Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW809897X

Inchikey : NXPQZPWXVHIWGN-UHFFFAOYSA-N

ChemSpider : 4486982

Pubchem CID : 5329831

ChEMBL : CHEMBL189353

	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 (19.67%)
TYK2	inactive (1.51%)
JAK2	inactive (20.68%)
JAK3	inactive (2.77%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	active (77.16%)
FES	inactive (22.52%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	active (53.07%)
ABL2	active (55.1%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (19.48%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	active (73.49%)
BTK	inactive (26.49%)
TXK	inactive (21.15%)
TEC	inactive (21.36%)
ITK	active (71.06%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (43.97%)
SRM	inactive (3.99%)
FRK	inactive (14.5%)
BLK	active (75.01%)
LCK	active (61.22%)
HCK	inactive (48.88%)
FGR	active (51.88%)
FYN	inactive (12.43%)
SRC	active (65.38%)
YES	inactive (28.16%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (7.74%)
EphA4	inactive (33.79%)
EphA3	inactive (7.13%)
EphB4	inactive (8.72%)
EphB3	inactive (4.62%)
EphB2	inactive (27.33%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (29.68%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-9.25%)
ZAP70	inactive (9.82%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (1.45%)
ALK	inactive (4.6%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (33.46%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (3.45%)
IGF1R	inactive (4.63%)
IRR	inactive (4.71%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (26.93%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	active (89.93%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	active (68.74%)
TRKB	active (55.43%)
TRKC	active (88.6%)

TK - Met

Bioactivity
Kinase	GPCR
RON	active (82.1%)
MET	active (85.01%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (28.56%)
MER	inactive (29.63%)
TYRO3	inactive (17.44%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (48.65%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (-0.4%)
FGFR2	inactive (13.36%)
FGFR3	inactive (5.59%)
FGFR4	inactive (2.06%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	active (51.01%)
KDR	active (56.31%)
FLT4	inactive (41.67%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	active (96.15%)
KIT	active (95.92%)
FLT3	active (84.92%)
PDGFRa	active (86.57%)
PDGFRb	active (77.68%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	active (72.13%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (4.21%)
TNK1	active (84.08%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (5.8%)
ErbB2	inactive (7.2%)
ErbB4	inactive (17.07%)

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 (1.26%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (4.11%)

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 (32.85%)
MST1	inactive (17.39%)
MST2	inactive (11.46%)
MST4	inactive (-3.71%)
HGK	active (73.42%)
MINK	active (64.51%)
LOK	active (86.48%)
PAK1	inactive (2.17%)
PAK3	inactive (1.38%)
PAK2	inactive (1.61%)
PAK5	inactive (11.93%)
PAK6	inactive (0.99%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (5.34%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (1.15%)
CK1g2	inactive (0.63%)
CK1g1	inactive (1.32%)
CK1g3	inactive (-1.25%)

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 (0.37%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	active (84.19%)
AurC	active (104.02%)
AurA	active (97.62%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (1.93%)
NEK2	inactive (1.07%)
NEK9	inactive (-6.03%)
NEK7	inactive (1.59%)
NEK6	inactive (1.86%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (8.89%)
IKKe	inactive (8.6%)
IKKb	inactive (2.65%)
IKKa	inactive (-10.05%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (19.44%)

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 (1.55%)
GPRK6	inactive (3.8%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (22.19%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (4.25%)
MSK2	inactive (4.1%)
RSK1	inactive (4.66%)
RSK2	inactive (3.81%)
RSK4	inactive (1.06%)
RSK3	inactive (1.78%)
p70S6K	inactive (2.4%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (2.1%)
AKT1	inactive (1.09%)
AKT3	inactive (-0.15%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (7.64%)
SGK3	inactive (4.02%)
SGK2	inactive (22.78%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (3.8%)
PKCg	inactive (6.65%)
PKCa	inactive (2.02%)
PKCt	inactive (3.24%)
PKCi	inactive (1.5%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (3.22%)
PKG1	inactive (3.77%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (3.64%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (2.01%)
ROCK2	inactive (9.15%)
MRCKb	inactive (0.92%)
MRCKa	inactive (2.97%)

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 (16.8%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (4.12%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-4.21%)
CaMK1d	inactive (-0.13%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (8.06%)
PHKg2	inactive (6.5%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (-0.38%)
CaMK2a	inactive (2.73%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (1.46%)
MAPKAPK2	inactive (1.08%)
MAPKAPK3	inactive (0.31%)
MNK2	inactive (45.59%)
MNK1	inactive (27.91%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (0.38%)
PKD1	inactive (1.18%)
PKD2	inactive (2%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (12.76%)
MARK3	inactive (13.27%)
MARK1	inactive (10.8%)
QIK	inactive (10.16%)
SIK	inactive (13.31%)
NuaK1	inactive (30.19%)
BRSK1	inactive (9.78%)
BRSK2	inactive (8.66%)
MELK	inactive (3.32%)
CHK1	inactive (4.63%)
PASK	inactive (2.77%)
AMPKa1	inactive (3.05%)
AMPKa2	inactive (3.21%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (1.93%)
TSSK1	inactive (3.33%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (4.43%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (0.1%)
PIM3	inactive (3.85%)
PIM1	inactive (0.34%)

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 (8.85%)
p38a	inactive (3.34%)
p38b	inactive (4.6%)
p38d	inactive (1.46%)
Erk2	inactive (2.83%)
Erk1	inactive (4.66%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (10.04%)
GSK3B	inactive (9.63%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (2.16%)
MSSK1	inactive (2.4%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (1.23%)
CLK2	inactive (5.49%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (5.39%)
HIPK4	inactive (18.42%)
DYRK1B	inactive (1.52%)
DYRK1A	inactive (0.63%)
DYRK2	inactive (1.29%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (6.66%)