Assays and Biophysics

Proteros offers full biochemical and biophysical profiling of protein-ligand interactions to support your drug discovery programs. We offer more than 300 established assays that deliver data as IC50, Kd, kon, koff, residence time, ΔH, ΔS, N and Tm.  Proteros also offers customized assay development for biochemical and biophysical profiling    

Profiling Services based on Proteros´Reporter Displacement Assay (RDA)

(See also list of targets with ready established RDA (Gallery Assays)):

 

Service

Application

Deliverable

Throughput

Library screening incl. fragment screening

Primary screen
Identification of binding ligands

Probe displacement
[%]

40,000 ligands/week

Time resolved screening

Primary screen
Identification of binding ligands + parallel  clustering in slow and fast binders

Probe displacement
[%] at 2 time points

30,000 ligands/week

Affinity profiling

Hit profiling, lead optimization
Quantification of binding affinities 

Kd

1,000

ligands/week

Kinetic profiling high throughput mode

Hit profiling
Identification of compounds with desired kon and residence time within large compound selections (e.g. entire hit set after HTS campaign)

kon, koff, residence time clustering

2,500 

ligands/week

Kinetic profiling
high precision mode

Hit profiling, lead optimization
Quantification of binding affinities & kinetics

Kd, kon, koff,
residence time

200 

ligands/week

Profiling of covalent inhibitors

Hit profiling, lead optimization
-Proof of covalent bond formation
-kinact, Ki quantification

 

-covalent bond formed: yes/no
-kinact, Ki

50 

ligands/week

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

  

 Profiling Services based on additional technologies:

Service

Technology

Application

Deliverable

Enzymatic profiling

FI, FRET, HTRF, FP, Abs, Luminescence

Identification and characterization of enzyme inhibitors

IC50, inhibition [%],

enzymatic mode of action analysis

Isothermal Calorimetry Titration (ITC) 

MicroCal200™

(Malvern)

Quantification of binding thermodynamics  

Kd ΔH, ΔS, N

Thermoshift Analysis (TSA)

CFX Connect™

(BioRad)

Identification of binding ligands

Protein melting temperature (Tm)

NanoDSF*

Prometheus™

(NanoTemper Technologies)

Identification of binding ligands

Protein melting temperature (Tm)

Gene Expression Profiling

nCounter™

(NanoString Technologies)

Cellular and in vivo profiling of inhibitor efficacy  

Quantification of mRNA levels  

 * Differential scanning fluorimetry

 

 

 

Technical References:
Catalogue of available Gallery Assays
Proteros Reporter Displacement Assay
Time resolved primary screening
Kinetic profiling
Thermodynamic profiling
Profiling of Biologics
Value of residence time in drug discovery

For further scientific questions regarding

Kinetic optimization of lead compounds

and/or to request a quote please contact

 

 

 

 

 

Dr. Lars Neumann

Assays, Biophysics & Screening
+49 89 700761-0
Requests[at]proteros.com