Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : CHEMBL181361

Inchikey : NQQBKOGAKSBCSI-UHFFFAOYSA-N

ChemSpider : 8098162

Pubchem CID : 9922527

ChEMBL : CHEMBL181361

	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 (4.22%)
TYK2	inactive (-1.33%)
JAK2	inactive (2%)
JAK3	inactive (-0.57%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (6.59%)
FES	inactive (3.07%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (12.5%)
ABL2	inactive (8.87%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (4.7%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (3.73%)
BTK	inactive (0.04%)
TXK	inactive (3.04%)
TEC	inactive (7.33%)
ITK	inactive (2.48%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (7.02%)
SRM	inactive (-2.72%)
FRK	inactive (1.57%)
BLK	inactive (1.8%)
LCK	inactive (0.19%)
HCK	inactive (6.89%)
FGR	inactive (2.08%)
FYN	inactive (-0.24%)
SRC	inactive (7.78%)
YES	inactive (0.23%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (0.89%)
EphA4	inactive (8.8%)
EphA3	inactive (3.28%)
EphB4	inactive (0.44%)
EphB3	inactive (3.23%)
EphB2	inactive (3.51%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (12.15%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-0.74%)
ZAP70	inactive (0.6%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (2.34%)
ALK	inactive (4.86%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (4.03%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (1.2%)
IGF1R	inactive (3.2%)
IRR	inactive (2.92%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (-1.29%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (4.69%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (1.12%)
TRKB	inactive (2.56%)
TRKC	inactive (4.07%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (6.53%)
MET	inactive (9.52%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-4.26%)
MER	inactive (4.5%)
TYRO3	inactive (2.67%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (4.76%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (5.84%)
FGFR2	inactive (7.02%)
FGFR3	inactive (4.97%)
FGFR4	inactive (0.28%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (5.82%)
KDR	inactive (8.02%)
FLT4	inactive (2.46%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (4.58%)
KIT	inactive (3.6%)
FLT3	inactive (2.99%)
PDGFRa	inactive (11.44%)
PDGFRb	inactive (7.71%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (1.68%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (2.94%)
TNK1	inactive (5.67%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (1.23%)
ErbB2	inactive (4.11%)
ErbB4	inactive (8.52%)

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 (1.27%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (7.22%)

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 (2.92%)
MST1	inactive (6.85%)
MST2	inactive (6.4%)
MST4	inactive (-0.98%)
HGK	inactive (9.69%)
MINK	inactive (7.86%)
LOK	inactive (5.82%)
PAK1	inactive (4.24%)
PAK3	inactive (3.63%)
PAK2	inactive (1.66%)
PAK5	inactive (4.49%)
PAK6	inactive (-5.19%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (2.78%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (6.1%)
CK1g2	inactive (10.1%)
CK1g1	inactive (12.61%)
CK1g3	inactive (17.39%)

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 (2.12%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (8.29%)
AurC	inactive (-13.31%)
AurA	inactive (9.43%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (4.91%)
NEK2	inactive (2.7%)
NEK9	inactive (6.84%)
NEK7	inactive (2.77%)
NEK6	inactive (1.16%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (5.59%)
IKKe	inactive (5.46%)
IKKb	inactive (4.54%)
IKKa	inactive (9.42%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (7.95%)

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 (-0.58%)
GPRK6	inactive (1.87%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (2.81%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (4.51%)
MSK2	inactive (3.24%)
RSK1	inactive (3.4%)
RSK2	inactive (1.07%)
RSK4	inactive (0.55%)
RSK3	inactive (1.96%)
p70S6K	inactive (1.17%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.5%)
AKT1	inactive (0.96%)
AKT3	inactive (1.17%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (2.85%)
SGK3	inactive (1.48%)
SGK2	inactive (1.55%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (2.77%)
PKCg	inactive (4.9%)
PKCa	inactive (1.65%)
PKCt	inactive (3.34%)
PKCi	inactive (1.17%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (6%)
PKG1	inactive (3.86%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (1.92%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (2.15%)
ROCK2	inactive (6.38%)
MRCKb	inactive (0.91%)
MRCKa	inactive (-0.21%)

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 (4.44%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (-0.77%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-1.69%)
CaMK1d	inactive (0.3%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (4.27%)
PHKg2	inactive (5.31%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (2.75%)
CaMK2a	inactive (2.01%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (1.64%)
MAPKAPK2	inactive (2.02%)
MAPKAPK3	inactive (3.66%)
MNK2	inactive (5.53%)
MNK1	inactive (5.61%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (3.13%)
PKD1	inactive (4.64%)
PKD2	inactive (3.27%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (2.26%)
MARK3	inactive (8.13%)
MARK1	inactive (6.18%)
QIK	inactive (4.74%)
SIK	inactive (3.52%)
NuaK1	inactive (5.19%)
BRSK1	inactive (2.4%)
BRSK2	inactive (3.83%)
MELK	inactive (7.64%)
CHK1	inactive (6.33%)
PASK	inactive (-0.49%)
AMPKa1	inactive (2.96%)
AMPKa2	inactive (3.76%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (1.96%)
TSSK1	inactive (2.87%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (3.99%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (0.01%)
PIM3	inactive (2.63%)
PIM1	inactive (2.21%)

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 (2.28%)
p38a	inactive (6.59%)
p38b	inactive (3.29%)
p38d	inactive (5.95%)
Erk2	inactive (2.54%)
Erk1	inactive (1.04%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (12.8%)
GSK3B	inactive (8.29%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-0.55%)
MSSK1	inactive (0.83%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (4.76%)
CLK2	inactive (0.69%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (10.35%)
HIPK4	inactive (10.14%)
DYRK1B	inactive (8.56%)
DYRK1A	inactive (18.3%)
DYRK2	inactive (4.58%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (10.05%)