Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW795493X

Inchikey : LSVIBAPJYUUVJJ-UHFFFAOYSA-N

ChemSpider : 23307382

Pubchem CID : 23646938

ChEMBL : CHEMBL273564

	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 (11.78%)
TYK2	inactive (-3.79%)
JAK2	inactive (9.83%)
JAK3	inactive (-2.01%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (33.57%)
FES	inactive (4.91%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	active (55.8%)
ABL2	active (64.69%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (44.37%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	active (71.31%)
BTK	inactive (6.68%)
TXK	inactive (5.17%)
TEC	inactive (5.89%)
ITK	inactive (12.3%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (7.46%)
SRM	inactive (-3.07%)
FRK	inactive (21.22%)
BLK	inactive (49.1%)
LCK	inactive (46.68%)
HCK	inactive (48.75%)
FGR	inactive (25.13%)
FYN	inactive (19.91%)
SRC	active (52.8%)
YES	inactive (45.73%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	active (84.99%)
EphA4	active (78.27%)
EphA3	active (50.59%)
EphB4	active (84.37%)
EphB3	active (68.25%)
EphB2	active (78.22%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (32.31%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-18.37%)
ZAP70	inactive (1.43%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (47.14%)
ALK	inactive (21.78%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (21.74%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (10.5%)
IGF1R	inactive (15.53%)
IRR	inactive (5.07%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	active (79.19%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	active (90.17%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	active (96.46%)
TRKB	active (91.1%)
TRKC	active (88.93%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (27.7%)
MET	inactive (28.97%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (45.32%)
MER	inactive (31.62%)
TYRO3	inactive (32.18%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	active (87.16%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (38.21%)
FGFR2	active (52.55%)
FGFR3	inactive (34.42%)
FGFR4	inactive (13.26%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	active (91.04%)
KDR	active (77.3%)
FLT4	active (99.57%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	active (77.99%)
KIT	active (97.34%)
FLT3	active (93.93%)
PDGFRa	active (93.11%)
PDGFRb	active (94.81%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	active (74.38%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (1.54%)
TNK1	active (52.81%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (7.97%)
ErbB2	inactive (3.75%)
ErbB4	inactive (15.21%)

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 (2.34%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (13.26%)

STE

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

STE - STE20

Bioactivity
Kinase	GPCR
GCK	active (59.25%)
MST1	inactive (15.6%)
MST2	inactive (13.3%)
MST4	inactive (-4.13%)
HGK	inactive (12.26%)
MINK	inactive (8.17%)
LOK	active (67.86%)
PAK1	inactive (5.2%)
PAK3	inactive (5.54%)
PAK2	inactive (1.5%)
PAK5	inactive (3.35%)
PAK6	inactive (-2.37%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (4.91%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (5.6%)
CK1g2	inactive (7.31%)
CK1g1	inactive (10.08%)
CK1g3	inactive (10.3%)

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 (5.99%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	active (66.66%)
AurC	active (88.77%)
AurA	active (60.37%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (41.87%)
NEK2	inactive (7.21%)
NEK9	inactive (17.86%)
NEK7	inactive (-0.46%)
NEK6	inactive (1.33%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (4.59%)
IKKe	inactive (9.66%)
IKKb	inactive (7.53%)
IKKa	inactive (11.13%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (18.14%)

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 (4.95%)
GPRK6	inactive (0.47%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (2.33%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (19.53%)
MSK2	inactive (20.82%)
RSK1	inactive (33.82%)
RSK2	inactive (26.13%)
RSK4	inactive (9.85%)
RSK3	active (52.93%)
p70S6K	active (73.52%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (2.15%)
AKT1	inactive (0.96%)
AKT3	inactive (2.7%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (3.96%)
SGK3	inactive (2.94%)
SGK2	inactive (4.73%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (6.96%)
PKCg	inactive (2.18%)
PKCa	inactive (1.68%)
PKCt	inactive (2.66%)
PKCi	inactive (3.34%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (3.85%)
PKG1	inactive (1.94%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (3.42%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (18.97%)
ROCK2	inactive (46.85%)
MRCKb	inactive (1.21%)
MRCKa	inactive (0.21%)

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 (6.09%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (1.61%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (4.17%)
CaMK1d	inactive (7.97%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (10.25%)
PHKg2	inactive (4.64%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (2.75%)
CaMK2a	inactive (1.03%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (1.36%)
MAPKAPK2	inactive (3.15%)
MAPKAPK3	inactive (20.66%)
MNK2	active (53.91%)
MNK1	inactive (38.7%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (5.91%)
PKD1	inactive (7.85%)
PKD2	inactive (4.09%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (4.23%)
MARK3	inactive (5.23%)
MARK1	inactive (8.44%)
QIK	inactive (3.6%)
SIK	inactive (9.69%)
NuaK1	inactive (8.04%)
BRSK1	inactive (10.17%)
BRSK2	inactive (9.75%)
MELK	inactive (-13.98%)
CHK1	inactive (5.24%)
PASK	inactive (0.31%)
AMPKa1	inactive (5.16%)
AMPKa2	inactive (5.34%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (2.55%)
TSSK1	inactive (4.9%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (4.16%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (0.72%)
PIM3	inactive (0.9%)
PIM1	inactive (2.28%)

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 (14.47%)
p38a	inactive (43.38%)
p38b	inactive (40.98%)
p38d	inactive (19.28%)
Erk2	inactive (6.77%)
Erk1	inactive (3.6%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (9.54%)
GSK3B	inactive (11.02%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (18.52%)
MSSK1	active (62.45%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (-31.39%)
CLK2	inactive (2.59%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (37.39%)
HIPK4	active (78.34%)
DYRK1B	inactive (1.94%)
DYRK1A	inactive (6.79%)
DYRK2	inactive (2.85%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (4.76%)