Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW577921A

Inchikey : IHXLWHUWFVFLCY-UHFFFAOYSA-N

ChemSpider : 9406987

Pubchem CID : 11231939

ChEMBL : CHEMBL1794062

	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 (5.2%)
TYK2	inactive (-0.92%)
JAK2	inactive (-0.51%)
JAK3	inactive (-1.96%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (11.22%)
FES	inactive (3.85%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (14.14%)
ABL2	inactive (11.15%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (3.11%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (6.53%)
BTK	inactive (3.39%)
TXK	inactive (6.86%)
TEC	inactive (7.28%)
ITK	inactive (3.07%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (6.6%)
SRM	inactive (2.11%)
FRK	inactive (5.01%)
BLK	inactive (5.8%)
LCK	inactive (9.64%)
HCK	inactive (13.35%)
FGR	inactive (12.1%)
FYN	inactive (8.38%)
SRC	inactive (11.23%)
YES	inactive (6.48%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (1.76%)
EphA4	inactive (12.8%)
EphA3	inactive (4.86%)
EphB4	inactive (5.33%)
EphB3	inactive (3.43%)
EphB2	inactive (10.83%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (11.11%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-4.41%)
ZAP70	inactive (4.36%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (4.49%)
ALK	inactive (9.47%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (11.21%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (3.48%)
IGF1R	inactive (1.64%)
IRR	inactive (3.73%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (0.42%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (2.74%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (4.51%)
TRKB	inactive (8.84%)
TRKC	inactive (9.48%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (1.59%)
MET	inactive (1.27%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-5.15%)
MER	inactive (1.66%)
TYRO3	inactive (2.12%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (6.88%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (5.99%)
FGFR2	inactive (13.7%)
FGFR3	inactive (13.12%)
FGFR4	inactive (0.7%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (16.39%)
KDR	inactive (19.16%)
FLT4	inactive (9.85%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	active (53.51%)
KIT	active (98.15%)
FLT3	active (87.16%)
PDGFRa	inactive (47.47%)
PDGFRb	inactive (47.74%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (6.44%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (3.33%)
TNK1	inactive (13.83%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (5.3%)
ErbB2	inactive (6.93%)
ErbB4	inactive (15.68%)

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 (2.99%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (7.19%)

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 (4.63%)
MST1	inactive (5.16%)
MST2	inactive (7.36%)
MST4	inactive (0.41%)
HGK	inactive (26.2%)
MINK	inactive (17.28%)
LOK	inactive (8.47%)
PAK1	inactive (12.65%)
PAK3	inactive (6.38%)
PAK2	inactive (1.5%)
PAK5	inactive (-2.65%)
PAK6	inactive (-9.8%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (3.89%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (2.52%)
CK1g2	inactive (3.85%)
CK1g1	inactive (5.25%)
CK1g3	inactive (5.78%)

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 (4.18%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (11.07%)
AurC	inactive (12.5%)
AurA	inactive (8.83%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (3%)
NEK2	inactive (6.16%)
NEK9	inactive (5.41%)
NEK7	inactive (5.45%)
NEK6	inactive (1.67%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (2.91%)
IKKe	inactive (7.83%)
IKKb	inactive (9.61%)
IKKa	inactive (9.03%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (11.9%)

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 (2.31%)
GPRK6	inactive (3.95%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (-0.48%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (-5.77%)
MSK2	inactive (2.42%)
RSK1	inactive (23.53%)
RSK2	inactive (0.19%)
RSK4	inactive (0.95%)
RSK3	inactive (4.52%)
p70S6K	inactive (2.44%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (2.82%)
AKT1	inactive (1.71%)
AKT3	inactive (3.9%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (4.31%)
SGK3	inactive (3.37%)
SGK2	inactive (0.66%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (7.33%)
PKCg	inactive (3.53%)
PKCa	inactive (1.01%)
PKCt	inactive (3.02%)
PKCi	inactive (3.75%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (2.81%)
PKG1	inactive (1.96%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (3.03%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (3.7%)
ROCK2	inactive (3.77%)
MRCKb	inactive (0.66%)
MRCKa	inactive (-2.78%)

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 (-3.53%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (0.52%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-8.72%)
CaMK1d	inactive (-0.14%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (13.13%)
PHKg2	inactive (5.8%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (4.92%)
CaMK2a	inactive (0.2%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (1.9%)
MAPKAPK2	inactive (-1.84%)
MAPKAPK3	inactive (1.35%)
MNK2	inactive (7.25%)
MNK1	inactive (5.88%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (4.66%)
PKD1	inactive (5.46%)
PKD2	inactive (2.18%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (4.33%)
MARK3	inactive (4.87%)
MARK1	inactive (5.68%)
QIK	inactive (5.2%)
SIK	inactive (14.08%)
NuaK1	inactive (-4.21%)
BRSK1	inactive (3.87%)
BRSK2	inactive (4.49%)
MELK	inactive (8.09%)
CHK1	inactive (-2.91%)
PASK	inactive (1.05%)
AMPKa1	inactive (3.31%)
AMPKa2	inactive (4.09%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (2.11%)
TSSK1	inactive (4.46%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (-4.43%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (0.53%)
PIM3	inactive (0.86%)
PIM1	inactive (1.55%)

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 (3.07%)
p38a	inactive (11%)
p38b	inactive (7.08%)
p38d	inactive (4.74%)
Erk2	inactive (6.15%)
Erk1	inactive (5.55%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (3.92%)
GSK3B	inactive (2.74%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-2.61%)
MSSK1	inactive (1.35%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (0.51%)
CLK2	inactive (0.86%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (0.57%)
HIPK4	inactive (0.15%)
DYRK1B	inactive (-1.3%)
DYRK1A	inactive (3.38%)
DYRK2	inactive (3.04%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (8.04%)