Assays


Figure 6. Kinase platform/technology likely to be displaced by FLT-based kinase platform TR-FRET (Time Resolved FRET eg HTRF, LANCE, TR-IMAP, LanthaScreen)


FRET (Fluorescent Resonance Energy Transfer) FI (Fluorescent Intensity) including fluorescent quench assays FI (Fluorescent Intensity) with microfluidic chip separation FP (Fluorescent Polarisation) with Ligand (ie NO antibody) Glow Luminescence


FP (Fluorescent Polarisation) with Antibody


FP Immunodetection of ADP (eg Transcreener) TRF (Time Resolved Fluorescence eg DELFIA) Chemiluminescent-based ELISA Assays AlphaScreen including AlphaLISA


Radiometric Filter (eg P33 incorporation) SPA/LEADseeker (Radiometric)


TR-FRET Immunodetection of ADP (eg Transcreener) Other


FI (Fluorescent Intensity) based ELISA assays 0% © HTStec 2010 14% 10%


6% 6%


5% 5% 5%


4%


3% 3% 3%


1% 1% 2% 2%


5% 10% 15% 20% 25% 30% % Responding


28%


Figure 7: Opinion on adoption of FLT over the coming years


After 5 years After 3 years Next 1-2 years


0% 10% 20% 30% 40% 50% 60% 70% 80% 90% % Responding


HIGHLY Important Tool – > 20% of targets screened LOW Importance Tool –


© HTStec 2010


MEDIUM Importance Tool – between 5 and 20% of targets screened UNIMPORTANT Tool – 0% of targets screened


100%


20% viewing it as high importance (>20% of targets screened) and 47% as medium importance (between 5% and 20% of targets screened). Supporting this finding is the fact that there is already significant adop- tion of FLT in some companies, eg the Protease Platform at Novartis6.


Latest vendor offerings


The following snapshots provide details of some of the current status and recent progress vendors have made in the development of FLT-related instru- mentation, dyes and assays.


Drug Discovery World Summer 2010


Tecan (www.tecan.com) pioneered the field of devel- oping multimode microplate readers that include a FLT detection module, when it marketed the ULTRA Evolution with FLT option in 2002. FLT measure- ments on the ULTRA Evolution are performed using the Time-Correlated Single Photon Counting (TCSPC) method, where a pulsed laser repeatedly excites the sample. The intensity of the excitation pulses is adjusted so that each individual pulse gen- erates one photon counting event in the detector. The time between the laser pulse and the detector event is measured, and count numbers versus time


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