Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : CHEMBL477978

Inchikey : OALMGWWMKRZIDJ-UHFFFAOYSA-N

ChemSpider : 24699354

Pubchem CID : 44578253

ChEMBL : CHEMBL477978

	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 (9.1%)
TYK2	inactive (-2.34%)
JAK2	inactive (4.08%)
JAK3	inactive (3.02%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (4.17%)
FES	inactive (2.29%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (6.52%)
ABL2	inactive (8.56%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (1.73%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (4.53%)
BTK	inactive (3.37%)
TXK	inactive (5.63%)
TEC	inactive (5.66%)
ITK	inactive (2.35%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (3.75%)
SRM	inactive (0.74%)
FRK	inactive (0.68%)
BLK	inactive (3.76%)
LCK	inactive (2.85%)
HCK	inactive (7.52%)
FGR	inactive (5.25%)
FYN	inactive (0.78%)
SRC	inactive (4.58%)
YES	inactive (1.09%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (1.67%)
EphA4	inactive (3.57%)
EphA3	inactive (5.14%)
EphB4	inactive (0.58%)
EphB3	inactive (1.76%)
EphB2	inactive (7.74%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (9.58%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (0.52%)
ZAP70	inactive (6.15%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (0.02%)
ALK	inactive (4.07%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (7.1%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (1.48%)
IGF1R	inactive (5.21%)
IRR	inactive (2.14%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (6.99%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (8.57%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (2.19%)
TRKB	inactive (-0.15%)
TRKC	inactive (-0.57%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (3.46%)
MET	inactive (5.05%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (3.11%)
MER	inactive (3.6%)
TYRO3	inactive (-0.08%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (7.84%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (5.66%)
FGFR2	inactive (6.2%)
FGFR3	inactive (4.7%)
FGFR4	inactive (2.89%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (2.09%)
KDR	inactive (8.4%)
FLT4	inactive (5.49%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (5.17%)
KIT	inactive (4.9%)
FLT3	inactive (-0.64%)
PDGFRa	inactive (12.78%)
PDGFRb	inactive (9.04%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (4.17%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (4.5%)
TNK1	inactive (-2.52%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (14.28%)
ErbB2	inactive (-2.24%)
ErbB4	inactive (17.91%)

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 (1.67%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (3.21%)

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 (2.05%)
MST1	inactive (4.46%)
MST2	inactive (4.05%)
MST4	inactive (-1.45%)
HGK	inactive (0.87%)
MINK	inactive (1.64%)
LOK	inactive (6.5%)
PAK1	inactive (4.6%)
PAK3	inactive (4.44%)
PAK2	inactive (1.97%)
PAK5	inactive (13.62%)
PAK6	inactive (-8.15%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (4.68%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (3.89%)
CK1g2	inactive (2.68%)
CK1g1	inactive (2.66%)
CK1g3	inactive (2.73%)

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 (2.23%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (7.57%)
AurC	inactive (13.97%)
AurA	inactive (4.4%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (1.48%)
NEK2	inactive (3.36%)
NEK9	inactive (-4.93%)
NEK7	inactive (3.76%)
NEK6	inactive (-2.96%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (3.86%)
IKKe	inactive (0.57%)
IKKb	inactive (-2.31%)
IKKa	inactive (-8.02%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (8.51%)

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 (6.92%)
GPRK6	inactive (-3.25%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (1.2%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (3.23%)
MSK2	inactive (2.43%)
RSK1	inactive (0.15%)
RSK2	inactive (0.57%)
RSK4	inactive (1.2%)
RSK3	inactive (0.27%)
p70S6K	inactive (0.99%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.72%)
AKT1	inactive (0.76%)
AKT3	inactive (0.64%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (2.69%)
SGK3	inactive (0.67%)
SGK2	inactive (-1.56%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (-0.62%)
PKCg	inactive (3.86%)
PKCa	inactive (2.17%)
PKCt	inactive (0.58%)
PKCi	inactive (2.97%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (2.94%)
PKG1	inactive (4.23%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (0.91%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (1.55%)
ROCK2	inactive (1.7%)
MRCKb	inactive (1.51%)
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 (1.29%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (-10.34%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (3.67%)
CaMK1d	inactive (2.73%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (-0.89%)
PHKg2	inactive (1.55%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (2.35%)
CaMK2a	inactive (4.57%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (-0.72%)
MAPKAPK2	inactive (0.95%)
MAPKAPK3	inactive (4.53%)
MNK2	inactive (-0.44%)
MNK1	inactive (2.58%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (2.53%)
PKD1	inactive (2.69%)
PKD2	inactive (2.9%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (1.5%)
MARK3	inactive (2.82%)
MARK1	inactive (0.65%)
QIK	inactive (1.96%)
SIK	inactive (8.02%)
NuaK1	inactive (2.62%)
BRSK1	inactive (0.64%)
BRSK2	inactive (-1.13%)
MELK	inactive (2.41%)
CHK1	inactive (5.14%)
PASK	inactive (-0.83%)
AMPKa1	inactive (0.6%)
AMPKa2	inactive (1.51%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (-1.47%)
TSSK1	inactive (-1.51%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (5.32%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (1.66%)
PIM3	inactive (-1%)
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 (6.33%)
p38a	inactive (17.35%)
p38b	inactive (14.23%)
p38d	inactive (2.53%)
Erk2	inactive (4.11%)
Erk1	inactive (0.88%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (1.84%)
GSK3B	inactive (0.33%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-2.48%)
MSSK1	inactive (0.5%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (1.19%)
CLK2	inactive (2.19%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (1.1%)
HIPK4	inactive (3.16%)
DYRK1B	inactive (0.46%)
DYRK1A	inactive (-0.59%)
DYRK2	inactive (1.81%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (-5.06%)