Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW876790X

Inchikey : RIIYKHQJSKRYKG-UHFFFAOYSA-N

ChemSpider : 23342591

Pubchem CID : 25023715

ChEMBL : CHEMBL506153

	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 (2.04%)
TYK2	inactive (-3.99%)
JAK2	inactive (0.73%)
JAK3	inactive (-2.17%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (3.14%)
FES	inactive (4.8%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (5.3%)
ABL2	inactive (4.11%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (4.95%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (5.15%)
BTK	inactive (0.11%)
TXK	inactive (1.12%)
TEC	inactive (4.27%)
ITK	inactive (0.3%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (5.45%)
SRM	inactive (-2.36%)
FRK	inactive (3.52%)
BLK	inactive (5.42%)
LCK	inactive (3.67%)
HCK	inactive (6.37%)
FGR	inactive (4.66%)
FYN	inactive (2%)
SRC	inactive (6.62%)
YES	inactive (5.52%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-0.9%)
EphA4	inactive (10.05%)
EphA3	inactive (5.09%)
EphB4	inactive (0.78%)
EphB3	inactive (3.19%)
EphB2	inactive (7.7%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (8.62%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-6.01%)
ZAP70	inactive (1.01%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (5.16%)
ALK	inactive (4.23%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (14.04%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (15.34%)
IGF1R	inactive (5.76%)
IRR	inactive (5.53%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (2.38%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (-0.23%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (3.09%)
TRKB	inactive (5.31%)
TRKC	inactive (3.4%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (1.07%)
MET	inactive (4.45%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-6.19%)
MER	inactive (3.22%)
TYRO3	inactive (5.41%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (7.16%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (4.72%)
FGFR2	inactive (5.33%)
FGFR3	inactive (5.02%)
FGFR4	inactive (1.09%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (3.5%)
KDR	inactive (13.49%)
FLT4	inactive (3.05%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (3.41%)
KIT	inactive (11.79%)
FLT3	inactive (4.29%)
PDGFRa	inactive (14.21%)
PDGFRb	inactive (12.41%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (7.24%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (2.15%)
TNK1	inactive (8.48%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (5.41%)
ErbB2	inactive (3.74%)
ErbB4	inactive (12.19%)

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 (3.05%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (7.26%)

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 (3.62%)
MST1	inactive (6.56%)
MST2	inactive (7.27%)
MST4	inactive (-4.29%)
HGK	inactive (11.28%)
MINK	inactive (10.8%)
LOK	inactive (17.97%)
PAK1	inactive (7.29%)
PAK3	inactive (5.12%)
PAK2	inactive (2.75%)
PAK5	inactive (7.69%)
PAK6	inactive (-1.02%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (3.62%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (4.77%)
CK1g2	inactive (5.17%)
CK1g1	inactive (5.89%)
CK1g3	inactive (3.84%)

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 (5.87%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (1.83%)
AurC	inactive (5.56%)
AurA	inactive (5.14%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (5.36%)
NEK2	inactive (6.84%)
NEK9	inactive (11.9%)
NEK7	inactive (4.72%)
NEK6	inactive (0.9%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (9.32%)
IKKe	inactive (17.63%)
IKKb	inactive (7.92%)
IKKa	inactive (14.13%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (10.5%)

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 (7.46%)
GPRK6	inactive (5.57%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (7.02%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	active (76.85%)
MSK2	active (71.44%)
RSK1	active (88.32%)
RSK2	active (78.71%)
RSK4	inactive (37.3%)
RSK3	active (73.84%)
p70S6K	active (78.22%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (10.54%)
AKT1	inactive (17.73%)
AKT3	inactive (26.21%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (18.1%)
SGK3	active (66.22%)
SGK2	inactive (17.74%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	active (93.64%)
PKCg	inactive (35.3%)
PKCa	active (58.16%)
PKCt	inactive (39.24%)
PKCi	inactive (39.96%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	active (73.81%)
PKG1	active (69.98%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	active (63.9%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	active (91.58%)
ROCK2	active (90.41%)
MRCKb	active (66.66%)
MRCKa	active (69.94%)

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 (5.44%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (1.62%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (0.71%)
CaMK1d	inactive (0.83%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (7.35%)
PHKg2	inactive (6.69%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (6.88%)
CaMK2a	inactive (-0.37%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (1.58%)
MAPKAPK2	inactive (1.53%)
MAPKAPK3	inactive (3.94%)
MNK2	inactive (13.45%)
MNK1	inactive (6.9%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (6.85%)
PKD1	inactive (8.53%)
PKD2	inactive (5.38%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (7.71%)
MARK3	inactive (16.59%)
MARK1	inactive (14.92%)
QIK	inactive (6.02%)
SIK	inactive (9.07%)
NuaK1	inactive (2.03%)
BRSK1	inactive (6.23%)
BRSK2	inactive (9.29%)
MELK	active (61.19%)
CHK1	inactive (-0.23%)
PASK	inactive (3.5%)
AMPKa1	inactive (8.23%)
AMPKa2	inactive (4.46%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (1.74%)
TSSK1	inactive (32.13%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (0.19%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (18.75%)
PIM3	active (69.28%)
PIM1	active (87.03%)

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 (4.73%)
p38a	inactive (6.55%)
p38b	inactive (3.55%)
p38d	inactive (5.07%)
Erk2	inactive (6.64%)
Erk1	inactive (5.7%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (49.73%)
GSK3B	inactive (42.33%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-2.66%)
MSSK1	inactive (-0.69%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (9.74%)
CLK2	inactive (10.46%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (10.23%)
HIPK4	inactive (3.11%)
DYRK1B	active (54.66%)
DYRK1A	active (72.39%)
DYRK2	inactive (37.16%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (2.99%)