Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : CHEMBL1096626

Inchikey : NPRGDRYIMFLLIG-OAHLLOKOSA-N

ChemSpider : 10133928

Pubchem CID : 11959682

ChEMBL : CHEMBL1096626

	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 (-0.29%)
TYK2	inactive (-3.88%)
JAK2	inactive (1.71%)
JAK3	inactive (-0.34%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (7.41%)
FES	inactive (7.88%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (2.9%)
ABL2	inactive (3.84%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (2.13%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (5.18%)
BTK	inactive (0.56%)
TXK	inactive (3.73%)
TEC	inactive (3.05%)
ITK	inactive (1.49%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (2.72%)
SRM	inactive (1.99%)
FRK	inactive (2.68%)
BLK	inactive (2.85%)
LCK	inactive (3.65%)
HCK	inactive (9.34%)
FGR	inactive (5.54%)
FYN	inactive (4.61%)
SRC	inactive (13.71%)
YES	inactive (7.77%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-0.31%)
EphA4	inactive (4.87%)
EphA3	inactive (1.87%)
EphB4	inactive (1.24%)
EphB3	inactive (1.06%)
EphB2	inactive (0.23%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (9.96%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (4.13%)
ZAP70	inactive (-2.5%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (17.07%)
ALK	inactive (9.07%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (9.48%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (1.38%)
IGF1R	inactive (2.6%)
IRR	inactive (2.71%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (1.65%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (5.52%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (3.54%)
TRKB	inactive (2.5%)
TRKC	inactive (6.42%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (-1.45%)
MET	inactive (1.76%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-3%)
MER	inactive (3.59%)
TYRO3	inactive (1.88%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (37.99%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (2.91%)
FGFR2	inactive (4.18%)
FGFR3	inactive (3.32%)
FGFR4	inactive (2.04%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (30.44%)
KDR	active (96.12%)
FLT4	active (62.64%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (5.51%)
KIT	inactive (1.58%)
FLT3	inactive (2.43%)
PDGFRa	inactive (43.79%)
PDGFRb	active (57.21%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (6.74%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (3.88%)
TNK1	inactive (-4.26%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (13.44%)
ErbB2	inactive (3.43%)
ErbB4	inactive (28.91%)

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 (1.37%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (5.43%)

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 (15.97%)
MST1	inactive (42.68%)
MST2	inactive (42.41%)
MST4	inactive (28.15%)
HGK	inactive (35.09%)
MINK	inactive (21.15%)
LOK	inactive (28.78%)
PAK1	inactive (3.91%)
PAK3	inactive (4.83%)
PAK2	inactive (10.94%)
PAK5	active (70.92%)
PAK6	active (77.33%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (4.39%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (11.44%)
CK1g2	inactive (5.45%)
CK1g1	inactive (5.61%)
CK1g3	inactive (4.23%)

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 (7.68%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (5.24%)
AurC	inactive (2.08%)
AurA	inactive (2.98%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (2.81%)
NEK2	inactive (4.1%)
NEK9	inactive (3.62%)
NEK7	inactive (3.72%)
NEK6	inactive (1.56%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (6.85%)
IKKe	inactive (37.94%)
IKKb	inactive (4.92%)
IKKa	inactive (2.58%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (11.21%)

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 (14.98%)
GPRK6	inactive (5.48%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (4.43%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (17.73%)
MSK2	inactive (20.5%)
RSK1	inactive (12.81%)
RSK2	inactive (14.53%)
RSK4	inactive (7.07%)
RSK3	inactive (10.65%)
p70S6K	inactive (33.14%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	active (91.99%)
AKT1	active (90.41%)
AKT3	active (91.65%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (3.49%)
SGK3	active (57.71%)
SGK2	inactive (13.41%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	active (97.12%)
PKCg	inactive (45.48%)
PKCa	inactive (32.29%)
PKCt	active (82.65%)
PKCi	inactive (3.1%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	active (78.78%)
PKG1	active (71.35%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	active (87.07%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (24.74%)
ROCK2	active (51.29%)
MRCKb	inactive (26.58%)
MRCKa	inactive (36.26%)

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 (11.33%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (1.52%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (4.09%)
CaMK1d	inactive (4.5%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (-1.37%)
PHKg2	inactive (5.27%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (8.64%)
CaMK2a	inactive (6.26%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (1.6%)
MAPKAPK2	inactive (2.99%)
MAPKAPK3	inactive (2.95%)
MNK2	inactive (2.92%)
MNK1	inactive (2.97%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (28.59%)
PKD1	inactive (29.93%)
PKD2	inactive (25.58%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (18.37%)
MARK3	inactive (35.37%)
MARK1	inactive (27.34%)
QIK	inactive (-1.51%)
SIK	inactive (7.29%)
NuaK1	inactive (47.31%)
BRSK1	inactive (1.15%)
BRSK2	inactive (5.58%)
MELK	active (82.11%)
CHK1	inactive (9.89%)
PASK	inactive (8.04%)
AMPKa1	active (65.67%)
AMPKa2	inactive (14.98%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (2.24%)
TSSK1	inactive (44.07%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (4.82%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (3.44%)
PIM3	inactive (4.27%)
PIM1	inactive (3.63%)

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 (9.81%)
p38a	inactive (7.11%)
p38b	inactive (4.89%)
p38d	inactive (1.9%)
Erk2	inactive (5.04%)
Erk1	inactive (2.26%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	active (73.58%)
GSK3B	active (71.18%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-1.89%)
MSSK1	inactive (-2.11%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (0.92%)
CLK2	inactive (12.09%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (12.33%)
HIPK4	inactive (6.13%)
DYRK1B	inactive (2.57%)
DYRK1A	inactive (2.24%)
DYRK2	inactive (4.79%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (4.54%)