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NanoBRET™ TE Intracellular Kinome-Wide Profiling Service (K192)Promega

Incorporating a cell-based assay in hit identification often provides advantages over biochemical assays when selecting and characterizing key compounds. As an example, membrane permeability and cytotoxicity, which cannot be determined by biochemical methods using isolated purified proteins, can be assessed in a cellular environment.
In this cell-based panel profiling service, your compound is evaluated collectively against 192 full-length kinases individually expressed in HEK293 cells under uniform assay conditions using the same tracer. Your compound’s interaction against each target in the cellular environment is quantified, allowing comparison of its efficacy against the primary target(s) and possible off targets.

NanoBRET™ Target Engagement (TE) Intracellular Kinase Assay System (Promega) is used in this broad panel of 192 kinase targets (see list), each expressed intracellularly by transient transfection. Compound evaluation against all targets is performed simultaneously at 1 compound concentration in duplicate, under the same assay conditions. Follow up IC50 determinations also available.

Collectively identify compound properties against 192 kinases, using uniform assay conditions!

Learn what can't be learned in biochemical assays!

Comparison data using 1μM Crizotinib in a biochemical assay (Mobility Shift Assay) and NanoBRET™ K192 cell assay panel (36 selected targets shown)

Biochemical (Km ATP)
K192 (NanoBRET™ Cell-Based Assay)

Comparison data using 0.3μM CC1 inhibitor in a biochemical assay (Mobility Shift Assay) and NanoBRET™ K192 cell assay panel

Biochemical (Km ATP)
Biochemical (1mM ATP)
K192 (NanoBRET™ Cell-Based Assay)

192 Panel Kinase Targets

AAK1
ACK (TNK2)
AKT2
AMPKα1 (PRKAA1)
AMPKα2 (PRKAA2)
ARG (ABL2)
AurA (Aurora A)
AurB (Aurora B)
AurC (Aurora C)
AXL
BMP2K
BMX
BRAF[V600E]
BRK (PTK6)
BRSK1
BRSK2
BTK
CaMK1α (CAMK1)
CaMK2α (CAMK2A)
CaMK2δ (CAMK2D)
CDC2 (CDK1)/CycB1
CDK2/CycE1
CDK3/CycE1
CDK4/CycD3
CDK5/p25 (CDK5R1)
CDK6/CycD1
CDK7/CycH
CDK9/CycK
CDK10/CycL2
CDK14/CycY
CDK15/CycY
CDK17/CycY
CDK18/CycY
CDK20/CycH
CDKL1
CDKL2
CDKL3
CDKL5
CHK2 (CHEK2)
CK1γ2 (CSNK1G2)
CK1δ (CSNK1D)
CK2α1 (CSNK2A1)
CK2α2 (CSNK2A2)
CLK1
CLK2
CLK4
CSNK1A1L
DAPK2
DCLK3
DLK (MAP3K12)
DRAK2 (STK17B)
DYRK1A
DYRK1B
EPHA1
EPHA4
EPHA6
EPHA7
EPHB1
EPHB4
ERN1
ERN2
FAK (PTK2)
FER
FES
FGFR1
FGFR2
FGFR3
FGFR4
FLT3
FYN [isoform a] (FYN)
GAK
HH498 (TNNI3K)
HIPK2
HIPK3
HIPK4
HPK1 (MAP4K1)
ICK
IGF1R
IKKε (IKBKE)
INSR
IRAK3
IRAK4
ITK
JAK2[V617F]
JAK3
JNK1
JNK2
JNK3
LATS1
LATS2
LCK
LIMK1
LIMK2
LKB1 (STK11)
LOK (STK10)
LRRK2
LTK
MAP3K2
MAP3K3
MAP3K4
MAP3K19
MAP4K2
MAP4K3
MAP4K5
MAPK4
MAPK6
MARK2
MARK4
MAST3
MAST4
MELK
MER (MERTK)
MET
MLK1 (MAP3K9)
MLK2 (MAP3K10)
MLK3 (MAP3K11)
MLK4 (MAP3K21)
MNK2 (MKNK2)
MPSK1 (STK16)
MSK2 (RPS6KA4)
MST1 (STK4)
MST2 (STK3)
MUSK
MYLK3
MYLK4
MYT1 (PKMYT1)
NDR1 (STK38)
NDR2 (STK38L)
NEK1
NEK2
NEK3
NEK4
NEK5
NEK9
NEK11
NIM1K (MGC42105)
NLK
NUAK1
p38α (MAPK14)
p38β (MAPK11)
PAK4
PAK6
PCTAIRE1 (CDK16)/CycY
PHKG1
PHKG2
PKACα (PRKACA)
PKACβ (PRKACB)
PKCε (PRKCE)
PLK2
PLK3
PLK4
PRKX
PYK2 (PTK2B)
QIK (SIK2)
RET
RIOK2
RIPK1
RIPK2
RON
RSK1
RSK2
RSK3
RSK4
SBK3
SGK (SGK1)
SIK (SIK1)
SIK3 (QSK)
skMLCK (MYLK2)
SLK
SNRK
SRM (SRMS)
STK32B
STK33
STK35
STK36
TBK1
TEC
TIE1
TIE2 (TEK)
TLK1
TLK2
TNK1
TRKA (NTRK1)
TRKB (NTRK2)
TXK
TYRO3
ULK1
ULK2
ULK3
WEE1
WEE2
ZAK (MLTK)
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