Protein transformations that change lives

Inhibitor | SB-590885

Compound name	Brutto	MW	CAS	PubChem CID	Action	Reference	Reference
SB-590885	C₂₇H₂₇N₅O₂	453.54	405554-55-4	11465183	B-Raf	King (2006) Cancer Res. 66 11100

Screen Conc: 0.10µM
Kinase	% Activity Remaining	Standard Deviation
ABL	100	8
AMPK	110	3
AMPK (hum)	97	4
ASK1	83	3
Aurora A	102	0
Aurora B	91	3
BRK	96	16
BRSK1	82	7
BRSK2	81	14
BTK	85	4
CAMK1	103	4
CAMKK beta	101	23
CDK2-Cyclin A	98	18
CDK9-Cyclin T1	71	4
CHK1	85	14
CHK2	89	2
CK1 delta	90	1
CK1 gamma 2	92	4
CK2	81	7
CLK2	85	4
CSK	88	8
DAPK1	96	2
DDR2	104	8
DYRK1A	90	19
DYRK2	84	2
DYRK3	112	8
EF2K	93	9
EIF2AK3	94	4
EPH-A2	84	14
EPH-A4	89	4
EPH-B1	71	6
EPH-B2	82	3
EPH-B3	85	1
EPH-B4	86	18
ERK1	80	16
ERK2	105	10
ERK5	82	0
ERK8	90	1
FGF-R1	115	20
GCK	106	7
GSK3 beta	102	4
HER4	85	5
HIPK1	108	17
HIPK2	89	9
HIPK3	93	6
IGF-1R	107	6
IKK beta	87	3
IKK epsilon	89	8
IR	87	4
IRAK1	94	21
IRAK4	88	5
IRR	89	1
JAK2	101	3
JNK1	107	1
JNK2	97	6
JNK3	81	21
Lck	82	11
LKB1	96	3
MAP4K3	95	19
MAP4K5	96	16
MAPKAP-K2	98	2
MAPKAP-K3	97	4
MARK1	76	1
MARK2	85	1
MARK3	91	2
MARK4	83	11
MEKK1	109	5
MELK	90	17
MINK1	83	2
MKK1	87	1
MKK2	95	1
MKK6	79	5
MLK1	105	9
MLK3	88	4
MNK1	87	5
MNK2	88	13
MPSK1	95	12
MSK1	104	5
MST2	98	8
MST3	94	0
MST4	85	10
NEK2a	100	2
NEK6	82	7
NUAK1	97	6
OSR1	94	8
p38 alpha MAPK	90	6
p38 beta MAPK	111	5
p38 delta MAPK	92	4
p38 gamma MAPK	99	0
PAK2	113	1
PAK4	93	1
PAK5	92	4
PAK6	92	1
PDGFRA	83	3
PDK1	84	1
PHK	70	32
PIM1	103	8
PIM2	118	1
PIM3	99	0
PKA	102	7
PKB alpha	89	2
PKB beta	96	16
PKC alpha	94	7
PKC gamma	93	1
PKC zeta	97	5
PKD1	83	5
PLK1	92	7
PRAK	95	14
PRK2	93	5
RIPK2	27	2
ROCK 2	83	2
RSK1	87	8
RSK2	80	5
S6K1	95	26
SGK1	82	10
SIK2	81	14
SIK3	85	4
SmMLCK	90	1
Src	101	6
SRPK1	97	2
STK33	87	3
SYK	96	6
TAK1	92	8
TAO1	98	1
TBK1	84	2
TESK1	81	4
TGFBR1	95	6
TIE2	99	20
TLK1	94	3
TrkA	87	11
TSSK1	83	24
TTBK1	97	13
TTBK2	87	3
TTK	86	7
ULK1	98	16
ULK2	94	0
VEGFR1	87	0
WNK1	99	2
YES1	94	14
ZAP70	77	33

Screen Conc: 1.00µM
Kinase	% Activity Remaining	Standard Deviation
ABL	99	4
AMPK	112	2
AMPK (hum)	114	9
ASK1	110	0
Aurora A	104	2
Aurora B	110	9
BRK	99	12
BRSK1	104	11
BRSK2	110	5
BTK	113	21
CAMK1	112	6
CAMKK beta	141	4
CDK2-Cyclin A	103	5
CDK9-Cyclin T1	100	12
CHK1	90	3
CHK2	103	3
CK1 delta	58	2
CK1 gamma 2	105	2
CK2	82	19
CLK2	107	18
CSK	93	5
DAPK1	103	0
DDR2	102	1
DYRK1A	108	13
DYRK2	93	8
DYRK3	98	7
EF2K	147	37
EIF2AK3	111	6
EPH-A2	115	5
EPH-A4	116	24
EPH-B1	104	0
EPH-B2	96	27
EPH-B3	90	4
EPH-B4	115	17
ERK1	110	21
ERK2	106	7
ERK5	119	4
ERK8	95	4
FGF-R1	106	2
GCK	106	11
GSK3 beta	103	4
HER4	92	1
HIPK1	106	21
HIPK2	94	7
HIPK3	105	4
IGF-1R	85	5
IKK beta	105	4
IKK epsilon	106	24
IR	107	9
IRAK1	112	12
IRAK4	109	4
IRR	93	4
JAK2	117	7
JNK1	109	6
JNK2	110	1
JNK3	97	21
Lck	102	9
LKB1	121	4
MAP4K3	102	4
MAP4K5	116	31
MAPKAP-K2	101	4
MAPKAP-K3	107	0
MARK1	97	5
MARK2	101	4
MARK3	94	5
MARK4	108	11
MEKK1	106	1
MELK	98	7
MINK1	84	3
MKK1	103	5
MKK2	80	5
MKK6	116	11
MLK1	99	7
MLK3	107	7
MNK1	106	6
MNK2	118	2
MPSK1	106	16
MSK1	103	13
MST2	126	18
MST3	102	7
MST4	96	7
NEK2a	107	0
NEK6	102	6
NUAK1	100	3
OSR1	108	9
p38 alpha MAPK	99	1
p38 beta MAPK	102	7
p38 delta MAPK	104	4
p38 gamma MAPK	108	3
PAK2	103	11
PAK4	104	2
PAK5	101	1
PAK6	99	5
PDGFRA	130	16
PDK1	101	15
PHK	95	3
PIM1	99	3
PIM2	116	20
PIM3	102	6
PKA	101	8
PKB alpha	102	15
PKB beta	103	5
PKC alpha	97	19
PKC gamma	105	11
PKC zeta	96	5
PKD1	97	15
PLK1	94	4
PRAK	101	1
PRK2	98	7
RIPK2	23	2
ROCK 2	91	7
RSK1	107	4
RSK2	105	4
S6K1	107	8
SGK1	99	7
SIK2	93	2
SIK3	109	1
SmMLCK	114	0
Src	115	2
SRPK1	100	10
STK33	116	11
SYK	106	1
TAK1	110	7
TAO1	105	20
TBK1	104	2
TESK1	100	10
TGFBR1	102	4
TIE2	92	2
TLK1	100	8
TrkA	97	14
TSSK1	92	5
TTBK1	111	9
TTBK2	106	13
TTK	102	6
ULK1	100	6
ULK2	110	7
VEGFR1	96	18
WNK1	104	4
YES1	94	14
ZAP70	102	11

Screen Conc: 10.00µM
Kinase	% Activity Remaining	Standard Deviation
ABL	47	3
AMPK	109	9
AMPK (hum)	105	23
ASK1	100	9
Aurora A	98	7
Aurora B	78	3
BRK	28	7
BRSK1	93	1
BRSK2	85	1
BTK	83	4
CAMK1	97	11
CAMKK beta	117	32
CDK2-Cyclin A	112	9
CDK9-Cyclin T1	94	12
CHK1	75	8
CHK2	76	2
CK1 delta	17	2
CK1 gamma 2	95	3
CK2	75	12
CLK2	62	8
CSK	130	11
DAPK1	100	5
DDR2	90	10
DYRK1A	81	1
DYRK2	75	12
DYRK3	91	9
EF2K	122	20
EIF2AK3	79	5
EPH-A2	101	11
EPH-A4	74	10
EPH-B1	100	10
EPH-B2	86	4
EPH-B3	77	13
EPH-B4	110	18
ERK1	93	1
ERK2	101	14
ERK5	84	12
ERK8	88	13
FGF-R1	124	5
GCK	78	0
GSK3 beta	84	10
HER4	55	8
HIPK1	66	6
HIPK2	62	9
HIPK3	92	1
IGF-1R	89	8
IKK beta	92	6
IKK epsilon	100	3
IR	106	8
IRAK1	84	13
IRAK4	95	1
IRR	72	2
JAK2	99	8
JNK1	105	9
JNK2	81	6
JNK3	94	2
Lck	29	5
LKB1	111	1
MAP4K3	81	19
MAP4K5	85	5
MAPKAP-K2	93	0
MAPKAP-K3	87	7
MARK1	84	2
MARK2	96	11
MARK3	95	2
MARK4	97	8
MEKK1	95	6
MELK	82	14
MINK1	30	5
MKK1	89	4
MKK2	100	13
MKK6	120	8
MLK1	88	4
MLK3	89	9
MNK1	99	5
MNK2	127	5
MPSK1	97	17
MSK1	84	15
MST2	116	37
MST3	85	0
MST4	79	14
NEK2a	91	1
NEK6	98	3
NUAK1	90	5
OSR1	108	9
p38 alpha MAPK	84	24
p38 beta MAPK	107	19
p38 delta MAPK	92	3
p38 gamma MAPK	92	10
PAK2	105	9
PAK4	99	2
PAK5	89	10
PAK6	91	3
PDGFRA	121	5
PDK1	109	23
PHK	96	12
PIM1	104	7
PIM2	90	10
PIM3	88	15
PKA	76	4
PKB alpha	81	6
PKB beta	99	11
PKC alpha	97	18
PKC gamma	92	3
PKC zeta	94	1
PKD1	68	6
PLK1	77	7
PRAK	107	4
PRK2	78	6
RIPK2	20	4
ROCK 2	48	11
RSK1	92	7
RSK2	93	26
S6K1	91	4
SGK1	76	0
SIK2	90	7
SIK3	83	8
SmMLCK	67	4
Src	104	7
SRPK1	86	0
STK33	108	11
SYK	102	4
TAK1	83	10
TAO1	102	5
TBK1	93	1
TESK1	61	3
TGFBR1	59	4
TIE2	45	6
TLK1	101	2
TrkA	85	9
TSSK1	92	2
TTBK1	97	1
TTBK2	102	2
TTK	91	4
ULK1	93	2
ULK2	113	12
VEGFR1	77	6
WNK1	105	5
YES1	73	24
ZAP70	89	12