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Compound Selectivity Profiling

 
 
☉ Comprehensive Enzyme Screening Panels
More than 700 Kinase Targets
⇨ 250 Kinase Mutants
⇨ 95% Lipid Kinase Coverage
More Than 75 Epigenetics Targets
   PDEs, Phosphatases and Growing

☉ Biochemical, Radiometric and Cell Based Assays
 
  Screening Highlights

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.

 
 
Figure 1: Compound Selectivity Profiling Against 48 Targets available as part of
SignalChem's Compound Profiling Service.
Figure 2: The IC50 value of a compound was determined by plotting the log of the
concentration of the compound vs. the % inhibition of the kinase.
 
 
  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   |   Kinases   |   Phosphatases   |   Kinase Mutants   |   Acetyltransferases   |   Methyltransferases   |   Histone Deacetylases   |   GTPases & ATPases   |   Lipid Kinases

 

Restrictions

JAK2*: Patent restrictions on this product exclude it as a profiling target for US customers.

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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