Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW612286X

Inchikey : SQQAPOSROFWHIB-UHFFFAOYSA-N

ChemSpider : 7998359

Pubchem CID : 9822610

ChEMBL : CHEMBL479079

	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	active (66.54%)
TYK2	inactive (33.27%)
JAK2	active (72.46%)
JAK3	inactive (27.75%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (36.09%)
FES	inactive (10.57%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	active (69.74%)
ABL2	active (69.87%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	active (67.92%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	active (64.78%)
BTK	inactive (34.93%)
TXK	active (61.88%)
TEC	active (63.12%)
ITK	inactive (7.07%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	active (55.42%)
SRM	inactive (12.59%)
FRK	inactive (11.51%)
BLK	active (69.3%)
LCK	active (82.39%)
HCK	active (67.74%)
FGR	active (57.46%)
FYN	active (85.44%)
SRC	active (92.08%)
YES	active (70.69%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	active (71.05%)
EphA4	active (75.18%)
EphA3	inactive (15.26%)
EphB4	active (54.84%)
EphB3	inactive (0.24%)
EphB2	active (65.53%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	active (84.35%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (42.8%)
ZAP70	inactive (32.67%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (33.3%)
ALK	inactive (39.29%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	active (70%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	active (64.7%)
IGF1R	active (76.8%)
IRR	inactive (3.74%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (43.06%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	active (72.48%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	active (64.07%)
TRKB	inactive (40.96%)
TRKC	inactive (17.28%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (34.43%)
MET	inactive (12.3%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (1.16%)
MER	inactive (14.42%)
TYRO3	inactive (27.93%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	active (84.05%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (24.79%)
FGFR2	inactive (39.78%)
FGFR3	inactive (30.51%)
FGFR4	inactive (2.48%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	active (87.99%)
KDR	active (72.47%)
FLT4	active (105.58%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	active (94.06%)
KIT	active (95.8%)
FLT3	active (90.35%)
PDGFRa	active (91.57%)
PDGFRb	active (87.53%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (49.76%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	active (52.89%)
TNK1	active (77.34%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (22.18%)
ErbB2	inactive (0.32%)
ErbB4	inactive (27.61%)

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 (6.36%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (9.2%)

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 (7.42%)
MST1	inactive (7.86%)
MST2	inactive (6.19%)
MST4	inactive (3%)
HGK	inactive (12.39%)
MINK	inactive (11.04%)
LOK	active (77.6%)
PAK1	inactive (7.51%)
PAK3	inactive (5.23%)
PAK2	inactive (3.21%)
PAK5	inactive (15.33%)
PAK6	inactive (-1.27%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (4.1%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (0.47%)
CK1g2	inactive (9.2%)
CK1g1	inactive (1.23%)
CK1g3	inactive (-0.68%)

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 (4.34%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (24.21%)
AurC	active (79.7%)
AurA	active (66.52%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (7.77%)
NEK2	inactive (0.41%)
NEK9	inactive (5.56%)
NEK7	inactive (2.17%)
NEK6	inactive (-0.68%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (26.33%)
IKKe	inactive (12.92%)
IKKb	inactive (16.97%)
IKKa	inactive (-0.92%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (8.41%)

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 (-1.95%)
GPRK6	inactive (-4.13%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (4.89%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (2.96%)
MSK2	inactive (2.58%)
RSK1	inactive (-0.01%)
RSK2	inactive (0.03%)
RSK4	inactive (2.74%)
RSK3	inactive (0.74%)
p70S6K	inactive (1.09%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.19%)
AKT1	inactive (1.09%)
AKT3	inactive (1.18%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (5.3%)
SGK3	inactive (1.07%)
SGK2	inactive (-0.14%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (-1.03%)
PKCg	inactive (5.39%)
PKCa	inactive (10.24%)
PKCt	inactive (-0.29%)
PKCi	inactive (3.92%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (2.71%)
PKG1	inactive (3.61%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (-0.26%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (7.47%)
ROCK2	inactive (12.08%)
MRCKb	inactive (1.78%)
MRCKa	inactive (-0.15%)

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 (9.02%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (2.5%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (4.68%)
CaMK1d	inactive (6.21%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (5.26%)
PHKg2	inactive (0.52%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (3.54%)
CaMK2a	inactive (4.38%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (-1.77%)
MAPKAPK2	inactive (0.86%)
MAPKAPK3	inactive (1.36%)
MNK2	inactive (19.23%)
MNK1	inactive (13.47%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (2.54%)
PKD1	inactive (2.11%)
PKD2	inactive (2.94%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (8%)
MARK3	inactive (9.39%)
MARK1	inactive (8.82%)
QIK	inactive (28.01%)
SIK	active (51.17%)
NuaK1	inactive (35.5%)
BRSK1	inactive (3.29%)
BRSK2	inactive (1.97%)
MELK	inactive (8.73%)
CHK1	inactive (3.35%)
PASK	inactive (0.33%)
AMPKa1	inactive (1.71%)
AMPKa2	inactive (5.95%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (-0.95%)
TSSK1	inactive (12.61%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (2.65%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (1.57%)
PIM3	inactive (-0.7%)
PIM1	inactive (1.26%)

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	inactive (13.63%)
p38a	inactive (10.03%)
p38b	inactive (6.13%)
p38d	inactive (4.71%)
Erk2	inactive (3.16%)
Erk1	inactive (2.18%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (17.3%)
GSK3B	inactive (16.09%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-3.51%)
MSSK1	inactive (0.79%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (6.44%)
CLK2	inactive (2.36%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (1.88%)
HIPK4	inactive (3.91%)
DYRK1B	inactive (5.43%)
DYRK1A	inactive (7.54%)
DYRK2	inactive (4.25%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (0.29%)