Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : -

Inchikey : KMHXVUCYJPXSIV-DHDCSXOGSA-N

ChemSpider : 8119881

Pubchem CID : 9944269

	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 (29.92%)
TYK2	inactive (12.32%)
JAK2	inactive (0.69%)
JAK3	inactive (6.49%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (11.23%)
FES	inactive (2.63%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (13.5%)
ABL2	inactive (7.69%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (7.33%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (4.54%)
BTK	inactive (-0.4%)
TXK	inactive (5.07%)
TEC	inactive (5.42%)
ITK	inactive (4.51%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (6%)
SRM	inactive (-0.18%)
FRK	inactive (3.04%)
BLK	inactive (19.67%)
LCK	inactive (9.02%)
HCK	inactive (11.74%)
FGR	inactive (12.76%)
FYN	inactive (7.09%)
SRC	inactive (19.2%)
YES	inactive (15.7%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (1.91%)
EphA4	inactive (12.34%)
EphA3	inactive (4.04%)
EphB4	inactive (2.59%)
EphB3	inactive (2.77%)
EphB2	inactive (8.52%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (24.68%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-1.86%)
ZAP70	inactive (7.33%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (7.47%)
ALK	inactive (11.82%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (8.39%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (14.75%)
IGF1R	inactive (16.73%)
IRR	inactive (5.98%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (0.37%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (30.87%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (44.22%)
TRKB	active (56.51%)
TRKC	active (58.36%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (6.25%)
MET	inactive (13.62%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-3.55%)
MER	inactive (5.61%)
TYRO3	inactive (10.2%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (48.57%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (9.98%)
FGFR2	inactive (24.95%)
FGFR3	inactive (22.01%)
FGFR4	inactive (2.81%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (24.05%)
KDR	inactive (37.31%)
FLT4	inactive (40.23%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (34.52%)
KIT	active (75.92%)
FLT3	active (53.71%)
PDGFRa	inactive (45.51%)
PDGFRb	inactive (33.35%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (4.4%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (2.83%)
TNK1	inactive (14.04%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (4.08%)
ErbB2	inactive (9.83%)
ErbB4	inactive (12.53%)

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 (2.52%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (6.87%)

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 (12.58%)
MST1	active (54.41%)
MST2	inactive (35.72%)
MST4	inactive (5.15%)
HGK	active (65.78%)
MINK	active (56.5%)
LOK	inactive (12.59%)
PAK1	inactive (8.31%)
PAK3	inactive (5.49%)
PAK2	inactive (2.17%)
PAK5	inactive (-2.52%)
PAK6	inactive (-21.47%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (6.15%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (10.32%)
CK1g2	inactive (8.25%)
CK1g1	inactive (7.11%)
CK1g3	inactive (5.16%)

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 (2.82%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (27.74%)
AurC	inactive (44.79%)
AurA	inactive (36.29%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (5.21%)
NEK2	inactive (4.16%)
NEK9	inactive (12.4%)
NEK7	inactive (4.4%)
NEK6	inactive (7.54%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (17.26%)
IKKe	inactive (16.35%)
IKKb	inactive (11.39%)
IKKa	inactive (2.05%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (47.89%)

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 (14.92%)
GPRK6	inactive (14.77%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (20%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (8.54%)
MSK2	inactive (13.41%)
RSK1	inactive (10.88%)
RSK2	inactive (8.64%)
RSK4	inactive (11.43%)
RSK3	inactive (14.23%)
p70S6K	inactive (9.06%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (0.9%)
AKT1	inactive (-0.09%)
AKT3	inactive (2.21%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (29.24%)
SGK3	inactive (8.06%)
SGK2	inactive (10.91%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (5.57%)
PKCg	inactive (2.93%)
PKCa	inactive (1.82%)
PKCt	inactive (4.7%)
PKCi	inactive (2.15%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (14.45%)
PKG1	inactive (5.48%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (7.18%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (1.71%)
ROCK2	inactive (7.17%)
MRCKb	inactive (1.08%)
MRCKa	inactive (3.59%)

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 (14.94%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (-2.02%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-2.92%)
CaMK1d	inactive (0.98%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (33.57%)
PHKg2	inactive (18.69%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (6.83%)
CaMK2a	inactive (4.05%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (4.02%)
MAPKAPK2	inactive (2.54%)
MAPKAPK3	inactive (3.15%)
MNK2	inactive (8.07%)
MNK1	inactive (14.78%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (6.5%)
PKD1	inactive (7.88%)
PKD2	inactive (6.07%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (17.89%)
MARK3	inactive (36.4%)
MARK1	inactive (25.44%)
QIK	inactive (11.57%)
SIK	inactive (9.8%)
NuaK1	inactive (38.68%)
BRSK1	inactive (17.16%)
BRSK2	inactive (26.29%)
MELK	inactive (25.83%)
CHK1	inactive (13.47%)
PASK	inactive (1.73%)
AMPKa1	inactive (19.34%)
AMPKa2	inactive (15.46%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (5.54%)
TSSK1	inactive (7.35%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (7.29%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (2.25%)
PIM3	inactive (4.7%)
PIM1	inactive (0.68%)

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 (12.08%)
p38a	inactive (6.86%)
p38b	inactive (8.05%)
p38d	inactive (5.56%)
Erk2	inactive (6.4%)
Erk1	inactive (6.36%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (28.23%)
GSK3B	inactive (25.39%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (1.26%)
MSSK1	inactive (-0.36%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (1.52%)
CLK2	inactive (21.62%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (5.5%)
HIPK4	inactive (3.17%)
DYRK1B	inactive (11.64%)
DYRK1A	inactive (14.32%)
DYRK2	inactive (6.8%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (12.81%)