Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW701427A

Inchikey : LIRNSPSAYSNIME-UHFFFAOYSA-N

ChemSpider : 28484517

Pubchem CID : 57399799

ChEMBL : CHEMBL1909373

	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 (2.01%)
TYK2	inactive (-0.42%)
JAK2	inactive (4.54%)
JAK3	inactive (0.66%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (2.49%)
FES	inactive (0.5%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (6.45%)
ABL2	inactive (3.96%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (-42.48%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (0.47%)
BTK	inactive (-2.57%)
TXK	inactive (1.48%)
TEC	inactive (0.87%)
ITK	inactive (-2.68%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (-0.37%)
SRM	inactive (0.74%)
FRK	inactive (0.91%)
BLK	inactive (0.01%)
LCK	inactive (-2.81%)
HCK	inactive (3.15%)
FGR	inactive (6.34%)
FYN	inactive (0.19%)
SRC	inactive (7.71%)
YES	inactive (2.43%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-4.67%)
EphA4	inactive (5.32%)
EphA3	inactive (-2.49%)
EphB4	inactive (-4.05%)
EphB3	inactive (-3.97%)
EphB2	inactive (3.77%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (6.37%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-0.23%)
ZAP70	inactive (-4.2%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (-0.52%)
ALK	inactive (-1.37%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (3.11%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (0.58%)
IGF1R	inactive (-7.4%)
IRR	inactive (2.82%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (48.83%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (2.82%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (3.47%)
TRKB	inactive (1.02%)
TRKC	inactive (3.8%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (5.64%)
MET	inactive (11.43%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-0.32%)
MER	inactive (2.01%)
TYRO3	inactive (3.17%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (14.13%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (-2.27%)
FGFR2	inactive (5.77%)
FGFR3	inactive (11.9%)
FGFR4	inactive (-1.22%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (8.22%)
KDR	inactive (12.62%)
FLT4	inactive (-5.74%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (8.4%)
KIT	inactive (18.75%)
FLT3	inactive (5.75%)
PDGFRa	inactive (39.32%)
PDGFRb	inactive (16.24%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (7.16%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (0.6%)
TNK1	inactive (17.44%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (-2.11%)
ErbB2	inactive (3.5%)
ErbB4	inactive (0.22%)

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 (0.26%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (-1.69%)

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 (1.11%)
MST1	inactive (11.23%)
MST2	inactive (10.92%)
MST4	inactive (3.41%)
HGK	inactive (5.9%)
MINK	inactive (4.38%)
LOK	inactive (7.1%)
PAK1	inactive (2.31%)
PAK3	inactive (0.98%)
PAK2	inactive (-0.31%)
PAK5	inactive (3.29%)
PAK6	inactive (4.26%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (0.97%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (0.72%)
CK1g2	inactive (-2.28%)
CK1g1	inactive (-2.13%)
CK1g3	inactive (-0.39%)

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 (0.8%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (9.37%)
AurC	inactive (37.7%)
AurA	inactive (12.78%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (2.1%)
NEK2	inactive (-6.05%)
NEK9	inactive (1.76%)
NEK7	inactive (-0.18%)
NEK6	inactive (-0.54%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (2.42%)
IKKe	inactive (3.63%)
IKKb	inactive (2.79%)
IKKa	inactive (-3.86%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (9.64%)

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 (-3.21%)
GPRK6	inactive (-0.77%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (2.77%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (1.28%)
MSK2	inactive (2.84%)
RSK1	inactive (2.55%)
RSK2	inactive (1.31%)
RSK4	inactive (1.45%)
RSK3	inactive (2%)
p70S6K	inactive (0.91%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (-2.42%)
AKT1	inactive (-3.33%)
AKT3	inactive (-3.6%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (1.96%)
SGK3	inactive (2.6%)
SGK2	inactive (1.89%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (3.15%)
PKCg	inactive (-0.24%)
PKCa	inactive (-3.65%)
PKCt	inactive (2.02%)
PKCi	inactive (-1.28%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (0.86%)
PKG1	inactive (2.77%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (1.8%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (1.55%)
ROCK2	inactive (5.7%)
MRCKb	inactive (-1.21%)
MRCKa	inactive (1.5%)

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 (6.26%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (-16.49%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-2.08%)
CaMK1d	inactive (-1.87%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (11.19%)
PHKg2	inactive (4.11%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (1.91%)
CaMK2a	inactive (3.09%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (1%)
MAPKAPK2	inactive (0.43%)
MAPKAPK3	inactive (-0.42%)
MNK2	inactive (3.85%)
MNK1	inactive (8.3%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (-3.85%)
PKD1	inactive (-1.96%)
PKD2	inactive (-1.55%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (1.97%)
MARK3	inactive (3.98%)
MARK1	inactive (3.08%)
QIK	inactive (2.04%)
SIK	inactive (1.25%)
NuaK1	inactive (8%)
BRSK1	inactive (2.91%)
BRSK2	inactive (9.32%)
MELK	inactive (0.37%)
CHK1	inactive (-0.43%)
PASK	inactive (1.66%)
AMPKa1	inactive (4.37%)
AMPKa2	inactive (2.8%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (0.93%)
TSSK1	inactive (0.96%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (0.01%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (-2.76%)
PIM3	inactive (3.84%)
PIM1	inactive (0.62%)

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 (-0.13%)
p38a	inactive (1.12%)
p38b	inactive (-1.18%)
p38d	inactive (-0.69%)
Erk2	inactive (0.1%)
Erk1	inactive (2.25%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (1.82%)
GSK3B	inactive (2.13%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (3.15%)
MSSK1	inactive (3.99%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (0.74%)
CLK2	inactive (0.77%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (0.32%)
HIPK4	inactive (3.06%)
DYRK1B	inactive (-1.48%)
DYRK1A	inactive (-1.76%)
DYRK2	inactive (-0.17%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (8.32%)