Compound in Profiling

Compound Information

Test on : RBC, Millipore

Compound Name
RBC, Millipore : AG-1478

Inchikey
Same : GFNNBHLJANVSQV-N
RBC, Millipore : GFNNBHLJANVSQV-UHFFFAOYSA-N

ChemSpider
RBC, Millipore : 1968

Pubchem CID
RBC, Millipore : 2051

ChEMBL
RBC, Millipore : CHEMBL7917

	DRx	RBC	Metz	Millipore	GPCR
bioactivity	Kd (nM)	Remain Activity (%)	Ki (nM)	Remain Activity (%)	Inhibition (%)
active criteria	<3000nM	<50%	<1000nM	<50%	>50%

AGC

Test Member No. in Family
Family	no. Member on 518kinase	RBC	Millipore
PDK1	1	1	1
Akt	3	3	3
DMPK	7	5	5
GRK	7	6	3
RSK	8	8	7
PKA	5	3	2
PKC	9	9	8
PKG	2	3	-
PKN	3	2	1
SGK	3	3	3
NDR	4	1	-

AGC - PDK1

Bioactivity
Kinase	RBC	Millipore
PDK1	inactive (81.9%)	inactive (97%)

AGC - Akt

Bioactivity
Kinase	RBC	Millipore
AKT1	inactive (89.94%)	inactive (86%)
AKT2	inactive (84.11%)	inactive (128%)
AKT3	inactive (98.34%)	inactive (112%)

AGC - DMPK

Bioactivity
Kinase	RBC	Millipore
DMPK1	inactive (102.08%)	inactive (103%)
MRCKa	inactive (82.24%)	inactive (107%)
MRCKb	inactive (84.93%)	inactive (102%)
ROCK1	inactive (95.89%)	inactive (112%)
ROCK2	inactive (92.58%)	inactive (103%)

AGC - GRK

Bioactivity
Kinase	RBC	Millipore
BARK1	inactive (96.58%)	-
BARK2	inactive (99.9%)	-
GPRK4	inactive (101.8%)	-
GPRK5	inactive (104.77%)	inactive (108%)
GPRK6	inactive (96.8%)	inactive (102%)
GPRK7	inactive (85.45%)	inactive (106%)

AGC - RSK

Bioactivity
Kinase	RBC	Millipore
MSK1	inactive (97.75%)	inactive (103%)
MSK2	inactive (94.48%)	inactive (93%)
p70S6K	inactive (88.52%)	inactive (82%)
p70S6Kb	inactive (104.6%)	-
RSK2	inactive (87.8%)	inactive (102%)
RSK4	inactive (90.51%)	inactive (123%)
RSK1	inactive (87.34%)	inactive (87%)
RSK3	inactive (85.49%)	inactive (90%)

AGC - PKA

Bioactivity
Kinase	RBC	Millipore
PKACg	inactive (87.91%)	-
PRKX	inactive (92.55%)	inactive (122%)
PKACa	inactive (98.61%)	inactive (111%)

AGC - PKC

Bioactivity
Kinase	RBC	Millipore
PKCa	inactive (111.32%)	inactive (103%)
PKCd	inactive (86.41%)	inactive (104%)
PKCe	inactive (97.76%)	inactive (94%)
PKCh	inactive (104.3%)	inactive (110%)
PKCg	inactive (105.46%)	inactive (114%)
PKCi	inactive (97.47%)	inactive (96%)
PKCt	inactive (105.01%)	inactive (105%)
PKCz	inactive (101.59%)	inactive (99%)
PKCb	inactive (95.54%)	-

AGC - PKG

Bioactivity
Kinase	RBC	Millipore
PKG2	inactive (92.21%)	-
PKG1	inactive (93.79%)	-

AGC - PKN

Bioactivity
Kinase	RBC	Millipore
PKN1	inactive (96.84%)	-
PKN2	inactive (89.76%)	inactive (94%)

AGC - SGK

Bioactivity
Kinase	RBC	Millipore
SGK1	inactive (91.3%)	inactive (89%)
SGK2	inactive (97.79%)	inactive (77%)
SGK3	inactive (90.88%)	inactive (91%)

AGC - NDR

Bioactivity
Kinase	RBC	Millipore
NDR1	inactive (104.18%)	-

TK

Test Member No. in Family
Family	no. Member on 518kinase	RBC	Millipore
Abl	2	2	2
Ack	2	1	1
ALK	2	2	1
Axl	3	3	3
Src	11	11	10
Tec	5	5	4
PDGFR	5	5	5
Csk	2	2	1
DDR	2	1	1
EGFR	4	3	2
Eph	14	12	11
FAK	2	2	2
Fer	2	2	2
FGFR	4	4	4
VEGFR	3	3	3
InsR	3	3	3
JakA	4	4	2
Musk	1	1	1
Ret	1	1	1
Met	2	2	2
Sev	1	1	1
Syk	2	2	2
Tie	2	1	1
Trk	3	3	2

TK - Abl

Bioactivity
Kinase	RBC	Millipore
ABL1	inactive (61.76%)	active (41%)
ABL2	inactive (52.6%)	active (48%)

TK - Ack

Bioactivity
Kinase	RBC	Millipore
ACK	active (28.57%)	active (34%)

TK - ALK

Bioactivity
Kinase	RBC	Millipore
ALK	inactive (91.53%)	inactive (100%)
LTK	inactive (60.28%)	-

TK - Axl

Bioactivity
Kinase	RBC	Millipore
AXL	inactive (95.33%)	inactive (102%)
MER	inactive (76.88%)	inactive (94%)
TYRO3	inactive (96.74%)	inactive (62%)

TK - Src

Bioactivity
Kinase	RBC	Millipore
BLK	inactive (68.22%)	active (43%)
BRK	active (39%)	active (33%)
SRC	inactive (71.89%)	inactive (58%)
FGR	inactive (75.32%)	inactive (52%)
FRK	inactive (81.09%)	inactive (53%)
FYN	inactive (85.73%)	active (41%)
HCK	inactive (61.84%)	active (48%)
LCK	inactive (74.93%)	inactive (52%)
SRM	inactive (93.78%)	-
YES	inactive (59.87%)	active (30%)
LYN	active (43.06%)	active (10%)

TK - Tec

Bioactivity
Kinase	RBC	Millipore
BMX	inactive (88.63%)	inactive (84%)
BTK	inactive (76.72%)	inactive (91%)
ITK	inactive (93.77%)	inactive (100%)
TEC	inactive (125.87%)	-
TXK	inactive (75.05%)	inactive (87%)

TK - PDGFR

Bioactivity
Kinase	RBC	Millipore
KIT	inactive (93.96%)	inactive (103%)
FLT3	active (37.61%)	inactive (111%)
FMS	inactive (98.16%)	inactive (88%)
PDGFRb	inactive (100.08%)	inactive (102%)
PDGFRa	inactive (93.26%)	inactive (104%)

TK - Csk

Bioactivity
Kinase	RBC	Millipore
CSK	inactive (91.09%)	inactive (111%)
CTK	inactive (102.77%)	-

TK - DDR

Bioactivity
Kinase	RBC	Millipore
DDR2	inactive (99.19%)	inactive (97%)

TK - EGFR

Bioactivity
Kinase	RBC	Millipore
EGFR	active (0.72%)	active (-5%)
ErbB2	active (22.46%)	-
ErbB4	active (35.52%)	active (35%)

TK - Eph

Bioactivity
Kinase	RBC	Millipore
EphA1	inactive (81.65%)	active (42%)
EphA2	inactive (85.15%)	inactive (89%)
EphA3	inactive (97.88%)	inactive (95%)
EphA4	inactive (81.65%)	inactive (103%)
EphA5	inactive (68.33%)	inactive (77%)
EphA6	active (27.76%)	-
EphA7	inactive (65.02%)	inactive (73%)
EphA8	inactive (81.49%)	inactive (85%)
EphB1	inactive (82.78%)	inactive (84%)
EphB2	inactive (98.09%)	inactive (92%)
EphB3	inactive (99.07%)	inactive (94%)
EphB4	inactive (59.66%)	active (45%)

TK - FAK

Bioactivity
Kinase	RBC	Millipore
FAK	inactive (95.08%)	inactive (146%)
PYK2	inactive (85.31%)	inactive (117%)

TK - Fer

Bioactivity
Kinase	RBC	Millipore
FER	inactive (77.1%)	inactive (113%)
FES	inactive (103.7%)	inactive (119%)

TK - FGFR

Bioactivity
Kinase	RBC	Millipore
FGFR1	inactive (84.85%)	inactive (99%)
FGFR2	inactive (97.48%)	inactive (101%)
FGFR3	inactive (88.54%)	inactive (104%)
FGFR4	inactive (78.68%)	inactive (90%)

TK - VEGFR

Bioactivity
Kinase	RBC	Millipore
FLT1	inactive (74.43%)	inactive (60%)
FLT4	inactive (99.31%)	active (47%)
KDR	inactive (74.67%)	inactive (60%)

TK - InsR

Bioactivity
Kinase	RBC	Millipore
IGF1R	inactive (75.91%)	inactive (111%)
IRR	inactive (99.04%)	inactive (105%)
INSR	inactive (77.55%)	inactive (110%)

TK - JakA

Bioactivity
Kinase	RBC	Millipore
JAK1	inactive (90.41%)	-
JAK2	inactive (97.44%)	inactive (123%)
JAK3	inactive (91.59%)	inactive (109%)
TYK2	inactive (98.14%)	-

TK - Musk

Bioactivity
Kinase	RBC	Millipore
MUSK	inactive (88.28%)	inactive (121%)

TK - Ret

Bioactivity
Kinase	RBC	Millipore
RET	active (35.3%)	active (39%)

TK - Met

Bioactivity
Kinase	RBC	Millipore
RON	inactive (87.8%)	inactive (116%)
MET	inactive (75.53%)	inactive (77%)

TK - Sev

Bioactivity
Kinase	RBC	Millipore
ROS	inactive (91.18%)	inactive (100%)

TK - Syk

Bioactivity
Kinase	RBC	Millipore
SYK	inactive (86.92%)	inactive (121%)
ZAP70	inactive (101.85%)	inactive (103%)

TK - Tie

Bioactivity
Kinase	RBC	Millipore
TIE2	inactive (88.63%)	inactive (111%)

TK - Trk

Bioactivity
Kinase	RBC	Millipore
TRKA	inactive (92.55%)	inactive (88%)
TRKB	inactive (93.26%)	active (50%)
TRKC	inactive (86.29%)	-

TKL

Test Member No. in Family
Family	no. Member on 518kinase	RBC	Millipore
STKR	12	5	2
RAF	5	3	1
IRAK	4	2	2
LISK	4	1	1
LRRK	2	1	-
MLK	10	5	2
RIPK	5	1	1

TKL - STKR

Bioactivity
Kinase	RBC	Millipore
ALK1	inactive (96.43%)	-
ALK2	inactive (107.86%)	-
ALK4	inactive (97.96%)	inactive (105%)
TGFbR1	inactive (100.45%)	inactive (100%)
TGFbR2	inactive (94.47%)	-

TKL - RAF

Bioactivity
Kinase	RBC	Millipore
ARAF	inactive (107.86%)	-
BRAF	inactive (96.01%)	-
RAF1	inactive (78.37%)	inactive (99%)

TKL - IRAK

Bioactivity
Kinase	RBC	Millipore
IRAK1	inactive (86.59%)	inactive (84%)
IRAK4	inactive (77.67%)	inactive (64%)

TKL - LISK

Bioactivity
Kinase	RBC	Millipore
LIMK1	inactive (72.35%)	inactive (111%)

TKL - LRRK

Bioactivity
Kinase	RBC	Millipore
LRRK2	inactive (60.89%)	-

TKL - MLK

Bioactivity
Kinase	RBC	Millipore
MLK1	inactive (82.84%)	inactive (76%)
MLK2	inactive (100.73%)	-
MLK3	inactive (84.05%)	-
TAK1	inactive (96.92%)	inactive (100%)
ZAK	inactive (99.27%)	-

TKL - RIPK

Bioactivity
Kinase	RBC	Millipore
RIPK2	active (45.39%)	active (26%)

CAMK

Test Member No. in Family
Family	no. Member on 518kinase	RBC	Millipore
CAMKL	20	13	12
CAMK1	5	5	3
CAMK2	4	4	3
RAD53	1	1	1
DAPK	5	4	4
DCAMKL	3	1	1
MAPKAPK	5	5	4
MLCK	5	2	1
PHK	2	2	1
PIM	3	3	3
PKD	3	3	2
TSSK	5	2	2
STK33	1	-	-

CAMK - CAMKL

Bioactivity
Kinase	RBC	Millipore
NuaK1	inactive (75.84%)	inactive (94%)
BRSK1	inactive (93.09%)	active (14%)
BRSK2	inactive (96.72%)	inactive (91%)
CHK1	inactive (93.7%)	inactive (97%)
LKB1	inactive (96.78%)	inactive (100%)
MARK1	inactive (94.01%)	inactive (94%)
MARK3	inactive (89.79%)	-
MARK4	inactive (98.5%)	-
MELK	inactive (81.78%)	inactive (89%)
PASK	inactive (90.2%)	inactive (92%)
QIK	inactive (98.73%)	-
NuaK2	inactive (142.35%)	-
MARK2	inactive (97.03%)	inactive (97%)
AMPKa1	-	inactive (94%)
AMPKa2	-	inactive (96%)
SIK	-	inactive (84%)

CAMK - CAMK1

Bioactivity
Kinase	RBC	Millipore
CaMK1a	inactive (99.22%)	inactive (108%)
CaMK1b	inactive (89.62%)	-
CaMK1d	inactive (96.6%)	inactive (107%)
CaMK1g	inactive (93.55%)	-
CaMK4	inactive (94.41%)	inactive (121%)

CAMK - CAMK2

Bioactivity
Kinase	RBC	Millipore
CaMK2a	inactive (98.19%)	-
CaMK2b	inactive (91.15%)	inactive (90%)
CaMK2d	inactive (96.1%)	inactive (60%)
CaMK2g	inactive (97.28%)	active (45%)

CAMK - RAD53

Bioactivity
Kinase	RBC	Millipore
CHK2	inactive (79.66%)	inactive (79%)

CAMK - DAPK

Bioactivity
Kinase	RBC	Millipore
DAPK1	inactive (107.59%)	inactive (104%)
DAPK2	inactive (93.25%)	inactive (86%)
DRAK1	inactive (95.43%)	inactive (103%)
DAPK3	inactive (94.63%)	inactive (89%)

CAMK - DCAMKL

Bioactivity
Kinase	RBC	Millipore
DCLK2	inactive (94.69%)	inactive (122%)

CAMK - MAPKAPK

Bioactivity
Kinase	RBC	Millipore
MAPKAPK2	inactive (98.03%)	inactive (108%)
MAPKAPK3	inactive (92.69%)	inactive (94%)
MAPKAPK5	inactive (89.5%)	inactive (93%)
MNK1	inactive (80.82%)	-
MNK2	active (39.52%)	active (33%)

CAMK - MLCK

Bioactivity
Kinase	RBC	Millipore
smMLCK	inactive (89.02%)	inactive (64%)
skMLCK	inactive (90.07%)	-

CAMK - PHK

Bioactivity
Kinase	RBC	Millipore
PHKg1	inactive (88.94%)	-
PHKg2	inactive (92.59%)	inactive (104%)

CAMK - PIM

Bioactivity
Kinase	RBC	Millipore
PIM1	inactive (91.49%)	inactive (62%)
PIM2	inactive (103.67%)	inactive (121%)
PIM3	inactive (99.38%)	inactive (112%)

CAMK - PKD

Bioactivity
Kinase	RBC	Millipore
PKD1	inactive (92.26%)	inactive (110%)
PKD3	inactive (86.54%)	-
PKD2	inactive (92.26%)	inactive (93%)

CAMK - TSSK

Bioactivity
Kinase	RBC	Millipore
TSSK1	inactive (95.72%)	inactive (98%)
TSSK2	inactive (94.8%)	inactive (89%)

CAMK - STK33

Bioactivity
Kinase	RBC	Millipore
STK33	inactive (88.31%)	inactive (96%)

STE

Test Member No. in Family
Family	no. Member on 518kinase	RBC	Millipore
STE11	8	3	1
STE-Unique	2	2	-
STE20	31	23	14
STE7	7	3	3

STE - STE11

Bioactivity
Kinase	RBC	Millipore
MAP3K5	inactive (105.74%)	inactive (103%)
MAP3K2	inactive (98.2%)	-
MAP3K3	inactive (88.28%)	-

STE - STE-Unique

Bioactivity
Kinase	RBC	Millipore
COT	inactive (104.21%)	-
NIK	inactive (107%)	-

STE - STE20

Bioactivity
Kinase	RBC	Millipore
GCK	inactive (98.08%)	inactive (96%)
HGK	inactive (68.07%)	-
KHS1	inactive (59.52%)	-
LOK	active (24.46%)	active (24%)
MINK	inactive (83.07%)	inactive (96%)
MST1	inactive (91.99%)	inactive (96%)
MST2	inactive (124.27%)	inactive (100%)
MST3	inactive (96.84%)	inactive (95%)
MST4	inactive (107.59%)	-
OSR1	inactive (91.97%)	-
PAK1	inactive (89.3%)	-
PAK2	inactive (90.71%)	inactive (126%)
PAK3	inactive (98.87%)	inactive (110%)
PAK4	inactive (76.47%)	inactive (95%)
PAK5	inactive (82.95%)	inactive (109%)
PAK6	inactive (81.63%)	inactive (102%)
SLK	inactive (64.6%)	-
YSK1	inactive (100.81%)	-
STLK3	inactive (97.01%)	-
TAO1	inactive (107.55%)	inactive (102%)
TAO2	inactive (96.07%)	inactive (113%)
TAO3	inactive (90.38%)	inactive (102%)
MYO3B	inactive (81.21%)	-

STE - STE7

Bioactivity
Kinase	RBC	Millipore
MAP2K1	inactive (98.46%)	inactive (114%)
MAP2K2	inactive (102.03%)	-
MAP2K6	inactive (88.74%)	active (47%)
MAP2K7	-	inactive (99%)

Other

Test Member No. in Family
Family	no. Member on 518kinase	RBC	Millipore
Aur	3	3	3
CAMKK	2	2	-
Haspin	1	1	1
IKK	4	4	3
NEK	11	8	5
TOPK	1	1	-
PLK	4	3	3
SgK496	1	1	-
NAK	4	1	-
TTK	1	1	-
ULK	5	3	2
WEE	3	1	-
WNK	4	2	2
TLK	2	1	1

Other - Aur

Bioactivity
Kinase	RBC	Millipore
AurA	inactive (93.26%)	inactive (94%)
AurB	inactive (74.4%)	inactive (64%)
AurC	inactive (85.78%)	inactive (100%)

Other - CAMKK

Bioactivity
Kinase	RBC	Millipore
CaMKK1	inactive (92.16%)	-
CaMKK2	inactive (97.5%)	-

Other - Haspin

Bioactivity
Kinase	RBC	Millipore
Haspin	inactive (84.76%)	inactive (130%)

Other - IKK

Bioactivity
Kinase	RBC	Millipore
IKKa	inactive (103.28%)	inactive (105%)
IKKb	inactive (102.42%)	inactive (95%)
IKKe	inactive (101.21%)	-
TBK1	inactive (78.03%)	inactive (98%)

Other - NEK

Bioactivity
Kinase	RBC	Millipore
NEK1	inactive (93.11%)	-
NEK11	inactive (96.95%)	inactive (102%)
NEK2	inactive (88.25%)	inactive (97%)
NEK4	inactive (87.55%)	-
NEK6	inactive (105.38%)	inactive (109%)
NEK7	inactive (99.01%)	inactive (102%)
NEK9	inactive (82.57%)	-
NEK3	inactive (84.35%)	inactive (111%)

Other - TOPK

Bioactivity
Kinase	RBC	Millipore
PBK	inactive (70.87%)	-

Other - PLK

Bioactivity
Kinase	RBC	Millipore
PLK1	inactive (104.6%)	inactive (112%)
PLK2	inactive (101.67%)	inactive (109%)
PLK3	inactive (92.3%)	inactive (83%)

Other - SgK496

Bioactivity
Kinase	RBC	Millipore
SgK496	inactive (90.81%)	-

Other - NAK

Bioactivity
Kinase	RBC	Millipore
MPSK1	inactive (101.37%)	-

Other - TTK

Bioactivity
Kinase	RBC	Millipore
TTK	inactive (107.88%)	-

Other - ULK

Bioactivity
Kinase	RBC	Millipore
ULK1	inactive (84.7%)	-
ULK2	inactive (103.11%)	inactive (104%)
ULK3	inactive (77.33%)	inactive (102%)

Other - WEE

Bioactivity
Kinase	RBC	Millipore
Wee1	inactive (92.44%)	-

Other - WNK

Bioactivity
Kinase	RBC	Millipore
Wnk2	inactive (98.59%)	inactive (112%)
Wnk3	inactive (97.82%)	inactive (93%)

Other - TLK

Bioactivity
Kinase	RBC	Millipore
TLK2	inactive (93.87%)	inactive (119%)

CK1

Test Member No. in Family
Family	no. Member on 518kinase	RBC	Millipore
CK1	7	6	4
VRK	3	1	1

CK1 - CK1

Bioactivity
Kinase	RBC	Millipore
CK1d	inactive (100.4%)	inactive (87%)
CK1g1	inactive (99.86%)	inactive (100%)
CK1g2	inactive (97.13%)	inactive (100%)
CK1g3	inactive (92.39%)	inactive (128%)
CK1a	inactive (92.53%)	-
CK1e	inactive (75.27%)	-

CK1 - VRK

Bioactivity
Kinase	RBC	Millipore
VRK1	inactive (105.35%)	-
VRK2	-	inactive (102%)

CMGC

Test Member No. in Family
Family	no. Member on 518kinase	RBC	Millipore
CK2	3	2	2
CLK	4	4	2
DYRK	10	9	4
MAPK	14	10	10
GSK	2	2	2
SRPK	3	3	3

CMGC - CK2

Bioactivity
Kinase	RBC	Millipore
CK2a1	-	inactive (110%)
CK2a2	inactive (92.29%)	inactive (128%)

CMGC - CLK

Bioactivity
Kinase	RBC	Millipore
CLK1	inactive (103.26%)	-
CLK2	inactive (89.61%)	inactive (110%)
CLK3	inactive (90.52%)	inactive (94%)
CLK4	inactive (98.16%)	-

CMGC - DYRK

Bioactivity
Kinase	RBC	Millipore
DYRK1A	inactive (90.72%)	-
DYRK1B	inactive (104.28%)	-
DYRK2	inactive (84.56%)	inactive (92%)
DYRK3	inactive (96.25%)	-
DYRK4	inactive (91.74%)	-
HIPK1	inactive (98.69%)	inactive (95%)
HIPK2	inactive (88.84%)	inactive (98%)
HIPK3	inactive (98.86%)	inactive (110%)
HIPK4	inactive (64.42%)	-

CMGC - MAPK

Bioactivity
Kinase	RBC	Millipore
Erk1	inactive (96.41%)	inactive (86%)
Erk2	inactive (91.68%)	inactive (101%)
JNK3	inactive (88.97%)	inactive (73%)
NLK	inactive (83.1%)	inactive (90%)
p38a	inactive (107.31%)	inactive (56%)
p38b	inactive (97.47%)	inactive (95%)
p38d	inactive (99.75%)	inactive (118%)
p38g	inactive (98.51%)	inactive (116%)
JNK1	inactive (93.81%)	inactive (112%)
JNK2	inactive (92.2%)	inactive (97%)

CMGC - GSK

Bioactivity
Kinase	RBC	Millipore
GSK3A	inactive (104.28%)	inactive (101%)
GSK3B	inactive (98.69%)	inactive (91%)

CMGC - SRPK

Bioactivity
Kinase	RBC	Millipore
MSSK1	inactive (90.13%)	inactive (104%)
SRPK1	inactive (102.33%)	inactive (101%)
SRPK2	inactive (88.22%)	inactive (104%)

Atypical

Test Member No. in Family
Family	no. Member on 518kinase	RBC	Millipore
PDHK	5	1	-
Alpha	6	-	1
PIKK	6	-	1

Atypical - PDHK

Bioactivity
Kinase	RBC	Millipore
PDHK1	inactive (81.9%)	-

Atypical - Alpha

Bioactivity
Kinase	RBC	Millipore
eEF2K	-	inactive (85%)

Atypical - PIKK

Bioactivity
Kinase	RBC	Millipore
FRAP	-	inactive (99%)