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Compound Selectivity Profiling
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Compound Selectivity Profiling

Key Features and Benefits

High Signal-to-Noise = Greater Confidence in Your Results

Assays Performed In Triplicate = Statistically Relevant Results

2-week Turnaround Time = Efficiency in the Discovery Process


Screening Highlights

SignalChem’s compound selectivity profiling service utilizes a large and diverse panel of highly active protein kinase and phosphatase targets that are produced internally. SignalChem’s active targets are subjected to rigorous quality control analyses and are extensively assayed against a panel of biologically relevant substrates ensuring that all reactions are performed under optimal assay conditions.


SignalChem’s compound selectivity profiling service determines the respective inhibitory profile and the putative mechanism of action. All compounds are profiled against a panel of targets either using an individual dose, a single concentration or at multiple concentrations in order to allow in-depth IC50 determinations. In addition, the protein kinase assays can be performed under varying ATP concentrations to evaluate the competitive effects of ATP.

The compound selectivity profiling service offered by SignalChem is a very economical and convenient approach to the drug discovery continuum with a two-week turnaround of your specific profiling results. Compounds can be supplied by the client as DMSO stocks of known concentration, as solid material in vials, or in 96-well plates.


SignalChem Targets

SignalChem produces a diverse and ever-expanding range of targets that are actively being pursued from a drug development perspective, with a main focus on signaling proteins including active protein kinases and phosphatases.

SignalChem’s highly purified active enzymes are generated from the full-length human genes and are mutation free. These targets do not harbor any activating mutations, as it is well established that these mutations do not occur in vivo in the disease state.

 
Target Categories:     All   |  Active Kinases  |  Active Phosphatases  |  Active Phosphodiesterases  |  Cellular Proteins  |  Active Histone Deacetylases

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ABL1   ABL1
ABL2   ACK
AKT1   AKT2
AKT2   AKT3
ALK1   ALK2
ALK4   AMPK (A1/B1/G1)
AMPK (A1/B1/G2)   AMPK (A1/B1/G3)
AMPK (A1/B2/G1)   AMPK (A2/B1/G1)
AMPK (A2/B2/G2)   AMPK(A2B2G1)
AMPK(A2B2G3)   ASK1
AURORA A   AURORA A
AURORA B   AURORA C
AXL   BLK
BMX   BRAF
BRAF (V599E)   BRK
BTK   c-KIT
c-KIT(V654A)   c-MER
CAMK1   CAMK1β
CAMK1δ   CAMK1γ
CAMK1γ   CAMK2α
CAMK2β   CAMK2δ
CAMK2γ   CAMK4
CAMKK1   CAMKK2
CDC25B   CDC25C
CDK1/CyclinA1   CDK1/CyclinA2
CDK1/CyclinB1   CDK2/CyclinA1
CDK2/CyclinA2   CDK2/CyclinE1
CDK3/CyclinE1   CDK4/CyclinD1
CDK4/CyclinD3   CDK5/p25
CDK5/p29   CDK5/p35
CDK6/CyclinD1   CDK6/CyclinD3
CDK7/CyclinH/MNAT1   CDK8/CyclinC
CDK9/CyclinK   CHK1
CHK1   CHK2
CK2α1   CK2α2
CLK1   CLK2
CLK3   COT
CSK   CSK
DAPK1   DAPK2
DAPK3   DCAMKL2
DDR1     DDR2
DMPK   DUSP22 (MKPX)
DYRK1α   DYRK3
EEF2K   EGFR
EIF2AK2   EIF2AK3
EPHA1   EPHA2
EPHA3   EPHA4
EPHA6   EPHB1
EPHB2   EPHB3
EPHB4   ERK1
ERK2   FAK
FER   FES
FGFR1 (FLT2)   FGFR1 (V561M)
FGFR2   FGFR3
FGFR4   FGR
FLT1   FLT3
FMS   FRK
FYN A   GCK
GRK2   GRK5
GRK6   GRK7
GSK3α   GSK3β
HCK   HDAC1  
HDAC10     HDAC11  
HDAC2     HDAC3  
HDAC5     HDAC7  
HDAC8     HDAC9  
HER2   HER4
HIPK1   HIPK3
HIPK4   IGF1R
InsR   IRAK2
IRAK4   IRR
ITK   JAK3
JNK1   JNK2
JNK3   KDR
KHS1   LCK
LIMK1   LKB1/MO25a/STRADa
LOK   LRRK2
LYN A   LYN B
MAPKAPK2   MAPKAPK2
MAPKAPK3   MAPKAPK5
MARK1   MARK2
MARK3   MARK4
MEK1   MEK1 (EE)
MEK2   MEK2
MEKK2   MEKK3
MET   MET
MINK1   MLCK
MLK3   MNK1
MNK2   MRCKα
MRCKβ   MSK1
MSSK1   MST1
MST3   MST4
MUSK   MYLK2
MYLK3   MYO3β
MYT1   NDR
NEK11   NEK2
NEK3   NEK6
NEK7   NEK9
NUAK2   p38α
p38β   p38δ
p38γ   p70S6K
p70S6Kb   PAK1/CDC42
PAK2   PAK3
PAK4   PAK6
PAK7   PASK
PDE10A   PDE11A
PDE1A   PDE1B  
PDE1C   PDE2A
PDE3A   PDE3B
PDE4A   PDE4B
PDE4C   PDE4D
PDE5A   PDE6A  
PDE6B   PDE7A
PDE7B     PDE8A
PDE9A   PDGFRα
PDGFRα   PDGFRβ
PDK1   PHKG2
PI3K (p110α(E545K)/p85α)   PI3K (p110α/p65α)
PI3K (p110β/p85α)   PI3K (p110α/p85α)
PI3K (p110δ/p85α)   PI3K (p120γ)
PI3K (Vps34/Vps15)   PIM1
PIM2   PKAcα
PKAcβ   PKAcγ
PKCα   PKCα
PKCβ I   PKCβ II
PKCδ   PKCε
PKCη   PKCγ
PKCι   PKCμ
PKCν   PKCθ
PKCζ   PKD2
PKN1   PKN2/PRK2
PLK1   PLK2
PLK4   PRKG1
PRKG2   PRKX
PTPN1 (PTP1B)   PTPN11 (SHP2)
PTPN12 (PTP-PEST)   PTPN13 (FAP-1)
PTPN2 (TC-PTP)   PTPN6 (SHP1)
PTPN7 (LC-PTP)   PTPRA (LRP)
PTPRC (CD45)   PTPRF (LAR)
PTPRS (PTPσ)   PYK2
QIK   RAF1
RAF1(EE)   RET
RIPK2   RIPK5
ROCK1   ROCK2
RON   ROR2
ROS1   RSK1
RSK2   RSK3
RSK4   SGK1
SGK2   SGK3
SIK   SIRT1  
SIRT2     SIRT3  
SIRT5     SIRT7  
SLK   SOK1
SPHK1   SPHK2
SRC   SRC
SRPK1   SRPK2
STK3   STK33
SYK   TAK1-TAB1
TAOK1   TAOK2
TAOK3   TBK1
TEC   TESK1
TGFβR2   TIE 2
TLK2   TOPK
TRKA   TRKB
TRKC   TSSK1
TSSK2   TTK
TXK   TYK2
TYRO3   ULK1
ULK2   ULK3  
WEE1   Yes1
ZAK   ZAP70
 


Background

The selectivity profile of any small molecule is of fundamental clinical importance as part of the drug development process. The information yielded from these studies will undoubtedly provide useful insight into the proposed mechanism of action of a given compound as well as leading to the identification of “off” target effects, thus leading to the selection of better lead candidates.

Confidentiality

SignalChem maintains all information under the strictest confidentiality. All information and or materials supplied by the customer will be used as directed by the client. Upon completion of the project, all materials will be either returned to the client or disposed of accordingly. SignalChem is willing to execute confidentiality agreements with its clients.


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Select from over 340 Active Kinases, Active Phosphatases & Active Phosphodiesterases in Screen. Majority of targets are full-length, free of activating mutations and are of human origin.
     

    Popular Products  
By Item:
AKT1, Active
AKT3, Active
PI3K (p110α/p85α), Active
p53 Protein
SMAD3 Protein
AKT2, Active
GSK3β, Active
AMPK (A1/B1/G1), Active
Akt(PKB) Substrate
SMAD2 Protein
By Category:
NfkB Pathway
Apoptosis/Autophagy
p38 Pathway
Phosphodiesterases
JAK/STAT Pathway
Cellular Stress
JNK/SAPK Pathway
PKA/PKC Pathway
Phosphatases
ERK/MAPK Pathway
     


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[phone]: 1-604-232-4600
[fax]: 1-604-232-4601

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