 (81%) 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
P2RY12	P2Y12 receptor	Antagonist	8.7	0.5%	Q9H244

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: P2Y purinoceptor 12.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
P2RY12	8.82	Kd	1.5	nM	CHEMBL_ACT_29187859

Target pathways

Aggregated over 1 target gene(s): P2RY12.

Top Reactome pathways

3 total, by targets touching each:

Pathway	Targets	Genes
ADP signalling through P2Y purinoceptor 12	1	P2RY12
P2Y receptors	1	P2RY12
G alpha (i) signalling events	1	P2RY12

Dominant GO biological processes

GO term	Targets
monoatomic ion transport	1
substrate-dependent cell migration, cell extension	1
G protein-coupled receptor signaling pathway	1
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	1
phospholipase C-activating G protein-coupled receptor signaling pathway	1
hemostasis	1
calcium-mediated signaling	1
cerebral cortex radial glia-guided migration	1
cell projection organization	1
lamellipodium assembly	1
platelet activation	1
positive regulation of integrin activation by cell surface receptor linked signal transduction	1
positive regulation of cell adhesion mediated by integrin	1
positive regulation of monoatomic ion transport	1
response to axon injury	1

Indications & clinical

Indications

3 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)	Phase	MONDO	EFO
acute myocardial infarction	3	MONDO:0004781	EFO:0008583
coronary artery disorder	2	MONDO:0005010	EFO:0001645
liver disorder	1	MONDO:0005154	EFO:0001421

Clinical trials

Total trials: 10.

Phase distribution

Phase	Trials
PHASE1	7
PHASE2	2
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04957719	PHASE3	ENROLLING_BY_INVITATION	Selatogrel Outcome Study in Suspected Acute Myocardial Infarction
NCT03384966	PHASE2	COMPLETED	A Medical Research Study to Evaluate the Effects of ACT-246475 in Adults With Coronary Artery Disease
NCT03487445	PHASE2	COMPLETED	A Medical Research Study to Evaluate the Effects of ACT-246475 in Adults With Heart Attack
NCT07615868	PHASE1	NOT_YET_RECRUITING	A Trial to Compare What the Body Does to Selatogrel and the Effect of Selatogrel in Chinese Adults With Chronic Coronary Syndrome
NCT03430661	PHASE1	COMPLETED	A Study to Investigate the Interaction Between ACT-246475 and Clopidogrel, Prasugrel, and Ticagrelor in Healthy Subjects
NCT03593278	PHASE1	COMPLETED	A Study to Evaluate ACT-246475 Fate in Healthy Male Subjects
NCT03814200	PHASE1	COMPLETED	A Study to Investigate the Effect of Rifampicin on the Uptake and Breakdown of ACT-246475 in Healthy Subjects
NCT04406896	PHASE1	COMPLETED	The Effect of Reduced Liver Function on Selatogrel Pharmacokinetics
NCT04557280	PHASE1	COMPLETED	A Comparative Study of Selatogrel (ACT-246475) Formulations in Healthy Subjects
NCT07133191	PHASE1	COMPLETED	A Trial to Compare What the Body Does to Selatogrel and the Effect of Selatogrel in Japanese and Caucasian Healthy Participants

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.

13 molecules share ≥1 primary target. Top 13 by shared-target count:

Molecule	Source	Status	Shared targets
ANAGRELIDE	ChEMBL + PubChem	Phase 4 (approved)	P2RY12
CANGRELOR	ChEMBL	Phase 4 (approved)	P2RY12
CANGRELOR TETRASODIUM	ChEMBL	Phase 4 (approved)	P2RY12
CLOPIDOGREL	ChEMBL	Phase 4 (approved)	P2RY12
PRASUGREL	ChEMBL	Phase 4 (approved)	P2RY12
TICAGRELOR	ChEMBL	Phase 4 (approved)	P2RY12
ELINOGREL	ChEMBL	Phase 2	P2RY12
LIXAZINONE	ChEMBL	Phase 2	P2RY12
REGRELOR	ChEMBL	Phase 2	P2RY12
REGRELOR DISODIUM	ChEMBL	Phase 2	P2RY12
Aspirin	PubChem	Approved	P2RY12
Doxorubicin	PubChem	Approved	P2RY12
Mitoxantrone	PubChem	Approved	P2RY12