Compound in Profiling

Compound Information

Test on : RBC, Millipore

Compound Name
RBC : 5-[(5-chloro-2-oxo-1H-indol-3-ylidene)methyl]-N-[2-(diethylamino)ethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
Millipore : SU11652

Inchikey
Same : XPLJEFSRINKZLC-N
RBC : XPLJEFSRINKZLC-UHFFFAOYSA-N
Millipore : XPLJEFSRINKZLC-ATVHPVEESA-N

ChemSpider
RBC : 21465193
Millipore : 4486265

Pubchem CID
RBC : 24906267
Millipore : 5329103

ChEMBL
RBC : -
Millipore : CHEMBL13485

RBC	Millipore

	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 (101.46%)	inactive (78%)

AGC - Akt

Bioactivity
Kinase	RBC	Millipore
AKT1	inactive (101.92%)	inactive (99%)
AKT2	inactive (86.85%)	inactive (91%)
AKT3	inactive (84.18%)	inactive (79%)

AGC - DMPK

Bioactivity
Kinase	RBC	Millipore
DMPK1	inactive (101.59%)	inactive (52%)
MRCKa	inactive (60%)	inactive (118%)
MRCKb	inactive (96.11%)	inactive (103%)
ROCK1	inactive (89.73%)	inactive (101%)
ROCK2	inactive (73.54%)	inactive (86%)

AGC - GRK

Bioactivity
Kinase	RBC	Millipore
BARK1	inactive (103.89%)	-
BARK2	inactive (97.83%)	-
GPRK4	inactive (80.81%)	-
GPRK5	inactive (82.69%)	inactive (68%)
GPRK6	active (46.26%)	inactive (68%)
GPRK7	inactive (62.24%)	inactive (57%)

AGC - RSK

Bioactivity
Kinase	RBC	Millipore
MSK1	inactive (59.04%)	inactive (80%)
MSK2	inactive (58.96%)	active (42%)
p70S6K	active (41.75%)	active (24%)
p70S6Kb	inactive (91.61%)	-
RSK2	active (15.1%)	active (11%)
RSK4	active (10.47%)	active (14%)
RSK1	active (13.06%)	active (9%)
RSK3	active (10.02%)	active (11%)

AGC - PKA

Bioactivity
Kinase	RBC	Millipore
PKACg	inactive (101.45%)	-
PRKX	inactive (83.93%)	inactive (63%)
PKACa	inactive (89.97%)	inactive (81%)

AGC - PKC

Bioactivity
Kinase	RBC	Millipore
PKCa	inactive (93.13%)	inactive (100%)
PKCd	inactive (90.42%)	inactive (95%)
PKCe	inactive (101.96%)	inactive (99%)
PKCh	inactive (86.11%)	inactive (110%)
PKCg	inactive (101.43%)	inactive (94%)
PKCi	inactive (91.9%)	inactive (84%)
PKCt	inactive (104.69%)	inactive (102%)
PKCz	inactive (103.54%)	inactive (103%)
PKCb	inactive (109.55%)	-

AGC - PKG

Bioactivity
Kinase	RBC	Millipore
PKG2	inactive (82.6%)	-
PKG1	inactive (64.25%)	-

AGC - PKN

Bioactivity
Kinase	RBC	Millipore
PKN1	active (36.49%)	-
PKN2	inactive (84.36%)	inactive (52%)

AGC - SGK

Bioactivity
Kinase	RBC	Millipore
SGK1	active (49.61%)	inactive (59%)
SGK2	inactive (62.77%)	inactive (60%)
SGK3	inactive (102.55%)	inactive (115%)

AGC - NDR

Bioactivity
Kinase	RBC	Millipore
NDR1	inactive (95.78%)	-

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	active (24.65%)	active (23%)
ABL2	active (46.79%)	active (47%)

TK - Ack

Bioactivity
Kinase	RBC	Millipore
ACK	active (22.62%)	active (25%)

TK - ALK

Bioactivity
Kinase	RBC	Millipore
ALK	active (3.45%)	active (8%)
LTK	active (11.57%)	-

TK - Axl

Bioactivity
Kinase	RBC	Millipore
AXL	active (25.17%)	active (9%)
MER	active (11.5%)	active (7%)
TYRO3	active (23.21%)	active (24%)

TK - Src

Bioactivity
Kinase	RBC	Millipore
BLK	active (15.81%)	active (1%)
BRK	inactive (51.28%)	inactive (65%)
SRC	active (26.02%)	active (48%)
FGR	active (11.48%)	active (8%)
FRK	inactive (59.3%)	active (31%)
FYN	active (28.39%)	active (6%)
HCK	active (34.3%)	active (13%)
LCK	active (11.8%)	active (12%)
SRM	inactive (101.75%)	-
YES	active (5.29%)	active (2%)
LYN	active (6.34%)	active (2%)

TK - Tec

Bioactivity
Kinase	RBC	Millipore
BMX	inactive (99.28%)	inactive (73%)
BTK	inactive (58.26%)	inactive (83%)
ITK	active (30.02%)	active (21%)
TEC	inactive (102.21%)	-
TXK	inactive (79.52%)	inactive (70%)

TK - PDGFR

Bioactivity
Kinase	RBC	Millipore
KIT	active (28.74%)	active (-1%)
FLT3	active (0.78%)	active (1%)
FMS	active (7.41%)	active (0%)
PDGFRb	active (9.28%)	active (1%)
PDGFRa	active (25.86%)	active (2%)

TK - Csk

Bioactivity
Kinase	RBC	Millipore
CSK	inactive (86.33%)	inactive (99%)
CTK	inactive (96.77%)	-

TK - DDR

Bioactivity
Kinase	RBC	Millipore
DDR2	inactive (104.24%)	inactive (94%)

TK - EGFR

Bioactivity
Kinase	RBC	Millipore
EGFR	inactive (96.98%)	inactive (107%)
ErbB2	inactive (102.32%)	-
ErbB4	inactive (86.08%)	inactive (86%)

TK - Eph

Bioactivity
Kinase	RBC	Millipore
EphA1	inactive (89.41%)	inactive (82%)
EphA2	inactive (93.49%)	inactive (94%)
EphA3	inactive (92.45%)	inactive (94%)
EphA4	inactive (87.97%)	inactive (101%)
EphA5	inactive (90.37%)	inactive (109%)
EphA6	active (45.7%)	-
EphA7	inactive (67.14%)	inactive (79%)
EphA8	inactive (99.48%)	inactive (100%)
EphB1	inactive (60.77%)	inactive (64%)
EphB2	inactive (87.5%)	inactive (89%)
EphB3	inactive (100.07%)	inactive (129%)
EphB4	inactive (76.92%)	inactive (100%)

TK - FAK

Bioactivity
Kinase	RBC	Millipore
FAK	active (25.84%)	active (15%)
PYK2	active (30.46%)	active (15%)

TK - Fer

Bioactivity
Kinase	RBC	Millipore
FER	active (17.72%)	inactive (79%)
FES	active (22.11%)	active (14%)

TK - FGFR

Bioactivity
Kinase	RBC	Millipore
FGFR1	active (20.28%)	active (7%)
FGFR2	active (29.28%)	active (14%)
FGFR3	active (12.34%)	active (8%)
FGFR4	inactive (70.54%)	inactive (101%)

TK - VEGFR

Bioactivity
Kinase	RBC	Millipore
FLT1	active (34.37%)	active (5%)
FLT4	active (12.1%)	active (0%)
KDR	active (13.76%)	active (2%)

TK - InsR

Bioactivity
Kinase	RBC	Millipore
IGF1R	active (35.22%)	inactive (135%)
IRR	active (4.33%)	active (13%)
INSR	active (30.12%)	active (32%)

TK - JakA

Bioactivity
Kinase	RBC	Millipore
JAK1	inactive (65.76%)	-
JAK2	inactive (54.05%)	inactive (72%)
JAK3	active (39.34%)	inactive (62%)
TYK2	active (30.85%)	-

TK - Musk

Bioactivity
Kinase	RBC	Millipore
MUSK	inactive (63.49%)	active (3%)

TK - Ret

Bioactivity
Kinase	RBC	Millipore
RET	active (2.47%)	active (-1%)

TK - Met

Bioactivity
Kinase	RBC	Millipore
RON	inactive (96.67%)	inactive (91%)
MET	inactive (77%)	active (45%)

TK - Sev

Bioactivity
Kinase	RBC	Millipore
ROS	active (43.89%)	inactive (106%)

TK - Syk

Bioactivity
Kinase	RBC	Millipore
SYK	inactive (59.22%)	inactive (92%)
ZAP70	inactive (91.23%)	inactive (116%)

TK - Tie

Bioactivity
Kinase	RBC	Millipore
TIE2	inactive (98.18%)	inactive (56%)

TK - Trk

Bioactivity
Kinase	RBC	Millipore
TRKA	active (8.73%)	active (-1%)
TRKB	active (8.43%)	active (40%)
TRKC	active (1.87%)	-

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 (88.99%)	-
ALK2	inactive (107.79%)	-
ALK4	inactive (103.21%)	inactive (126%)
TGFbR1	inactive (95.51%)	inactive (101%)
TGFbR2	inactive (112.79%)	-

TKL - RAF

Bioactivity
Kinase	RBC	Millipore
ARAF	inactive (132.1%)	-
BRAF	inactive (109%)	-
RAF1	inactive (116.83%)	inactive (97%)

TKL - IRAK

Bioactivity
Kinase	RBC	Millipore
IRAK1	active (14.06%)	active (9%)
IRAK4	active (22.73%)	active (22%)

TKL - LISK

Bioactivity
Kinase	RBC	Millipore
LIMK1	inactive (98.38%)	inactive (99%)

TKL - LRRK

Bioactivity
Kinase	RBC	Millipore
LRRK2	active (1.44%)	-

TKL - MLK

Bioactivity
Kinase	RBC	Millipore
MLK1	active (49.57%)	active (24%)
MLK2	inactive (82.77%)	-
MLK3	active (20.99%)	-
TAK1	active (3.51%)	active (4%)
ZAK	inactive (95.82%)	-

TKL - RIPK

Bioactivity
Kinase	RBC	Millipore
RIPK2	inactive (84.06%)	inactive (62%)

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 (2.06%)	active (6%)
BRSK1	active (36.48%)	active (6%)
BRSK2	inactive (53.66%)	active (29%)
CHK1	active (15.15%)	active (24%)
LKB1	inactive (80.67%)	inactive (98%)
MARK1	active (18.07%)	active (14%)
MARK3	active (7.86%)	-
MARK4	active (7.19%)	-
MELK	active (16.69%)	active (8%)
PASK	inactive (89.65%)	inactive (70%)
QIK	active (42.68%)	-
NuaK2	inactive (70.66%)	-
MARK2	active (9.74%)	active (11%)
AMPKa1	-	active (7%)
AMPKa2	-	active (4%)
SIK	-	active (31%)

CAMK - CAMK1

Bioactivity
Kinase	RBC	Millipore
CaMK1a	inactive (75.9%)	inactive (51%)
CaMK1b	inactive (70.47%)	-
CaMK1d	inactive (60.22%)	active (42%)
CaMK1g	active (49.47%)	-
CaMK4	inactive (94.99%)	inactive (88%)

CAMK - CAMK2

Bioactivity
Kinase	RBC	Millipore
CaMK2a	active (3.6%)	-
CaMK2b	active (27.26%)	active (8%)
CaMK2d	active (7.25%)	active (3%)
CaMK2g	active (8.13%)	active (3%)

CAMK - RAD53

Bioactivity
Kinase	RBC	Millipore
CHK2	active (6.42%)	active (6%)

CAMK - DAPK

Bioactivity
Kinase	RBC	Millipore
DAPK1	active (47.71%)	inactive (75%)
DAPK2	inactive (86.67%)	inactive (63%)
DRAK1	active (16.09%)	active (3%)
DAPK3	inactive (54.3%)	active (44%)

CAMK - DCAMKL

Bioactivity
Kinase	RBC	Millipore
DCLK2	inactive (82.84%)	inactive (68%)

CAMK - MAPKAPK

Bioactivity
Kinase	RBC	Millipore
MAPKAPK2	inactive (102.94%)	inactive (98%)
MAPKAPK3	inactive (100.87%)	inactive (108%)
MAPKAPK5	inactive (91.65%)	inactive (97%)
MNK1	inactive (75.39%)	-
MNK2	inactive (88.8%)	inactive (99%)

CAMK - MLCK

Bioactivity
Kinase	RBC	Millipore
smMLCK	active (17.62%)	active (9%)
skMLCK	active (10%)	-

CAMK - PHK

Bioactivity
Kinase	RBC	Millipore
PHKg1	active (3.19%)	-
PHKg2	active (16.61%)	active (8%)

CAMK - PIM

Bioactivity
Kinase	RBC	Millipore
PIM1	inactive (91.67%)	inactive (85%)
PIM2	inactive (101.3%)	inactive (99%)
PIM3	inactive (74.04%)	inactive (92%)

CAMK - PKD

Bioactivity
Kinase	RBC	Millipore
PKD1	active (11.25%)	active (38%)
PKD3	active (8.04%)	-
PKD2	active (11.95%)	inactive (73%)

CAMK - TSSK

Bioactivity
Kinase	RBC	Millipore
TSSK1	active (8.45%)	active (8%)
TSSK2	inactive (66.92%)	inactive (62%)

CAMK - STK33

Bioactivity
Kinase	RBC	Millipore
STK33	active (20.61%)	active (33%)

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 (98.11%)	inactive (60%)
MAP3K2	active (20.08%)	-
MAP3K3	active (30.63%)	-

STE - STE-Unique

Bioactivity
Kinase	RBC	Millipore
COT	inactive (113.12%)	-
NIK	inactive (118.37%)	-

STE - STE20

Bioactivity
Kinase	RBC	Millipore
GCK	active (8.07%)	active (5%)
HGK	active (4.33%)	-
KHS1	active (0.83%)	-
LOK	active (7.11%)	active (15%)
MINK	active (4.4%)	active (9%)
MST1	active (2.98%)	active (12%)
MST2	active (16.86%)	active (34%)
MST3	active (22.18%)	active (8%)
MST4	inactive (73.21%)	-
OSR1	inactive (80.08%)	-
PAK1	inactive (93.44%)	-
PAK2	inactive (92.7%)	inactive (110%)
PAK3	inactive (93.79%)	inactive (64%)
PAK4	inactive (76.71%)	inactive (52%)
PAK5	inactive (58.89%)	active (30%)
PAK6	inactive (100.54%)	inactive (73%)
SLK	active (38.05%)	-
YSK1	inactive (56.13%)	-
STLK3	inactive (81.9%)	-
TAO1	inactive (65.85%)	inactive (71%)
TAO2	inactive (72.59%)	inactive (89%)
TAO3	active (45.5%)	inactive (79%)
MYO3B	active (41.25%)	-

STE - STE7

Bioactivity
Kinase	RBC	Millipore
MAP2K1	active (33.08%)	active (21%)
MAP2K2	active (41.4%)	-
MAP2K6	inactive (86.19%)	inactive (66%)
MAP2K7	-	inactive (92%)

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 (80.33%)	active (47%)
AurB	active (31.9%)	active (7%)
AurC	inactive (74.67%)	active (38%)

Other - CAMKK

Bioactivity
Kinase	RBC	Millipore
CaMKK1	active (47.74%)	-
CaMKK2	active (48%)	-

Other - Haspin

Bioactivity
Kinase	RBC	Millipore
Haspin	inactive (82.89%)	active (43%)

Other - IKK

Bioactivity
Kinase	RBC	Millipore
IKKa	inactive (101.57%)	inactive (93%)
IKKb	inactive (100.87%)	inactive (98%)
IKKe	active (29.42%)	-
TBK1	active (16.27%)	active (15%)

Other - NEK

Bioactivity
Kinase	RBC	Millipore
NEK1	inactive (94.73%)	-
NEK11	inactive (83.38%)	inactive (80%)
NEK2	inactive (77.19%)	inactive (67%)
NEK4	inactive (97.04%)	-
NEK6	inactive (97.83%)	inactive (91%)
NEK7	inactive (99.32%)	inactive (102%)
NEK9	inactive (95.92%)	-
NEK3	inactive (93.98%)	inactive (111%)

Other - TOPK

Bioactivity
Kinase	RBC	Millipore
PBK	inactive (103.94%)	-

Other - PLK

Bioactivity
Kinase	RBC	Millipore
PLK1	inactive (105.12%)	inactive (92%)
PLK2	inactive (91.24%)	inactive (98%)
PLK3	inactive (89.77%)	inactive (94%)

Other - SgK496

Bioactivity
Kinase	RBC	Millipore
SgK496	inactive (104.95%)	-

Other - NAK

Bioactivity
Kinase	RBC	Millipore
MPSK1	inactive (72.86%)	-

Other - TTK

Bioactivity
Kinase	RBC	Millipore
TTK	inactive (59.78%)	-

Other - ULK

Bioactivity
Kinase	RBC	Millipore
ULK1	active (13.58%)	-
ULK2	active (43%)	active (23%)
ULK3	active (21.57%)	active (17%)

Other - WEE

Bioactivity
Kinase	RBC	Millipore
Wee1	inactive (94.79%)	-

Other - WNK

Bioactivity
Kinase	RBC	Millipore
Wnk2	inactive (100.84%)	inactive (105%)
Wnk3	inactive (86.26%)	inactive (94%)

Other - TLK

Bioactivity
Kinase	RBC	Millipore
TLK2	inactive (79.64%)	inactive (69%)

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	active (49.66%)	active (23%)
CK1g1	inactive (69.23%)	inactive (64%)
CK1g2	active (45.25%)	active (30%)
CK1g3	active (47.67%)	active (42%)
CK1a	inactive (75.69%)	-
CK1e	active (46.67%)	-

CK1 - VRK

Bioactivity
Kinase	RBC	Millipore
VRK1	inactive (90.74%)	-
VRK2	-	inactive (108%)

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 (91.4%)	inactive (86%)
CK2a2	inactive (64.26%)	inactive (113%)

CMGC - CLK

Bioactivity
Kinase	RBC	Millipore
CLK1	active (34.24%)	-
CLK2	active (15.77%)	active (9%)
CLK3	inactive (101.13%)	inactive (77%)
CLK4	active (16.82%)	-

CMGC - DYRK

Bioactivity
Kinase	RBC	Millipore
DYRK1A	active (47.23%)	-
DYRK1B	active (47.47%)	-
DYRK2	inactive (82.67%)	inactive (78%)
DYRK3	inactive (81.76%)	-
DYRK4	inactive (97.91%)	-
HIPK1	inactive (96.88%)	active (32%)
HIPK2	active (20.03%)	active (6%)
HIPK3	inactive (50.82%)	active (9%)
HIPK4	inactive (61.74%)	-

CMGC - MAPK

Bioactivity
Kinase	RBC	Millipore
Erk1	inactive (98.8%)	inactive (91%)
Erk2	inactive (97.13%)	inactive (97%)
JNK3	inactive (104.47%)	inactive (80%)
NLK	inactive (100.87%)	inactive (102%)
p38a	inactive (102.63%)	inactive (82%)
p38b	inactive (100%)	inactive (95%)
p38d	inactive (103.6%)	inactive (100%)
p38g	inactive (96.58%)	inactive (108%)
JNK1	inactive (97.23%)	inactive (97%)
JNK2	inactive (108.52%)	inactive (111%)

CMGC - GSK

Bioactivity
Kinase	RBC	Millipore
GSK3A	inactive (88.28%)	inactive (104%)
GSK3B	inactive (93.08%)	inactive (87%)

CMGC - SRPK

Bioactivity
Kinase	RBC	Millipore
MSSK1	inactive (92.82%)	inactive (98%)
SRPK1	inactive (95.91%)	inactive (112%)
SRPK2	inactive (93.66%)	inactive (98%)

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 (101.46%)	-

Atypical - Alpha

Bioactivity
Kinase	RBC	Millipore
eEF2K	-	inactive (105%)

Atypical - PIKK

Bioactivity
Kinase	RBC	Millipore
FRAP	-	inactive (102%)