ClariCELL™ Kinase Assays

Cell-based compound potency measurements are important components of the drug discovery process since biochemical potency values often do not translate to cellular activity due to compound membrane permeability, cellular ATP concentration, compound localization, etc. ClariCELL™ cell-based kinase assays effectively bridge the gap between biochemical and functional assays for testing the inhibitory activities of small molecules against a specific kinase of interest in human cells.

ClariCELL assays are a direct measure of kinase activity, quantifying phosphorylation levels on expressed full-length kinase/substrate pairs in human cells. All assays are rigorously validated with kinase-dead mutants and reference compounds and can be used to determine compound potencies in a cellular setting, correlate cellular potencies with functional cellular effects and determine cellular selectivity versus other kinases.

Utility of ClariCELL Kinase Assays

Screen/profile biochemical hits for cellular activity against targets of interest
- more physiologically relevant activity measurement
- confirm or disprove target activity
- compare compound potency vs. known inhibitors
Determine selectivity against other kinases in a cellular environment
- ex. Pim-1, Pim-2, Pim-3 selectivity
Determine or confirm mechanism of action
Define SAR of compound series in a cell-based environment
Address safety concerns with cellular potency data for kinases implicated in adverse events

AVAILABLE TARGETS

Tyrosine Kinases

Abl, Abl [E255V], Abl [T315I], ACK, BLK, BMX, BRK (PTK6), BTK, BTK [C481S], BTK [T474A], BTK [T474M], CSK, FGR, FYN, HCK, ITK, JAK1, JAK2, JAK2 [V617F], JAK3, JAK3 [Y981F], LCK, LYN, SRC, SYK, TEC, TXK, TYK2, YES

Receptor Tyrosine Kinases

ALK, EGFR, EGFR [T790M], EphA2, EphB1, EphB2, EphB3, EphB4, FGFR1, FLT3, HER2 (ERBB2), KDR (VEGFR-2), KIT, KIT [T670I], KIT [V654A], MET, PDGFR-A, PDGFR-A [T674I], PDGFR-B, RET, TrkA

Serine/Threonine Kinases

AKT1, DYRK1A, MST1, PDK1, Pim-1, Pim-2, Pim-3

Don't see your kinase of interest? In most cases we can quickly validate your kinase of interest on the ClariCell platform. Screening and profiling services are also avialable. Contact us for details and pricing at sales@mayflowerbio.com.

CASE STUDY

BTK and BTK mutants

Products

Note: product availability depends on country. Product detail pages show availability of each product.