Seralutinib

Summary

Seralutinib (CHEMBL4650333) is a phase-3 clinical-stage small molecule targeting PDGFRA and PDGFRB; indicated across 2 conditions including pulmonary arterial hypertension and pulmonary hypertension.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 2 (PDGFRA, PDGFRB)
• Indications: 2 conditions
• Clinical trials: 7
• Chemistry: 469.5 Da · C27H27N5O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4650333
Name	Seralutinib
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	91663352
Molecular formula	C27H27N5O3
Molecular weight	469.5
InChIKey	JHJNPOSPVGRIAN-SFHVURJKSA-N

SMILES: CC1=CC(=CN=C1)C(=O)NC2=CC=CC(=C2)[C@H](C)NC3=NC(=CN=C3)C4=CC(=C(C=C4)OC)OC

IUPAC name: N-[3-[(1S)-1-[[6-(3,4-dimethoxyphenyl)pyrazin-2-yl]amino]ethyl]phenyl]-5-methylpyridine-3-carboxamide

Also known as: GB-002, Gb002, GB002, PK-10571, Seralutinib, SERALUTINIB

Patent coverage: 42 distinct patent families (100 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 67 (67%) 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
PDGFRA	platelet derived growth factor receptor alpha	Inhibition		6.2%	P16234
PDGFRB	platelet derived growth factor receptor beta	Inhibition		2.3%	P09619

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 2 target gene(s): PDGFRA, PDGFRB.

Top Reactome pathways

13 total, by targets touching each:

Pathway	Targets	Genes
PIP3 activates AKT signaling	2	PDGFRA, PDGFRB
Downstream signal transduction	2	PDGFRA, PDGFRB
Signaling by PDGF	2	PDGFRA, PDGFRB
Constitutive Signaling by Aberrant PI3K in Cancer	2	PDGFRA, PDGFRB
RAF/MAP kinase cascade	2	PDGFRA, PDGFRB
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	2	PDGFRA, PDGFRB
Signaling by PDGFRA transmembrane, juxtamembrane and kinase domain mutants	1	PDGFRA
Signaling by PDGFRA extracellular domain mutants	1	PDGFRA
Imatinib-resistant PDGFR mutants	1	PDGFRA
Sunitinib-resistant PDGFR mutants	1	PDGFRA
Regorafenib-resistant PDGFR mutants	1	PDGFRA
Sorafenib-resistant PDGFR mutants	1	PDGFRA
PDGFR mutants bind TKIs	1	PDGFRA

Dominant GO biological processes

GO term	Targets
cell surface receptor protein tyrosine kinase signaling pathway	2
positive regulation of cell population proliferation	2
cell migration	2
peptidyl-tyrosine phosphorylation	2
positive regulation of cell migration	2
regulation of actin cytoskeleton organization	2
positive regulation of cell proliferation by VEGF-activated platelet derived growth factor receptor signaling pathway	2
protein autophosphorylation	2
platelet-derived growth factor receptor signaling pathway	2
positive regulation of calcium-mediated signaling	2
positive regulation of chemotaxis	2
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	2
cardiac myofibril assembly	2
cell chemotaxis	2
retina vasculature development in camera-type eye	2

Indications & clinical

Indications

2 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
pulmonary arterial hypertension	3	MONDO:0015924	EFO:0001361
pulmonary hypertension	3	MONDO:0005149	MONDO:0005149

Clinical trials

Total trials: 7.

Phase distribution

Phase	Trials
PHASE3	3
PHASE2	2
PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06274801	PHASE3	ACTIVE_NOT_RECRUITING	Open-label Extension Study of Seralutinib in Adult Subjects With PAH (PROSERA-EXT)
NCT05934526	PHASE3	COMPLETED	Efficacy and Safety of Seralutinib in Adult Subjects With PAH (PROSERA)
NCT07181382	PHASE3	SUSPENDED	Efficacy and Safety of Seralutinib in Adult Subjects With Pulmonary Hypertension Associated With Interstitial Lung Disease (PH-ILD)
NCT04816604	PHASE2	ACTIVE_NOT_RECRUITING	Open-label Extension Study of GB002 in Adult Subjects With Pulmonary Arterial Hypertension (PAH)
NCT04456998	PHASE2	COMPLETED	GB002 in Adult Subjects With Pulmonary Arterial Hypertension (PAH)
NCT03473236	PHASE1	COMPLETED	Phase 1A Safety Trial of Inhaled PK10571 (GB002)
NCT03926793	PHASE1	COMPLETED	Clinical Study of Inhaled GB002 for Treatment of WHO Group I Pulmonary Arterial Hypertension

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.

106 molecules share ≥1 primary target. Top 100 by shared-target count:

Molecule	Source	Status	Shared targets
PAZOPANIB	ChEMBL + PubChem	Phase 4 (approved)	PDGFRA, PDGFRB
REGORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	PDGFRA, PDGFRB
AXITINIB	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
BOSUTINIB	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
DASATINIB	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
ERLOTINIB	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
FEDRATINIB	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
IMATINIB	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
LENVATINIB	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
MIDOSTAURIN	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
NILOTINIB	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
NINTEDANIB	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
NINTEDANIB ESYLATE	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
PEXIDARTINIB	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
PONATINIB	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
QUIZARTINIB	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
SORAFENIB	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
SUNITINIB	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
TIVOZANIB	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
VANDETANIB	ChEMBL	Phase 4 (approved)	PDGFRA, PDGFRB
BARASERTIB	ChEMBL	Phase 3	PDGFRA, PDGFRB
BRIVANIB	ChEMBL	Phase 3	PDGFRA, PDGFRB
CANERTINIB	ChEMBL	Phase 3	PDGFRA, PDGFRB
CEDIRANIB	ChEMBL	Phase 3	PDGFRA, PDGFRB
CRENOLANIB	ChEMBL	Phase 3	PDGFRA, PDGFRB
DOVITINIB	ChEMBL	Phase 3	PDGFRA, PDGFRB
LESTAURTINIB	ChEMBL	Phase 3	PDGFRA, PDGFRB
LINIFANIB	ChEMBL	Phase 3	PDGFRA, PDGFRB
MASITINIB	ChEMBL	Phase 3	PDGFRA, PDGFRB
MOTESANIB	ChEMBL	Phase 3	PDGFRA, PDGFRB
SARACATINIB	ChEMBL	Phase 3	PDGFRA, PDGFRB
SEMAXANIB	ChEMBL	Phase 3	PDGFRA, PDGFRB
VATALANIB	ChEMBL	Phase 3	PDGFRA, PDGFRB
VIMSELTINIB	ChEMBL	Phase 3	PDGFRA, PDGFRB
CENISERTIB	ChEMBL	Phase 2	PDGFRA, PDGFRB
DEFOSBARASERTIB	ChEMBL	Phase 2	PDGFRA, PDGFRB
DORAMAPIMOD	ChEMBL	Phase 2	PDGFRA, PDGFRB
FORETINIB	ChEMBL	Phase 2	PDGFRA, PDGFRB
ILORASERTIB	ChEMBL	Phase 2	PDGFRA, PDGFRB
NEFLAMAPIMOD	ChEMBL	Phase 2	PDGFRA, PDGFRB
OSI-632	ChEMBL	Phase 2	PDGFRA, PDGFRB
R-406	ChEMBL	Phase 2	PDGFRA, PDGFRB
RAF-265	ChEMBL	Phase 2	PDGFRA, PDGFRB
SOTULETINIB	ChEMBL	Phase 2	PDGFRA, PDGFRB
SU-014813	ChEMBL	Phase 2	PDGFRA, PDGFRB
TANDUTINIB	ChEMBL	Phase 2	PDGFRA, PDGFRB
TOZASERTIB	ChEMBL	Phase 2	PDGFRA, PDGFRB
Afatinib	PubChem	Approved	PDGFRA, PDGFRB
Crizotinib	PubChem	Approved	PDGFRA, PDGFRB
Idelalisib	PubChem	Approved	PDGFRA, PDGFRB
Selumetinib	PubChem	Approved	PDGFRA, PDGFRB
AVAPRITINIB	ChEMBL + PubChem	Phase 4 (approved)	PDGFRA
CERITINIB	ChEMBL	Phase 4 (approved)	PDGFRA
GILTERITINIB	ChEMBL	Phase 4 (approved)	PDGFRB
INFIGRATINIB	ChEMBL	Phase 4 (approved)	PDGFRA
LAPATINIB	ChEMBL	Phase 4 (approved)	PDGFRB
PACRITINIB	ChEMBL	Phase 4 (approved)	PDGFRB
RIPRETINIB	ChEMBL	Phase 4 (approved)	PDGFRA
SUNITINIB MALATE	ChEMBL	Phase 4 (approved)	PDGFRB
TOVORAFENIB	ChEMBL	Phase 4 (approved)	PDGFRB
ALVOCIDIB	ChEMBL	Phase 3	PDGFRA
BRIVANIB ALANINATE	ChEMBL	Phase 3	PDGFRB
CATEQUENTINIB	ChEMBL	Phase 3	PDGFRB
ENZASTAURIN	ChEMBL	Phase 3	PDGFRB
FAMITINIB	ChEMBL	Phase 3	PDGFRB
FLUMATINIB	ChEMBL	Phase 3	PDGFRB
IBCASERTIB	ChEMBL	Phase 3	PDGFRA
NAPORAFENIB	ChEMBL	Phase 3	PDGFRB
OLVEREMBATINIB	ChEMBL	Phase 3	PDGFRA
ORANTINIB	ChEMBL	Phase 3	PDGFRB
PIMICOTINIB	ChEMBL	Phase 3	PDGFRA
RETASPIMYCIN	ChEMBL	Phase 3	PDGFRA
RUBOXISTAURIN	ChEMBL	Phase 3	PDGFRB
AEE-788	ChEMBL	Phase 2	PDGFRB
AMUVATINIB	ChEMBL	Phase 2	PDGFRA
AT-9283	ChEMBL	Phase 2	PDGFRA
BAFETINIB	ChEMBL	Phase 2	PDGFRB
BEMCENTINIB	ChEMBL	Phase 2	PDGFRA
BFH-772	ChEMBL	Phase 2	PDGFRB
BMS-777607	ChEMBL	Phase 2	PDGFRA
CEP-11981	ChEMBL	Phase 2	PDGFRA
CEP-32496	ChEMBL	Phase 2	PDGFRB
CI-1040	ChEMBL	Phase 2	PDGFRB
ELLAGIC ACID	ChEMBL	Phase 2	PDGFRB
ELLIPTINIUM	ChEMBL	Phase 2	PDGFRA
ENMD-2076	ChEMBL	Phase 2	PDGFRA
GLESATINIB	ChEMBL	Phase 2	PDGFRB
GOLVATINIB	ChEMBL	Phase 2	PDGFRB
LUCITANIB	ChEMBL	Phase 2	PDGFRB
MILCICLIB	ChEMBL	Phase 2	PDGFRB
MIVAVOTINIB	ChEMBL	Phase 2	PDGFRA
MK-2461	ChEMBL	Phase 2	PDGFRB
NARAZACICLIB	ChEMBL	Phase 2	PDGFRB
RAVOXERTINIB	ChEMBL	Phase 2	PDGFRB
REBASTINIB	ChEMBL	Phase 2	PDGFRA
SOTRASTAURIN	ChEMBL	Phase 2	PDGFRB
TELATINIB	ChEMBL	Phase 2	PDGFRB
TG100-801	ChEMBL	Phase 2	PDGFRB
TOCERANIB	ChEMBL	Phase 2	PDGFRB
UCN-01	ChEMBL	Phase 2	PDGFRB