Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : SB-223133

Inchikey : YNEJNUAUXPCFAS-UHFFFAOYSA-N

ChemSpider : 13469628

Pubchem CID : 22464120

ChEMBL : CHEMBL319988

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

TK

Test Member No. in Family
Family	no. Member on 518kinase	GPCR
JakA	4	4
Fer	2	2
Abl	2	2
Csk	2	1
Tec	5	5
Src	11	10
Eph	14	6
FAK	2	1
Syk	2	2
ALK	2	2
Sev	1	1
InsR	3	3
DDR	2	1
Musk	1	1
Trk	3	3
Met	2	2
Axl	3	3
Ret	1	1
FGFR	4	4
VEGFR	3	3
PDGFR	5	5
Tie	2	1
Ack	2	2
EGFR	4	3

TK - JakA

Bioactivity
Kinase	GPCR
JAK1	inactive (-2.41%)
TYK2	inactive (0.09%)
JAK2	inactive (-0.27%)
JAK3	inactive (2.69%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (19.78%)
FES	inactive (-2.56%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (36.78%)
ABL2	inactive (30.34%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (-0.86%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (3.78%)
BTK	inactive (1.08%)
TXK	inactive (19.23%)
TEC	inactive (5.34%)
ITK	inactive (0.63%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (13.99%)
SRM	inactive (2.5%)
FRK	inactive (5.08%)
BLK	inactive (5.98%)
LCK	inactive (29.17%)
HCK	inactive (12.72%)
FGR	inactive (16.51%)
FYN	inactive (6.58%)
SRC	inactive (18.34%)
YES	inactive (39.99%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (2.11%)
EphA4	inactive (14.48%)
EphA3	inactive (-1.48%)
EphB4	inactive (14.72%)
EphB3	inactive (32.07%)
EphB2	inactive (35.91%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (2.44%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (4.19%)
ZAP70	inactive (1.54%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (0.8%)
ALK	inactive (2.88%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	active (76.38%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (-0.36%)
IGF1R	inactive (-1.17%)
IRR	inactive (-2.71%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (13.32%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (4.37%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (-0.08%)
TRKB	inactive (5.91%)
TRKC	inactive (11.29%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (13.3%)
MET	inactive (3.65%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (6.29%)
MER	inactive (7.13%)
TYRO3	inactive (2.9%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (19.32%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (11.26%)
FGFR2	inactive (1.23%)
FGFR3	inactive (1.39%)
FGFR4	inactive (0.55%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (1.16%)
KDR	inactive (17.24%)
FLT4	inactive (-0.22%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (14.68%)
KIT	inactive (17.1%)
FLT3	inactive (-0.14%)
PDGFRa	inactive (21.61%)
PDGFRb	inactive (30.31%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (4.5%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (0.4%)
TNK1	inactive (8.33%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (35.69%)
ErbB2	inactive (4.64%)
ErbB4	inactive (45.86%)

TKL

Test Member No. in Family
Family	no. Member on 518kinase	GPCR
IRAK	4	1
RAF	5	1

TKL - IRAK

Bioactivity
Kinase	GPCR
IRAK4	inactive (-1%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (-1.06%)

STE

Test Member No. in Family
Family	no. Member on 518kinase	GPCR
STE20	31	12
STE7	7	1

STE - STE20

Bioactivity
Kinase	GPCR
GCK	inactive (16.21%)
MST1	inactive (22.01%)
MST2	inactive (14.6%)
MST4	inactive (4.04%)
HGK	active (72.85%)
MINK	active (62.41%)
LOK	inactive (9.11%)
PAK1	inactive (-3.74%)
PAK3	inactive (-3.59%)
PAK2	inactive (-0.18%)
PAK5	inactive (0.21%)
PAK6	inactive (-1.54%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (-3.2%)

CK1

Test Member No. in Family
Family	no. Member on 518kinase	GPCR
CK1	7	4

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	active (90.07%)
CK1g2	inactive (3.41%)
CK1g1	inactive (5.79%)
CK1g3	inactive (10.81%)

Other

Test Member No. in Family
Family	no. Member on 518kinase	GPCR
PLK	4	1
Aur	3	3
NEK	11	5
IKK	4	4
TTK	1	1

Other - PLK

Bioactivity
Kinase	GPCR
PLK1	inactive (-1.2%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (4.15%)
AurC	inactive (-2.2%)
AurA	inactive (22.01%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (0.03%)
NEK2	inactive (-3.67%)
NEK9	inactive (-1.68%)
NEK7	inactive (-4.78%)
NEK6	inactive (-1.66%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (1.41%)
IKKe	inactive (-2.64%)
IKKb	inactive (-1.66%)
IKKa	inactive (5.56%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (-0.22%)

AGC

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

AGC - GRK

Bioactivity
Kinase	GPCR
GPRK7	inactive (-1.89%)
GPRK6	inactive (-1.92%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (1.62%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (-0.24%)
MSK2	inactive (-0.73%)
RSK1	inactive (2.78%)
RSK2	inactive (-0.98%)
RSK4	inactive (3.39%)
RSK3	inactive (0.59%)
p70S6K	inactive (-1.84%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (-1.44%)
AKT1	inactive (-1.14%)
AKT3	inactive (0.5%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (-1.85%)
SGK3	inactive (1.61%)
SGK2	inactive (7.09%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (-1.04%)
PKCg	inactive (2.37%)
PKCa	inactive (10.25%)
PKCt	inactive (0.4%)
PKCi	inactive (0.01%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (-0.24%)
PKG1	inactive (0.27%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (-0.96%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (0.73%)
ROCK2	inactive (-1.96%)
MRCKb	inactive (0.56%)
MRCKa	inactive (-0.81%)

CAMK

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

CAMK - RAD53

Bioactivity
Kinase	GPCR
CHK2	inactive (-1.72%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (5.59%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-0.1%)
CaMK1d	inactive (-0.75%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (0.55%)
PHKg2	inactive (-5.93%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (1.53%)
CaMK2a	inactive (-3.25%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (-0.32%)
MAPKAPK2	inactive (-1.57%)
MAPKAPK3	inactive (36.42%)
MNK2	inactive (0.46%)
MNK1	inactive (0.48%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (19.45%)
PKD1	inactive (18.51%)
PKD2	inactive (23.29%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (1.28%)
MARK3	inactive (0.22%)
MARK1	inactive (0.51%)
QIK	inactive (28.63%)
SIK	inactive (4.75%)
NuaK1	inactive (39.86%)
BRSK1	inactive (1.44%)
BRSK2	inactive (1.19%)
MELK	inactive (1.19%)
CHK1	inactive (0.13%)
PASK	inactive (-1.02%)
AMPKa1	inactive (0.93%)
AMPKa2	inactive (-1.6%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (-0.41%)
TSSK1	inactive (-1.96%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (-0.38%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (0.53%)
PIM3	inactive (0.35%)
PIM1	inactive (-1.37%)

CMGC

Test Member No. in Family
Family	no. Member on 518kinase	GPCR
MAPK	14	6
GSK	2	2
SRPK	3	2
CLK	4	2
DYRK	10	5
CK2	3	1

CMGC - MAPK

Bioactivity
Kinase	GPCR
JNK2	active (53.33%)
p38a	active (92.52%)
p38b	active (62.18%)
p38d	inactive (-2.89%)
Erk2	inactive (-2.72%)
Erk1	-

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (5.67%)
GSK3B	inactive (14.12%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (4.67%)
MSSK1	inactive (0.84%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (3.28%)
CLK2	inactive (0.55%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (4%)
HIPK4	inactive (3.26%)
DYRK1B	inactive (5.6%)
DYRK1A	inactive (5.97%)
DYRK2	inactive (-2.78%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (1.03%)