Compound in Profiling

Compound Information

Test on : RBC, Millipore

Compound Name
RBC, Millipore : TPCA-1

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

ChemSpider
RBC, Millipore : 8079440

Pubchem CID
RBC, Millipore : 9903786

ChEMBL
RBC, Millipore : CHEMBL257167

	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 (85.7%)	inactive (57%)

AGC - Akt

Bioactivity
Kinase	RBC	Millipore
AKT1	inactive (98.96%)	inactive (114%)
AKT2	inactive (93.61%)	inactive (95%)
AKT3	inactive (98.31%)	inactive (85%)

AGC - DMPK

Bioactivity
Kinase	RBC	Millipore
DMPK1	inactive (103.74%)	inactive (100%)
MRCKa	inactive (105.99%)	inactive (111%)
MRCKb	inactive (98.71%)	inactive (80%)
ROCK1	inactive (103.27%)	inactive (118%)
ROCK2	inactive (94.8%)	inactive (89%)

AGC - GRK

Bioactivity
Kinase	RBC	Millipore
BARK1	inactive (93.95%)	-
BARK2	inactive (101.84%)	-
GPRK4	inactive (99.04%)	-
GPRK5	inactive (104.73%)	inactive (93%)
GPRK6	inactive (104.12%)	inactive (85%)
GPRK7	inactive (88.59%)	inactive (67%)

AGC - RSK

Bioactivity
Kinase	RBC	Millipore
MSK1	inactive (92.64%)	inactive (120%)
MSK2	inactive (90.82%)	inactive (85%)
p70S6K	inactive (95.11%)	inactive (78%)
p70S6Kb	inactive (104.73%)	-
RSK2	inactive (57.54%)	active (33%)
RSK4	active (43.77%)	active (32%)
RSK1	inactive (51.95%)	active (30%)
RSK3	active (46.91%)	inactive (85%)

AGC - PKA

Bioactivity
Kinase	RBC	Millipore
PKACg	-	-
PRKX	inactive (96.69%)	inactive (85%)
PKACa	inactive (96.61%)	inactive (92%)

AGC - PKC

Bioactivity
Kinase	RBC	Millipore
PKCa	inactive (97.88%)	inactive (91%)
PKCd	inactive (76.48%)	inactive (78%)
PKCe	inactive (87.3%)	inactive (102%)
PKCh	inactive (83.51%)	inactive (74%)
PKCg	inactive (97.98%)	inactive (76%)
PKCi	inactive (89.2%)	inactive (109%)
PKCt	inactive (87.72%)	inactive (83%)
PKCz	inactive (97.78%)	inactive (114%)
PKCb	inactive (95.69%)	-

AGC - PKG

Bioactivity
Kinase	RBC	Millipore
PKG2	inactive (95.51%)	-
PKG1	inactive (96.27%)	-

AGC - PKN

Bioactivity
Kinase	RBC	Millipore
PKN1	inactive (77.24%)	-
PKN2	inactive (78.03%)	inactive (82%)

AGC - SGK

Bioactivity
Kinase	RBC	Millipore
SGK1	inactive (96.57%)	inactive (96%)
SGK2	inactive (99.76%)	inactive (111%)
SGK3	inactive (105.33%)	inactive (93%)

AGC - NDR

Bioactivity
Kinase	RBC	Millipore
NDR1	active (0%)	-

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 (88.4%)	inactive (63%)
ABL2	inactive (66.14%)	inactive (71%)

TK - Ack

Bioactivity
Kinase	RBC	Millipore
ACK	active (5.62%)	active (10%)

TK - ALK

Bioactivity
Kinase	RBC	Millipore
ALK	inactive (81.08%)	inactive (78%)
LTK	inactive (80.29%)	-

TK - Axl

Bioactivity
Kinase	RBC	Millipore
AXL	inactive (92.88%)	inactive (77%)
MER	inactive (81.81%)	inactive (54%)
TYRO3	inactive (83.75%)	inactive (91%)

TK - Src

Bioactivity
Kinase	RBC	Millipore
BLK	inactive (81.75%)	active (39%)
BRK	inactive (72.63%)	inactive (77%)
SRC	inactive (58.71%)	inactive (54%)
FGR	active (48.84%)	active (28%)
FRK	inactive (83.85%)	inactive (63%)
FYN	inactive (64.31%)	active (24%)
HCK	inactive (67.2%)	active (24%)
LCK	inactive (73.79%)	active (29%)
SRM	inactive (97.84%)	-
YES	active (44.54%)	active (38%)
LYN	inactive (77.44%)	active (16%)

TK - Tec

Bioactivity
Kinase	RBC	Millipore
BMX	inactive (61.18%)	active (18%)
BTK	inactive (56.57%)	active (38%)
ITK	inactive (77.45%)	active (22%)
TEC	inactive (121.84%)	-
TXK	inactive (62.42%)	active (49%)

TK - PDGFR

Bioactivity
Kinase	RBC	Millipore
KIT	inactive (63.87%)	inactive (56%)
FLT3	active (13.87%)	active (22%)
FMS	inactive (55.64%)	active (11%)
PDGFRb	inactive (72.84%)	inactive (89%)
PDGFRa	inactive (83.28%)	active (41%)

TK - Csk

Bioactivity
Kinase	RBC	Millipore
CSK	inactive (76.17%)	inactive (92%)
CTK	inactive (102.12%)	-

TK - DDR

Bioactivity
Kinase	RBC	Millipore
DDR2	inactive (134.41%)	inactive (77%)

TK - EGFR

Bioactivity
Kinase	RBC	Millipore
EGFR	inactive (94.02%)	inactive (112%)
ErbB2	inactive (105.96%)	-
ErbB4	inactive (92.29%)	inactive (91%)

TK - Eph

Bioactivity
Kinase	RBC	Millipore
EphA1	inactive (56.6%)	active (9%)
EphA2	active (37.51%)	active (32%)
EphA3	inactive (86.95%)	inactive (80%)
EphA4	inactive (79.35%)	inactive (93%)
EphA5	inactive (88.22%)	inactive (90%)
EphA6	-	-
EphA7	inactive (87.46%)	inactive (74%)
EphA8	inactive (96.71%)	inactive (84%)
EphB1	active (28.94%)	active (11%)
EphB2	inactive (86.94%)	inactive (93%)
EphB3	inactive (87.68%)	inactive (117%)
EphB4	inactive (66.61%)	active (49%)

TK - FAK

Bioactivity
Kinase	RBC	Millipore
FAK	inactive (78.91%)	inactive (68%)
PYK2	inactive (72.18%)	inactive (56%)

TK - Fer

Bioactivity
Kinase	RBC	Millipore
FER	inactive (74.44%)	inactive (83%)
FES	inactive (82.08%)	inactive (78%)

TK - FGFR

Bioactivity
Kinase	RBC	Millipore
FGFR1	inactive (57.69%)	active (29%)
FGFR2	inactive (94.81%)	active (50%)
FGFR3	inactive (84.09%)	inactive (81%)
FGFR4	inactive (99.35%)	inactive (106%)

TK - VEGFR

Bioactivity
Kinase	RBC	Millipore
FLT1	inactive (79.1%)	active (17%)
FLT4	inactive (57.89%)	active (4%)
KDR	inactive (82.03%)	active (41%)

TK - InsR

Bioactivity
Kinase	RBC	Millipore
IGF1R	inactive (88.73%)	inactive (82%)
IRR	inactive (62.53%)	inactive (69%)
INSR	inactive (76.81%)	inactive (55%)

TK - JakA

Bioactivity
Kinase	RBC	Millipore
JAK1	active (5.45%)	-
JAK2	active (7.2%)	active (4%)
JAK3	inactive (60.5%)	active (42%)
TYK2	active (6.3%)	-

TK - Musk

Bioactivity
Kinase	RBC	Millipore
MUSK	inactive (84.36%)	inactive (62%)

TK - Ret

Bioactivity
Kinase	RBC	Millipore
RET	active (18.36%)	active (30%)

TK - Met

Bioactivity
Kinase	RBC	Millipore
RON	inactive (81.74%)	inactive (73%)
MET	inactive (101.29%)	inactive (142%)

TK - Sev

Bioactivity
Kinase	RBC	Millipore
ROS	inactive (76.78%)	inactive (91%)

TK - Syk

Bioactivity
Kinase	RBC	Millipore
SYK	inactive (62.46%)	inactive (76%)
ZAP70	inactive (98.43%)	inactive (96%)

TK - Tie

Bioactivity
Kinase	RBC	Millipore
TIE2	inactive (100.1%)	inactive (82%)

TK - Trk

Bioactivity
Kinase	RBC	Millipore
TRKA	inactive (69.06%)	active (8%)
TRKB	active (42.47%)	active (27%)
TRKC	active (23.19%)	-

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 (103.84%)	-
ALK2	inactive (136.63%)	-
ALK4	inactive (106.88%)	inactive (112%)
TGFbR1	inactive (97.32%)	inactive (75%)
TGFbR2	inactive (119.88%)	-

TKL - RAF

Bioactivity
Kinase	RBC	Millipore
ARAF	inactive (92.87%)	-
BRAF	inactive (87.16%)	-
RAF1	inactive (91.65%)	inactive (54%)

TKL - IRAK

Bioactivity
Kinase	RBC	Millipore
IRAK1	inactive (58.79%)	inactive (84%)
IRAK4	inactive (105.72%)	active (46%)

TKL - LISK

Bioactivity
Kinase	RBC	Millipore
LIMK1	active (43.8%)	active (46%)

TKL - LRRK

Bioactivity
Kinase	RBC	Millipore
LRRK2	inactive (89.81%)	-

TKL - MLK

Bioactivity
Kinase	RBC	Millipore
MLK1	active (22.61%)	active (9%)
MLK2	inactive (77.09%)	-
MLK3	active (38.86%)	-
TAK1	inactive (68.14%)	active (48%)
ZAK	inactive (81.98%)	-

TKL - RIPK

Bioactivity
Kinase	RBC	Millipore
RIPK2	inactive (76.36%)	inactive (67%)

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	active (17.21%)	active (29%)
BRSK1	inactive (75.65%)	inactive (55%)
BRSK2	inactive (69.79%)	inactive (83%)
CHK1	active (29.12%)	active (37%)
LKB1	inactive (86.3%)	inactive (92%)
MARK1	inactive (78.41%)	inactive (57%)
MARK3	inactive (85.65%)	-
MARK4	inactive (78.27%)	-
MELK	inactive (81.08%)	inactive (72%)
PASK	inactive (90.8%)	inactive (107%)
QIK	inactive (76.24%)	-
NuaK2	inactive (82.81%)	-
MARK2	inactive (77.46%)	inactive (80%)
AMPKa1	-	inactive (69%)
AMPKa2	-	inactive (66%)
SIK	-	active (28%)

CAMK - CAMK1

Bioactivity
Kinase	RBC	Millipore
CaMK1a	inactive (86.75%)	inactive (74%)
CaMK1b	inactive (108.13%)	-
CaMK1d	inactive (89.87%)	inactive (76%)
CaMK1g	inactive (98.24%)	-
CaMK4	inactive (96.34%)	inactive (96%)

CAMK - CAMK2

Bioactivity
Kinase	RBC	Millipore
CaMK2a	inactive (95.48%)	-
CaMK2b	inactive (102.83%)	inactive (86%)
CaMK2d	inactive (95.09%)	inactive (83%)
CaMK2g	inactive (90.73%)	inactive (82%)

CAMK - RAD53

Bioactivity
Kinase	RBC	Millipore
CHK2	active (38.43%)	active (34%)

CAMK - DAPK

Bioactivity
Kinase	RBC	Millipore
DAPK1	inactive (87.52%)	inactive (83%)
DAPK2	inactive (108.31%)	inactive (95%)
DRAK1	inactive (77.83%)	inactive (69%)
DAPK3	inactive (94.6%)	inactive (85%)

CAMK - DCAMKL

Bioactivity
Kinase	RBC	Millipore
DCLK2	inactive (95.34%)	inactive (96%)

CAMK - MAPKAPK

Bioactivity
Kinase	RBC	Millipore
MAPKAPK2	inactive (105.65%)	inactive (92%)
MAPKAPK3	inactive (101.08%)	inactive (98%)
MAPKAPK5	inactive (98.14%)	inactive (96%)
MNK1	inactive (93.69%)	-
MNK2	inactive (76.1%)	inactive (72%)

CAMK - MLCK

Bioactivity
Kinase	RBC	Millipore
smMLCK	inactive (88.2%)	inactive (92%)
skMLCK	inactive (65.97%)	-

CAMK - PHK

Bioactivity
Kinase	RBC	Millipore
PHKg1	inactive (82.25%)	-
PHKg2	inactive (97.36%)	inactive (105%)

CAMK - PIM

Bioactivity
Kinase	RBC	Millipore
PIM1	inactive (89.75%)	inactive (95%)
PIM2	inactive (109.69%)	inactive (93%)
PIM3	inactive (84.77%)	inactive (80%)

CAMK - PKD

Bioactivity
Kinase	RBC	Millipore
PKD1	inactive (79.58%)	inactive (58%)
PKD3	inactive (75.61%)	-
PKD2	inactive (60.59%)	inactive (100%)

CAMK - TSSK

Bioactivity
Kinase	RBC	Millipore
TSSK1	inactive (68.43%)	inactive (62%)
TSSK2	inactive (93.41%)	inactive (88%)

CAMK - STK33

Bioactivity
Kinase	RBC	Millipore
STK33	inactive (77.72%)	inactive (89%)

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 (75.63%)	active (48%)
MAP3K2	inactive (75.46%)	-
MAP3K3	inactive (84.64%)	-

STE - STE-Unique

Bioactivity
Kinase	RBC	Millipore
COT	inactive (103.26%)	-
NIK	inactive (77.1%)	-

STE - STE20

Bioactivity
Kinase	RBC	Millipore
GCK	inactive (72.8%)	active (25%)
HGK	inactive (58.44%)	-
KHS1	inactive (70.86%)	-
LOK	inactive (63.23%)	inactive (51%)
MINK	inactive (64.92%)	inactive (81%)
MST1	inactive (53.75%)	active (28%)
MST2	inactive (62.13%)	inactive (68%)
MST3	inactive (54.08%)	active (38%)
MST4	inactive (76.16%)	-
OSR1	inactive (96.97%)	-
PAK1	inactive (89.13%)	-
PAK2	inactive (89.44%)	inactive (93%)
PAK3	inactive (90.18%)	inactive (96%)
PAK4	inactive (106.2%)	inactive (55%)
PAK5	inactive (93.19%)	inactive (67%)
PAK6	inactive (92.53%)	inactive (88%)
SLK	inactive (78.35%)	-
YSK1	inactive (86.97%)	-
STLK3	inactive (96.96%)	-
TAO1	inactive (89.93%)	active (42%)
TAO2	inactive (75.3%)	active (39%)
TAO3	inactive (77.54%)	inactive (61%)
MYO3B	active (0%)	-

STE - STE7

Bioactivity
Kinase	RBC	Millipore
MAP2K1	inactive (97.82%)	active (44%)
MAP2K2	inactive (97.4%)	-
MAP2K6	inactive (90.81%)	inactive (97%)
MAP2K7	-	inactive (96%)

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	active (39.7%)	active (32%)
AurB	active (22.68%)	active (1%)
AurC	active (49.86%)	active (9%)

Other - CAMKK

Bioactivity
Kinase	RBC	Millipore
CaMKK1	inactive (108.44%)	-
CaMKK2	inactive (100.02%)	-

Other - Haspin

Bioactivity
Kinase	RBC	Millipore
Haspin	inactive (81.19%)	inactive (63%)

Other - IKK

Bioactivity
Kinase	RBC	Millipore
IKKa	inactive (100%)	active (45%)
IKKb	active (8.98%)	active (12%)
IKKe	inactive (90.78%)	-
TBK1	inactive (74.93%)	active (35%)

Other - NEK

Bioactivity
Kinase	RBC	Millipore
NEK1	inactive (92.6%)	-
NEK11	inactive (82.08%)	active (25%)
NEK2	inactive (111.22%)	inactive (87%)
NEK4	inactive (91.09%)	-
NEK6	inactive (96.5%)	inactive (104%)
NEK7	inactive (104.85%)	inactive (102%)
NEK9	inactive (91.14%)	-
NEK3	inactive (97.13%)	inactive (69%)

Other - TOPK

Bioactivity
Kinase	RBC	Millipore
PBK	inactive (89.72%)	-

Other - PLK

Bioactivity
Kinase	RBC	Millipore
PLK1	inactive (96.02%)	inactive (70%)
PLK2	inactive (110.81%)	inactive (101%)
PLK3	inactive (93.37%)	inactive (88%)

Other - SgK496

Bioactivity
Kinase	RBC	Millipore
SgK496	inactive (99.84%)	-

Other - NAK

Bioactivity
Kinase	RBC	Millipore
MPSK1	inactive (84.41%)	-

Other - TTK

Bioactivity
Kinase	RBC	Millipore
TTK	inactive (107.88%)	-

Other - ULK

Bioactivity
Kinase	RBC	Millipore
ULK1	inactive (72.44%)	-
ULK2	inactive (103.1%)	inactive (86%)
ULK3	active (0%)	inactive (69%)

Other - WEE

Bioactivity
Kinase	RBC	Millipore
Wee1	inactive (89.03%)	-

Other - WNK

Bioactivity
Kinase	RBC	Millipore
Wnk2	inactive (99.3%)	inactive (90%)
Wnk3	inactive (91.11%)	inactive (81%)

Other - TLK

Bioactivity
Kinase	RBC	Millipore
TLK2	active (0%)	inactive (72%)

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 (93.98%)	inactive (71%)
CK1g1	inactive (107.33%)	inactive (104%)
CK1g2	inactive (95.4%)	inactive (100%)
CK1g3	inactive (94.51%)	inactive (94%)
CK1a	inactive (95.21%)	-
CK1e	inactive (83.84%)	-

CK1 - VRK

Bioactivity
Kinase	RBC	Millipore
VRK1	inactive (88.52%)	-
VRK2	-	inactive (95%)

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 (91.44%)	inactive (68%)
CK2a2	inactive (91.75%)	inactive (78%)

CMGC - CLK

Bioactivity
Kinase	RBC	Millipore
CLK1	inactive (102.65%)	-
CLK2	inactive (95.72%)	inactive (105%)
CLK3	inactive (75.9%)	inactive (71%)
CLK4	inactive (95.37%)	-

CMGC - DYRK

Bioactivity
Kinase	RBC	Millipore
DYRK1A	inactive (102.22%)	-
DYRK1B	inactive (96.96%)	-
DYRK2	inactive (93.49%)	inactive (96%)
DYRK3	inactive (103.85%)	-
DYRK4	inactive (99.03%)	-
HIPK1	inactive (102.03%)	inactive (106%)
HIPK2	inactive (104.27%)	inactive (94%)
HIPK3	inactive (101.05%)	inactive (100%)
HIPK4	inactive (104.83%)	-

CMGC - MAPK

Bioactivity
Kinase	RBC	Millipore
Erk1	inactive (90.05%)	inactive (80%)
Erk2	inactive (94.14%)	inactive (108%)
JNK3	inactive (92.02%)	inactive (60%)
NLK	inactive (97.63%)	inactive (89%)
p38a	inactive (100.64%)	inactive (91%)
p38b	inactive (95.05%)	inactive (89%)
p38d	inactive (100.42%)	inactive (90%)
p38g	inactive (103.9%)	inactive (90%)
JNK1	inactive (100.16%)	inactive (94%)
JNK2	inactive (95.64%)	inactive (84%)

CMGC - GSK

Bioactivity
Kinase	RBC	Millipore
GSK3A	inactive (98.82%)	inactive (64%)
GSK3B	inactive (84.96%)	inactive (101%)

CMGC - SRPK

Bioactivity
Kinase	RBC	Millipore
MSSK1	inactive (90.71%)	inactive (96%)
SRPK1	inactive (96.26%)	inactive (105%)
SRPK2	inactive (98.33%)	inactive (102%)

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 (85.7%)	-

Atypical - Alpha

Bioactivity
Kinase	RBC	Millipore
eEF2K	-	inactive (77%)

Atypical - PIKK

Bioactivity
Kinase	RBC	Millipore
FRAP	-	inactive (114%)