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ICH E/IC50ELECT℠ – Personalized Screening & Profiling

Quantitate compound potency against any EPIscan℠ cell-based bromodomain and histone methyltransferase binding assay. Compound half maximal effective concentrations (intracellular EC50s) are calculated from duplicate 10-point dose-response curves. Measurements are made under optimized conditions to generate consistent and reproducible data that reliably reflects the drug's potency.

ICH E/IC50ELECT may be used as an ideal follow-up study tool to quantify the potency of compound-bromodomain or compound-histone methyltransferase target interactions identified in primary screens, to supplement existing data, or support lead optimization and SAR activity.

Panel Features & Benefits

  • 10-point dose response curves in duplicate
  • Choose from a growing menu of bromodomain and Histone Methyltransferase assays
  • High quality reproducible data
  • Binding mode available
  • Rapid data turnaround
 How it Works

ICH E/IC50ELECT Services – Rank Order Compounds Based on Cellular Potency

Based on the proven InCELL Hunter™ technology, ICH E/IC50ELECT services provide you a way to detect the binding of test compounds to novel epigenetic targets in intact mammalian cells. This whole cell assay platform allows you to rank order compounds based on cellular binding and potency.

 
Increasing concentrations of four BET family  bromodomain inhibitors were added to the InCELL Hunter Brd4(1) cell line and incubated for 6 hours at 37°C. Cells were then lysed  in the presence of enzyme substrate and the complementary EA enzyme fragment to quantify the abundance of Brd4(1) tagged with the enhanced ProLabel enzyme fragment.

ICH E/IC50ELECT Assay 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 

What does the term EC50 mean?

The term half maximal effective concentration (EC50) refers to the concentration of a drug or biologic which induces a response half way between the baseline and the maximum. Therefore, the EC50 of a compound or biologic represents the concentration where 50% of it's maximal effect can be observed. It is commonly used as a measure of the drug's potency.

How are cellular EC50’s calculated?

For each compound/bromodomain or compound/methyltransferase interaction, dose response curves are generated using 10 concentrations of agonist (10-point curve). The results are reported as cellular EC50 which is derived using the Hill equation:

hill equation