Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : CHEMBL477979

Inchikey : HWUIKJWOZNTZQM-UHFFFAOYSA-N

ChemSpider : 24699455

Pubchem CID : 44578254

ChEMBL : CHEMBL477979

	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 (-1.59%)
TYK2	inactive (2.94%)
JAK2	inactive (-1.28%)
JAK3	inactive (1.51%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (-1.61%)
FES	inactive (-3%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (1.26%)
ABL2	inactive (-0.41%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (-10.06%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (-4.09%)
BTK	inactive (-1.32%)
TXK	inactive (-1.03%)
TEC	inactive (-2.37%)
ITK	inactive (-0.47%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (-4.09%)
SRM	inactive (2.24%)
FRK	inactive (-0.89%)
BLK	inactive (-1.6%)
LCK	inactive (0.84%)
HCK	inactive (-1.19%)
FGR	inactive (-1.1%)
FYN	inactive (0.91%)
SRC	inactive (-6.71%)
YES	inactive (-0.56%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-2.07%)
EphA4	inactive (-6.72%)
EphA3	inactive (-6.99%)
EphB4	inactive (-2.91%)
EphB3	inactive (-4.82%)
EphB2	inactive (0.35%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (-10.5%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-0.36%)
ZAP70	inactive (-1.41%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (-1.83%)
ALK	inactive (-3.45%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (0.55%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (-4.51%)
IGF1R	inactive (-3.34%)
IRR	inactive (-4.41%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (0.09%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (-2.53%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (0.4%)
TRKB	inactive (0.73%)
TRKC	inactive (1.79%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (0.06%)
MET	inactive (-5.28%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (4.77%)
MER	inactive (-0.29%)
TYRO3	inactive (-0.5%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (0.64%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (-2.8%)
FGFR2	inactive (-3.57%)
FGFR3	inactive (-3.57%)
FGFR4	inactive (0.47%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (-1.81%)
KDR	inactive (0.78%)
FLT4	inactive (2.58%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (0.94%)
KIT	inactive (-4.83%)
FLT3	inactive (-1.66%)
PDGFRa	inactive (2.31%)
PDGFRb	inactive (2.4%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (-0.28%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (0.35%)
TNK1	inactive (-5.58%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (1.34%)
ErbB2	inactive (-4.79%)
ErbB4	inactive (-12.02%)

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 (-0.58%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (-5.03%)

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 (1.59%)
MST1	inactive (-3.63%)
MST2	inactive (-4.98%)
MST4	inactive (1.12%)
HGK	inactive (1.81%)
MINK	inactive (-1.09%)
LOK	inactive (-5.65%)
PAK1	inactive (-0.84%)
PAK3	inactive (-3.2%)
PAK2	inactive (-3.39%)
PAK5	inactive (-2.22%)
PAK6	inactive (-15.13%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (-1.83%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (-5.5%)
CK1g2	inactive (-3.47%)
CK1g1	inactive (-2.32%)
CK1g3	inactive (-1.44%)

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 (0.01%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (2.24%)
AurC	inactive (1.27%)
AurA	inactive (-2.53%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (-1.39%)
NEK2	inactive (-3.6%)
NEK9	inactive (4.93%)
NEK7	inactive (-4.59%)
NEK6	inactive (-3.72%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (-1.07%)
IKKe	inactive (-4.16%)
IKKb	inactive (-1.83%)
IKKa	inactive (-1.81%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (-5.81%)

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 (-7.32%)
GPRK6	inactive (-2.12%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (-1.38%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (-3.9%)
MSK2	inactive (-2.17%)
RSK1	inactive (-0.32%)
RSK2	inactive (1.68%)
RSK4	inactive (0.59%)
RSK3	inactive (0.47%)
p70S6K	inactive (-2.29%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (-3%)
AKT1	inactive (-2.49%)
AKT3	inactive (-1.32%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (-0.09%)
SGK3	inactive (-2.17%)
SGK2	inactive (-7.09%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (-3.07%)
PKCg	inactive (-2.88%)
PKCa	inactive (0.46%)
PKCt	inactive (-1.29%)
PKCi	inactive (-0.8%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (-0.98%)
PKG1	inactive (-2.98%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (-1.51%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (-0.1%)
ROCK2	inactive (-1.76%)
MRCKb	inactive (0.39%)
MRCKa	inactive (-2.08%)

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 (-2.4%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (-1.07%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-2.57%)
CaMK1d	inactive (0.57%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (1.18%)
PHKg2	inactive (-6.57%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (-1.11%)
CaMK2a	inactive (-3.85%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (-1.11%)
MAPKAPK2	inactive (-1.8%)
MAPKAPK3	inactive (9.15%)
MNK2	inactive (1.12%)
MNK1	inactive (-0.97%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (-2.84%)
PKD1	inactive (-3.57%)
PKD2	inactive (-0.88%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (0.5%)
MARK3	inactive (-0.42%)
MARK1	inactive (0.65%)
QIK	inactive (-9.28%)
SIK	inactive (-1.49%)
NuaK1	inactive (3.92%)
BRSK1	inactive (-1.28%)
BRSK2	inactive (1.61%)
MELK	inactive (-2.99%)
CHK1	inactive (-3.38%)
PASK	inactive (0.4%)
AMPKa1	inactive (-1.42%)
AMPKa2	inactive (-5.48%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (-1.52%)
TSSK1	inactive (-1.52%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (-2.3%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (1.24%)
PIM3	inactive (2.53%)
PIM1	inactive (0.56%)

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 (-0.22%)
p38a	inactive (39.45%)
p38b	inactive (37%)
p38d	inactive (-4.39%)
Erk2	inactive (-4.45%)
Erk1	inactive (-0.93%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (3.31%)
GSK3B	inactive (3.01%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (30.84%)
MSSK1	inactive (-0.59%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (0.67%)
CLK2	inactive (-0.78%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (1.88%)
HIPK4	inactive (3.79%)
DYRK1B	inactive (3.96%)
DYRK1A	inactive (2.28%)
DYRK2	inactive (-3.21%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (0.22%)