Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW429374A

Inchikey : FIGCSMLMEFLPMM-UHFFFAOYSA-N

ChemSpider : 26639368

Pubchem CID : 56667992

ChEMBL : CHEMBL1794050

	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 (1.97%)
TYK2	inactive (6.13%)
JAK2	inactive (3.68%)
JAK3	inactive (15.85%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (9.05%)
FES	inactive (2.85%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (8.78%)
ABL2	inactive (5.72%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (-1.69%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (4.31%)
BTK	inactive (1.61%)
TXK	inactive (6.14%)
TEC	inactive (8.99%)
ITK	inactive (2.67%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (10.7%)
SRM	active (57.94%)
FRK	inactive (5.49%)
BLK	inactive (10.78%)
LCK	inactive (13.25%)
HCK	inactive (11.12%)
FGR	inactive (7.55%)
FYN	inactive (10.48%)
SRC	inactive (12.11%)
YES	inactive (5.79%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (0.76%)
EphA4	inactive (5.16%)
EphA3	inactive (3.94%)
EphB4	inactive (3.11%)
EphB3	inactive (2.28%)
EphB2	inactive (11.03%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (9.16%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-2.96%)
ZAP70	inactive (-8.3%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (22.96%)
ALK	inactive (9.22%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (18.32%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (0.1%)
IGF1R	inactive (4.14%)
IRR	inactive (2.51%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (5.97%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (5.67%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (12.84%)
TRKB	inactive (12.17%)
TRKC	inactive (24.08%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (8.32%)
MET	inactive (5.75%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-2.44%)
MER	inactive (2.23%)
TYRO3	inactive (9.95%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (7.95%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (1.74%)
FGFR2	inactive (5.51%)
FGFR3	inactive (8.18%)
FGFR4	inactive (3.07%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (2.06%)
KDR	inactive (10.05%)
FLT4	inactive (4.42%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (7.78%)
KIT	inactive (3.66%)
FLT3	inactive (7.91%)
PDGFRa	inactive (20.18%)
PDGFRb	-

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (2.63%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (3.05%)
TNK1	active (80.57%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (5.08%)
ErbB2	inactive (4.88%)
ErbB4	inactive (14.86%)

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 (4.22%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (18.29%)

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 (2.93%)
MST1	inactive (39.59%)
MST2	inactive (37.31%)
MST4	inactive (36.04%)
HGK	active (91.6%)
MINK	active (81.56%)
LOK	inactive (3.51%)
PAK1	inactive (6.31%)
PAK3	inactive (4.77%)
PAK2	inactive (2.17%)
PAK5	inactive (-0.35%)
PAK6	inactive (7.69%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (5.62%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (3.87%)
CK1g2	inactive (4.44%)
CK1g1	inactive (4.74%)
CK1g3	inactive (3.74%)

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 (7.7%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (15.97%)
AurC	inactive (31.67%)
AurA	active (88.35%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (0.46%)
NEK2	inactive (2.79%)
NEK9	inactive (0.27%)
NEK7	inactive (4.87%)
NEK6	inactive (0.55%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (7.51%)
IKKe	active (92.13%)
IKKb	inactive (2.14%)
IKKa	inactive (7.66%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (7.48%)

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	active (60.3%)
GPRK6	inactive (46.13%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (7.6%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (3.39%)
MSK2	inactive (2.67%)
RSK1	inactive (2.73%)
RSK2	inactive (-1.29%)
RSK4	inactive (5.51%)
RSK3	inactive (3.66%)
p70S6K	inactive (2.15%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (2.84%)
AKT1	inactive (2.74%)
AKT3	inactive (1.67%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (3.05%)
SGK3	inactive (2%)
SGK2	inactive (6.41%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (0.7%)
PKCg	inactive (6.29%)
PKCa	inactive (2.45%)
PKCt	inactive (2.57%)
PKCi	inactive (3.35%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (4.63%)
PKG1	inactive (11%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (-0.22%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (4.77%)
ROCK2	inactive (7.43%)
MRCKb	inactive (1.01%)
MRCKa	inactive (-0.62%)

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 (8.93%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (0.92%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-0.48%)
CaMK1d	inactive (4.01%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (9.21%)
PHKg2	inactive (-0.09%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (7.6%)
CaMK2a	inactive (5.84%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (0.45%)
MAPKAPK2	inactive (1.49%)
MAPKAPK3	inactive (2.92%)
MNK2	inactive (35.97%)
MNK1	inactive (12.73%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (5.23%)
PKD1	inactive (4.25%)
PKD2	inactive (4.38%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (3.53%)
MARK3	inactive (6.43%)
MARK1	inactive (9.1%)
QIK	inactive (-0.16%)
SIK	inactive (4.86%)
NuaK1	inactive (4.71%)
BRSK1	inactive (4.37%)
BRSK2	inactive (2.32%)
MELK	inactive (10.43%)
CHK1	inactive (0.96%)
PASK	inactive (1.32%)
AMPKa1	inactive (3.3%)
AMPKa2	inactive (7.03%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (-0.14%)
TSSK1	inactive (1.29%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (-6.21%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (46.51%)
PIM3	inactive (49.04%)
PIM1	inactive (37.63%)

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 (3.04%)
p38a	inactive (7.67%)
p38b	inactive (1.36%)
p38d	inactive (3.3%)
Erk2	inactive (3.37%)
Erk1	inactive (1.77%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (26.14%)
GSK3B	inactive (21.39%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-2.45%)
MSSK1	inactive (1.95%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (38.62%)
CLK2	active (84.59%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (22.36%)
HIPK4	inactive (13.83%)
DYRK1B	inactive (46.7%)
DYRK1A	active (63.48%)
DYRK2	inactive (15.5%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (14.51%)