Selectivity data for probe SGK3-PROTAC1 and control cisSGK3-PROTAC1


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SGK3-PROTAC1

Protein kinase profiling was undertaken at the International Centre for Protein Kinase Profiling. The result for each kinase was presented as a mean kinase activity of the reaction taken in triplicate relative to a control sample treated with DMSO. Assay conditions are available here. Shown are data from PMID: 31461270 (Supplementary Table 2) .

Conclusion: Closest off-targets are [% activity remaining] SGK1 (34; IC50 = 220 nM) , RPS6KB1 (19; IC50 = 1.8 µM).

Target protein HGNC name Species % Activity remaining at 1 µM IC50 [µM] % Standard-deviation
ABL ABL1 Homo sapiens 111.0 8.15
AMPK (hum) PRKAA1
 PRKAB2
 PRKAG1
 		Homo sapiens 105.0 1.88
ASK1 MAP3K5 Homo sapiens 113.2 1.25
Aurora A AURKA Homo sapiens 90.3 9.25
Aurora B AURKB Homo sapiens 92.5 8.90
BRK PTK6 Homo sapiens 86.8 21.52
BRSK1 BRSK1 Homo sapiens 107.5 1.38
BRSK2 BRSK2 Homo sapiens 97.2 15.95
BTK BTK Homo sapiens 96.9 3.72
CAMK1 CAMK1 Homo sapiens 86.3 1.25
CAMKK beta CAMKK2 Homo sapiens 98.9 3.58
CDK2-Cyclin A CDK2
 CCNA2
 		Homo sapiens 100.6 5.91
CDK9-Cyclin T1 CDK9
 CCNT1
 		Homo sapiens 102.6 1.74
CHK1 CHEK1 Homo sapiens 110.6 9.56
CHK2 CHEK2 Homo sapiens 84.8 8.62
CK1 delta CSNK1D Homo sapiens 95.0 2.99
CK1 gamma 2 CSNK1G2 Homo sapiens 100.7 1.79
CK2 CSNK2A1 Homo sapiens 90.2 1.12
CLK2 CLK2 Homo sapiens 103.5 3.46
CSK CSK Homo sapiens 117.5 9.50
DAPK1 DAPK1 Homo sapiens 100.0 6.87
DDR2 DDR2 Homo sapiens 114.0 17.41
DYRK1A DYRK1A Homo sapiens 105.0 21.15
DYRK2 DYRK2 Homo sapiens 102.0 21.99
DYRK3 DYRK3 Homo sapiens 102.4 13.09
EF2K EEF2K Homo sapiens 97.5 10.51
EIF2AK3 EIF2AK3 Homo sapiens 106.5 15.05
EPH-A2 EPHA2 Homo sapiens 94.1 10.60
EPH-A4 EPHA4 Homo sapiens 105.9 18.66
EPH-B1 EPHB1 Homo sapiens 99.9 18.63
EPH-B2 ERBB2 Homo sapiens 93.9 0.48
EPH-B3 EPHB3 Homo sapiens 91.6 8.87
EPH-B4 EPHB4 Homo sapiens 106.6 3.62
ERK1 MAPK3 Homo sapiens 103.4 11.90
ERK2 MAPK1 Homo sapiens 104.0 5.34
ERK5 MAPK7 Homo sapiens 101.8 14.26
ERK8 MAPK15 Homo sapiens 94.2 3.09
FGF-R1 FGFR1 Homo sapiens 107.7 10.31
GCK GCK Homo sapiens 99.0 6.11
GSK3 beta GSK3B Homo sapiens 107.9 8.74
HER4 ERBB4 Homo sapiens 92.0 6.70
HIPK1 HIPK1 Homo sapiens 135.1 4.06
HIPK2 HIPK2 Homo sapiens 108.7 11.77
HIPK3 HIPK3 Homo sapiens 110.7 8.41
IGF-1R IGF1R Homo sapiens 82.4 6.09
IKK beta IKBKB Homo sapiens 99.9 11.72
IKK epsilon IKBKE Homo sapiens 108.2 7.06
IR INSR Homo sapiens 103.0 8.14
IRAK1 IRAK1 Homo sapiens 98.3 0.68
IRAK4 IRAK4 Homo sapiens 114.4 24.06
IRR INSRR Homo sapiens 102.9 17.40
JAK2 JAK2 Homo sapiens 95.4 5.25
JNK1 MAPK8 Homo sapiens 117.5 0.29
JNK2 MAPK9 Homo sapiens 117.4 1.20
JNK3 MAPK10 Homo sapiens 92.1 2.14
Lck LCK Homo sapiens 123.8 41.29
LKB1 STK11 Homo sapiens 105.4 21.03
MAP4K3 MAP4K3 Homo sapiens 98.8 0.21
MAP4K5 MAP4K5 Homo sapiens 98.6 1.28
MAPKAP-K2 MAPKAPK2 Homo sapiens 85.8 14.15
MAPKAP-K3 MAPKAPK3 Homo sapiens 79.0 4.81
MARK1 MARK1 Homo sapiens 99.4 13.85
MARK2 MARK2 Homo sapiens 102.1 14.51
MARK3 MARK3 Homo sapiens 98.4 24.66
MARK4 MARK4 Homo sapiens 104.8 12.01
MEKK1 MAP3K1 Homo sapiens 123.9 9.89
MELK MELK Homo sapiens 91.5 4.82
MINK1 MINK1 Homo sapiens 115.2 12.33
MKK1 MAP2K1 Homo sapiens 106.5 11.12
MKK2 MAP2K2 Homo sapiens 114.2 8.47
MKK6 MAP2K6 Homo sapiens 123.2 16.59
MLK1 MAP3K9 Homo sapiens 81.9 1.04
MLK3 MAP3K11 Homo sapiens 70.5 7.15
MNK1 MKNK1 Homo sapiens 107.6 7.59
MNK2 MKNK2 Homo sapiens 121.5 11.62
MPSK1 STK16 Homo sapiens 126.6 25.63
MSK1 RPS6KA5 Homo sapiens 49.6 5.20
MST2 STK3 Homo sapiens 111.6 16.17
MST3 STK24 Homo sapiens 102.4 0.67
MST4 STK26 Homo sapiens 106.3 18.04
NEK2a NEK2 Homo sapiens 161.8 14.40
NEK6 NEK6 Homo sapiens 105.7 2.08
NUAK1 NUAK1 Homo sapiens 97.9 13.81
OSR1 OXSR1 Homo sapiens 103.5 12.71
p38 alpha MAPK MAPK14 Homo sapiens 124.9 6.53
p38 beta MAPK MAPK11 Homo sapiens 106.8 12.10
p38 delta MAPK MAPK13 Homo sapiens 103.3 0.31
p38 gamma MAPK MAPK12 Homo sapiens 106.6 4.02
PAK2 PAK2 Homo sapiens 116.2 1.70
PAK4 PAK4 Homo sapiens 81.1 5.99
PAK5 PAK5 Homo sapiens 87.6 1.53
PAK6 PAK6 Homo sapiens 97.9 4.39
PDGFRA PDGFRA Homo sapiens 101.2 6.06
PDK1 PDK1 Homo sapiens 99.3 7.35
PHK PHKA2 Homo sapiens 112.7 4.17
PIM1 PIM1 Homo sapiens 94.5 2.53
PIM2 PIM2 Homo sapiens 98.2 5.10
PIM3 PIM3 Homo sapiens 88.1 20.19
PINK PINK1 Homo sapiens 108.5 13.68
PKA PRKACA Homo sapiens 107.7 7.56
PKB alpha AKT1 Homo sapiens 105.4 13.83
PKB beta AKT2 Homo sapiens 98.7 1.65
PKC alpha PRKCA Homo sapiens 120.8 7.15
PKC gamma PRKCG Homo sapiens 103.1 2.43
PKC zeta PRKCZ Homo sapiens 96.4 7.32
PKD1 PRKD1 Homo sapiens 94.0 16.77
PLK1 PLK1 Homo sapiens 97.9 7.90
PRAK MAPKAPK5 Homo sapiens 115.4 5.89
PRK2 PKN2 Homo sapiens 104.6 0.36
RIPK2 RIPK2 Homo sapiens 88.4 7.91
ROCK 2 ROCK2 Homo sapiens 113.0 9.26
RSK1 RPS6KA1 Homo sapiens 83.1 0.21
RSK2 RPS6KA3 Homo sapiens 120.1 17.27
S6K1 RPS6KB1 Homo sapiens 19.0 1.80 0.94
SGK1 SGK1 Homo sapiens 34.5 0.22 1.50
SIK2 SIK2 Homo sapiens 94.6 0.38
SIK3 SIK3 Homo sapiens 78.7 21.29
SmMLCK MYLK Homo sapiens 52.9 18.86
Src SRC Homo sapiens 83.4 10.02
SRPK1 SRPK1 Homo sapiens 95.8 0.46
STK33 STK33 Homo sapiens 110.3 15.94
SYK SYK Homo sapiens 115.7 10.04
TAK1 MAP3K7 Homo sapiens 108.4 0.31
TAO1 TAOK1 Homo sapiens 99.0 9.79
TBK1 TBK1 Homo sapiens 93.4 4.10
TESK1 TESK1 Homo sapiens 122.3 14.67
TGFBR1 TGFBR1 Homo sapiens 124.2 7.90
TIE2 TEK Homo sapiens 63.8 13.63
TLK1 TLK1 Homo sapiens 101.9 2.01
TrkA NTRK1 Homo sapiens 112.1 17.62
TSSK1 TSSK1B Homo sapiens 114.9 0.04
TTBK1 TTBK1 Homo sapiens 105.2 6.78
TTBK2 TTBK2 Homo sapiens 93.5 2.98
TTK TTK Homo sapiens 89.4 15.62
ULK1 ULK1 Homo sapiens 116.4 3.33
ULK2 ULK2 Homo sapiens 102.8 5.64
VEGFR1 FLT1 Homo sapiens 120.4 6.01
WNK1 WNK1 Homo sapiens 93.9 4.93
YES1 YES1 Homo sapiens 107.7 6.79
ZAP70 ZAP70 Homo sapiens 75.0 12.97
 

cisSGK3-PROTAC1

Conclusion: Closest off-targets are [% activity remaining] SGK1 (50; IC50 = 1.4 µM) , RPS6KB1 (20; IC50 = 1.7 µM).

Target protein HGNC name Species % Activity remaining at 1 µM IC50 [µM] % Standard-deviation
ABL ABL1 Homo sapiens 112.3 9.70
AMPK (hum) PRKAA1,PRKAB2,PRKAG1 Homo sapiens 108.0 6.19
ASK1 MAP3K5 Homo sapiens 102.0 11.35
Aurora A AURKA Homo sapiens 91.4 7.07
Aurora B AURKB Homo sapiens 94.7 0.90
BRK PTK6 Homo sapiens 104.7 10.58
BRSK1 BRSK1 Homo sapiens 105.7 6.06
BRSK2 BRSK2 Homo sapiens 100.7 1.14
BTK BTK Homo sapiens 90.6 2.38
CAMK1 CAMK1 Homo sapiens 105.5 4.56
CAMKK beta CAMKK2 Homo sapiens 108.0 8.15
CDK2-Cyclin A CDK2,CCNA2 Homo sapiens 102.5 11.25
CDK9-Cyclin T1 CDK9,CCNT1 Homo sapiens 105.2 11.18
CHK1 CHEK1 Homo sapiens 126.4 20.81
CHK2 CHEK2 Homo sapiens 99.1 4.18
CK1 delta CSNK1D Homo sapiens 107.7 11.72
CK1 gamma 2 CSNK1G2 Homo sapiens 105.9 12.46
CK2 CSNK2A1 Homo sapiens 96.4 1.27
CLK2 CLK2 Homo sapiens 84.8 21.52
CSK CSK Homo sapiens 113.2 10.83
DAPK1 DAPK1 Homo sapiens 108.4 23.54
DDR2 DDR2 Homo sapiens 133.8 12.99
DYRK1A DYRK1A Homo sapiens 99.0 18.14
DYRK2 DYRK2 Homo sapiens 97.3 7.31
DYRK3 DYRK3 Homo sapiens 103.9 8.28
EF2K EEF2K Homo sapiens 104.9 6.70
EIF2AK3 EIF2AK3 Homo sapiens 111.1 17.36
EPH-A2 EPHA2 Homo sapiens 103.6 0.47
EPH-A4 EPHA4 Homo sapiens 89.4 19.72
EPH-B1 EPHB1 Homo sapiens 107.9 16.21
EPH-B2 ERBB2 Homo sapiens 97.4 4.87
EPH-B3 EPHB3 Homo sapiens 103.6 26.84
EPH-B4 EPHB4 Homo sapiens 107.9 5.87
ERK1 MAPK3 Homo sapiens 100.6 3.35
ERK2 MAPK1 Homo sapiens 95.2 3.15
ERK5 MAPK7 Homo sapiens 108.0 10.44
ERK8 MAPK15 Homo sapiens 86.4 3.36
FGF-R1 FGFR1 Homo sapiens 105.5 26.91
GCK GCK Homo sapiens 96.3 19.29
GSK3 beta GSK3B Homo sapiens 106.2 13.08
HER4 ERBB4 Homo sapiens 102.7 10.38
HIPK1 HIPK1 Homo sapiens 126.3 11.95
HIPK2 HIPK2 Homo sapiens 99.6 4.75
HIPK3 HIPK3 Homo sapiens 105.3 18.14
IGF-1R IGF1R Homo sapiens 93.2 28.14
IKK beta IKBKB Homo sapiens 101.4 6.17
IKK epsilon IKBKE Homo sapiens 99.0 10.36
IR INSR Homo sapiens 93.9 4.74
IRAK1 IRAK1 Homo sapiens 105.4 8.84
IRAK4 IRAK4 Homo sapiens 98.0 4.68
IRR INSRR Homo sapiens 89.9 17.20
JAK2 JAK2 Homo sapiens 93.6 15.05
JNK1 MAPK8 Homo sapiens 118.8 11.27
JNK2 MAPK9 Homo sapiens 109.1 6.60
JNK3 MAPK10 Homo sapiens 82.5 5.14
Lck LCK Homo sapiens 116.0 21.03
LKB1 STK11 Homo sapiens 111.7 11.60
MAP4K3 MAP4K3 Homo sapiens 95.5 3.64
MAP4K5 MAP4K5 Homo sapiens 101.4 5.28
MAPKAP-K2 MAPKAPK2 Homo sapiens 91.6 13.95
MAPKAP-K3 MAPKAPK3 Homo sapiens 77.0 9.01
MARK1 MARK1 Homo sapiens 93.0 11.04
MARK2 MARK2 Homo sapiens 111.6 1.53
MARK3 MARK3 Homo sapiens 108.8 1.31
MARK4 MARK4 Homo sapiens 100.2 5.49
MEKK1 MAP3K1 Homo sapiens 127.8 11.76
MELK MELK Homo sapiens 99.5 16.71
MINK1 MINK1 Homo sapiens 115.5 10.51
MKK1 MAP2K1 Homo sapiens 101.6 7.24
MKK2 MAP2K2 Homo sapiens 124.4 7.29
MKK6 MAP2K6 Homo sapiens 108.0 2.18
MLK1 MAP3K9 Homo sapiens 93.9 2.46
MLK3 MAP3K11 Homo sapiens 75.6 6.73
MNK1 MKNK1 Homo sapiens 103.2 18.69
MNK2 MKNK2 Homo sapiens 122.2 19.39
MPSK1 STK16 Homo sapiens 138.9 22.29
MSK1 RPS6KA5 Homo sapiens 56.5 0.61
MST2 STK3 Homo sapiens 100.4 1.22
MST3 STK24 Homo sapiens 112.7 0.38
MST4 STK26 Homo sapiens 99.0 2.66
NEK2a NEK2 Homo sapiens 138.9 25.93
NEK6 NEK6 Homo sapiens 111.0 9.15
NUAK1 NUAK1 Homo sapiens 90.0 0.83
OSR1 OXSR1 Homo sapiens 117.6 6.96
p38 alpha MAPK MAPK14 Homo sapiens 108.7 8.80
p38 beta MAPK MAPK11 Homo sapiens 111.7 22.50
p38 delta MAPK MAPK13 Homo sapiens 120.7 16.22
p38 gamma MAPK MAPK12 Homo sapiens 126.7 8.26
PAK2 PAK2 Homo sapiens 98.7 3.93
PAK4 PAK4 Homo sapiens 113.3 16.79
PAK5 PAK5 Homo sapiens 104.9 10.69
PAK6 PAK6 Homo sapiens 99.5 9.98
PDGFRA PDGFRA Homo sapiens 94.8 1.38
PDK1 PDK1 Homo sapiens 86.5 4.43
PHK PHKA2 Homo sapiens 122.0 1.19
PIM1 PIM1 Homo sapiens 96.5 3.88
PIM2 PIM2 Homo sapiens 105.4 4.25
PIM3 PIM3 Homo sapiens 88.8 14.82
PINK PINK1 Homo sapiens 108.8 4.99
PKA PRKACA Homo sapiens 111.0 4.28
PKB alpha AKT1 Homo sapiens 117.0 6.89
PKB beta AKT2 Homo sapiens 100.5 0.01
PKC alpha PRKCA Homo sapiens 118.4 5.60
PKC gamma PRKCG Homo sapiens 99.9 10.85
PKC zeta PRKCZ Homo sapiens 110.0 27.04
PKD1 PRKD1 Homo sapiens 91.7 11.93
PLK1 PLK1 Homo sapiens 98.4 4.13
PRAK MAPKAPK5 Homo sapiens 118.9 6.99
PRK2 PKN2 Homo sapiens 100.5 4.59
RIPK2 RIPK2 Homo sapiens 94.2 15.58
ROCK 2 ROCK2 Homo sapiens 119.0 2.79
RSK1 RPS6KA1 Homo sapiens 90.2 1.41
RSK2 RPS6KA3 Homo sapiens 109.5 3.50
S6K1 RPS6KB1 Homo sapiens 20.2 1.70 3.17
SGK1 SGK1 Homo sapiens 50.9 1.40 10.15
SIK2 SIK2 Homo sapiens 93.8 11.48
SIK3 SIK3 Homo sapiens 117.1 16.79
SmMLCK MYLK Homo sapiens 70.7 10.41
Src SRC Homo sapiens 86.8 21.46
SRPK1 SRPK1 Homo sapiens 104.4 6.24
STK33 STK33 Homo sapiens 108.6 6.52
SYK SYK Homo sapiens 103.2 25.88
TAK1 MAP3K7 Homo sapiens 107.4 4.70
TAO1 TAOK1 Homo sapiens 104.9 3.99
TBK1 TBK1 Homo sapiens 110.9 8.97
TESK1 TESK1 Homo sapiens 119.7 2.52
TGFBR1 TGFBR1 Homo sapiens 114.3 5.48
TIE2 TEK Homo sapiens 80.8 2.83
TLK1 TLK1 Homo sapiens 108.6 0.37
TrkA NTRK1 Homo sapiens 102.4 10.55
TSSK1 TSSK1B Homo sapiens 112.9 0.94
TTBK1 TTBK1 Homo sapiens 113.3 7.06
TTBK2 TTBK2 Homo sapiens 89.7 6.45
TTK TTK Homo sapiens 99.4 9.97
ULK1 ULK1 Homo sapiens 112.5 5.19
ULK2 ULK2 Homo sapiens 117.3 18.13
VEGFR1 FLT1 Homo sapiens 102.5 8.43
WNK1 WNK1 Homo sapiens 96.6 7.70
YES1 YES1 Homo sapiens 105.2 2.88
ZAP70 ZAP70 Homo sapiens 74.7 18.12