General
Preferred name
LY 364947
Synonyms
HTS466284 ()
LY364947 ()
LY-364947 ()
HTS-466284 ()
HTS 466284 ()
GW271431X ()
4-(3-Pyridin-2-Yl-1h-Pyrazol-4-Yl)Quinoline ()
TGF-beta RI kinase inhibitor ()
P&D ID
PD006641
CAS
396129-53-6
Tags
available
drug candidate
Drug indication
Discovery agent
Drug Status
experimental
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
Selective inhibitor of TGF-βRI
(GtoPdb)
DESCRIPTION
LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGF¦ÂR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGF¦ÂR-II[1].
PRICE
60
DESCRIPTION
LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGF??R-I.
DESCRIPTION
Selective PDE4 inhibitor
(Tocris Bioactive Compound Library)
DESCRIPTION
Selective inhibitor of TGF-betaRI
(Tocriscreen Plus)
DESCRIPTION
Selective inhibitor of TGF-βRI
(Tocriscreen Total)
DESCRIPTION
LY364947 is a selective inhibitor of TGF-β type-I receptor with potential anticancer activity. LY364947 inhibits TGF-β-dependent luciferase production in mink lung cells (p3TP lux) and growth in mouse fibroblasts (NIH 3T3).
(BOC Sciences Bioactive Compounds)
DESCRIPTION
LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
2
Organisms
0
Compound Sets
18
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
Chemical proteomics reveals the target landscape of 1,000 kinase inhibitors
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
Tocriscreen Total
ZINC Tool Compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
33
Molecular Weight
272.11
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
1
Rotatable Bonds
2
Ring Count
4
Aromatic Ring Count
4
cLogP
3.69
TPSA
54.46
Fraction CSP3
0.0
Chiral centers
0.0
Largest ring
6.0
QED
0.61
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Enzyme-Linked Receptors
Pathway
Apoptosis
MAPK
Metabolism
NF-κB
Stem Cells
TGF-beta/Smad
Primary Target
TGF-? Receptors
MOA
Inhibitor
Inhibitors of Signal Transduction Pathways
Activin Receptor Like Kinase 5 (ALK5
TbetaR-I) Inhibitors
p38 MAPK Inhibitors
p38 MAPK inhibitor, TGF beta receptor inhibitor
Member status
member
Target
TGFBR1
ALK5 inhibitor
TGF-β Receptor
Casein Kinase,Mixed Lineage Kinase,RIP kinase,TGF-beta/Smad
TGF-¦Â Receptor
CK1δ
MLK-7K
RIPK2
TGFβRI
TGFβRII
Source data
