Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW829877X

Inchikey : QRNLICFNSFQHBO-FOKLQQMPSA-N

ChemSpider : 7879077

Pubchem CID : 9604958

ChEMBL : CHEMBL303687

	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 (3.83%)
TYK2	inactive (-1.47%)
JAK2	inactive (1.98%)
JAK3	inactive (1.11%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (17.47%)
FES	inactive (10.32%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	active (62.09%)
ABL2	inactive (40.52%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (8.35%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (10.61%)
BTK	inactive (0.44%)
TXK	inactive (7.5%)
TEC	inactive (5.78%)
ITK	inactive (3.5%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (5.43%)
SRM	inactive (-0.01%)
FRK	inactive (5.6%)
BLK	inactive (7.15%)
LCK	inactive (21.31%)
HCK	inactive (16.17%)
FGR	inactive (18.89%)
FYN	inactive (16.49%)
SRC	inactive (32.88%)
YES	inactive (13.83%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (1.1%)
EphA4	inactive (11.28%)
EphA3	inactive (3.46%)
EphB4	inactive (3.21%)
EphB3	inactive (4.17%)
EphB2	inactive (9.45%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (15.75%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (0.76%)
ZAP70	inactive (11.02%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (8.61%)
ALK	inactive (22.31%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (38.35%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	active (82.2%)
IGF1R	inactive (22.88%)
IRR	inactive (15.27%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (2.37%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (13%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (5.28%)
TRKB	inactive (5.08%)
TRKC	inactive (2.64%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (9.64%)
MET	inactive (7.4%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-6.6%)
MER	inactive (4.53%)
TYRO3	inactive (4.49%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (11.48%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (17.71%)
FGFR2	inactive (7.12%)
FGFR3	inactive (6.72%)
FGFR4	inactive (1.93%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (0.15%)
KDR	inactive (19.15%)
FLT4	inactive (4.5%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (12.89%)
KIT	inactive (10.61%)
FLT3	inactive (5.84%)
PDGFRa	inactive (23.24%)
PDGFRb	inactive (21.05%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (5.1%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (5.39%)
TNK1	inactive (9.73%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (4.71%)
ErbB2	inactive (3.43%)
ErbB4	inactive (11.91%)

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 (4.05%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (11.23%)

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 (4.23%)
MST1	inactive (13.22%)
MST2	inactive (11.45%)
MST4	inactive (-3.2%)
HGK	inactive (20.98%)
MINK	inactive (16.11%)
LOK	inactive (10.94%)
PAK1	inactive (9.32%)
PAK3	inactive (6.42%)
PAK2	inactive (1.47%)
PAK5	inactive (10.67%)
PAK6	inactive (-8.44%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (3.78%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (8.69%)
CK1g2	inactive (11.96%)
CK1g1	inactive (11.2%)
CK1g3	inactive (8.48%)

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 (14.19%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (6.65%)
AurC	inactive (4.66%)
AurA	inactive (11.76%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (9.78%)
NEK2	inactive (10.68%)
NEK9	inactive (9.51%)
NEK7	inactive (10.13%)
NEK6	inactive (3.08%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (5.4%)
IKKe	inactive (6.9%)
IKKb	inactive (9.36%)
IKKa	inactive (9.99%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (19.05%)

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 (7.9%)
GPRK6	inactive (5.93%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (3.14%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (-2.7%)
MSK2	inactive (5.55%)
RSK1	inactive (6.59%)
RSK2	inactive (5.14%)
RSK4	inactive (3.14%)
RSK3	inactive (4.8%)
p70S6K	inactive (3.95%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.75%)
AKT1	inactive (0.76%)
AKT3	inactive (1.94%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (3.62%)
SGK3	inactive (2.61%)
SGK2	inactive (2.8%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (4.73%)
PKCg	inactive (-9.04%)
PKCa	inactive (1.66%)
PKCt	inactive (4.16%)
PKCi	inactive (1.86%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (5.99%)
PKG1	inactive (7.27%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (4.53%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (4.15%)
ROCK2	inactive (5.34%)
MRCKb	inactive (1.73%)
MRCKa	inactive (5.98%)

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 (2.47%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (2.82%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (4.68%)
CaMK1d	inactive (3.47%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (10.03%)
PHKg2	inactive (5.98%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (12.46%)
CaMK2a	inactive (5.56%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (2.22%)
MAPKAPK2	inactive (0.98%)
MAPKAPK3	inactive (-0.87%)
MNK2	inactive (11.23%)
MNK1	inactive (9.69%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (9.61%)
PKD1	inactive (10.71%)
PKD2	inactive (8.29%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (5.11%)
MARK3	inactive (6.9%)
MARK1	inactive (6.21%)
QIK	inactive (14.69%)
SIK	inactive (12.6%)
NuaK1	inactive (16.18%)
BRSK1	inactive (9.05%)
BRSK2	inactive (12.68%)
MELK	inactive (12.55%)
CHK1	inactive (-5.11%)
PASK	inactive (0.57%)
AMPKa1	inactive (6.98%)
AMPKa2	inactive (6%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (3.89%)
TSSK1	inactive (15.15%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (-4.37%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (0.75%)
PIM3	inactive (8.3%)
PIM1	inactive (3.51%)

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 (11.6%)
p38a	inactive (9.02%)
p38b	inactive (4.42%)
p38d	inactive (6.26%)
Erk2	inactive (7.67%)
Erk1	inactive (3.26%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	active (55.65%)
GSK3B	inactive (47.03%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-1.68%)
MSSK1	inactive (0.15%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (1.46%)
CLK2	inactive (6.42%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (13.27%)
HIPK4	inactive (11.45%)
DYRK1B	inactive (11.32%)
DYRK1A	inactive (16.54%)
DYRK2	inactive (13.61%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (23.14%)