Gallery Assays

Please click on target for specifications

GPCRs

5HT1B Receptor

Proteinkinases

ABL1 (wt)ABL1 (G250E)ABL1 (Y253F)ABL1 (E255K)ACK1 (TNK2)ALK ALK5B-RafB-Raf (V600E)BTKc-Kitc-Metc-RAF (RAF1),
CDK2/CycACDK7/CycH/MAT1CDK8/CycCCDK9/CycTCDK19/CycCCLK1CSF1-R (FMS), DDR1DDR2EGFR (wt)EGFR (L858R),
EGFR (T790M L858R)EGFR (T790M)EPHA1EPHA2EPHB4ERK2 inact. (MAPK2)ERK5 (MAPK7)FAK1 (PTK2)FGFR1FGFR2FGFR3,
FGFR4FLT3FLT3 ITDFLT3 (D835Y)GRK1GRK5GRK6GRK7GSK3-αGSK3-βHPK1IGF1RIKKepsilonINSR IRAK1IRAK4ITK,
JAK1 (kinase domain)JAK1 (pseudo domain)JAK2 (kinase domain)JAK3 (kinase domain)JNK1 (MAPK8)JNK2 (MAPK9)LCKLRRK2,
LYN MAP3K1 (MEKK1)MAPK11 (p38b)MAPK14 active (p38a), MAPK14 inact. (p38a)MEK1 (MAP2K1) inact., MEK1 (MAP2K1) active, MERTKNEW, MLCK, MLCK2, MNK1MST-1, mTORNEW, mTOR / MLST8NEW, MUSKMYLK3NIKNLKPDGFR-αPDGFR-βPKC-α (PRKCA)PKC-theta (PRKCQ)PTK2B (PYK2)RETROCK2,
RON (MST1R)ROS1SRCSTK33SYKTAK1 (MAP3K7-TAB1)TAOK3TBK1,  TIE2 (TEK)TRKATRKBTYK2TYRO3VEGFR2,
ZAP70

Lipidkinases

PI3K-α/p85αPI3K-α (E545K/p85α)PI3K-β/p85αPI3K-δ/p85αPI3K-γPI4K-β, SPHK1 

PDEs

PDE10A2, PDE2A1, PDE2A3, PDE4B1PDE4B2PDE4D3    

Epigenetic Targets

HDAC1NEW, HDAC2NEW, LSD1

Protein-Protein Interaction

Mdm2/p53Mdm4/p53 

Other Enzymes

GyrB

Biologics


Established catalogue of > 100 ready-to-use Proteros reporter probe displacement assays for rapid kinetic profiling services of protein ligand interactions. Please enquiry for customized assay development for targets that are not part of the Gallery Assay list.

Service

Application

Deliverable

Throughput

Library screening incl. fragment screening

Primary screen
Identification of binding ligands

Probe displacement
[%]

100,000 ligands/week

Time resolved screening

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

Probe displacement
[%] at 2 time points

70,000 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)

konkoff, residence time clustering

2,500 

ligands/week

Kinetic profiling
high precision mode

Hit profiling, lead optimization
Quantification of binding affinities & kinetics

Kd, konkoff,
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