Compound in Profiling

Compound Information

Test on : RBC, Millipore

Compound Name
RBC : REL-(9R,12S)-9,10,11,12-TETRAHYDRO-9,12-EPOXY-1H-DIINDOLO[1,2,3-FG:3',2',1'-KL]PYRROLO[3,4-I][1,6]BENZODIAZOCINE-1,3(2H)-DIONE
Millipore : SB 218078

Inchikey
Same : OTPNDVKVEAIXTI-N
RBC : OTPNDVKVEAIXTI-IYBDPMFKSA-N
Millipore : OTPNDVKVEAIXTI-UHFFFAOYSA-N

ChemSpider
RBC : 394549
Millipore : 2632300

Pubchem CID
RBC : 447446
Millipore : 3387354

ChEMBL
RBC : CHEMBL289422
Millipore : CHEMBL304428

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	active (10.62%)	active (27%)

AGC - Akt

Bioactivity
Kinase	RBC	Millipore
AKT1	inactive (63.9%)	inactive (107%)
AKT2	active (48.52%)	inactive (101%)
AKT3	active (27.14%)	inactive (96%)

AGC - DMPK

Bioactivity
Kinase	RBC	Millipore
DMPK1	inactive (98.85%)	inactive (110%)
MRCKa	inactive (84.03%)	inactive (116%)
MRCKb	inactive (101.58%)	inactive (103%)
ROCK1	inactive (88.7%)	inactive (110%)
ROCK2	inactive (73.67%)	inactive (101%)

AGC - GRK

Bioactivity
Kinase	RBC	Millipore
BARK1	inactive (97.92%)	-
BARK2	inactive (101.24%)	-
GPRK4	inactive (77%)	-
GPRK5	inactive (88.73%)	inactive (105%)
GPRK6	inactive (55.58%)	inactive (104%)
GPRK7	inactive (53.41%)	inactive (109%)

AGC - RSK

Bioactivity
Kinase	RBC	Millipore
MSK1	active (9.88%)	active (41%)
MSK2	active (12.36%)	inactive (56%)
p70S6K	active (2.38%)	inactive (51%)
p70S6Kb	active (35.01%)	-
RSK2	active (2.35%)	active (11%)
RSK4	active (1.08%)	active (9%)
RSK1	active (1.58%)	active (8%)
RSK3	active (1.33%)	active (13%)

AGC - PKA

Bioactivity
Kinase	RBC	Millipore
PKACg	active (39.81%)	-
PRKX	active (17.46%)	inactive (84%)
PKACa	active (44.74%)	inactive (70%)

AGC - PKC

Bioactivity
Kinase	RBC	Millipore
PKCa	active (13.94%)	inactive (96%)
PKCd	active (19.05%)	inactive (103%)
PKCe	active (28.44%)	inactive (116%)
PKCh	active (47.62%)	inactive (89%)
PKCg	active (32.85%)	inactive (92%)
PKCi	inactive (86.42%)	inactive (115%)
PKCt	active (43.17%)	active (7%)
PKCz	inactive (87.41%)	inactive (111%)
PKCb	active (6.42%)	-

AGC - PKG

Bioactivity
Kinase	RBC	Millipore
PKG2	active (6.01%)	-
PKG1	active (35.65%)	-

AGC - PKN

Bioactivity
Kinase	RBC	Millipore
PKN1	active (2.68%)	-
PKN2	active (15.9%)	active (47%)

AGC - SGK

Bioactivity
Kinase	RBC	Millipore
SGK1	active (23.85%)	inactive (53%)
SGK2	active (18.57%)	inactive (77%)
SGK3	inactive (71.7%)	inactive (98%)

AGC - NDR

Bioactivity
Kinase	RBC	Millipore
NDR1	active (46.19%)	-

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 (72.66%)	inactive (114%)
ABL2	inactive (68.05%)	inactive (103%)

TK - Ack

Bioactivity
Kinase	RBC	Millipore
ACK	active (2.39%)	active (8%)

TK - ALK

Bioactivity
Kinase	RBC	Millipore
ALK	active (36.91%)	inactive (81%)
LTK	active (21.81%)	-

TK - Axl

Bioactivity
Kinase	RBC	Millipore
AXL	active (38.13%)	inactive (91%)
MER	active (13.63%)	active (34%)
TYRO3	inactive (55.28%)	inactive (70%)

TK - Src

Bioactivity
Kinase	RBC	Millipore
BLK	active (37.68%)	inactive (101%)
BRK	inactive (83.92%)	inactive (100%)
SRC	inactive (69.51%)	inactive (103%)
FGR	active (30.86%)	inactive (102%)
FRK	inactive (101.52%)	inactive (71%)
FYN	inactive (59.91%)	inactive (81%)
HCK	active (24.79%)	inactive (76%)
LCK	active (36.21%)	active (50%)
SRM	inactive (104.62%)	-
YES	active (31.86%)	inactive (115%)
LYN	active (35.38%)	active (10%)

TK - Tec

Bioactivity
Kinase	RBC	Millipore
BMX	active (27.48%)	active (14%)
BTK	active (43.26%)	active (22%)
ITK	active (8.29%)	inactive (88%)
TEC	inactive (142.03%)	-
TXK	active (22.69%)	inactive (71%)

TK - PDGFR

Bioactivity
Kinase	RBC	Millipore
KIT	inactive (60.84%)	inactive (101%)
FLT3	active (0.19%)	active (24%)
FMS	active (29.34%)	active (30%)
PDGFRb	active (19.08%)	inactive (90%)
PDGFRa	active (32.83%)	inactive (93%)

TK - Csk

Bioactivity
Kinase	RBC	Millipore
CSK	inactive (79.7%)	inactive (111%)
CTK	inactive (91.75%)	-

TK - DDR

Bioactivity
Kinase	RBC	Millipore
DDR2	inactive (80.13%)	inactive (77%)

TK - EGFR

Bioactivity
Kinase	RBC	Millipore
EGFR	inactive (78.34%)	inactive (102%)
ErbB2	inactive (98.38%)	-
ErbB4	inactive (72.46%)	inactive (118%)

TK - Eph

Bioactivity
Kinase	RBC	Millipore
EphA1	inactive (90.12%)	inactive (113%)
EphA2	inactive (91.26%)	inactive (94%)
EphA3	inactive (96.53%)	inactive (102%)
EphA4	inactive (91.44%)	inactive (112%)
EphA5	inactive (78.68%)	inactive (94%)
EphA6	inactive (63.93%)	-
EphA7	inactive (69.21%)	inactive (100%)
EphA8	inactive (89.87%)	inactive (96%)
EphB1	inactive (80.21%)	inactive (112%)
EphB2	inactive (98.38%)	inactive (104%)
EphB3	inactive (93.23%)	inactive (118%)
EphB4	inactive (75.42%)	inactive (107%)

TK - FAK

Bioactivity
Kinase	RBC	Millipore
FAK	active (23.48%)	inactive (105%)
PYK2	active (41.51%)	inactive (90%)

TK - Fer

Bioactivity
Kinase	RBC	Millipore
FER	active (5.39%)	active (33%)
FES	active (42.08%)	inactive (90%)

TK - FGFR

Bioactivity
Kinase	RBC	Millipore
FGFR1	active (29.13%)	inactive (72%)
FGFR2	active (34.11%)	inactive (83%)
FGFR3	active (36.32%)	inactive (82%)
FGFR4	inactive (70.4%)	inactive (103%)

TK - VEGFR

Bioactivity
Kinase	RBC	Millipore
FLT1	active (13.31%)	active (7%)
FLT4	active (4.97%)	active (0%)
KDR	active (4.55%)	active (38%)

TK - InsR

Bioactivity
Kinase	RBC	Millipore
IGF1R	inactive (63.79%)	inactive (73%)
IRR	active (7.16%)	inactive (74%)
INSR	active (17.19%)	inactive (94%)

TK - JakA

Bioactivity
Kinase	RBC	Millipore
JAK1	active (22.22%)	-
JAK2	active (14.19%)	inactive (86%)
JAK3	active (1.87%)	active (8%)
TYK2	active (4.32%)	-

TK - Musk

Bioactivity
Kinase	RBC	Millipore
MUSK	active (25.83%)	inactive (103%)

TK - Ret

Bioactivity
Kinase	RBC	Millipore
RET	active (3.21%)	active (37%)

TK - Met

Bioactivity
Kinase	RBC	Millipore
RON	inactive (87.75%)	inactive (92%)
MET	inactive (76.89%)	inactive (130%)

TK - Sev

Bioactivity
Kinase	RBC	Millipore
ROS	active (1.6%)	inactive (94%)

TK - Syk

Bioactivity
Kinase	RBC	Millipore
SYK	active (15.79%)	inactive (90%)
ZAP70	inactive (88.44%)	inactive (132%)

TK - Tie

Bioactivity
Kinase	RBC	Millipore
TIE2	inactive (94.13%)	inactive (97%)

TK - Trk

Bioactivity
Kinase	RBC	Millipore
TRKA	active (4.98%)	active (12%)
TRKB	active (6.87%)	active (19%)
TRKC	active (1.41%)	-

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 (78.58%)	-
ALK2	inactive (85.82%)	-
ALK4	inactive (113.16%)	inactive (90%)
TGFbR1	inactive (110.47%)	inactive (114%)
TGFbR2	inactive (70.34%)	-

TKL - RAF

Bioactivity
Kinase	RBC	Millipore
ARAF	inactive (126.66%)	-
BRAF	inactive (105.05%)	-
RAF1	inactive (120.59%)	inactive (77%)

TKL - IRAK

Bioactivity
Kinase	RBC	Millipore
IRAK1	active (37.52%)	inactive (101%)
IRAK4	active (14.04%)	active (38%)

TKL - LISK

Bioactivity
Kinase	RBC	Millipore
LIMK1	active (49.34%)	inactive (106%)

TKL - LRRK

Bioactivity
Kinase	RBC	Millipore
LRRK2	active (1.91%)	-

TKL - MLK

Bioactivity
Kinase	RBC	Millipore
MLK1	active (8.72%)	active (1%)
MLK2	active (2.66%)	-
MLK3	active (1.37%)	-
TAK1	active (6.06%)	inactive (88%)
ZAK	inactive (89.7%)	-

TKL - RIPK

Bioactivity
Kinase	RBC	Millipore
RIPK2	inactive (79.65%)	inactive (105%)

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 (2.09%)	active (39%)
BRSK1	active (14.81%)	inactive (98%)
BRSK2	active (13.56%)	inactive (53%)
CHK1	active (3.63%)	active (25%)
LKB1	inactive (50.46%)	inactive (106%)
MARK1	active (10.43%)	active (38%)
MARK3	active (8.53%)	-
MARK4	active (5.31%)	-
MELK	active (7.13%)	inactive (55%)
PASK	active (43.27%)	inactive (117%)
QIK	active (33.92%)	-
NuaK2	inactive (52%)	-
MARK2	active (4.88%)	inactive (63%)
AMPKa1	-	inactive (74%)
AMPKa2	-	inactive (55%)
SIK	-	inactive (123%)

CAMK - CAMK1

Bioactivity
Kinase	RBC	Millipore
CaMK1a	inactive (69.74%)	inactive (63%)
CaMK1b	inactive (50.49%)	-
CaMK1d	active (33.57%)	inactive (89%)
CaMK1g	inactive (56.53%)	-
CaMK4	inactive (98.71%)	inactive (90%)

CAMK - CAMK2

Bioactivity
Kinase	RBC	Millipore
CaMK2a	active (2.84%)	-
CaMK2b	active (9.85%)	active (32%)
CaMK2d	active (7.03%)	active (-1%)
CaMK2g	active (8.36%)	active (0%)

CAMK - RAD53

Bioactivity
Kinase	RBC	Millipore
CHK2	active (13%)	active (26%)

CAMK - DAPK

Bioactivity
Kinase	RBC	Millipore
DAPK1	active (32.66%)	active (49%)
DAPK2	active (39.35%)	inactive (54%)
DRAK1	active (8.65%)	active (16%)
DAPK3	active (24.58%)	inactive (80%)

CAMK - DCAMKL

Bioactivity
Kinase	RBC	Millipore
DCLK2	inactive (89.62%)	inactive (77%)

CAMK - MAPKAPK

Bioactivity
Kinase	RBC	Millipore
MAPKAPK2	inactive (99.24%)	inactive (104%)
MAPKAPK3	inactive (93.06%)	inactive (95%)
MAPKAPK5	inactive (80.43%)	inactive (90%)
MNK1	active (48.64%)	-
MNK2	active (9.71%)	inactive (97%)

CAMK - MLCK

Bioactivity
Kinase	RBC	Millipore
smMLCK	active (4.01%)	inactive (90%)
skMLCK	active (7.76%)	-

CAMK - PHK

Bioactivity
Kinase	RBC	Millipore
PHKg1	active (2.75%)	-
PHKg2	inactive (75.57%)	inactive (112%)

CAMK - PIM

Bioactivity
Kinase	RBC	Millipore
PIM1	active (0.44%)	active (-2%)
PIM2	active (1.86%)	active (6%)
PIM3	active (0.24%)	active (38%)

CAMK - PKD

Bioactivity
Kinase	RBC	Millipore
PKD1	active (1.89%)	inactive (87%)
PKD3	active (-0.05%)	-
PKD2	active (2.02%)	inactive (92%)

CAMK - TSSK

Bioactivity
Kinase	RBC	Millipore
TSSK1	active (17.7%)	inactive (92%)
TSSK2	inactive (87.15%)	inactive (82%)

CAMK - STK33

Bioactivity
Kinase	RBC	Millipore
STK33	active (12.73%)	inactive (106%)

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 (56.2%)	inactive (96%)
MAP3K2	active (13.97%)	-
MAP3K3	active (18.37%)	-

STE - STE-Unique

Bioactivity
Kinase	RBC	Millipore
COT	inactive (94.63%)	-
NIK	inactive (134.48%)	-

STE - STE20

Bioactivity
Kinase	RBC	Millipore
GCK	active (3.75%)	active (20%)
HGK	active (0.99%)	-
KHS1	active (2.69%)	-
LOK	active (9.25%)	inactive (116%)
MINK	active (0.9%)	inactive (86%)
MST1	active (3.56%)	active (19%)
MST2	active (3.22%)	active (10%)
MST3	active (14.25%)	inactive (80%)
MST4	active (20.52%)	-
OSR1	inactive (92.41%)	-
PAK1	active (23.61%)	-
PAK2	active (43.9%)	inactive (91%)
PAK3	active (41.67%)	inactive (79%)
PAK4	inactive (75.29%)	inactive (84%)
PAK5	inactive (64.66%)	inactive (120%)
PAK6	inactive (85.4%)	active (19%)
SLK	active (25.97%)	-
YSK1	active (34.36%)	-
STLK3	inactive (88.33%)	-
TAO1	inactive (66.92%)	inactive (75%)
TAO2	inactive (57.41%)	inactive (113%)
TAO3	active (24.47%)	inactive (96%)
MYO3B	active (19.07%)	-

STE - STE7

Bioactivity
Kinase	RBC	Millipore
MAP2K1	active (29.48%)	active (40%)
MAP2K2	inactive (87.94%)	-
MAP2K6	active (19.27%)	active (27%)
MAP2K7	-	inactive (100%)

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 (22.28%)	inactive (95%)
AurB	active (9.52%)	active (2%)
AurC	active (36.48%)	inactive (104%)

Other - CAMKK

Bioactivity
Kinase	RBC	Millipore
CaMKK1	active (27.21%)	-
CaMKK2	active (7.93%)	-

Other - Haspin

Bioactivity
Kinase	RBC	Millipore
Haspin	active (18.46%)	active (50%)

Other - IKK

Bioactivity
Kinase	RBC	Millipore
IKKa	inactive (106.5%)	inactive (93%)
IKKb	inactive (97.84%)	inactive (107%)
IKKe	active (23.86%)	-
TBK1	active (7.4%)	inactive (54%)

Other - NEK

Bioactivity
Kinase	RBC	Millipore
NEK1	inactive (50.86%)	-
NEK11	inactive (60.63%)	inactive (91%)
NEK2	inactive (93.76%)	inactive (113%)
NEK4	active (22.03%)	-
NEK6	inactive (93.08%)	inactive (108%)
NEK7	inactive (99.12%)	inactive (107%)
NEK9	active (23.41%)	-
NEK3	inactive (101.94%)	inactive (87%)

Other - TOPK

Bioactivity
Kinase	RBC	Millipore
PBK	active (39.85%)	-

Other - PLK

Bioactivity
Kinase	RBC	Millipore
PLK1	inactive (50.22%)	inactive (88%)
PLK2	inactive (62.39%)	inactive (105%)
PLK3	inactive (52.49%)	inactive (88%)

Other - SgK496

Bioactivity
Kinase	RBC	Millipore
SgK496	active (45.54%)	-

Other - NAK

Bioactivity
Kinase	RBC	Millipore
MPSK1	inactive (58.05%)	-

Other - TTK

Bioactivity
Kinase	RBC	Millipore
TTK	inactive (76.43%)	-

Other - ULK

Bioactivity
Kinase	RBC	Millipore
ULK1	inactive (73.13%)	-
ULK2	inactive (89.1%)	inactive (114%)
ULK3	active (33%)	inactive (58%)

Other - WEE

Bioactivity
Kinase	RBC	Millipore
Wee1	active (16.86%)	-

Other - WNK

Bioactivity
Kinase	RBC	Millipore
Wnk2	inactive (93.57%)	inactive (100%)
Wnk3	inactive (85.98%)	inactive (94%)

Other - TLK

Bioactivity
Kinase	RBC	Millipore
TLK2	active (14.11%)	inactive (62%)

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 (93.77%)	inactive (75%)
CK1g1	inactive (96.1%)	inactive (106%)
CK1g2	inactive (81.83%)	inactive (52%)
CK1g3	inactive (107.87%)	inactive (61%)
CK1a	inactive (103.6%)	-
CK1e	active (47.33%)	-

CK1 - VRK

Bioactivity
Kinase	RBC	Millipore
VRK1	inactive (90.16%)	-
VRK2	-	inactive (104%)

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	active (16.74%)	inactive (74%)
CK2a2	active (4.47%)	inactive (63%)

CMGC - CLK

Bioactivity
Kinase	RBC	Millipore
CLK1	active (43.08%)	-
CLK2	inactive (52.12%)	inactive (100%)
CLK3	inactive (97.02%)	inactive (95%)
CLK4	active (20.32%)	-

CMGC - DYRK

Bioactivity
Kinase	RBC	Millipore
DYRK1A	active (8.74%)	-
DYRK1B	active (3.15%)	-
DYRK2	active (5.94%)	inactive (91%)
DYRK3	active (16.58%)	-
DYRK4	inactive (87.77%)	-
HIPK1	inactive (93.61%)	inactive (104%)
HIPK2	active (32.57%)	active (42%)
HIPK3	active (49.89%)	active (-2%)
HIPK4	active (29.15%)	-

CMGC - MAPK

Bioactivity
Kinase	RBC	Millipore
Erk1	inactive (102.37%)	inactive (128%)
Erk2	inactive (88.68%)	inactive (115%)
JNK3	inactive (138.09%)	inactive (63%)
NLK	inactive (74.13%)	inactive (109%)
p38a	inactive (101.7%)	inactive (90%)
p38b	inactive (107.94%)	inactive (115%)
p38d	inactive (113.7%)	inactive (106%)
p38g	inactive (112.88%)	inactive (97%)
JNK1	inactive (98.53%)	inactive (98%)
JNK2	inactive (96.15%)	inactive (102%)

CMGC - GSK

Bioactivity
Kinase	RBC	Millipore
GSK3A	active (2.19%)	active (15%)
GSK3B	active (4.6%)	active (40%)

CMGC - SRPK

Bioactivity
Kinase	RBC	Millipore
MSSK1	inactive (63.63%)	inactive (99%)
SRPK1	inactive (88.08%)	inactive (92%)
SRPK2	inactive (106.72%)	inactive (106%)

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	active (10.62%)	-

Atypical - Alpha

Bioactivity
Kinase	RBC	Millipore
eEF2K	-	inactive (111%)

Atypical - PIKK

Bioactivity
Kinase	RBC	Millipore
FRAP	-	inactive (95%)