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FLIPR

These assays are easy to perform. Cells are plated 24h before the assay, preloaded with the dye, and allowed to incubate for a period of time, generally 1 h. Agonist and/or antagonist is added to the cells, the cells are incubated, and then read on the FLIPR. [Pg.47]

The truth most likely lies somewhere in between. Bender [67] published the most quantitative study to date on the success of HTS at Novartis. Several conclusions could be drawn. Particular target types and assay technologies have a great impact on screening success, and this was not always correlated to the number of identifying hits in the HTS runs. For assay formats used a minimum of five times, LC/MS readouts succeed 83% of the time, followed by FP assays, which succeed in 72% of the cases. TR-FRET showed a success rate of 70%, with FLIPR assays (61%), fluorescence intensity readouts (59%), and AlphaScreen (60%) performing... [Pg.59]

CXCR2 Binding IC50 4.6 (rM CXCR2 FLIPR IC50 2.4... [Pg.202]

CXCR2 Binding IC50 0.028 (rM CXCR2 FLIPR IC50 0.048... [Pg.202]

CCR1 FLIPR IC50 1.65 gM CCR1 FLIPR ICgc, 0.09 nM... [Pg.208]

Fig. 3. Comparison between IP-One kit versus calcium mobilization assay (384-well format). Human embryonic kidney (HEK) 293 cells expressing a chemokine receptor were evaluated on HTRF IP-One kit (CisBio, Bedford, MA) and fluroescent imaging plate reader (FLIPR) with Calcium 3 kit (Molecular Devices, Mountain View, CA). Fig. 3. Comparison between IP-One kit versus calcium mobilization assay (384-well format). Human embryonic kidney (HEK) 293 cells expressing a chemokine receptor were evaluated on HTRF IP-One kit (CisBio, Bedford, MA) and fluroescent imaging plate reader (FLIPR) with Calcium 3 kit (Molecular Devices, Mountain View, CA).
A series of 4,4-disubstituted quinazolin-2-ones derived from HTV nonnucleoside reverse transcriptase inhibitor leads have shown good in vitro potency and in vivo efficacy [28]. Using FLIPR assays on cell lines with different resting membrane potentials, TTA-Q3 (10) and TTA-Q6 (11)... [Pg.9]

Compound T-type FLIPR IP (nM) hERG IC50 (nM) L-type IC50 (nM) CL... [Pg.442]

Recent reports have emerged of several TRPV1 antagonists possessing a biaryl amide (14-16), urea (17), or urea isostere (18-20) scaffolds. Bicyclic derivatives 14-16 block capsaicin- or pH-stimulated calcium influx in FLIPR-based assays... [Pg.84]

Cronk D (2001) Cell-based high-throughput screening of ion channels using FLIPR and VIPR membrane potential assay technology. Presented at 7th annual conference of Society for Biomolecular Screening, Baltimore, MD, 10-13 September 2001. SBS, Danbury, Abstract no 119... [Pg.25]

Fluorescent, voltage-sensitive dyes can be employed to investigate the activity of ion channels by reflecting the cellular membrane potential (Epps et al. 1994 Plasek and Sigler 1996). This approach is suitable for use in conjunction with different measurement systems including Fluorometric imaging plate readers (FLIPR), Voltage/Ion probe readers (VIPR) or conventional fluorescence readers. [Pg.73]

Benjamin ER. 2006. Pharmacological characterization of recombinant N-type calcium channel (Cav2.2) mediated calcium mobilization using FLIPR. Biochem. Pharmacol. 72, 770-782. [Pg.180]

Reporter gene assay (RGA), e.gv lucHerase, SEAP Secondary m essengers, e.g., Ca24(FLIPR), cAMP, IP3 J Cell-based ELISA e.g.,QytoBlDt Cell based physiological assay... [Pg.248]

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See also in sourсe #XX -- [ Pg.2 , Pg.51 ]

See also in sourсe #XX -- [ Pg.646 ]

See also in sourсe #XX -- [ Pg.51 ]



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FLIPR assay

FLIPR imaging

FLIPR plate reader

Fluorescence imaging plate reader (FLIPR

Fluorescent imaging plate reader (FLIPR

Fluorimetric imaging plate reader (FLIPR

Fluorometric imaging plate reader (FLIPR

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