General
Preferred name
WZ4003
Synonyms
WZ 4003 ()
WZ-4003 ()
P&D ID
PD003267
CAS
1214265-58-3
Tags
available
probe
drug candidate
Drug indication
Discovery agent
Probe info
Probe type
calculated probe
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
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)
COMMENT
The compound has good kinase selectivity, but the cellular activity is not at the level I would consider useful for a bona fide probe (<1 uM). The authors have highlighted a few more potent compounds that could be used in parallel. They suffer from a worse kinome profile. This compound has excellent kinase selectivity but is only weekly active in cells. Jun 16 2016 - 5:59pm; This appears to be a highly selective NUAK1 inhibitor without significant off-target actions at 140 other tested kinases. There are no data available for potential off-target actions at other druggable targets (e.g., GPCRs, ion channels and so on). Jun 29 2016 - 7:46pm; No available PK or toxicology data; no way to judge whether or not it should be utilized in vivo. The probe is selective and has a target not well addressed by other molecules. Further work on physiochemistry, pharmacokinetics, and toxicology scouting could prove the probe useful (or disqualify for further use). Jun 30 2016 - 4:52am
DESCRIPTION
WZ4003 is the first potent and highly specific NUAK kinase inhibitor with IC50 of 20 nM/100 nM for NUAK1 (ARK5)/NUAK2, without significant inhibition on other 139 kinases.
PRICE
69
DESCRIPTION
WZ4003 is a selective inhibitor of the AMP-activated protein kinases, NUAK1 and NUAK2 .
N.B. compare to which is selective for NUAK1. HTH-01-015 and WZ4003 can be used as chemical probes to delineate the biological roles of the NUAK kinases. (GtoPdb)
N.B. compare to which is selective for NUAK1. HTH-01-015 and WZ4003 can be used as chemical probes to delineate the biological roles of the NUAK kinases. (GtoPdb)
MOA
Inhibitor
(Chemical Probes.org)
DESCRIPTION
WZ4003 is the first potent and highly specific NUAK kinase inhibitor with IC50 of 20 nM for NUAK1 (ARK5).
(Enamine Bioactive Compounds)
DESCRIPTION
WZ4003 exhibits a high, specific affinity to the L858R/T790M mutant EGFR, while a significantly reduced cellular IC50 against T790M containing Ba/F3 cells.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
WZ4003, a highly selective NUAK kinase inhibitor, is with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2, respectively. It is no significant inhibition on 139 other kinases.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Selective ubiquitin C-terminal hydrolase-L3 (UCH-L3) inhibitor
(Tocris Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
0
Compound Sets
25
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
Chemical Probes.org
Chemical proteomics reveals the target landscape of 1,000 kinase inhibitors
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
Enamine Bioactive Compounds
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
High-quality chemical probes
JUMP-MOA Compound Set
Kinase Chemogenomic Set (KCGS)
Kinase Inhibitors (best-in-class)
LINCS compound set
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tool Compound Set
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
13
Molecular Weight
496.2
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
2
Rotatable Bonds
8
Ring Count
4
Aromatic Ring Count
3
cLogP
4.77
TPSA
91.85
Fraction CSP3
0.32
Chiral centers
0.0
Largest ring
6.0
QED
0.46
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
NuaK1/2
NUAK family SNF1-like kinase 1
NUAK family SNF1-like kinase 2
AMPK
NUAK1
NUAK2
NUAK1, NUAK2
NUAK inhibitor
Kinase group
CAMK
Primary Target
NUAKs
MOA
Inhibitor
inhibitor of NUAK1 and NUAK2
AMPK inhibitor
Member status
member
Target class
Protein kinase
Kinase, Kinase
Pathway
Chromatin/Epigenetic
PI3K/Akt/mTOR signaling
Epigenetics
PI3K/Akt/mTOR
Target subclass
CAMK, CAMK
Recommended Cell Concentration
1 uM
Source data
