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 Name | Accession Number |
BAZ2A | | NM_013449.3 |
Brd2(1) | BRD2 | NM_005104.3 |
BRD2(1,2) | BRD2 | NM_005104.3 |
BRD3(1) | BRD3 | NM_007371.3 |
BRD3(1,2) | BRD3 | NM_007371.3 |
Brd4(1) | BRD4 | NM_058243 |
BrdT(1) | BRDT | NM_001242806 |
BRDT(1,2) | BRDT | NM_001726 |
EP300 | | NM_001429.3 |
SMARCA4 | | NM_001128844 |
TAF1L(2) | | NM_153809.2 |
Histone Methyltransferase Assays
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:
