Compound in Profiling

Compound Information

Test on : RBC

Compound Name : Tpl2 Kinase Inhibitor

Inchikey : NMEUKWOOQOHUNA-UHFFFAOYSA-N

ChemSpider : 7828216

Pubchem CID : 9549300

ChEMBL : CHEMBL200381

	DRx	RBC	Metz	Millipore	GPCR
bioactivity	Kd (nM)	Remain Activity (%)	Ki (nM)	Remain Activity (%)	Inhibition (%)
active criteria	<3000nM	<50%	<1000nM	<50%	>50%

AGC

Test Member No. in Family
Family	no. Member on 518kinase	RBC
PDK1	1	1
Akt	3	3
DMPK	7	5
GRK	7	6
RSK	8	8
PKA	5	3
PKC	9	9
PKG	2	3
PKN	3	2
SGK	3	3
NDR	4	1

AGC - PDK1

Bioactivity
Kinase	RBC
PDK1	inactive (85.34%)

AGC - Akt

Bioactivity
Kinase	RBC
AKT1	inactive (98.59%)
AKT2	inactive (100.71%)
AKT3	inactive (95.14%)

AGC - DMPK

Bioactivity
Kinase	RBC
DMPK1	inactive (103.84%)
MRCKa	inactive (80.04%)
MRCKb	inactive (124.11%)
ROCK1	inactive (99.81%)
ROCK2	inactive (97.08%)

AGC - GRK

Bioactivity
Kinase	RBC
BARK1	inactive (95.66%)
BARK2	inactive (100.25%)
GPRK4	inactive (98.77%)
GPRK5	inactive (106.87%)
GPRK6	inactive (106.28%)
GPRK7	inactive (95.47%)

AGC - RSK

Bioactivity
Kinase	RBC
MSK1	inactive (102.25%)
MSK2	inactive (91.95%)
p70S6K	inactive (89.43%)
p70S6Kb	inactive (99.52%)
RSK2	inactive (99.13%)
RSK4	inactive (103.81%)
RSK1	inactive (94.58%)
RSK3	inactive (87.28%)

AGC - PKA

Bioactivity
Kinase	RBC
PKACg	inactive (115.01%)
PRKX	inactive (101.14%)
PKACa	inactive (92.17%)

AGC - PKC

Bioactivity
Kinase	RBC
PKCa	inactive (89.66%)
PKCd	inactive (95.21%)
PKCe	inactive (100.96%)
PKCh	inactive (116.69%)
PKCg	inactive (111.33%)
PKCi	inactive (94.66%)
PKCt	inactive (113.16%)
PKCz	inactive (93.85%)
PKCb	inactive (86.19%)

AGC - PKG

Bioactivity
Kinase	RBC
PKG2	inactive (90.88%)
PKG1	inactive (90.81%)

AGC - PKN

Bioactivity
Kinase	RBC
PKN1	inactive (100.93%)
PKN2	inactive (85.94%)

AGC - SGK

Bioactivity
Kinase	RBC
SGK1	inactive (93.23%)
SGK2	inactive (98.55%)
SGK3	inactive (91.53%)

AGC - NDR

Bioactivity
Kinase	RBC
NDR1	inactive (93.87%)

TK

Test Member No. in Family
Family	no. Member on 518kinase	RBC
Abl	2	2
Ack	2	1
ALK	2	2
Axl	3	3
Src	11	11
Tec	5	5
PDGFR	5	5
Csk	2	2
DDR	2	1
EGFR	4	3
Eph	14	12
FAK	2	2
Fer	2	2
FGFR	4	4
VEGFR	3	3
InsR	3	3
JakA	4	4
Musk	1	1
Ret	1	1
Met	2	2
Sev	1	1
Syk	2	2
Tie	2	1
Trk	3	3

TK - Abl

Bioactivity
Kinase	RBC
ABL1	inactive (93.37%)
ABL2	inactive (87.35%)

TK - Ack

Bioactivity
Kinase	RBC
ACK	inactive (89.87%)

TK - ALK

Bioactivity
Kinase	RBC
ALK	inactive (107.37%)
LTK	inactive (95.59%)

TK - Axl

Bioactivity
Kinase	RBC
AXL	inactive (102.56%)
MER	inactive (67.18%)
TYRO3	inactive (97.99%)

TK - Src

Bioactivity
Kinase	RBC
BLK	inactive (99.94%)
BRK	inactive (84.13%)
SRC	inactive (92.56%)
FGR	inactive (84.46%)
FRK	inactive (100.84%)
FYN	inactive (103.39%)
HCK	inactive (92.47%)
LCK	inactive (97.3%)
SRM	inactive (104.29%)
YES	inactive (93.64%)
LYN	inactive (90.44%)

TK - Tec

Bioactivity
Kinase	RBC
BMX	inactive (84.04%)
BTK	inactive (98.29%)
ITK	inactive (99.08%)
TEC	inactive (117.83%)
TXK	inactive (88.15%)

TK - PDGFR

Bioactivity
Kinase	RBC
KIT	inactive (92.89%)
FLT3	inactive (83.61%)
FMS	inactive (96.25%)
PDGFRb	inactive (101.35%)
PDGFRa	inactive (94.34%)

TK - Csk

Bioactivity
Kinase	RBC
CSK	inactive (95.15%)
CTK	inactive (95.85%)

TK - DDR

Bioactivity
Kinase	RBC
DDR2	inactive (91.94%)

TK - EGFR

Bioactivity
Kinase	RBC
EGFR	active (24.29%)
ErbB2	inactive (91.71%)
ErbB4	inactive (72.63%)

TK - Eph

Bioactivity
Kinase	RBC
EphA1	inactive (94.54%)
EphA2	inactive (101.71%)
EphA3	inactive (122.47%)
EphA4	inactive (92.76%)
EphA5	inactive (90.6%)
EphA6	inactive (76.23%)
EphA7	inactive (83.72%)
EphA8	inactive (91.18%)
EphB1	inactive (93.13%)
EphB2	inactive (97.41%)
EphB3	inactive (98.51%)
EphB4	inactive (85.24%)

TK - FAK

Bioactivity
Kinase	RBC
FAK	inactive (99.55%)
PYK2	inactive (99.97%)

TK - Fer

Bioactivity
Kinase	RBC
FER	inactive (82.88%)
FES	inactive (107.99%)

TK - FGFR

Bioactivity
Kinase	RBC
FGFR1	inactive (83.38%)
FGFR2	inactive (103.3%)
FGFR3	inactive (91.67%)
FGFR4	inactive (92.6%)

TK - VEGFR

Bioactivity
Kinase	RBC
FLT1	inactive (88%)
FLT4	inactive (96.16%)
KDR	inactive (96.27%)

TK - InsR

Bioactivity
Kinase	RBC
IGF1R	inactive (93.8%)
IRR	inactive (97.04%)
INSR	inactive (85.06%)

TK - JakA

Bioactivity
Kinase	RBC
JAK1	inactive (93.58%)
JAK2	inactive (99.05%)
JAK3	inactive (86.19%)
TYK2	inactive (102.78%)

TK - Musk

Bioactivity
Kinase	RBC
MUSK	inactive (55.62%)

TK - Ret

Bioactivity
Kinase	RBC
RET	inactive (106.84%)

TK - Met

Bioactivity
Kinase	RBC
RON	inactive (89.59%)
MET	inactive (94.88%)

TK - Sev

Bioactivity
Kinase	RBC
ROS	inactive (98.3%)

TK - Syk

Bioactivity
Kinase	RBC
SYK	inactive (94.37%)
ZAP70	inactive (102.53%)

TK - Tie

Bioactivity
Kinase	RBC
TIE2	inactive (95.49%)

TK - Trk

Bioactivity
Kinase	RBC
TRKA	inactive (96.17%)
TRKB	inactive (100.61%)
TRKC	inactive (93.22%)

TKL

Test Member No. in Family
Family	no. Member on 518kinase	RBC
STKR	12	5
RAF	5	3
IRAK	4	2
LISK	4	1
LRRK	2	1
MLK	10	5
RIPK	5	1

TKL - STKR

Bioactivity
Kinase	RBC
ALK1	inactive (96.92%)
ALK2	inactive (95.57%)
ALK4	inactive (99.03%)
TGFbR1	inactive (99.55%)
TGFbR2	inactive (117.82%)

TKL - RAF

Bioactivity
Kinase	RBC
ARAF	inactive (105.66%)
BRAF	inactive (105.99%)
RAF1	inactive (90.94%)

TKL - IRAK

Bioactivity
Kinase	RBC
IRAK1	inactive (114.17%)
IRAK4	inactive (100.5%)

TKL - LISK

Bioactivity
Kinase	RBC
LIMK1	inactive (101.25%)

TKL - LRRK

Bioactivity
Kinase	RBC
LRRK2	inactive (86.64%)

TKL - MLK

Bioactivity
Kinase	RBC
MLK1	inactive (87.47%)
MLK2	inactive (101.23%)
MLK3	inactive (88.97%)
TAK1	inactive (89.49%)
ZAK	inactive (105.64%)

TKL - RIPK

Bioactivity
Kinase	RBC
RIPK2	inactive (85.31%)

CAMK

Test Member No. in Family
Family	no. Member on 518kinase	RBC
CAMKL	20	13
CAMK1	5	5
CAMK2	4	4
RAD53	1	1
DAPK	5	4
DCAMKL	3	1
MAPKAPK	5	5
MLCK	5	2
PHK	2	2
PIM	3	3
PKD	3	3
TSSK	5	2
STK33	1	-

CAMK - CAMKL

Bioactivity
Kinase	RBC
NuaK1	inactive (103.36%)
BRSK1	inactive (94.55%)
BRSK2	inactive (100.45%)
CHK1	inactive (90.22%)
LKB1	inactive (91.14%)
MARK1	inactive (91.64%)
MARK3	inactive (100.94%)
MARK4	inactive (96.38%)
MELK	inactive (88.04%)
PASK	inactive (123.63%)
QIK	inactive (97.59%)
NuaK2	inactive (134.85%)
MARK2	inactive (93.18%)

CAMK - CAMK1

Bioactivity
Kinase	RBC
CaMK1a	inactive (99.11%)
CaMK1b	inactive (99.77%)
CaMK1d	inactive (97.83%)
CaMK1g	inactive (96.13%)
CaMK4	inactive (95.23%)

CAMK - CAMK2

Bioactivity
Kinase	RBC
CaMK2a	inactive (105.05%)
CaMK2b	inactive (97.39%)
CaMK2d	inactive (102.82%)
CaMK2g	inactive (91.16%)

CAMK - RAD53

Bioactivity
Kinase	RBC
CHK2	inactive (90.54%)

CAMK - DAPK

Bioactivity
Kinase	RBC
DAPK1	inactive (102.18%)
DAPK2	inactive (107.78%)
DRAK1	inactive (79.6%)
DAPK3	inactive (101.02%)

CAMK - DCAMKL

Bioactivity
Kinase	RBC
DCLK2	inactive (97.2%)

CAMK - MAPKAPK

Bioactivity
Kinase	RBC
MAPKAPK2	inactive (100.01%)
MAPKAPK3	inactive (93.96%)
MAPKAPK5	inactive (99.6%)
MNK1	inactive (73.19%)
MNK2	inactive (79.32%)

CAMK - MLCK

Bioactivity
Kinase	RBC
smMLCK	inactive (105.03%)
skMLCK	inactive (96.18%)

CAMK - PHK

Bioactivity
Kinase	RBC
PHKg1	inactive (92.02%)
PHKg2	inactive (88.26%)

CAMK - PIM

Bioactivity
Kinase	RBC
PIM1	inactive (92.73%)
PIM2	inactive (101.1%)
PIM3	inactive (84.95%)

CAMK - PKD

Bioactivity
Kinase	RBC
PKD1	inactive (94.55%)
PKD3	inactive (90.39%)
PKD2	inactive (99.72%)

CAMK - TSSK

Bioactivity
Kinase	RBC
TSSK1	inactive (84.42%)
TSSK2	inactive (100.41%)

CAMK - STK33

Bioactivity
Kinase	RBC
STK33	inactive (87.38%)

STE

Test Member No. in Family
Family	no. Member on 518kinase	RBC
STE11	8	3
STE-Unique	2	2
STE20	31	23
STE7	7	3

STE - STE11

Bioactivity
Kinase	RBC
MAP3K5	inactive (106.14%)
MAP3K2	inactive (81.18%)
MAP3K3	inactive (75.03%)

STE - STE-Unique

Bioactivity
Kinase	RBC
COT	inactive (79.08%)
NIK	inactive (117.8%)

STE - STE20

Bioactivity
Kinase	RBC
GCK	inactive (72.17%)
HGK	active (44.43%)
KHS1	inactive (61.66%)
LOK	inactive (52.8%)
MINK	inactive (77.53%)
MST1	inactive (100.19%)
MST2	inactive (94.3%)
MST3	inactive (95.62%)
MST4	inactive (94.98%)
OSR1	inactive (87.66%)
PAK1	inactive (95.73%)
PAK2	inactive (66.58%)
PAK3	inactive (99.17%)
PAK4	inactive (85.41%)
PAK5	inactive (98.26%)
PAK6	inactive (104.18%)
SLK	inactive (86.55%)
YSK1	inactive (95.59%)
STLK3	inactive (78.59%)
TAO1	inactive (89.9%)
TAO2	inactive (86.08%)
TAO3	inactive (99.16%)
MYO3B	inactive (87.91%)

STE - STE7

Bioactivity
Kinase	RBC
MAP2K1	inactive (86.23%)
MAP2K2	inactive (104.55%)
MAP2K6	inactive (114.93%)

Other

Test Member No. in Family
Family	no. Member on 518kinase	RBC
Aur	3	3
CAMKK	2	2
Haspin	1	1
IKK	4	4
NEK	11	8
TOPK	1	1
PLK	4	3
SgK496	1	1
NAK	4	1
TTK	1	1
ULK	5	3
WEE	3	1
WNK	4	2
TLK	2	1

Other - Aur

Bioactivity
Kinase	RBC
AurA	inactive (98.1%)
AurB	inactive (90.11%)
AurC	inactive (91.81%)

Other - CAMKK

Bioactivity
Kinase	RBC
CaMKK1	inactive (105.3%)
CaMKK2	inactive (90.15%)

Other - Haspin

Bioactivity
Kinase	RBC
Haspin	inactive (82.49%)

Other - IKK

Bioactivity
Kinase	RBC
IKKa	inactive (96.32%)
IKKb	inactive (102.94%)
IKKe	inactive (90.59%)
TBK1	inactive (83.45%)

Other - NEK

Bioactivity
Kinase	RBC
NEK1	active (20.5%)
NEK11	inactive (87.1%)
NEK2	inactive (75.19%)
NEK4	inactive (71.65%)
NEK6	inactive (104.45%)
NEK7	inactive (102.41%)
NEK9	inactive (96.35%)
NEK3	inactive (55.97%)

Other - TOPK

Bioactivity
Kinase	RBC
PBK	inactive (84.76%)

Other - PLK

Bioactivity
Kinase	RBC
PLK1	inactive (92.64%)
PLK2	inactive (110.45%)
PLK3	inactive (91.13%)

Other - SgK496

Bioactivity
Kinase	RBC
SgK496	inactive (87.25%)

Other - NAK

Bioactivity
Kinase	RBC
MPSK1	inactive (93.83%)

Other - TTK

Bioactivity
Kinase	RBC
TTK	inactive (99.1%)

Other - ULK

Bioactivity
Kinase	RBC
ULK1	inactive (76.13%)
ULK2	inactive (102.39%)
ULK3	inactive (72.02%)

Other - WEE

Bioactivity
Kinase	RBC
Wee1	inactive (74.31%)

Other - WNK

Bioactivity
Kinase	RBC
Wnk2	inactive (91.09%)
Wnk3	inactive (92.4%)

Other - TLK

Bioactivity
Kinase	RBC
TLK2	inactive (106.06%)

CK1

Test Member No. in Family
Family	no. Member on 518kinase	RBC
CK1	7	6
VRK	3	1

CK1 - CK1

Bioactivity
Kinase	RBC
CK1d	inactive (88.4%)
CK1g1	inactive (86.95%)
CK1g2	inactive (102.2%)
CK1g3	inactive (102.81%)
CK1a	inactive (100.93%)
CK1e	inactive (81.84%)

CK1 - VRK

Bioactivity
Kinase	RBC
VRK1	inactive (99.22%)

CMGC

Test Member No. in Family
Family	no. Member on 518kinase	RBC
CK2	3	2
CLK	4	4
DYRK	10	9
MAPK	14	10
GSK	2	2
SRPK	3	3

CMGC - CK2

Bioactivity
Kinase	RBC
CK2a1	inactive (95.85%)
CK2a2	inactive (75.23%)

CMGC - CLK

Bioactivity
Kinase	RBC
CLK1	inactive (91.04%)
CLK2	inactive (79.89%)
CLK3	inactive (96.74%)
CLK4	inactive (63.32%)

CMGC - DYRK

Bioactivity
Kinase	RBC
DYRK1A	inactive (52.7%)
DYRK1B	inactive (65.17%)
DYRK2	inactive (95.46%)
DYRK3	inactive (96.26%)
DYRK4	inactive (84.37%)
HIPK1	inactive (98.6%)
HIPK2	inactive (93.16%)
HIPK3	inactive (96.52%)
HIPK4	inactive (93.08%)

CMGC - MAPK

Bioactivity
Kinase	RBC
Erk1	inactive (99.95%)
Erk2	inactive (104.6%)
JNK3	inactive (95.01%)
NLK	inactive (87.97%)
p38a	inactive (114.54%)
p38b	inactive (101.98%)
p38d	inactive (100.98%)
p38g	inactive (96.96%)
JNK1	inactive (110.05%)
JNK2	inactive (100.13%)

CMGC - GSK

Bioactivity
Kinase	RBC
GSK3A	inactive (88.53%)
GSK3B	inactive (99.75%)

CMGC - SRPK

Bioactivity
Kinase	RBC
MSSK1	inactive (96.41%)
SRPK1	inactive (101.67%)
SRPK2	inactive (100.84%)

Atypical

Test Member No. in Family
Family	no. Member on 518kinase	RBC
PDHK	5	1

Atypical - PDHK

Bioactivity
Kinase	RBC
PDHK1	inactive (85.34%)