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ICH ELECT - Personalized Screening & Profiling

Select from our growing menu of cell-based bromodomain and histone methyltransferase assays and create your own custom panel.  InCELL Hunter (ICH) ELECT services is a flexible solution with multiple applications including high-throughput screening & lead discovery as well as lead optimization & SAR. Select only the target or targets of interest and identify hits or rank order lead compounds based on intracellular binding and cellular potency.

Panel Features & Benefits

  • Customized screening and profiling - choose only the targets you need
  • Bromodomain and Histone Methyltransferase assays available
  • Flexible service options - personalized panels or single target selection
  • High quality reproducible data
  • Binding mode available
  • Rapid data turnaround
How it Works
 

ICH ELECT Services – Determine Cellular Potency Against Novel Targets

Unlike other biochemical or cell-based epigenetic assays that are limited by the availability of specific antibodies or reagents that detect  histone modifications, InCELL Hunter bromodomain and methyltransferase assays are non-antibody-based, high-throughput friendly chemiluminescent assays and can provide a direct measure of compound permeability and binding to a proteins’ catalytic domain in live cells.

Assay Performance

BRD4(1)

   

G9a Methyltransferase

 
InCELL Hunter BRD4(1) cells (Left panel) and G9a Methyltransferase cells (Right panel) stimulated with the indicated compounds for 6 hours. Signal was detected using the InCELL Hunter Detection kit. The data demonstrates that an increase in signal is specific to a molecule that binds the target.

Plate Uniformity

 




C0638 Hill Slop IC50 (nM) S:B
CRC1 1.391 66 13.6
CRC2 1.501 80 12.5
CRC3 1.384 98 13.1
CRC4 1.381 94 13.1
CRC5 1.354 90 11.2
CRC6 1.247 106 12.1
CRC7 1.407 102 12.0
CRC8 1.393 76 12.0
InCELL Hunter G9a Methyltransferase cells were plated in 384-well format and 8 replicates of a 10-point control response curves (run in duplicate ) were performed.  Assay performance was consistent across the entire plate

ICH ELECT Panel

Listed below are the assays currently available for screening and profiling.

Bromodomain Assays

Assay Name ▲Common NameAccession Number
BAZ2A NM_013449.3
Brd2(1)BRD2NM_005104.3
BRD2(1,2)BRD2NM_005104.3
BRD3(1)BRD3NM_007371.3
BRD3(1,2)BRD3NM_007371.3
Brd4(1)BRD4NM_058243
BrdT(1)BRDTNM_001242806
BRDT(1,2)BRDTNM_001726
EP300 NM_001429.3
SMARCA4 NM_001128844
TAF1L(2) NM_153809.2

Histone Methyltransferase Assays

Assay Name ▲Common NameAccession Number
G9aEHMT2NM_006709
GLPEHMT1NM_024757
PRMT3PRMT3NM_005788.3

Data Analysis & Interpretation 

Definitions

Percent Binding

The results for single concentration (primary screen) for tested compound(s) are reported in your study report and spreadsheets as '% Binding' and are calculated in the following manner:
 

% Binding =
100% x
[
Mean RLU (test sample)- Mean RLU(vehicle control)

Mean MAX RLU (control ligand)- Mean RLU (vehicle control)
]
 

test sample = client supplied compound
vehicle control = DMSO (0% activity)
control ligand = control compound (100% activity)

 

Dose Response Curve (EC50)

The results for 10-point dose response curve compound/target interactions are reported in the study report and spreadsheets as cellular EC50s, which are values derived using the following equation:

hill equation