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pathE/IC50ELECT

Quantitate compound potency against any PATHscan functional cell-based assay. Agonist half maximal effective concentrations (EC50s) and antagonist half maximal inhibitory concentrations (IC50s) 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.

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

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Panel Features & Benefits

  • 10-point dose response curve in duplicate
  • Choose from a growing list of novel pathway signaling assays
  • High quality reproducible data
  • Inhibitor and agonist mode – identify small molecule inhibitors and/or antibody therapeutics
  • Rapid turnaround time
How it Works

Screen for Activators or Inhibitors of PI3-K/AKT Signalling



PathHunter® assays are able to measure FOXO translocation in response to PI3 or AKT inhibition.

pathE/IC50ELECT Assay Panel

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

 
Target Gene ▲Common NameFamilyAccession No.
BCL2-BAXBCL2 B-cell CLL/lymphoma 2 (Bcl-2)BCL2NM_000633
BCL2-BIMBCL2 B-cell CLL/lymphoma 2 (Bcl-2)BCL2NM_000633
BCL2L1-BAXBCL2-like 1 (Bcl-xL)BCL2NM_138578.1
BCL2L1-BIMBCL2-like 1 (Bcl-xL)BCL2NM_138578.1
CDC25ACell division cycle 25 homolog A (CDC25A)Cell Cycle ProteinNM_001789.2
FOXO3forkhead box O3 (forkhead box O3)PathwayNM_001455
IκBnuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor, alpha (NFKBIA)PathwayNM_020529
Keap1-NRF2nuclear factor (erythroid-derived 2)-like 2 (NFE2L2)Transcription FactorNM_006164
MCL1-BIMMyeloid cell leukemia sequence 1 (Mcl-1)BCL2NM_021960
NIKmitogen-activated protein kinase kinase kinase 14 (NIK)STENP_003945.2
NPR1Natriuretic peptide receptor A (NPR1)Guanylate Cyclase ANM_000906.3
P53P53 (P53)Nuclear TranslocationNM_000546.2
RANK-IκBTumor necrosis factor receptor superfamily, member 11a (TNFRSF11A)Tumor Necrosis Factor Receptor SuperfamilyNM_003839.3
RELA-IκBv-rel reticuloendotheliosis viral oncogene homolog A (avian) (RELA)Transcription factorNM_021975
SREBP2Sterol regulatory element binding transcription factor 2 (SREBF2)Transcription FactorNM_004599.2
TORC1CREB regulated transcription coactivator 1 (CRTC1)Transcription factorNM_015321.1
TORC2CREB regulated transcription coactivator 2 (CRTC2)Transcription factorNM_181715
XBP1X-box binding protein 1 (XBP1)Transcription factorBC012841
β-CateninCatenin (cadherin-associated protein), beta 1 (CTNNB1)Wnt-Frizzled signallingNM_001904

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 halfway 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.

What does an IC50 measure?

The term half maximal inhibitory concentration (EC50) is a measure of the effectiveness of a compound to inhibit a given biological response. Therefore, the IC50 of a compound or biologic represents the half maximal (50%) inhibitory concentration and is commonly used as a measure of antagonist drug’s potency.

How are the EC50/IC50s calculated?

For each compound/GPCR target interaction, dose response curves  are generated using 10 concentrations of agonist or antagonist (10-point curve). The results are reported as EC50/IC50 which derived using the Hill equation:

hill equation