Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW673715X

Inchikey : IDBPJJQGJZOVMW-UHFFFAOYSA-N

ChemSpider : 8336283

Pubchem CID : 10160775

ChEMBL : CHEMBL243907

	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 (1.27%)
TYK2	inactive (-2.46%)
JAK2	inactive (4.62%)
JAK3	inactive (1.13%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (1.84%)
FES	inactive (0.62%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (23.75%)
ABL2	inactive (44.77%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (3.75%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (1.67%)
BTK	inactive (1.57%)
TXK	inactive (5.13%)
TEC	inactive (3.91%)
ITK	inactive (1.87%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (1.76%)
SRM	inactive (1.28%)
FRK	inactive (2.98%)
BLK	inactive (0.6%)
LCK	inactive (8.47%)
HCK	inactive (7.28%)
FGR	inactive (5.18%)
FYN	inactive (4.72%)
SRC	inactive (5.84%)
YES	inactive (-1.93%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	active (65.73%)
EphA4	active (72.35%)
EphA3	inactive (10.08%)
EphB4	inactive (27.48%)
EphB3	inactive (3.66%)
EphB2	active (62.99%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (8.1%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-0.99%)
ZAP70	inactive (-1.32%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (0.04%)
ALK	inactive (3.68%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (0.49%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (0.47%)
IGF1R	inactive (2.45%)
IRR	inactive (3.39%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	active (80.25%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (31.15%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (43.73%)
TRKB	inactive (30.67%)
TRKC	inactive (30.31%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (5.62%)
MET	inactive (27.41%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (25.52%)
MER	inactive (3.11%)
TYRO3	inactive (21.38%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	active (79.88%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (3.26%)
FGFR2	inactive (8.89%)
FGFR3	inactive (6.95%)
FGFR4	inactive (-0.63%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (43.83%)
KDR	active (66.82%)
FLT4	inactive (16.26%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	active (54.63%)
KIT	active (93.05%)
FLT3	inactive (48.04%)
PDGFRa	active (96.81%)
PDGFRb	active (56.33%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	active (55.68%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (1.35%)
TNK1	inactive (13.82%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (7.33%)
ErbB2	inactive (7%)
ErbB4	inactive (15.29%)

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 (1.04%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (12.22%)

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 (5.21%)
MST1	inactive (8.88%)
MST2	inactive (4.89%)
MST4	inactive (2.74%)
HGK	inactive (3.37%)
MINK	inactive (3.01%)
LOK	active (57.82%)
PAK1	inactive (2.79%)
PAK3	inactive (2.93%)
PAK2	inactive (0.26%)
PAK5	inactive (-2.14%)
PAK6	inactive (1.29%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (1.44%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (0.76%)
CK1g2	inactive (0.48%)
CK1g1	inactive (0.85%)
CK1g3	inactive (2.93%)

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 (1.1%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (15.58%)
AurC	inactive (37.45%)
AurA	inactive (8.38%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (1.24%)
NEK2	inactive (1.1%)
NEK9	inactive (3.95%)
NEK7	inactive (-2.89%)
NEK6	inactive (3.24%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (0.79%)
IKKe	inactive (3.32%)
IKKb	inactive (2.83%)
IKKa	inactive (-0.97%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (6.45%)

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 (15.58%)
GPRK6	inactive (2.68%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (1.09%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (-1.65%)
MSK2	inactive (1.3%)
RSK1	inactive (1.59%)
RSK2	inactive (0.96%)
RSK4	inactive (1.25%)
RSK3	inactive (1.5%)
p70S6K	inactive (5.19%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.45%)
AKT1	inactive (0.06%)
AKT3	inactive (-0.71%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (1.59%)
SGK3	inactive (3.61%)
SGK2	inactive (-0.81%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (2.14%)
PKCg	inactive (2%)
PKCa	inactive (0.72%)
PKCt	inactive (1.12%)
PKCi	inactive (-1.58%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (0.86%)
PKG1	inactive (3.08%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (3.18%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (18.3%)
ROCK2	inactive (8.2%)
MRCKb	inactive (0.65%)
MRCKa	inactive (2.04%)

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 (-2.63%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (1.42%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-2.32%)
CaMK1d	inactive (1.18%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (2.94%)
PHKg2	inactive (3.57%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (2.63%)
CaMK2a	inactive (3.77%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (0.96%)
MAPKAPK2	inactive (-1.61%)
MAPKAPK3	inactive (-3.85%)
MNK2	inactive (12.21%)
MNK1	inactive (15.75%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (0.75%)
PKD1	inactive (1.01%)
PKD2	inactive (1.88%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (-1.15%)
MARK3	inactive (3.47%)
MARK1	inactive (0.31%)
QIK	inactive (0.48%)
SIK	inactive (2.27%)
NuaK1	inactive (4.18%)
BRSK1	inactive (0.32%)
BRSK2	inactive (5.96%)
MELK	inactive (2.29%)
CHK1	inactive (-6.72%)
PASK	inactive (1.44%)
AMPKa1	inactive (0.41%)
AMPKa2	inactive (-0.72%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (1.72%)
TSSK1	inactive (1.11%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (-5.23%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (-0.24%)
PIM3	inactive (3.52%)
PIM1	inactive (0.49%)

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 (1.01%)
p38a	inactive (3.05%)
p38b	inactive (6.14%)
p38d	inactive (0.33%)
Erk2	inactive (0.03%)
Erk1	inactive (2.79%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (4.83%)
GSK3B	inactive (6.49%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (1.37%)
MSSK1	inactive (2.28%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (0.82%)
CLK2	inactive (1.38%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (4.9%)
HIPK4	inactive (13.88%)
DYRK1B	inactive (1.1%)
DYRK1A	inactive (1.26%)
DYRK2	inactive (1.13%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (4.86%)