Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW743024X

Inchikey : HNOVOESCCUJDRT-UHFFFAOYSA-N

ChemSpider : 24698388

Pubchem CID : 44593640

ChEMBL : CHEMBL477583

	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 (2.95%)
TYK2	inactive (-0.16%)
JAK2	inactive (-1.25%)
JAK3	inactive (-0.47%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (-0.39%)
FES	inactive (1.55%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (1.49%)
ABL2	inactive (2.36%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (0.18%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (1.66%)
BTK	inactive (0.35%)
TXK	inactive (2.18%)
TEC	inactive (3.18%)
ITK	inactive (1.05%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (4.58%)
SRM	inactive (-2.77%)
FRK	inactive (2.51%)
BLK	inactive (3.07%)
LCK	inactive (3.87%)
HCK	inactive (5.55%)
FGR	inactive (3.07%)
FYN	inactive (1.16%)
SRC	inactive (4.32%)
YES	inactive (1.5%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-0.44%)
EphA4	inactive (6.13%)
EphA3	inactive (2.02%)
EphB4	inactive (0.82%)
EphB3	inactive (3.35%)
EphB2	inactive (5.88%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (-0.07%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-2.99%)
ZAP70	inactive (1.63%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (3.16%)
ALK	inactive (4.11%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (-0.03%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (3.42%)
IGF1R	inactive (1.25%)
IRR	inactive (0.32%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (2.43%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (1.19%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (1.15%)
TRKB	inactive (1.82%)
TRKC	inactive (0.07%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (-3.5%)
MET	inactive (0.85%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-2.93%)
MER	inactive (1.81%)
TYRO3	inactive (3.21%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (0.04%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (3.99%)
FGFR2	inactive (3.44%)
FGFR3	inactive (5.14%)
FGFR4	inactive (1.63%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (8.07%)
KDR	active (62.01%)
FLT4	inactive (6.22%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (2.71%)
KIT	inactive (0.22%)
FLT3	inactive (0.9%)
PDGFRa	inactive (4.97%)
PDGFRb	inactive (-0.8%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (3.38%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (0.64%)
TNK1	inactive (5.38%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (6.36%)
ErbB2	inactive (5.7%)
ErbB4	inactive (10.58%)

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%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (2.28%)

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 (0.39%)
MST1	inactive (2.08%)
MST2	inactive (4.5%)
MST4	inactive (-2.75%)
HGK	inactive (1.38%)
MINK	inactive (1.4%)
LOK	inactive (5.18%)
PAK1	inactive (4.54%)
PAK3	inactive (1.14%)
PAK2	inactive (-1.68%)
PAK5	inactive (2.58%)
PAK6	inactive (-2.77%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (2.27%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (1.47%)
CK1g2	inactive (3.57%)
CK1g1	inactive (3.5%)
CK1g3	inactive (2.71%)

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 (-0.9%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (4.85%)
AurC	inactive (1%)
AurA	inactive (2.57%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (0.36%)
NEK2	inactive (3.48%)
NEK9	inactive (4.64%)
NEK7	inactive (1.16%)
NEK6	inactive (0.14%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (0.72%)
IKKe	inactive (2.47%)
IKKb	inactive (3.86%)
IKKa	inactive (7.23%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (4.41%)

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 (-1.36%)
GPRK6	inactive (1.27%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (-1.28%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (-1.39%)
MSK2	inactive (-0.44%)
RSK1	inactive (0.4%)
RSK2	inactive (0.11%)
RSK4	inactive (-0.14%)
RSK3	inactive (1.72%)
p70S6K	inactive (-1.48%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.23%)
AKT1	inactive (0.55%)
AKT3	inactive (1.87%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (0.73%)
SGK3	inactive (3.98%)
SGK2	inactive (-0.89%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (3.88%)
PKCg	inactive (-0.41%)
PKCa	inactive (0.82%)
PKCt	inactive (0.76%)
PKCi	inactive (-0.02%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (1.02%)
PKG1	inactive (1.09%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (0.55%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (-0.4%)
ROCK2	inactive (-1.14%)
MRCKb	inactive (-1.77%)
MRCKa	inactive (-2.81%)

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 (1.43%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (-0.45%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-1.43%)
CaMK1d	inactive (-1.53%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (1.73%)
PHKg2	inactive (3.24%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (-0.48%)
CaMK2a	inactive (-3.72%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (0.83%)
MAPKAPK2	inactive (-0.32%)
MAPKAPK3	inactive (30.93%)
MNK2	inactive (2.22%)
MNK1	inactive (4.75%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (2.95%)
PKD1	inactive (2.32%)
PKD2	inactive (3.55%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (0.19%)
MARK3	inactive (1.79%)
MARK1	inactive (1.39%)
QIK	inactive (5.33%)
SIK	inactive (0.11%)
NuaK1	inactive (-0.78%)
BRSK1	inactive (0.43%)
BRSK2	inactive (0.95%)
MELK	inactive (-0.33%)
CHK1	inactive (1.01%)
PASK	inactive (0.47%)
AMPKa1	inactive (1.06%)
AMPKa2	inactive (1.09%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (1.22%)
TSSK1	inactive (3.27%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (4.7%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (0.6%)
PIM3	inactive (-0.9%)
PIM1	inactive (0.47%)

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 (2.57%)
p38a	active (79.16%)
p38b	active (61.16%)
p38d	inactive (0.81%)
Erk2	inactive (3.37%)
Erk1	inactive (2.32%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (0.83%)
GSK3B	inactive (-0.68%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-0.85%)
MSSK1	inactive (-1.92%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (0.49%)
CLK2	inactive (-2.64%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (0.37%)
HIPK4	inactive (0.22%)
DYRK1B	inactive (2.65%)
DYRK1A	inactive (3.4%)
DYRK2	inactive (0.34%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (1.38%)