Selectivity data for probe ABT-546 and control A-545


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ABT-546


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1A HTR1A 20.57
5-HT1B HTR1B 2.64
5-HT1D HTR1D -13.76
5-HT1E HTR1E 3.64
5-HT2A HTR2A 8.83
5-HT2B HTR2B -9.89
5-HT2C HTR2C -18.69
5-HT3 HTR3A 14.73
5-HT5A HTR5A -5.07
5-HT6 HTR6 -11.39
5-HT7A HTR7 -2.24
D1 DRD1 4.66
D2 DRD2 21.28
D3 DRD3 17.33
D4 DRD4 21.74
D5 DRD5 16.97
SERT SLC6A4 15.32
NET SLC6A2 -19.90
DAT SLC6A3 -0.59
MOR OPRM1 14.22
DOR OPRD1 25.63
KOR OPRK1 -1.47
GABAA -5.72
H1 HRH1 53.59 > 10000.00 < 5.00
H2 HRH2 24.34
H3 HRH3 -3.57
H4 HRH4 -0.61
Alpha1A ADRA1A -2.13
Alpha1B ADRA1B -7.90
Alpha2A ADRA2A -17.08
Alpha2B ADRA2B 9.73
Alpha2C ADRA2C -18.39
Beta1 ADRB1 -6.60
Beta2 ADRB2 -10.45
M1 CHRM1 -19.44
M2 CHRM2 -1.89
M3 CHRM3 -9.94
M4 CHRM4 8.50
M5 CHRM5 -13.84
Beta3 ADRB3 2.71
GABAA/BZP 19.72
GABA/PBR 43.21
Alpha1D ADRA1D -11.73
Sigma 2 TMEM97 48.45
Sigma 1 SIGMAR1 29.62

A-545


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1A HTR1A 76.26 189.00 6.72
5-HT1B HTR1B -2.98
5-HT1D HTR1D -3.72
5-HT1E HTR1E 27.11
5-HT2A HTR2A 7.84
5-HT2B HTR2B 75.95 6516.00 average (n=2) 5.24
5-HT2C HTR2C 15.69
5-HT3 HTR3A 2.22
5-HT5A HTR5A 43.49
5-HT6 HTR6 33.53
5-HT7A HTR7 -11.69
D1 DRD1 16.61
D2 DRD2 21.32
D3 DRD3 16.65
D4 DRD4 87.07 5.50 8.26
D5 DRD5 30.53
SERT SLC6A4 -7.99
NET SLC6A2 38.52
DAT SLC6A3 22.99
MOR OPRM1 58.49 2781.00 5.56
DOR OPRD1 41.15
KOR OPRK1 69.87 2784.50 average (n=2) 5.55
H1 HRH1 47.40
H2 HRH2 8.46
H3 HRH3 16.97
H4 HRH4 4.10
Alpha1A ADRA1A 23.33
Alpha1B ADRA1B 6.50
Alpha2A ADRA2A 19.08
Alpha2B ADRA2B 50.00 4643.50 average (n=2) 5.38
Alpha2C ADRA2C 56.12 5766.00 5.20
Beta1 ADRB1 -10.84
Beta2 ADRB2 -6.31
M1 CHRM1 12.42
M2 CHRM2 3.71
M3 CHRM3 10.29
M4 CHRM4 -19.22
M5 CHRM5 1.10
Beta3 ADRB3 28.40
GABAA/BZP 8.52
GABA/PBR 22.92
Alpha1D ADRA1D 6.55
Sigma 2 TMEM97 41.30
Sigma 1 SIGMAR1 93.60 298.00 6.53

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Primary results are shown as '% Ctrl', i.e. the negative control (DMSO) is equal 100% control and the positive control (control compound) is equal 0% control. For compounds showing less than 50% of control in the primary screening assay, a Kd will be determined. Note: It cannot be excluded that 0 % control values are due to assay artefacts.
View assay details

Jump to control KinomeScan data

ABT-546


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 1000
ABL1 ABL1-phosphorylated 99.0 1000
ABL2 ABL2 94.0 1000
ACVR1 ACVR1 100.0 1000
ACVR1B ACVR1B 85.0 1000
ACVR2A ACVR2A 100.0 1000
ACVR2B ACVR2B 100.0 1000
ACVRL1 ACVRL1 100.0 1000
COQ8A ADCK3 80.0 1000
COQ8B ADCK4 93.0 1000
AKT1 AKT1 89.0 1000
AKT2 AKT2 100.0 1000
AKT3 AKT3 85.0 1000
ALK ALK(L1196M) 100.0 1000
PRKAA1 AMPK-alpha1 100.0 1000
PRKAA2 AMPK-alpha2 100.0 1000
ANKK1 ANKK1 100.0 1000
NUAK1 ARK5 100.0 1000
MAP3K5 ASK1 100.0 1000
MAP3K6 ASK2 92.0 1000
AURKA AURKA 89.0 1000
AURKB AURKB 93.0 1000
AURKC AURKC 100.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 100.0 1000
BLK BLK 100.0 1000
BMPR1A BMPR1A 84.0 1000
BMPR1B BMPR1B 100.0 1000
BMPR2 BMPR2 100.0 1000
BMX BMX 100.0 1000
BRAF BRAF(V600E) 100.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 80.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 61.0 1000
BUB1 BUB1 100.0 1000
CAMK1 CAMK1 100.0 1000
PNCK CAMK1B 24.0 1000 > 10000.0
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 100.0 1000
CAMK2B CAMK2B 100.0 1000
CAMK2D CAMK2D 80.0 1000
CAMK2G CAMK2G 100.0 1000
CAMK4 CAMK4 100.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 100.0 1000
CASK CASK 52.0 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 100.0 1000
CDK13 CDC2L5 100.0 1000
CDK19 CDK11 100.0 1000
CDK2 CDK2 95.0 1000
CDK3 CDK3 100.0 1000
CDK4 CDK4-cyclinD3 99.0 1000
CDK5 CDK5 85.0 1000
CDK7 CDK7 82.0 1000
CDK8 CDK8 100.0 1000
CDK9 CDK9 100.0 1000
CDKL1 CDKL1 90.0 1000
CDKL2 CDKL2 99.0 1000
CDKL3 CDKL3 93.0 1000
CDKL5 CDKL5 100.0 1000
CHEK1 CHEK1 100.0 1000
CHEK2 CHEK2 99.0 1000
CIT CIT 79.0 1000
CLK1 CLK1 84.0 1000
CLK2 CLK2 79.0 1000
CLK3 CLK3 92.0 1000
CLK4 CLK4 100.0 1000
CSF1R CSF1R-autoinhibited 88.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 89.0 1000
CSNK1A1L CSNK1A1L 100.0 1000
CSNK1D CSNK1D 90.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 95.0 1000
CSNK1G2 CSNK1G2 84.0 1000
CSNK1G3 CSNK1G3 78.0 1000
CSNK2A1 CSNK2A1 91.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 100.0 1000
DAPK1 DAPK1 100.0 1000
DAPK2 DAPK2 94.0 1000
DAPK3 DAPK3 25.0 1000 > 10000.0
DCLK1 DCAMKL1 47.0 1000 > 10000.0
DCLK2 DCAMKL2 100.0 1000
DCLK3 DCAMKL3 100.0 1000
DDR1 DDR1 100.0 1000
DDR2 DDR2 100.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 89.0 1000
CDC42BPG DMPK2 100.0 1000
STK17A DRAK1 100.0 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 100.0 1000
DYRK1B DYRK1B 100.0 1000
DYRK2 DYRK2 100.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 95.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 100.0 1000
EPHA3 EPHA3 100.0 1000
EPHA4 EPHA4 100.0 1000
EPHA5 EPHA5 82.0 1000
EPHA6 EPHA6 100.0 1000
EPHA7 EPHA7 87.0 1000
EPHA8 EPHA8 71.0 1000
EPHB1 EPHB1 84.0 1000
EPHB2 EPHB2 100.0 1000
EPHB3 EPHB3 93.0 1000
EPHB4 EPHB4 100.0 1000
EPHB6 EPHB6 78.0 1000
ERBB2 ERBB2 52.0 1000
ERBB3 ERBB3 100.0 1000
ERBB4 ERBB4 92.0 1000
MAPK3 ERK1 92.0 1000
MAPK1 ERK2 77.0 1000
MAPK6 ERK3 100.0 1000
MAPK4 ERK4 100.0 1000
MAPK7 ERK5 100.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 100.0 1000
PTK2 FAK 88.0 1000
FER FER 81.0 1000
FES FES 100.0 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 92.0 1000
FGFR3 FGFR3(G697C) 100.0 1000
FGFR4 FGFR4 87.0 1000
FGR FGR 100.0 1000
FLT1 FLT1 100.0 1000
FLT3 FLT3-autoinhibited 100.0 1000
FLT4 FLT4 84.0 1000
FRK FRK 100.0 1000
FYN FYN 100.0 1000
GAK GAK 100.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 71.0 1000
GRK1 GRK1 84.0 1000
GRK2 GRK2 100.0 1000
GRK3 GRK3 56.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 100.0 1000
GSK3A GSK3A 73.0 1000
GSK3B GSK3B 90.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 99.0 1000
HIPK1 HIPK1 87.0 1000
HIPK2 HIPK2 76.0 1000
HIPK3 HIPK3 100.0 1000
HIPK4 HIPK4 64.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 94.0 1000
CILK1 ICK 100.0 1000
IGF1R IGF1R 92.0 1000
CHUK IKK-alpha 100.0 1000
IKBKB IKK-beta 100.0 1000
IKBKE IKK-epsilon 100.0 1000
INSR INSR 100.0 1000
INSRR INSRR 86.0 1000
IRAK1 IRAK1 100.0 1000
IRAK3 IRAK3 97.0 1000
IRAK4 IRAK4 100.0 1000
ITK ITK 100.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 86.0 1000
JAK2 JAK2(JH1domain-catalytic) 100.0 1000
JAK3 JAK3(JH1domain-catalytic) 100.0 1000
MAPK8 JNK1 100.0 1000
MAPK9 JNK2 100.0 1000
MAPK10 JNK3 100.0 1000
KIT KIT-autoinhibited 95.0 1000
LATS1 LATS1 100.0 1000
LATS2 LATS2 66.0 1000
LCK LCK 100.0 1000
LIMK1 LIMK1 100.0 1000
LIMK2 LIMK2 100.0 1000
STK11 LKB1 82.0 1000
STK10 LOK 100.0 1000
LRRK2 LRRK2(G2019S) 87.0 1000
LTK LTK 100.0 1000
LYN LYN 100.0 1000
MAP3K13 LZK 100.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 84.0 1000
MAP3K15 MAP3K15 99.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 100.0 1000
MAP3K4 MAP3K4 100.0 1000
MAP4K2 MAP4K2 100.0 1000
MAP4K3 MAP4K3 100.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 100.0 1000
MAPKAPK5 MAPKAPK5 90.0 1000
MARK1 MARK1 91.0 1000
MARK2 MARK2 100.0 1000
MARK3 MARK3 100.0 1000
MARK4 MARK4 94.0 1000
MAST1 MAST1 72.0 1000
MAP2K1 MEK1 100.0 1000
MAP2K2 MEK2 85.0 1000
MAP2K3 MEK3 90.0 1000
MAP2K4 MEK4 100.0 1000
MAP2K5 MEK5 100.0 1000
MAP2K6 MEK6 100.0 1000
MELK MELK 100.0 1000
MERTK MERTK 88.0 1000
MET MET(Y1235D) 100.0 1000
MINK1 MINK 100.0 1000
MAP2K7 MKK7 100.0 1000
MKNK1 MKNK1 100.0 1000
MKNK2 MKNK2 100.0 1000
MYLK3 MLCK 100.0 1000
MAP3K9 MLK1 77.0 1000
MAP3K10 MLK2 100.0 1000
MAP3K11 MLK3 95.0 1000
CDC42BPA MRCKA 100.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 95.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 100.0 1000
STK24 MST3 100.0 1000
STK26 MST4 100.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 100.0 1000
MYLK MYLK 76.0 1000
MYLK2 MYLK2 100.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 95.0 1000
STK38 NDR1 78.0 1000
STK38L NDR2 68.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 100.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 96.0 1000
NEK3 NEK3 100.0 1000
NEK4 NEK4 100.0 1000
NEK5 NEK5 100.0 1000
NEK6 NEK6 84.0 1000
NEK7 NEK7 78.0 1000
NEK9 NEK9 82.0 1000
MAP3K14 NIK 100.0 1000
NIM1K NIM1 100.0 1000
NLK NLK 97.0 1000
OXSR1 OSR1 100.0 1000
MAPK14 p38-alpha 92.0 1000
MAPK11 p38-beta 91.0 1000
MAPK13 p38-delta 100.0 1000
MAPK12 p38-gamma 67.0 1000
PAK1 PAK1 100.0 1000
PAK2 PAK2 100.0 1000
PAK3 PAK3 100.0 1000
PAK4 PAK4 97.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 100.0 1000
CDK17 PCTK2 100.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 89.0 1000
PDGFRB PDGFRB 100.0 1000
PDPK1 PDPK1 85.0 1000
CDPK1 PFCDPK1(P.falciparum) 100.0 1000
PK5 PFPK5(P.falciparum) 100.0 1000
CDK15 PFTAIRE2 79.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 81.0 1000
PIK3C2B PIK3C2B 91.0 1000
PIK3C2G PIK3C2G 89.0 1000
PIK3CA PIK3CA(Q546K) 100.0 1000
PIK3CB PIK3CB 100.0 1000
PIK3CD PIK3CD 95.0 1000
PIK3CG PIK3CG 100.0 1000
PI4KB PIK4CB 100.0 1000
PIKFYVE PIKFYVE 100.0 1000
PIM1 PIM1 88.0 1000
PIM2 PIM2 88.0 1000
PIM3 PIM3 100.0 1000
PIP5K1A PIP5K1A 85.0 1000
PIP5K1C PIP5K1C 73.0 1000
PIP4K2B PIP5K2B 100.0 1000
PIP4K2C PIP5K2C 89.0 1000
PRKACA PKAC-alpha 86.0 1000
PRKACB PKAC-beta 90.0 1000
PKMYT1 PKMYT1 100.0 1000
PKN1 PKN1 71.0 1000
PKN2 PKN2 92.0 1000
PKNB PKNB(M.tuberculosis) 81.0 1000
PLK1 PLK1 100.0 1000
PLK2 PLK2 100.0 1000
PLK3 PLK3 94.0 1000
PLK4 PLK4 86.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 100.0 1000
PRKCH PRKCH 95.0 1000
PRKCI PRKCI 100.0 1000
PRKCQ PRKCQ 88.0 1000
PRKD1 PRKD1 100.0 1000
PRKD2 PRKD2 95.0 1000
PRKD3 PRKD3 82.0 1000
PRKG1 PRKG1 99.0 1000
PRKG2 PRKG2 100.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 100.0 1000
PRPF4B PRP4 61.0 1000
PTK2B PYK2 91.0 1000
SIK3 QSK 100.0 1000
RAF1 RAF1 93.0 1000
RET RET(V804M) 96.0 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 100.0 1000
RIOK3 RIOK3 100.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 90.0 1000
RIPK4 RIPK4 100.0 1000
DSTYK RIPK5 97.0 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 79.0 1000
ROS1 ROS1 98.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 98.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KB1 S6K1 83.0 1000
SBK1 SBK1 100.0 1000
SGK1 SGK 100.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 100.0 1000
SGK3 SGK3 100.0 1000
SIK1 SIK 47.0 1000 > 10000.0
SIK2 SIK2 91.0 1000
SLK SLK 80.0 1000
NUAK2 SNARK 100.0 1000
SNRK SNRK 100.0 1000
SRC SRC 87.0 1000
SRMS SRMS 94.0 1000
SRPK1 SRPK1 87.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 97.0 1000
STK33 STK33 100.0 1000
STK35 STK35 100.0 1000
STK36 STK36 100.0 1000
STK39 STK39 100.0 1000
SYK SYK 90.0 1000
MAP3K7 TAK1 100.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 78.0 1000
TAOK3 TAOK3 93.0 1000
TBK1 TBK1 74.0 1000
TEC TEC 75.0 1000
TESK1 TESK1 94.0 1000
TGFBR1 TGFBR1 97.0 1000
TGFBR2 TGFBR2 100.0 1000
TIE1 TIE1 89.0 1000
TEK TIE2 93.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 100.0 1000
TNK1 TNK1 71.0 1000
TNK2 TNK2 100.0 1000
TNNI3K TNNI3K 100.0 1000
NTRK1 TRKA 100.0 1000
NTRK2 TRKB 83.0 1000
NTRK3 TRKC 70.0 1000
TRPM6 TRPM6 100.0 1000
TSSK1B TSSK1B 81.0 1000
TSSK3 TSSK3 97.0 1000
TTK TTK 100.0 1000
TXK TXK 100.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 100.0 1000
ULK2 ULK2 94.0 1000
ULK3 ULK3 100.0 1000
KDR VEGFR2 100.0 1000
PIK3C3 VPS34 100.0 1000
VRK2 VRK2 94.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 100.0 1000
WNK2 WNK2 100.0 1000
WNK3 WNK3 100.0 1000
WNK4 WNK4 100.0 1000
STK32A YANK1 89.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 94.0 1000
YES1 YES 100.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 100.0 1000
MAP3K20 ZAK 95.0 1000
ZAP70 ZAP70 100.0 1000

A-545


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 1000
ABL1 ABL1-phosphorylated 100.0 1000
ABL2 ABL2 100.0 1000
ACVR1 ACVR1 100.0 1000
ACVR1B ACVR1B 96.4 1000
ACVR2A ACVR2A 85.1 1000
ACVR2B ACVR2B 85.1 1000
ACVRL1 ACVRL1 99.4 1000
COQ8A ADCK3 99.4 1000
COQ8B ADCK4 80.2 1000
AKT1 AKT1 85.7 1000
AKT2 AKT2 100.0 1000
AKT3 AKT3 100.0 1000
ALK ALK(L1196M) 100.0 1000
PRKAA1 AMPK-alpha1 96.7 1000
PRKAA2 AMPK-alpha2 92.6 1000
ANKK1 ANKK1 95.7 1000
NUAK1 ARK5 82.4 1000
MAP3K5 ASK1 100.0 1000
MAP3K6 ASK2 100.0 1000
AURKA AURKA 90.2 1000
AURKB AURKB 100.0 1000
AURKC AURKC 100.0 1000
AXL AXL 87.2 1000
BMP2K BIKE 100.0 1000
BLK BLK 100.0 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 100.0 1000
BMPR2 BMPR2 86.7 1000
BMX BMX 84.6 1000
BRAF BRAF(V600E) 100.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 88.9 1000
BRSK2 BRSK2 98.3 1000
BTK BTK 100.0 1000
BUB1 BUB1 94.9 1000
CAMK1 CAMK1 100.0 1000
PNCK CAMK1B 100.0 1000
CAMK1D CAMK1D 94.4 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 100.0 1000
CAMK2B CAMK2B 100.0 1000
CAMK2D CAMK2D 99.9 1000
CAMK2G CAMK2G 94.3 1000
CAMK4 CAMK4 100.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 87.2 1000
CASK CASK 90.5 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 98.3 1000
CDK13 CDC2L5 100.0 1000
CDK19 CDK11 99.6 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 88.1 1000
CDK4 CDK4-cyclinD3 92.7 1000
CDK5 CDK5 97.7 1000
CDK7 CDK7 89.5 1000
CDK8 CDK8 78.0 1000
CDK9 CDK9 100.0 1000
CDKL1 CDKL1 74.9 1000
CDKL2 CDKL2 39.2 1000
CDKL3 CDKL3 83.6 1000
CDKL5 CDKL5 100.0 1000
CHEK1 CHEK1 100.0 1000
CHEK2 CHEK2 87.8 1000
CIT CIT 90.5 1000
CLK1 CLK1 100.0 1000
CLK2 CLK2 100.0 1000
CLK3 CLK3 100.0 1000
CLK4 CLK4 72.4 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 99.1 1000
CSNK1A1L CSNK1A1L 91.1 1000
CSNK1D CSNK1D 98.9 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 100.0 1000
CSNK1G2 CSNK1G2 96.3 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 88.6 1000
CSNK2A2 CSNK2A2 77.1 1000
MATK CTK 100.0 1000
DAPK1 DAPK1 82.8 1000
DAPK2 DAPK2 99.6 1000
DAPK3 DAPK3 100.0 1000
DCLK1 DCAMKL1 81.5 1000
DCLK2 DCAMKL2 87.4 1000
DCLK3 DCAMKL3 100.0 1000
DDR1 DDR1 100.0 1000
DDR2 DDR2 99.1 1000
MAP3K12 DLK 89.9 1000
DMPK DMPK 100.0 1000
CDC42BPG DMPK2 94.4 1000
STK17A DRAK1 100.0 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 96.3 1000
DYRK1B DYRK1B 95.0 1000
DYRK2 DYRK2 82.9 1000
EGFR EGFR(T790M) 86.7 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 85.5 1000
EPHA2 EPHA2 97.8 1000
EPHA3 EPHA3 95.3 1000
EPHA4 EPHA4 95.7 1000
EPHA5 EPHA5 81.9 1000
EPHA6 EPHA6 100.0 1000
EPHA7 EPHA7 100.0 1000
EPHA8 EPHA8 99.9 1000
EPHB1 EPHB1 100.0 1000
EPHB2 EPHB2 73.0 1000
EPHB3 EPHB3 100.0 1000
EPHB4 EPHB4 98.5 1000
EPHB6 EPHB6 87.7 1000
ERBB2 ERBB2 92.1 1000
ERBB3 ERBB3 100.0 1000
ERBB4 ERBB4 95.0 1000
MAPK3 ERK1 100.0 1000
MAPK1 ERK2 82.1 1000
MAPK6 ERK3 96.5 1000
MAPK4 ERK4 100.0 1000
MAPK7 ERK5 100.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 100.0 1000
PTK2 FAK 100.0 1000
FER FER 100.0 1000
FES FES 100.0 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 83.2 1000
FGFR3 FGFR3(G697C) 94.0 1000
FGFR4 FGFR4 95.8 1000
FGR FGR 92.4 1000
FLT1 FLT1 100.0 1000
FLT3 FLT3-autoinhibited 97.4 1000
FLT4 FLT4 100.0 1000
FRK FRK 100.0 1000
FYN FYN 99.1 1000
GAK GAK 95.8 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 100.0 1000
GRK1 GRK1 100.0 1000
GRK2 GRK2 97.8 1000
GRK3 GRK3 87.6 1000
GRK4 GRK4 95.8 1000
GRK7 GRK7 90.8 1000
GSK3A GSK3A 79.9 1000
GSK3B GSK3B 100.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 82.8 1000
HIPK1 HIPK1 77.3 1000
HIPK2 HIPK2 97.1 1000
HIPK3 HIPK3 100.0 1000
HIPK4 HIPK4 100.0 1000
MAP4K1 HPK1 99.6 1000
HUNK HUNK 96.8 1000
CILK1 ICK 83.5 1000
IGF1R IGF1R 97.0 1000
CHUK IKK-alpha 100.0 1000
IKBKB IKK-beta 100.0 1000
IKBKE IKK-epsilon 89.7 1000
INSR INSR 89.0 1000
INSRR INSRR 93.2 1000
IRAK1 IRAK1 76.6 1000
IRAK3 IRAK3 85.0 1000
IRAK4 IRAK4 94.5 1000
ITK ITK 100.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 100.0 1000
JAK2 JAK2(JH1domain-catalytic) 91.0 1000
JAK3 JAK3(JH1domain-catalytic) 93.6 1000
MAPK8 JNK1 92.1 1000
MAPK9 JNK2 100.0 1000
MAPK10 JNK3 100.0 1000
KIT KIT-autoinhibited 94.9 1000
LATS1 LATS1 75.2 1000
LATS2 LATS2 100.0 1000
LCK LCK 99.1 1000
LIMK1 LIMK1 99.0 1000
LIMK2 LIMK2 86.8 1000
STK11 LKB1 82.2 1000
STK10 LOK 82.4 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 94.1 1000
LYN LYN 75.1 1000
MAP3K13 LZK 100.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 100.0 1000
MAP3K15 MAP3K15 99.0 1000
MAP3K2 MAP3K2 84.6 1000
MAP3K3 MAP3K3 100.0 1000
MAP3K4 MAP3K4 85.5 1000
MAP4K2 MAP4K2 100.0 1000
MAP4K3 MAP4K3 94.1 1000
MAP4K4 MAP4K4 88.9 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 84.2 1000
MAPKAPK5 MAPKAPK5 100.0 1000
MARK1 MARK1 88.7 1000
MARK2 MARK2 100.0 1000
MARK3 MARK3 93.7 1000
MARK4 MARK4 93.0 1000
MAST1 MAST1 100.0 1000
MAP2K1 MEK1 100.0 1000
MAP2K2 MEK2 98.0 1000
MAP2K3 MEK3 89.5 1000
MAP2K4 MEK4 93.3 1000
MAP2K5 MEK5 100.0 1000
MAP2K6 MEK6 90.8 1000
MELK MELK 100.0 1000
MERTK MERTK 100.0 1000
MET MET(Y1235D) 100.0 1000
MINK1 MINK 100.0 1000
MAP2K7 MKK7 88.6 1000
MKNK1 MKNK1 100.0 1000
MKNK2 MKNK2 96.5 1000
MYLK3 MLCK 100.0 1000
MAP3K9 MLK1 98.8 1000
MAP3K10 MLK2 65.4 1000
MAP3K11 MLK3 100.0 1000
CDC42BPA MRCKA 96.6 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 94.4 1000
MST1R MST1R 100.0 1000
STK3 MST2 100.0 1000
STK24 MST3 93.9 1000
STK26 MST4 100.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 78.7 1000
MYLK MYLK 84.4 1000
MYLK2 MYLK2 100.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 91.0 1000
STK38 NDR1 95.2 1000
STK38L NDR2 92.4 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 100.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 98.7 1000
NEK3 NEK3 72.9 1000
NEK4 NEK4 93.9 1000
NEK5 NEK5 87.9 1000
NEK6 NEK6 98.1 1000
NEK7 NEK7 86.6 1000
NEK9 NEK9 84.2 1000
MAP3K14 NIK 100.0 1000
NIM1K NIM1 100.0 1000
NLK NLK 100.0 1000
OXSR1 OSR1 94.0 1000
MAPK14 p38-alpha 81.3 1000
MAPK11 p38-beta 99.2 1000
MAPK13 p38-delta 100.0 1000
MAPK12 p38-gamma 100.0 1000
PAK1 PAK1 95.9 1000
PAK2 PAK2 83.5 1000
PAK3 PAK3 89.4 1000
PAK4 PAK4 90.2 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 96.6 1000
CDK16 PCTK1 100.0 1000
CDK17 PCTK2 93.3 1000
CDK18 PCTK3 92.4 1000
PDGFRA PDGFRA 100.0 1000
PDGFRB PDGFRB 99.0 1000
PDPK1 PDPK1 77.3 1000
CDPK1 PFCDPK1(P.falciparum) 86.9 1000
PK5 PFPK5(P.falciparum) 95.9 1000
CDK15 PFTAIRE2 93.8 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 97.5 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 73.6 1000
PIK3C2G PIK3C2G 80.3 1000
PIK3CA PIK3CA(Q546K) 100.0 1000
PIK3CB PIK3CB 100.0 1000
PIK3CD PIK3CD 87.0 1000
PIK3CG PIK3CG 90.8 1000
PI4KB PIK4CB 97.6 1000
PIKFYVE PIKFYVE 81.4 1000
PIM1 PIM1 91.7 1000
PIM2 PIM2 96.3 1000
PIM3 PIM3 81.5 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 100.0 1000
PIP4K2B PIP5K2B 59.8 1000
PIP4K2C PIP5K2C 80.7 1000
PRKACA PKAC-alpha 81.9 1000
PRKACB PKAC-beta 100.0 1000
PKMYT1 PKMYT1 100.0 1000
PKN1 PKN1 85.0 1000
PKN2 PKN2 100.0 1000
PKNB PKNB(M.tuberculosis) 92.8 1000
PLK1 PLK1 100.0 1000
PLK2 PLK2 98.4 1000
PLK3 PLK3 93.5 1000
PLK4 PLK4 84.1 1000
PRKCD PRKCD 98.2 1000
PRKCE PRKCE 100.0 1000
PRKCH PRKCH 0.0 1000
PRKCI PRKCI 100.0 1000
PRKCQ PRKCQ 78.6 1000
PRKD1 PRKD1 100.0 1000
PRKD2 PRKD2 90.6 1000
PRKD3 PRKD3 100.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 100.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 87.7 1000
PRPF4B PRP4 99.3 1000
PTK2B PYK2 93.4 1000
SIK3 QSK 74.8 1000
RAF1 RAF1 93.3 1000
RET RET(V804M) 82.4 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 83.2 1000
RIOK3 RIOK3 100.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 100.0 1000
RIPK4 RIPK4 77.2 1000
DSTYK RIPK5 99.7 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 100.0 1000
ROS1 ROS1 100.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 97.2 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 98.5 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 75.7 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 85.4 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 90.2 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 79.2 1000
RPS6KB1 S6K1 99.0 1000
SBK1 SBK1 90.6 1000
SGK1 SGK 77.6 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 78.5 1000
SGK3 SGK3 100.0 1000
SIK1 SIK 100.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 92.5 1000
NUAK2 SNARK 100.0 1000
SNRK SNRK 98.4 1000
SRC SRC 75.2 1000
SRMS SRMS 90.6 1000
SRPK1 SRPK1 62.5 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 100.0 1000
STK33 STK33 100.0 1000
STK35 STK35 100.0 1000
STK36 STK36 75.0 1000
STK39 STK39 100.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 84.7 1000
TAOK1 TAOK1 97.4 1000
TAOK2 TAOK2 95.4 1000
TAOK3 TAOK3 67.9 1000
TBK1 TBK1 100.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 94.3 1000
TGFBR1 TGFBR1 100.0 1000
TGFBR2 TGFBR2 98.6 1000
TIE1 TIE1 94.7 1000
TEK TIE2 100.0 1000
TLK1 TLK1 82.4 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 86.0 1000
TNK1 TNK1 100.0 1000
TNK2 TNK2 91.6 1000
TNNI3K TNNI3K 95.9 1000
NTRK1 TRKA 86.7 1000
NTRK2 TRKB 98.3 1000
NTRK3 TRKC 87.6 1000
TRPM6 TRPM6 90.4 1000
TSSK1B TSSK1B 100.0 1000
TSSK3 TSSK3 100.0 1000
TTK TTK 100.0 1000
TXK TXK 100.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 95.8 1000
TYRO3 TYRO3 97.1 1000
ULK1 ULK1 89.2 1000
ULK2 ULK2 89.2 1000
ULK3 ULK3 90.7 1000
KDR VEGFR2 88.1 1000
PIK3C3 VPS34 98.7 1000
VRK2 VRK2 95.4 1000
WEE1 WEE1 84.8 1000
WEE2 WEE2 89.1 1000
WNK1 WNK1 96.8 1000
WNK2 WNK2 99.3 1000
WNK3 WNK3 65.5 1000
WNK4 WNK4 100.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 98.4 1000
STK32C YANK3 100.0 1000
YES1 YES 95.3 1000
STK25 YSK1 88.1 1000
MAP3K19 YSK4 100.0 1000
MAP3K20 ZAK 91.3 1000
ZAP70 ZAP70 98.5 1000

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ABT-546

The screen was done at 10 µM compound. Results are expressed as percent inhibition of radioligand binding. Shown are data from PMID: 15087502 (Table 2) .

Conclusion: Clean panel; ABT-546 is specific for the ETA receptor.

Target protein HGNC name Species % inhibition at 10 µM
Adenosine A1 receptor (h) ADORA1 Homo sapiens 23.0
Adenosine A 2A receptor (h) ADORA2A Homo sapiens < 10.0
Adenosine A 3 receptor (h) ADORA3 Homo sapiens 32.0
alpha1-adrenoceptor (non-selective) < 10.0
alpha2-adrenoceptor (non-selective) 18.0
Vasopresine V1a receptor (h) AVPR1A Homo sapiens < 10.0
beta1-adrenoceptor (h) ADRB1 Homo sapiens < 10.0
beta2-adrenoceptor (h) ADRB2 Homo sapiens < 10.0
Norepinephrine uptake < 10.0
Angiotensin AT1 receptor (h) AGTR1 Homo sapiens < 10.0
Angiotensin AT2 receptor (h) AGTR2 Homo sapiens < 10.0
Benzodiazepine (central) < 10.0
Benzodiazepine (peripheral) < 10.0
Bombesin receptor < 10.0
Bradykinin B2 receptor (h) BDKRB2 Homo sapiens < 10.0
Calcitonin gene-related peptide < 10.0
Cannabinoid CB1 receptor (h) CNR1 Homo sapiens < 10.0
Cannabinoid CB2 receptor (h) CNR2 Homo sapiens 11.0
CholecystokininA receptor (h) CCKAR Homo sapiens < 10.0
CholecystokininB receptor (h) CCKBR Homo sapiens < 10.0
Dopamine D1 receptor (h) DRD1 Homo sapiens 14.0
Dopamine D2 receptor (h) DRD2 Homo sapiens < 10.0
Dopamine D3 receptor (h) DRD3 Homo sapiens < 10.0
Dopamine D4 receptor (h) DRD4 Homo sapiens < 10.0
Dopamine D5 receptor (h) DRD5 Homo sapiens < 10.0
Dopamine uptake (h) Homo sapiens < 10.0
Endothelin ETA receptor (h) EDNRA Homo sapiens 98.0
Endothelin ETB receptor (h) EDNRB Homo sapiens 56.0
GABA receptor (non-selective) < 10.0
Galanin receptor (h) Homo sapiens < 10.0
Platlet-derived growth factor receptor < 10.0
Interleukin-1beta IL1B < 10.0
Tumor necrosis factor-alpha TNF < 10.0
Histamine H1 receptor (central) HRH1 < 10.0
Histamine H2 receptor HRH2 < 10.0
Melatonin ML1 receptor MTNR1A 12.0
Muscarinic M1 receptors (h) CHRM1 Homo sapiens < 10.0
Muscarinic M2 receptors (h) CHRM2 Homo sapiens < 10.0
Muscarinic M3 receptors (h) CHRM3 Homo sapiens < 10.0
Muscarinic M4 receptors (h) CHRM4 Homo sapiens < 10.0
Muscarinic M5 receptors (h) CHRM5 Homo sapiens < 10.0
Neurokinin A receptor (h) TACR2 Homo sapiens < 10.0
NK3 tachykinin receptor (h) TACR3 Homo sapiens < 10.0
Neurokinin-1 receptor (h) TACR1 Homo sapiens < 10.0
Y1 receptor NPY1R < 10.0
Y2 receptor NPY2R < 10.0
Neurotensin receptor (h) Homo sapiens < 10.0
delta-Opioid receptor (h) OPRD1 Homo sapiens 62.0
kappa-Opioid receptor (h) OPRK1 Homo sapiens 28.0
mu-Opioid receptor (h) OPRM1 Homo sapiens 17.0
PCP receptor < 10.0
Thromboxane A2/ prostaglandin H2 receptors TBXA2R 16.0
Prostaglandin I2 receptor PTGIR 15.0
P2X-purinergic receptor 37.0
P2Y-purinergic receptor < 10.0
5-Hydroxytryptamine1A (h) HTR1A Homo sapiens < 10.0
5-Hydroxytryptamine1B HTR1B < 10.0
5-Hydroxytryptamine2A (h) HTR2A Homo sapiens < 10.0
5-Hydroxytryptamine2C (h) HTR2C Homo sapiens < 10.0
5-Hydroxytryptamine3 HTR3A < 10.0
5-Hydroxytryptamine5A (h) HTR5A Homo sapiens < 10.0
5-Hydroxytryptamine7 (h) HTR7 Homo sapiens < 10.0
5-Hydroxytryptamine6 (h) HTR6 Homo sapiens < 10.0
sigma-Receptor (non-selective) < 10.0
Somatostatin receptor < 10.0
Vasoactive intestinal peptide receptor < 10.0
Vasopresine V2 receptor AVPR2 < 10.0
Ca2+ channel (L, verapamil site) 29.0
K+ channel (volt-dependent) < 10.0
K+ channel (Ca2+-dependent) < 10.0
Na+ channel (site1) 22.0
Na+ channel (site 2) < 10.0
Cl- ionophore 61.0