Compound in Profiling

Compound Information

Test on : RBC

Compound Name : MEK Inhibitor II

Inchikey : GYQSWJNGTWVFOL-UHFFFAOYSA-N

ChemSpider : 345595

Pubchem CID : 389898

ChEMBL : CHEMBL404939

	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 (100.16%)

AGC - Akt

Bioactivity
Kinase	RBC
AKT1	inactive (103.31%)
AKT2	inactive (96.29%)
AKT3	inactive (104.54%)

AGC - DMPK

Bioactivity
Kinase	RBC
DMPK1	inactive (98.5%)
MRCKa	inactive (102.89%)
MRCKb	inactive (98.58%)
ROCK1	inactive (106.38%)
ROCK2	inactive (91.5%)

AGC - GRK

Bioactivity
Kinase	RBC
BARK1	inactive (105.48%)
BARK2	inactive (103.1%)
GPRK4	inactive (97.64%)
GPRK5	inactive (91.54%)
GPRK6	inactive (98.49%)
GPRK7	inactive (108.91%)

AGC - RSK

Bioactivity
Kinase	RBC
MSK1	inactive (101.07%)
MSK2	inactive (115.13%)
p70S6K	inactive (100.77%)
p70S6Kb	inactive (101.87%)
RSK2	inactive (101.3%)
RSK4	inactive (99.9%)
RSK1	inactive (96.58%)
RSK3	inactive (103.9%)

AGC - PKA

Bioactivity
Kinase	RBC
PKACg	inactive (95.11%)
PRKX	inactive (102.65%)
PKACa	inactive (88.79%)

AGC - PKC

Bioactivity
Kinase	RBC
PKCa	inactive (99.05%)
PKCd	inactive (97.76%)
PKCe	-
PKCh	inactive (93.13%)
PKCg	inactive (97.55%)
PKCi	inactive (96.63%)
PKCt	inactive (114.45%)
PKCz	inactive (114.15%)
PKCb	inactive (107.68%)

AGC - PKG

Bioactivity
Kinase	RBC
PKG2	inactive (113.51%)
PKG1	inactive (97.78%)

AGC - PKN

Bioactivity
Kinase	RBC
PKN1	inactive (108.2%)
PKN2	inactive (107.91%)

AGC - SGK

Bioactivity
Kinase	RBC
SGK1	inactive (104.16%)
SGK2	inactive (99.48%)
SGK3	inactive (102.59%)

AGC - NDR

Bioactivity
Kinase	RBC
NDR1	inactive (102.31%)

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 (103.08%)
ABL2	inactive (106.34%)

TK - Ack

Bioactivity
Kinase	RBC
ACK	inactive (91.46%)

TK - ALK

Bioactivity
Kinase	RBC
ALK	inactive (88.47%)
LTK	inactive (100.29%)

TK - Axl

Bioactivity
Kinase	RBC
AXL	inactive (103.65%)
MER	inactive (90.29%)
TYRO3	inactive (114.24%)

TK - Src

Bioactivity
Kinase	RBC
BLK	inactive (110.78%)
BRK	inactive (94.77%)
SRC	inactive (95.08%)
FGR	inactive (102.1%)
FRK	inactive (103.12%)
FYN	inactive (111.26%)
HCK	inactive (94.24%)
LCK	inactive (105.57%)
SRM	inactive (108.15%)
YES	inactive (103.05%)
LYN	inactive (93.46%)

TK - Tec

Bioactivity
Kinase	RBC
BMX	inactive (102.89%)
BTK	inactive (103.21%)
ITK	inactive (87.49%)
TEC	inactive (100.67%)
TXK	inactive (95.55%)

TK - PDGFR

Bioactivity
Kinase	RBC
KIT	inactive (84.74%)
FLT3	inactive (107.97%)
FMS	inactive (101.75%)
PDGFRb	inactive (102.82%)
PDGFRa	inactive (109.33%)

TK - Csk

Bioactivity
Kinase	RBC
CSK	inactive (79.53%)
CTK	inactive (88.04%)

TK - DDR

Bioactivity
Kinase	RBC
DDR2	inactive (95.76%)

TK - EGFR

Bioactivity
Kinase	RBC
EGFR	inactive (98.4%)
ErbB2	inactive (95.41%)
ErbB4	inactive (109.57%)

TK - Eph

Bioactivity
Kinase	RBC
EphA1	inactive (97.59%)
EphA2	inactive (106.65%)
EphA3	inactive (105.12%)
EphA4	inactive (101.23%)
EphA5	inactive (112.53%)
EphA6	inactive (89.46%)
EphA7	inactive (106.28%)
EphA8	inactive (107%)
EphB1	inactive (97.16%)
EphB2	inactive (98.69%)
EphB3	inactive (97.05%)
EphB4	inactive (98.71%)

TK - FAK

Bioactivity
Kinase	RBC
FAK	inactive (98.43%)
PYK2	inactive (105.23%)

TK - Fer

Bioactivity
Kinase	RBC
FER	inactive (103.06%)
FES	inactive (97.46%)

TK - FGFR

Bioactivity
Kinase	RBC
FGFR1	inactive (99.53%)
FGFR2	inactive (101.67%)
FGFR3	inactive (106.07%)
FGFR4	inactive (105.31%)

TK - VEGFR

Bioactivity
Kinase	RBC
FLT1	inactive (87.81%)
FLT4	inactive (102.44%)
KDR	inactive (88.29%)

TK - InsR

Bioactivity
Kinase	RBC
IGF1R	inactive (106.71%)
IRR	inactive (96.94%)
INSR	inactive (105.06%)

TK - JakA

Bioactivity
Kinase	RBC
JAK1	inactive (106.88%)
JAK2	inactive (103.67%)
JAK3	inactive (101.21%)
TYK2	inactive (101.96%)

TK - Musk

Bioactivity
Kinase	RBC
MUSK	inactive (103.66%)

TK - Ret

Bioactivity
Kinase	RBC
RET	inactive (97.97%)

TK - Met

Bioactivity
Kinase	RBC
RON	inactive (94.54%)
MET	inactive (109.39%)

TK - Sev

Bioactivity
Kinase	RBC
ROS	inactive (95.79%)

TK - Syk

Bioactivity
Kinase	RBC
SYK	inactive (95.94%)
ZAP70	inactive (93.77%)

TK - Tie

Bioactivity
Kinase	RBC
TIE2	inactive (96.7%)

TK - Trk

Bioactivity
Kinase	RBC
TRKA	inactive (96.99%)
TRKB	inactive (103.54%)
TRKC	inactive (98.65%)

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 (105.03%)
ALK2	inactive (96.93%)
ALK4	inactive (105.69%)
TGFbR1	inactive (100.53%)
TGFbR2	inactive (130.07%)

TKL - RAF

Bioactivity
Kinase	RBC
ARAF	inactive (104.99%)
BRAF	inactive (96.26%)
RAF1	inactive (93.02%)

TKL - IRAK

Bioactivity
Kinase	RBC
IRAK1	inactive (100.55%)
IRAK4	inactive (89.13%)

TKL - LISK

Bioactivity
Kinase	RBC
LIMK1	inactive (92.49%)

TKL - LRRK

Bioactivity
Kinase	RBC
LRRK2	inactive (102.74%)

TKL - MLK

Bioactivity
Kinase	RBC
MLK1	inactive (105.75%)
MLK2	inactive (92.75%)
MLK3	inactive (101.8%)
TAK1	inactive (99.46%)
ZAK	inactive (97.9%)

TKL - RIPK

Bioactivity
Kinase	RBC
RIPK2	inactive (84.78%)

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 (105.22%)
BRSK1	inactive (96.93%)
BRSK2	inactive (100.27%)
CHK1	inactive (110.98%)
LKB1	inactive (99.75%)
MARK1	inactive (99.26%)
MARK3	inactive (87.78%)
MARK4	inactive (99.62%)
MELK	inactive (96.43%)
PASK	inactive (102.71%)
QIK	inactive (92.81%)
NuaK2	inactive (86.7%)
MARK2	inactive (79.44%)

CAMK - CAMK1

Bioactivity
Kinase	RBC
CaMK1a	inactive (98.25%)
CaMK1b	inactive (100.35%)
CaMK1d	inactive (101.52%)
CaMK1g	inactive (98.19%)
CaMK4	inactive (102.61%)

CAMK - CAMK2

Bioactivity
Kinase	RBC
CaMK2a	inactive (89.65%)
CaMK2b	inactive (105.53%)
CaMK2d	inactive (108.6%)
CaMK2g	inactive (103.74%)

CAMK - RAD53

Bioactivity
Kinase	RBC
CHK2	inactive (95.66%)

CAMK - DAPK

Bioactivity
Kinase	RBC
DAPK1	inactive (100.56%)
DAPK2	inactive (133.27%)
DRAK1	inactive (101.28%)
DAPK3	inactive (113.81%)

CAMK - DCAMKL

Bioactivity
Kinase	RBC
DCLK2	inactive (100.22%)

CAMK - MAPKAPK

Bioactivity
Kinase	RBC
MAPKAPK2	inactive (104.53%)
MAPKAPK3	inactive (103.48%)
MAPKAPK5	inactive (73.56%)
MNK1	inactive (135.03%)
MNK2	inactive (84.48%)

CAMK - MLCK

Bioactivity
Kinase	RBC
smMLCK	inactive (99.42%)
skMLCK	inactive (98.08%)

CAMK - PHK

Bioactivity
Kinase	RBC
PHKg1	inactive (96.53%)
PHKg2	inactive (100.5%)

CAMK - PIM

Bioactivity
Kinase	RBC
PIM1	inactive (100.07%)
PIM2	inactive (122.94%)
PIM3	inactive (100.92%)

CAMK - PKD

Bioactivity
Kinase	RBC
PKD1	inactive (104.02%)
PKD3	inactive (88.17%)
PKD2	inactive (95.72%)

CAMK - TSSK

Bioactivity
Kinase	RBC
TSSK1	inactive (103.97%)
TSSK2	inactive (103.19%)

CAMK - STK33

Bioactivity
Kinase	RBC
STK33	inactive (91.51%)

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 (99.14%)
MAP3K2	inactive (108.35%)
MAP3K3	inactive (95.46%)

STE - STE-Unique

Bioactivity
Kinase	RBC
COT	inactive (91.81%)
NIK	inactive (102.35%)

STE - STE20

Bioactivity
Kinase	RBC
GCK	inactive (89.58%)
HGK	inactive (93.72%)
KHS1	inactive (90.39%)
LOK	-
MINK	inactive (95.63%)
MST1	inactive (89.05%)
MST2	inactive (98.18%)
MST3	inactive (86.98%)
MST4	inactive (98.25%)
OSR1	inactive (107.89%)
PAK1	inactive (96.3%)
PAK2	inactive (103.59%)
PAK3	inactive (103.9%)
PAK4	inactive (113.77%)
PAK5	inactive (107.79%)
PAK6	inactive (89.59%)
SLK	inactive (104.43%)
YSK1	inactive (107.43%)
STLK3	inactive (97.29%)
TAO1	inactive (83.11%)
TAO2	inactive (99.17%)
TAO3	inactive (95.35%)
MYO3B	inactive (112.06%)

STE - STE7

Bioactivity
Kinase	RBC
MAP2K1	inactive (76.5%)
MAP2K2	inactive (106.01%)
MAP2K6	inactive (107.32%)

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 (104.5%)
AurB	inactive (103.19%)
AurC	inactive (97.87%)

Other - CAMKK

Bioactivity
Kinase	RBC
CaMKK1	inactive (112.36%)
CaMKK2	inactive (86.12%)

Other - Haspin

Bioactivity
Kinase	RBC
Haspin	inactive (100.8%)

Other - IKK

Bioactivity
Kinase	RBC
IKKa	inactive (101.15%)
IKKb	inactive (100.82%)
IKKe	inactive (99.6%)
TBK1	inactive (97.88%)

Other - NEK

Bioactivity
Kinase	RBC
NEK1	inactive (89.99%)
NEK11	inactive (100.57%)
NEK2	inactive (88.62%)
NEK4	inactive (99.57%)
NEK6	inactive (103.71%)
NEK7	inactive (95.42%)
NEK9	inactive (98.34%)
NEK3	inactive (102.09%)

Other - TOPK

Bioactivity
Kinase	RBC
PBK	inactive (105.88%)

Other - PLK

Bioactivity
Kinase	RBC
PLK1	inactive (97.61%)
PLK2	inactive (96%)
PLK3	inactive (96.62%)

Other - SgK496

Bioactivity
Kinase	RBC
SgK496	inactive (95.44%)

Other - NAK

Bioactivity
Kinase	RBC
MPSK1	inactive (100.21%)

Other - TTK

Bioactivity
Kinase	RBC
TTK	inactive (108.17%)

Other - ULK

Bioactivity
Kinase	RBC
ULK1	inactive (107.4%)
ULK2	inactive (108.2%)
ULK3	inactive (102.24%)

Other - WEE

Bioactivity
Kinase	RBC
Wee1	inactive (93.01%)

Other - WNK

Bioactivity
Kinase	RBC
Wnk2	inactive (108.33%)
Wnk3	inactive (96.41%)

Other - TLK

Bioactivity
Kinase	RBC
TLK2	inactive (117%)

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 (99.42%)
CK1g1	inactive (147.05%)
CK1g2	inactive (99.29%)
CK1g3	inactive (93.45%)
CK1a	inactive (99.25%)
CK1e	inactive (101.86%)

CK1 - VRK

Bioactivity
Kinase	RBC
VRK1	inactive (92.37%)

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 (99.29%)
CK2a2	inactive (100.38%)

CMGC - CLK

Bioactivity
Kinase	RBC
CLK1	inactive (103.12%)
CLK2	inactive (90.71%)
CLK3	inactive (113.52%)
CLK4	inactive (94.11%)

CMGC - DYRK

Bioactivity
Kinase	RBC
DYRK1A	inactive (99.05%)
DYRK1B	inactive (102.92%)
DYRK2	inactive (98.57%)
DYRK3	inactive (95.42%)
DYRK4	inactive (94.11%)
HIPK1	inactive (103.82%)
HIPK2	inactive (104.49%)
HIPK3	inactive (111.94%)
HIPK4	inactive (98.16%)

CMGC - MAPK

Bioactivity
Kinase	RBC
Erk1	inactive (99.28%)
Erk2	inactive (73.64%)
JNK3	inactive (93.56%)
NLK	inactive (104.77%)
p38a	inactive (88.11%)
p38b	inactive (105.46%)
p38d	inactive (105.84%)
p38g	inactive (100.14%)
JNK1	inactive (122.2%)
JNK2	inactive (93.63%)

CMGC - GSK

Bioactivity
Kinase	RBC
GSK3A	inactive (99.76%)
GSK3B	inactive (99.97%)

CMGC - SRPK

Bioactivity
Kinase	RBC
MSSK1	inactive (93.62%)
SRPK1	inactive (102.8%)
SRPK2	inactive (100.28%)

Atypical

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

Atypical - PDHK

Bioactivity
Kinase	RBC
PDHK1	inactive (100.16%)