General
Preferred name
GALUNISERTIB
Synonyms
LY-2157299 ()
LY2157299 ()
LY 2157299 ()
Galunisertib (LY2157299) ()
P&D ID
PD003327
CAS
700874-72-2
Tags
available
drug candidate
Drug indication
Myelodysplastic syndrome
Hepatocellular carcinoma
Solid tumour/cancer
Non-small-cell lung cancer
Pancreatic cancer
Glioma
Arteriosclerosis
Drug Status
investigational
Max Phase
2.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Galunisertib is an investigational inhibitor of the receptor tyrosine kinase, TGFβR.
DESCRIPTION
Galunisertib is a first-in-class investigational inhibitor of the receptor tyrosine kinase, growth factor-β receptor type I (TGFβRI) . It is being evaluated as a novel anticancer agent.
(GtoPdb)
DESCRIPTION
Galunisertib (LY2157299) is an oral and selective TGF-¦Â receptor type I (TGF-¦ÂRI) kinase inhibitor with an IC50 of 56 nM.
PRICE
44
DESCRIPTION
Galunisertib (LY2157299) is a TGF-?? receptor type I (TGF-??RI) inhibitor (IC50=56 nM) that is selective. Galunisertib has antitumor activity and can be used in combination with PD-1 inhibitors.
DESCRIPTION
inhibitor of the transforming growth factor beta type 1 receptor
(Informer Set)
DESCRIPTION
Highly potent EGFR and ErbB2 inhibitor; inhibts wild type and mutated receptors
(Tocris Bioactive Compound Library)
DESCRIPTION
Galunisertib (LY2157299) is a TGF-β receptor type I (TGF-βRI) inhibitor (IC50=56 nM) that is selective. Galunisertib has antitumor activity and can be used in combination with PD-1 inhibitors.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
22
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
ChEMBL Drugs
Clinical kinase drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
Informer Set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
32
Molecular Weight
369.16
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
3
Ring Count
5
Aromatic Ring Count
4
cLogP
3.51
TPSA
86.69
Fraction CSP3
0.18
Chiral centers
0.0
Largest ring
6.0
QED
0.6
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
TGFBR1
TGF-¦Â Receptor
TGF-??Receptor
TGF-ßR2 inhibitor
TGF-β Receptor
TβRI
Compound status
probe
Pathway
Stem Cells
Primary Target
TGF-? Receptors
MOA
TGF-beta/Smad
Inhibitor
Inhibitors of Signal Transduction Pathways
Activin Receptor Like Kinase 5 (ALK5
TbetaR-I) Inhibitors
TGF beta receptor inhibitor
Member status
member
Recommended Cell Concentration
None
Source data
