Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW627512B

Inchikey : CKYLEUNHWFIYOR-UHFFFAOYSA-N

ChemSpider : 4487005

Pubchem CID : 5329854

ChEMBL : CHEMBL443563

	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 (-0.54%)
TYK2	inactive (6.55%)
JAK2	inactive (5.24%)
JAK3	inactive (12.65%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (2.66%)
FES	inactive (-1.45%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	active (52.34%)
ABL2	active (52.07%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (-0.86%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (8.49%)
BTK	inactive (0.25%)
TXK	inactive (16.18%)
TEC	inactive (4.55%)
ITK	inactive (2.92%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (4.16%)
SRM	inactive (3.83%)
FRK	inactive (4.26%)
BLK	inactive (41.11%)
LCK	inactive (25.02%)
HCK	inactive (31.25%)
FGR	inactive (29.4%)
FYN	inactive (37.54%)
SRC	active (72.42%)
YES	inactive (46.61%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-1.26%)
EphA4	inactive (1.47%)
EphA3	inactive (-5.8%)
EphB4	inactive (3.25%)
EphB3	inactive (-2.19%)
EphB2	inactive (5.83%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (5.39%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-1.68%)
ZAP70	inactive (0.62%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (1.47%)
ALK	inactive (-0.68%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (15.84%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (-0.22%)
IGF1R	inactive (2.07%)
IRR	inactive (-1.95%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (8.58%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (14.47%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (23.09%)
TRKB	inactive (28.27%)
TRKC	inactive (25.25%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (3.47%)
MET	inactive (2.13%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-1.68%)
MER	inactive (3.53%)
TYRO3	inactive (1.3%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (15.51%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (8.79%)
FGFR2	inactive (26.97%)
FGFR3	inactive (16.62%)
FGFR4	inactive (1.36%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	-
KDR	inactive (47.95%)
FLT4	inactive (36.72%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	active (57.64%)
KIT	active (98.71%)
FLT3	active (90.85%)
PDGFRa	active (69.58%)
PDGFRb	active (74.18%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (5.14%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (0.48%)
TNK1	inactive (28.38%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (13.8%)
ErbB2	inactive (-1.74%)
ErbB4	inactive (-2.66%)

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 (0.55%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (-1.94%)

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 (11.47%)
MST1	-
MST2	inactive (-1.87%)
MST4	inactive (-4.83%)
HGK	inactive (26.44%)
MINK	inactive (17.27%)
LOK	inactive (11.12%)
PAK1	inactive (-0.52%)
PAK3	inactive (-0.07%)
PAK2	inactive (-0.61%)
PAK5	inactive (7.2%)
PAK6	inactive (-10.78%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (0.69%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (1.29%)
CK1g2	inactive (-0.69%)
CK1g1	inactive (-0.76%)
CK1g3	inactive (-0.18%)

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 (2.1%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (49.98%)
AurC	active (71.77%)
AurA	active (75.5%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (1.71%)
NEK2	inactive (-0.62%)
NEK9	inactive (8.49%)
NEK7	inactive (3.67%)
NEK6	inactive (-3.53%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (13.74%)
IKKe	inactive (1.15%)
IKKb	inactive (4.06%)
IKKa	inactive (4.62%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (-1.01%)

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 (-9.33%)
GPRK6	inactive (-0.02%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (6.05%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (0.82%)
MSK2	inactive (0.02%)
RSK1	inactive (3.07%)
RSK2	inactive (2.83%)
RSK4	inactive (6.6%)
RSK3	inactive (6.88%)
p70S6K	inactive (3.55%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (-1.88%)
AKT1	inactive (-1.61%)
AKT3	inactive (1.14%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (5.44%)
SGK3	inactive (0.29%)
SGK2	inactive (1.18%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (-4.38%)
PKCg	inactive (1.46%)
PKCa	inactive (1.1%)
PKCt	inactive (-0.9%)
PKCi	inactive (0.77%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (1.47%)
PKG1	inactive (1.3%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (0.75%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (1.85%)
ROCK2	inactive (3.74%)
MRCKb	inactive (0.86%)
MRCKa	inactive (3.73%)

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 (1.28%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (1.6%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (0.09%)
CaMK1d	inactive (-0.01%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (20.86%)
PHKg2	inactive (-2.15%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (5.55%)
CaMK2a	inactive (-0.38%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (0.01%)
MAPKAPK2	inactive (-0.59%)
MAPKAPK3	inactive (-2.22%)
MNK2	inactive (24.2%)
MNK1	inactive (30.45%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (-1.6%)
PKD1	inactive (-1.47%)
PKD2	inactive (-0.05%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (13.44%)
MARK3	inactive (22.12%)
MARK1	inactive (15.58%)
QIK	inactive (30.6%)
SIK	inactive (27.36%)
NuaK1	active (60.95%)
BRSK1	inactive (5.91%)
BRSK2	inactive (10.52%)
MELK	inactive (5.74%)
CHK1	inactive (5.64%)
PASK	inactive (-0.67%)
AMPKa1	inactive (9.16%)
AMPKa2	inactive (5.35%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (-1.3%)
TSSK1	inactive (-0.04%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (1.28%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (1.06%)
PIM3	inactive (1.87%)
PIM1	inactive (2.12%)

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 (-3.35%)
p38a	inactive (-4.25%)
p38b	inactive (0.04%)
p38d	inactive (-1.63%)
Erk2	inactive (-1.83%)
Erk1	inactive (1.29%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (34.44%)
GSK3B	inactive (35.8%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (1%)
MSSK1	inactive (0.18%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (0.88%)
CLK2	inactive (3.33%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (11.24%)
HIPK4	inactive (3.87%)
DYRK1B	inactive (3.72%)
DYRK1A	inactive (6.39%)
DYRK2	inactive (-1.69%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (4.02%)