Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : -

Inchikey : UGKCASUMDGHTLI-UVTDQMKNSA-N

ChemSpider : 8034362

Pubchem CID : 9858662

	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 (5.33%)
TYK2	inactive (9.24%)
JAK2	inactive (1.03%)
JAK3	inactive (8.16%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (5.06%)
FES	inactive (-1.95%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (11.02%)
ABL2	inactive (8.69%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (-6.43%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (0.63%)
BTK	inactive (-0.9%)
TXK	inactive (1.85%)
TEC	inactive (0.17%)
ITK	inactive (3.61%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (-2.23%)
SRM	inactive (1.32%)
FRK	inactive (0.76%)
BLK	inactive (18.22%)
LCK	inactive (5.83%)
HCK	inactive (14.07%)
FGR	inactive (15.03%)
FYN	inactive (4.85%)
SRC	inactive (8.01%)
YES	inactive (10.37%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-1.5%)
EphA4	inactive (-2.53%)
EphA3	inactive (-4.36%)
EphB4	inactive (-0.64%)
EphB3	inactive (-3.88%)
EphB2	inactive (0.55%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (20.14%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-3.83%)
ZAP70	inactive (-2.93%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (3.76%)
ALK	inactive (5.88%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (6.73%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (8.57%)
IGF1R	inactive (5.77%)
IRR	inactive (-1.01%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (0.83%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (35.86%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (46.69%)
TRKB	active (58.61%)
TRKC	active (57.01%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (6.3%)
MET	inactive (-0.23%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (4.47%)
MER	inactive (3.63%)
TYRO3	inactive (6.06%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (49.43%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (5.82%)
FGFR2	inactive (27.13%)
FGFR3	inactive (25.54%)
FGFR4	inactive (5.07%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (20.81%)
KDR	inactive (46.72%)
FLT4	inactive (30.61%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (41.66%)
KIT	active (86.59%)
FLT3	active (74.13%)
PDGFRa	inactive (41.93%)
PDGFRb	inactive (37.97%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (2.36%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (1.32%)
TNK1	inactive (6.96%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (1.45%)
ErbB2	inactive (-1.76%)
ErbB4	inactive (-9.44%)

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 (-0.15%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (-2.55%)

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 (18.57%)
MST1	active (51.9%)
MST2	inactive (24.55%)
MST4	inactive (-0.36%)
HGK	active (72.97%)
MINK	active (63.75%)
LOK	inactive (0.71%)
PAK1	inactive (-3.06%)
PAK3	inactive (-2.59%)
PAK2	inactive (-3.37%)
PAK5	inactive (0.84%)
PAK6	inactive (-8.06%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (-0.2%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (7.96%)
CK1g2	inactive (2.22%)
CK1g1	inactive (1.81%)
CK1g3	inactive (3.9%)

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 (-1.15%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (43%)
AurC	active (61.07%)
AurA	inactive (47.57%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (-2.34%)
NEK2	inactive (-3.33%)
NEK9	inactive (9.7%)
NEK7	inactive (-3.48%)
NEK6	inactive (-2.98%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (14.23%)
IKKe	inactive (7.71%)
IKKb	inactive (-1.38%)
IKKa	inactive (13.66%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (18.94%)

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 (-5.45%)
GPRK6	inactive (0.5%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (32.21%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (-0.97%)
MSK2	inactive (7.44%)
RSK1	inactive (9.64%)
RSK2	inactive (9.89%)
RSK4	inactive (11%)
RSK3	inactive (13.84%)
p70S6K	inactive (3.4%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (-2.28%)
AKT1	inactive (-2.1%)
AKT3	inactive (1.91%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (12.28%)
SGK3	inactive (-0.79%)
SGK2	inactive (1.93%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (-4.5%)
PKCg	inactive (0.03%)
PKCa	inactive (0.61%)
PKCt	inactive (-0.74%)
PKCi	inactive (-0.98%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (3.29%)
PKG1	inactive (-1.49%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (0.66%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (1.4%)
ROCK2	inactive (1.99%)
MRCKb	inactive (-0.45%)
MRCKa	inactive (-0.5%)

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 (10.41%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (-4.45%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-1.35%)
CaMK1d	inactive (0.24%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (31.53%)
PHKg2	inactive (5.2%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (4.73%)
CaMK2a	inactive (-2.22%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (-0.07%)
MAPKAPK2	inactive (-1.69%)
MAPKAPK3	inactive (-2.88%)
MNK2	inactive (5.59%)
MNK1	inactive (-0.33%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (-0.06%)
PKD1	inactive (3.18%)
PKD2	inactive (2.63%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (18.9%)
MARK3	inactive (16.09%)
MARK1	inactive (23.82%)
QIK	inactive (-6.11%)
SIK	inactive (2.58%)
NuaK1	inactive (43.91%)
BRSK1	inactive (16.48%)
BRSK2	inactive (30.55%)
MELK	inactive (20.89%)
CHK1	inactive (5.75%)
PASK	inactive (0.59%)
AMPKa1	inactive (12.04%)
AMPKa2	inactive (4.21%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (-1.19%)
TSSK1	inactive (2.2%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (-2.55%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (0.67%)
PIM3	inactive (2.02%)
PIM1	inactive (0.04%)

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 (5.63%)
p38a	inactive (-2.23%)
p38b	inactive (3.42%)
p38d	inactive (-3.87%)
Erk2	inactive (-2.51%)
Erk1	inactive (-3.47%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (19.55%)
GSK3B	inactive (17.25%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (1.9%)
MSSK1	inactive (0.17%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (1.06%)
CLK2	inactive (3.62%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (3.36%)
HIPK4	inactive (4.82%)
DYRK1B	inactive (13.93%)
DYRK1A	inactive (10.41%)
DYRK2	inactive (-0.97%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (0.34%)