General
Preferred name
WNT-974
Synonyms
LGK 974 ()
LGK-974 ()
NVP-LGK974 ()
WNT974 ()
LGK974 ()
NVP-LGK974, WNT974 ()
Wnt974 ()
P&D ID
PD010599
CAS
1243244-14-5
243244-14-5
Tags
available
drug candidate
Drug indication
Squamous cell carcinoma
Solid tumour/cancer
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
LGK974 is a clinical stage porcupine inhibitor . It is being developed as an oncology therapeutic . It is the first porcupine inhibitor to advance to clinical trial.
(GtoPdb)
DESCRIPTION
LGK974 (WNT974) is an orally bioavailable and specific Porcupine (PORCN) inhibitor with an IC50 of 0.1 nM[1].
PRICE
138
DESCRIPTION
LGK974 is a selective and orally bioavailable Porcupine inhibitor under development for the treatment of cancers that are driven by the Wnt pathway in a Wnt ligand-dependent manner. LGK974 was shown to induce tumor regression in a Wnt-driven murine tumor model.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
LGK974 (NVP-LGK974) is an effective and selective PORCN inhibitor and inhibits Wnt signaling (IC50: 0.4 nM) in TM3 cells. It has been used in trials studying the treatment of Metastatic Colorectal Cancer and Squamous Cell Carcinoma, Head And Neck.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
1
Compound Sets
17
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
JUMP-Target 1 Compound Set
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
28
Molecular Weight
396.17
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
1
Rotatable Bonds
5
Ring Count
4
Aromatic Ring Count
4
cLogP
3.79
TPSA
93.55
Fraction CSP3
0.13
Chiral centers
0.0
Largest ring
6.0
QED
0.55
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
PORCN
Porcupine
Member status
virtual
MOA
Porcupine Antagonist
Porcupine inhibitor
Pathway
Stem Cells
Stem Cell/Wnt
Source data
