Selectivity data for probe A-485 and control A-486


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A-485


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
GABAA/BZP 19.71
Beta2 ADRB2 19.04
GABAA 8.97
M3 CHRM3 9.06
M4 CHRM4 11.19
Alpha1A ADRA1A -11.26
Alpha1B ADRA1B 1.93
Alpha1D ADRA1D -1.58
D5 DRD5 21.10
5-HT1A HTR1A 6.87
5-HT1B HTR1B 9.82
5-HT1D HTR1D 17.98
5-HT1E HTR1E 4.23
5-HT5A HTR5A 5.99
5-HT6 HTR6 32.62
D2 DRD2 15.49
D3 DRD3 1.52
Sigma 1 SIGMAR1 34.47
Sigma 2 TMEM97 50.00 5525.39 average (n=2) 5.29
D1 DRD1 9.97
5-HT2B HTR2B 81.36 1292.04 average (n=2) 5.92
5-HT2C HTR2C 16.47
5-HT3 HTR3A -8.97
5-HT7A HTR7 7.83
Alpha2A ADRA2A 3.72
Alpha2B ADRA2B 26.47
Alpha2C ADRA2C 20.70
DAT SLC6A3 63.88 1817.04 average (n=2) 5.75
DOR OPRD1 -2.53
H1 HRH1 1.99
H3 HRH3 0.39
KOR OPRK1 18.54
M1 CHRM1 2.64
M2 CHRM2 -0.28
M5 CHRM5 2.39
MOR OPRM1 -13.26
NET SLC6A2 -3.76
GABA/PBR 59.96 1107.62 average (n=2) 5.96
SERT SLC6A4 95.58 223.27 average (n=2) 6.66
5-HT2A HTR2A 34.58
H2 HRH2 28.24
H4 HRH4 10.08
Beta1 ADRB1 -5.22
Beta3 ADRB3 -13.86
D4 DRD4 7.26

A-486


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
Beta2 ADRB2 24.67
GABAA 9.54
Beta1 ADRB1 -4.40
Beta3 ADRB3 -12.13
D4 DRD4 8.38
5-HT2A HTR2A 26.64
H2 HRH2 6.93
H4 HRH4 5.16
5-HT1A HTR1A 4.17
5-HT1B HTR1B 11.24
5-HT1E HTR1E 0.33
5-HT5A HTR5A 2.78
5-HT6 HTR6 24.11
D2 DRD2 -8.75
D3 DRD3 57.80 1136.58 average (n=2) 5.96
Sigma 1 SIGMAR1 17.67
Sigma 2 TMEM97 55.55 3272.55 average (n=2) 5.50
D1 DRD1 0.29
5-HT2B HTR2B 29.23
5-HT2C HTR2C -3.43
5-HT3 HTR3A -13.02
5-HT7A HTR7 -13.02
Alpha2A ADRA2A -1.40
Alpha2B ADRA2B 10.20
Alpha2C ADRA2C 8.88
DAT SLC6A3 -6.45
DOR OPRD1 -10.62
H1 HRH1 -7.68
H3 HRH3 13.21
KOR OPRK1 8.21
M1 CHRM1 5.42
M2 CHRM2 3.15
M5 CHRM5 -2.77
MOR OPRM1 -5.11
GABA/PBR 50.59 2577.30 average (n=2) 5.60
SERT SLC6A4 31.03
NET SLC6A2 -14.43
Alpha1A ADRA1A 0.04
Alpha1B ADRA1B -1.33
Alpha1D ADRA1D 9.73
D5 DRD5 20.52
M3 CHRM3 8.23
M4 CHRM4 30.37
5-HT1D HTR1D 2.22
GABAA/BZP 15.55

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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

A-485


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 1000
ABL1 ABL1-phosphorylated 72.0 1000
ABL2 ABL2 88.0 1000
ACVR1 ACVR1 85.0 1000
ACVR1B ACVR1B 86.0 1000
ACVR2A ACVR2A 85.0 1000
ACVR2B ACVR2B 96.0 1000
ACVRL1 ACVRL1 72.0 1000
COQ8A ADCK3 74.0 1000
COQ8B ADCK4 100.0 1000
AKT1 AKT1 91.0 1000
AKT2 AKT2 80.0 1000
AKT3 AKT3 100.0 1000
ALK ALK(L1196M) 75.0 1000
PRKAA1 AMPK-alpha1 100.0 1000
PRKAA2 AMPK-alpha2 99.0 1000
ANKK1 ANKK1 81.0 1000
NUAK1 ARK5 94.0 1000
MAP3K5 ASK1 94.0 1000
MAP3K6 ASK2 86.0 1000
AURKA AURKA 80.0 1000
AURKB AURKB 86.0 1000
AURKC AURKC 100.0 1000
AXL AXL 90.0 1000
BMP2K BIKE 98.0 1000
BLK BLK 100.0 1000
BMPR1A BMPR1A 91.0 1000
BMPR1B BMPR1B 82.0 1000
BMPR2 BMPR2 100.0 1000
BMX BMX 72.0 1000
BRAF BRAF(V600E) 100.0 1000
PTK6 BRK 87.0 1000
BRSK1 BRSK1 97.0 1000
BRSK2 BRSK2 70.0 1000
BTK BTK 87.0 1000
BUB1 BUB1 66.0 1000
CAMK1 CAMK1 95.0 1000
PNCK CAMK1B 100.0 1000
CAMK1D CAMK1D 94.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 91.0 1000
CAMK2B CAMK2B 81.0 1000
CAMK2D CAMK2D 91.0 1000
CAMK2G CAMK2G 76.0 1000
CAMK4 CAMK4 75.0 1000
CAMKK1 CAMKK1 70.0 1000
CAMKK2 CAMKK2 76.0 1000
CASK CASK 86.0 1000
CDK11B CDC2L1 84.0 1000
CDK11A CDC2L2 83.0 1000
CDK13 CDC2L5 96.0 1000
CDK19 CDK11 96.0 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 100.0 1000
CDK4 CDK4-cyclinD3 79.0 1000
CDK5 CDK5 84.0 1000
CDK7 CDK7 78.0 1000
CDK8 CDK8 100.0 1000
CDK9 CDK9 85.0 1000
CDKL1 CDKL1 86.0 1000
CDKL2 CDKL2 100.0 1000
CDKL3 CDKL3 85.0 1000
CDKL5 CDKL5 69.0 1000
CHEK1 CHEK1 98.0 1000
CHEK2 CHEK2 100.0 1000
CIT CIT 92.0 1000
CLK1 CLK1 69.0 1000
CLK2 CLK2 97.0 1000
CLK3 CLK3 83.0 1000
CLK4 CLK4 90.0 1000
CSF1R CSF1R-autoinhibited 90.0 1000
MARK3 MARK3 100.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 93.0 1000
CSNK1A1L CSNK1A1L 88.0 1000
CSNK1D CSNK1D 99.0 1000
CSNK1E CSNK1E 80.0 1000
CSNK1G1 CSNK1G1 94.0 1000
CSNK1G2 CSNK1G2 87.0 1000
CSNK1G3 CSNK1G3 84.0 1000
CSNK2A1 CSNK2A1 63.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 71.0 1000
DAPK1 DAPK1 96.0 1000
DAPK2 DAPK2 92.0 1000
DAPK3 DAPK3 86.0 1000
DCLK1 DCAMKL1 96.0 1000
DCLK2 DCAMKL2 70.0 1000
DCLK3 DCAMKL3 83.0 1000
DDR1 DDR1 100.0 1000
DDR2 DDR2 75.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 100.0 1000
CDC42BPG DMPK2 88.0 1000
STK17A DRAK1 100.0 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 64.0 1000
DYRK1B DYRK1B 81.0 1000
DYRK2 DYRK2 88.0 1000
EGFR EGFR(T790M) 73.0 1000
EIF2AK1 EIF2AK1 80.0 1000
EPHA1 EPHA1 88.0 1000
EPHA2 EPHA2 76.0 1000
EPHA3 EPHA3 100.0 1000
EPHA4 EPHA4 89.0 1000
EPHA5 EPHA5 96.0 1000
EPHA6 EPHA6 79.0 1000
EPHA7 EPHA7 88.0 1000
EPHA8 EPHA8 85.0 1000
EPHB1 EPHB1 97.0 1000
EPHB2 EPHB2 72.0 1000
EPHB3 EPHB3 80.0 1000
EPHB4 EPHB4 80.0 1000
EPHB6 EPHB6 96.0 1000
ERBB2 ERBB2 100.0 1000
ERBB3 ERBB3 89.0 1000
ERBB4 ERBB4 100.0 1000
MAPK3 ERK1 92.0 1000
MAPK1 ERK2 91.0 1000
MAPK6 ERK3 100.0 1000
MAPK4 ERK4 84.0 1000
MAPK7 ERK5 60.0 1000
MAPK15 ERK8 74.0 1000
ERN1 ERN1 56.0 1000
PTK2 FAK 94.0 1000
FER FER 87.0 1000
FES FES 94.0 1000
FGFR1 FGFR1 82.0 1000
FGFR2 FGFR2 88.0 1000
FGFR3 FGFR3(G697C) 79.0 1000
FGFR4 FGFR4 100.0 1000
FGR FGR 75.0 1000
FLT1 FLT1 100.0 1000
FLT3 FLT3-autoinhibited 85.0 1000
FLT4 FLT4 89.0 1000
FRK FRK 94.0 1000
FYN FYN 100.0 1000
GAK GAK 100.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 92.0 1000
GRK1 GRK1 82.0 1000
GRK2 GRK2 74.0 1000
GRK3 GRK3 100.0 1000
GRK4 GRK4 98.0 1000
GRK7 GRK7 83.0 1000
GSK3A GSK3A 99.0 1000
GSK3B GSK3B 82.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 99.0 1000
HIPK1 HIPK1 85.0 1000
HIPK2 HIPK2 95.0 1000
HIPK3 HIPK3 73.0 1000
HIPK4 HIPK4 97.0 1000
MAP4K1 HPK1 99.0 1000
HUNK HUNK 100.0 1000
CILK1 ICK 72.0 1000
IGF1R IGF1R 85.0 1000
CHUK IKK-alpha 92.0 1000
IKBKB IKK-beta 83.0 1000
IKBKE IKK-epsilon 51.0 1000
INSR INSR 81.0 1000
INSRR INSRR 96.0 1000
IRAK1 IRAK1 71.0 1000
IRAK3 IRAK3 95.0 1000
IRAK4 IRAK4 78.0 1000
ITK ITK 85.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 100.0 1000
JAK2 JAK2(JH1domain-catalytic) 83.0 1000
JAK3 JAK3(JH1domain-catalytic) 73.0 1000
MAPK8 JNK1 65.0 1000
MAPK9 JNK2 70.0 1000
MAPK10 JNK3 73.0 1000
KIT KIT-autoinhibited 97.0 1000
LATS1 LATS1 60.0 1000
LATS2 LATS2 47.0 1000
LCK LCK 84.0 1000
LIMK1 LIMK1 91.0 1000
LIMK2 LIMK2 88.0 1000
STK11 LKB1 100.0 1000
STK10 LOK 100.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 100.0 1000
LYN LYN 89.0 1000
MAP3K13 LZK 68.0 1000
MAK MAK 84.0 1000
MAP3K1 MAP3K1 68.0 1000
MAP3K15 MAP3K15 77.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 86.0 1000
MAP3K4 MAP3K4 89.0 1000
MAP4K2 MAP4K2 76.0 1000
MAP4K3 MAP4K3 76.0 1000
MAP4K4 MAP4K4 87.0 1000
MAP4K5 MAP4K5 88.0 1000
MAPKAPK2 MAPKAPK2 87.0 1000
MAPKAPK5 MAPKAPK5 82.0 1000
MARK1 MARK1 89.0 1000
MARK2 MARK2 100.0 1000
MARK4 MARK4 84.0 1000
MAST1 MAST1 94.0 1000
MAP2K1 MEK1 85.0 1000
MAP2K2 MEK2 96.0 1000
MAP2K3 MEK3 71.0 1000
MAP2K4 MEK4 100.0 1000
MAP2K5 MEK5 83.0 1000
MAP2K6 MEK6 100.0 1000
MELK MELK 91.0 1000
MERTK MERTK 82.0 1000
MET MET(Y1235D) 81.0 1000
MINK1 MINK 95.0 1000
MAP2K7 MKK7 97.0 1000
MKNK1 MKNK1 67.0 1000
MKNK2 MKNK2 82.0 1000
MYLK3 MLCK 90.0 1000
MAP3K9 MLK1 89.0 1000
MAP3K10 MLK2 57.0 1000
MAP3K11 MLK3 73.0 1000
CDC42BPA MRCKA 100.0 1000
CDC42BPB MRCKB 73.0 1000
STK4 MST1 100.0 1000
MST1R MST1R 77.0 1000
STK3 MST2 100.0 1000
STK24 MST3 90.0 1000
STK26 MST4 90.0 1000
MTOR MTOR 92.0 1000
MUSK MUSK 91.0 1000
MYLK MYLK 66.0 1000
MYLK2 MYLK2 84.0 1000
MYLK4 MYLK4 70.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 88.0 1000
STK38 NDR1 100.0 1000
STK38L NDR2 66.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 81.0 1000
NEK11 NEK11 91.0 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 58.0 1000
NEK4 NEK4 94.0 1000
NEK5 NEK5 100.0 1000
NEK6 NEK6 86.0 1000
NEK7 NEK7 91.0 1000
NEK9 NEK9 78.0 1000
MAP3K14 NIK 67.0 1000
NIM1K NIM1 71.0 1000
NLK NLK 82.0 1000
OXSR1 OSR1 80.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 85.0 1000
MAPK13 p38-delta 83.0 1000
MAPK12 p38-gamma 63.0 1000
PAK1 PAK1 88.0 1000
PAK2 PAK2 85.0 1000
PAK3 PAK3 91.0 1000
PAK4 PAK4 89.0 1000
PAK6 PAK6 91.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 75.0 1000
CDK17 PCTK2 96.0 1000
CDK18 PCTK3 85.0 1000
PDGFRA PDGFRA 93.0 1000
PDGFRB PDGFRB 100.0 1000
PDPK1 PDPK1 88.0 1000
CDPK1 PFCDPK1(P.falciparum) 83.0 1000
PK5 PFPK5(P.falciparum) 91.0 1000
CDK15 PFTAIRE2 85.0 1000
CDK14 PFTK1 79.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 97.0 1000
PIK3C2B PIK3C2B 100.0 1000
PIK3C2G PIK3C2G 75.0 1000
PIK3CA PIK3CA(Q546K) 79.0 1000
PIK3CB PIK3CB 94.0 1000
PIK3CD PIK3CD 92.0 1000
PIK3CG PIK3CG 95.0 1000
PI4KB PIK4CB 74.0 1000
PIKFYVE PIKFYVE 58.0 1000
PIM1 PIM1 100.0 1000
PIM2 PIM2 98.0 1000
PIM3 PIM3 97.0 1000
PIP5K1A PIP5K1A 95.0 1000
PIP5K1C PIP5K1C 100.0 1000
PIP4K2B PIP5K2B 69.0 1000
PIP4K2C PIP5K2C 93.0 1000
PRKACA PKAC-alpha 100.0 1000
PRKACB PKAC-beta 100.0 1000
PKMYT1 PKMYT1 74.0 1000
PKN1 PKN1 85.0 1000
PKN2 PKN2 97.0 1000
PKNB PKNB(M.tuberculosis) 83.0 1000
PLK1 PLK1 63.0 1000
PLK2 PLK2 91.0 1000
PLK3 PLK3 86.0 1000
PLK4 PLK4 100.0 1000
PRKCD PRKCD 76.0 1000
PRKCE PRKCE 22.0 1000
PRKCH PRKCH 93.0 1000
PRKCI PRKCI 85.0 1000
PRKCQ PRKCQ 71.0 1000
PRKD1 PRKD1 99.0 1000
PRKD2 PRKD2 100.0 1000
PRKD3 PRKD3 100.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 86.0 1000
EIF2AK2 PRKR 92.0 1000
PRKX PRKX 92.0 1000
PRPF4B PRP4 86.0 1000
PTK2B PYK2 73.0 1000
SIK3 QSK 94.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 98.0 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 67.0 1000
RIOK3 RIOK3 89.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 100.0 1000
RIPK4 RIPK4 56.0 1000
DSTYK RIPK5 78.0 1000
ROCK1 ROCK1 72.0 1000
ROCK2 ROCK2 96.0 1000
ROS1 ROS1 80.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 72.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 63.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 88.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 87.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 90.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 84.0 1000
RPS6KB1 S6K1 100.0 1000
SBK1 SBK1 79.0 1000
SGK1 SGK 63.0 1000
SBK3 SgK110 93.0 1000
SGK2 SGK2 100.0 1000
SGK3 SGK3 68.0 1000
SIK1 SIK 98.0 1000
SIK2 SIK2 88.0 1000
SLK SLK 82.0 1000
NUAK2 SNARK 74.0 1000
SNRK SNRK 96.0 1000
SRC SRC 91.0 1000
SRMS SRMS 83.0 1000
SRPK1 SRPK1 95.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 95.0 1000
STK16 STK16 84.0 1000
STK33 STK33 100.0 1000
STK35 STK35 89.0 1000
STK36 STK36 77.0 1000
STK39 STK39 100.0 1000
SYK SYK 70.0 1000
MAP3K7 TAK1 77.0 1000
TAOK1 TAOK1 94.0 1000
TAOK2 TAOK2 91.0 1000
TAOK3 TAOK3 74.0 1000
TBK1 TBK1 83.0 1000
TEC TEC 90.0 1000
TESK1 TESK1 73.0 1000
TGFBR1 TGFBR1 98.0 1000
TGFBR2 TGFBR2 90.0 1000
TIE1 TIE1 89.0 1000
TEK TIE2 87.0 1000
TLK1 TLK1 88.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 93.0 1000
TNK1 TNK1 86.0 1000
TNK2 TNK2 90.0 1000
TNNI3K TNNI3K 97.0 1000
NTRK1 TRKA 81.0 1000
NTRK2 TRKB 95.0 1000
NTRK3 TRKC 84.0 1000
TRPM6 TRPM6 100.0 1000
TSSK1B TSSK1B 84.0 1000
TSSK3 TSSK3 88.0 1000
TTK TTK 100.0 1000
TXK TXK 78.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 86.0 1000
TYRO3 TYRO3 81.0 1000
ULK1 ULK1 70.0 1000
ULK2 ULK2 82.0 1000
ULK3 ULK3 90.0 1000
KDR VEGFR2 83.0 1000
PIK3C3 VPS34 88.0 1000
VRK2 VRK2 91.0 1000
WEE1 WEE1 80.0 1000
WEE2 WEE2 75.0 1000
WNK1 WNK1 93.0 1000
WNK2 WNK2 100.0 1000
WNK3 WNK3 83.0 1000
WNK4 WNK4 73.0 1000
STK32A YANK1 88.0 1000
STK32B YANK2 90.0 1000
STK32C YANK3 88.0 1000
YES1 YES 76.0 1000
STK25 YSK1 99.0 1000
MAP3K19 YSK4 78.0 1000
MAP3K20 ZAK 82.0 1000
ZAP70 ZAP70 73.0 1000

A-486


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 1000
ABL1 ABL1-phosphorylated 84.0 1000
ABL2 ABL2 84.0 1000
ACVR1 ACVR1 89.0 1000
ACVR1B ACVR1B 100.0 1000
ACVR2A ACVR2A 100.0 1000
ACVR2B ACVR2B 100.0 1000
ACVRL1 ACVRL1 78.0 1000
COQ8A ADCK3 88.0 1000
COQ8B ADCK4 95.0 1000
AKT1 AKT1 77.0 1000
AKT2 AKT2 99.0 1000
AKT3 AKT3 94.0 1000
ALK ALK(L1196M) 88.0 1000
PRKAA1 AMPK-alpha1 91.0 1000
PRKAA2 AMPK-alpha2 57.0 1000
ANKK1 ANKK1 61.0 1000
NUAK1 ARK5 88.0 1000
MAP3K5 ASK1 100.0 1000
MAP3K6 ASK2 82.0 1000
AURKA AURKA 79.0 1000
AURKB AURKB 93.0 1000
AURKC AURKC 100.0 1000
AXL AXL 67.0 1000
BMP2K BIKE 100.0 1000
BLK BLK 100.0 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 100.0 1000
BMPR2 BMPR2 100.0 1000
BMX BMX 99.0 1000
BRAF BRAF(V600E) 96.0 1000
PTK6 BRK 90.0 1000
BRSK1 BRSK1 100.0 1000
BRSK2 BRSK2 90.0 1000
BTK BTK 97.0 1000
BUB1 BUB1 77.0 1000
CAMK1 CAMK1 100.0 1000
PNCK CAMK1B 90.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 100.0 1000
CAMK2B CAMK2B 100.0 1000
CAMK2D CAMK2D 100.0 1000
CAMK2G CAMK2G 98.0 1000
CAMK4 CAMK4 85.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 99.0 1000
CASK CASK 66.0 1000
CDK11B CDC2L1 97.0 1000
CDK11A CDC2L2 94.0 1000
CDK13 CDC2L5 92.0 1000
CDK19 CDK11 100.0 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 100.0 1000
CDK4 CDK4-cyclinD3 100.0 1000
CDK5 CDK5 79.0 1000
CDK7 CDK7 76.0 1000
CDK8 CDK8 96.0 1000
CDK9 CDK9 91.0 1000
CDKL1 CDKL1 91.0 1000
CDKL2 CDKL2 83.0 1000
CDKL3 CDKL3 92.0 1000
CDKL5 CDKL5 82.0 1000
CHEK1 CHEK1 100.0 1000
CHEK2 CHEK2 100.0 1000
CIT CIT 100.0 1000
CLK1 CLK1 82.0 1000
CLK2 CLK2 100.0 1000
CLK3 CLK3 84.0 1000
CLK4 CLK4 78.0 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 83.0 1000
CSNK1A1L CSNK1A1L 100.0 1000
CSNK1D CSNK1D 100.0 1000
CSNK1E CSNK1E 80.0 1000
CSNK1G1 CSNK1G1 78.0 1000
CSNK1G2 CSNK1G2 100.0 1000
CSNK1G3 CSNK1G3 89.0 1000
CSNK2A1 CSNK2A1 60.0 1000
CSNK2A2 CSNK2A2 90.0 1000
MATK CTK 100.0 1000
DAPK1 DAPK1 100.0 1000
DAPK2 DAPK2 100.0 1000
DAPK3 DAPK3 100.0 1000
DCLK1 DCAMKL1 76.0 1000
DCLK2 DCAMKL2 89.0 1000
DCLK3 DCAMKL3 81.0 1000
DDR1 DDR1 100.0 1000
DDR2 DDR2 100.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 92.0 1000
CDC42BPG DMPK2 88.0 1000
STK17A DRAK1 88.0 1000
STK17B DRAK2 77.0 1000
DYRK1A DYRK1A 77.0 1000
DYRK1B DYRK1B 100.0 1000
DYRK2 DYRK2 92.0 1000
EGFR EGFR(T790M) 73.0 1000
EIF2AK1 EIF2AK1 96.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 100.0 1000
EPHA3 EPHA3 100.0 1000
EPHA4 EPHA4 86.0 1000
EPHA5 EPHA5 94.0 1000
EPHA6 EPHA6 91.0 1000
EPHA7 EPHA7 100.0 1000
EPHA8 EPHA8 96.0 1000
EPHB1 EPHB1 100.0 1000
EPHB2 EPHB2 87.0 1000
EPHB3 EPHB3 86.0 1000
EPHB4 EPHB4 91.0 1000
EPHB6 EPHB6 0.0 1000
ERBB2 ERBB2 98.0 1000
ERBB3 ERBB3 81.0 1000
ERBB4 ERBB4 100.0 1000
MAPK3 ERK1 100.0 1000
MAPK1 ERK2 91.0 1000
MAPK6 ERK3 97.0 1000
MAPK4 ERK4 98.0 1000
MAPK7 ERK5 85.0 1000
MAPK15 ERK8 93.0 1000
ERN1 ERN1 100.0 1000
PTK2 FAK 100.0 1000
FER FER 79.0 1000
FES FES 85.0 1000
FGFR1 FGFR1 84.0 1000
FGFR2 FGFR2 87.0 1000
FGFR3 FGFR3(G697C) 96.0 1000
FGFR4 FGFR4 98.0 1000
FGR FGR 88.0 1000
FLT1 FLT1 100.0 1000
FLT3 FLT3-autoinhibited 92.0 1000
FLT4 FLT4 100.0 1000
FRK FRK 95.0 1000
FYN FYN 79.0 1000
GAK GAK 100.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 100.0 1000
GRK1 GRK1 73.0 1000
GRK2 GRK2 76.0 1000
GRK3 GRK3 100.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 85.0 1000
GSK3A GSK3A 92.0 1000
GSK3B GSK3B 95.0 1000
HASPIN HASPIN 83.0 1000
HCK HCK 100.0 1000
HIPK1 HIPK1 78.0 1000
HIPK2 HIPK2 78.0 1000
HIPK3 HIPK3 90.0 1000
HIPK4 HIPK4 100.0 1000
MAP4K1 HPK1 90.0 1000
HUNK HUNK 100.0 1000
CILK1 ICK 67.0 1000
IGF1R IGF1R 100.0 1000
CHUK IKK-alpha 100.0 1000
IKBKB IKK-beta 92.0 1000
IKBKE IKK-epsilon 75.0 1000
INSR INSR 73.0 1000
INSRR INSRR 100.0 1000
IRAK1 IRAK1 88.0 1000
IRAK3 IRAK3 100.0 1000
IRAK4 IRAK4 94.0 1000
ITK ITK 92.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 85.0 1000
JAK2 JAK2(JH1domain-catalytic) 100.0 1000
JAK3 JAK3(JH1domain-catalytic) 91.0 1000
MAPK8 JNK1 71.0 1000
MAPK9 JNK2 69.0 1000
MAPK10 JNK3 67.0 1000
KIT KIT-autoinhibited 89.0 1000
LATS1 LATS1 59.0 1000
LATS2 LATS2 68.0 1000
LCK LCK 86.0 1000
LIMK1 LIMK1 87.0 1000
LIMK2 LIMK2 90.0 1000
STK11 LKB1 100.0 1000
STK10 LOK 92.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 100.0 1000
LYN LYN 100.0 1000
MAP3K13 LZK 100.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 95.0 1000
MAP3K15 MAP3K15 90.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 75.0 1000
MAP3K4 MAP3K4 87.0 1000
MAP4K2 MAP4K2 92.0 1000
MAP4K3 MAP4K3 89.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 100.0 1000
MAPKAPK5 MAPKAPK5 86.0 1000
MARK1 MARK1 100.0 1000
MARK2 MARK2 100.0 1000
MARK3 MARK3 100.0 1000
MARK4 MARK4 92.0 1000
MAST1 MAST1 85.0 1000
MAP2K1 MEK1 98.0 1000
MAP2K2 MEK2 99.0 1000
MAP2K3 MEK3 87.0 1000
MAP2K4 MEK4 95.0 1000
MAP2K5 MEK5 89.0 1000
MAP2K6 MEK6 100.0 1000
MELK MELK 100.0 1000
MERTK MERTK 100.0 1000
MET MET(Y1235D) 93.0 1000
MINK1 MINK 78.0 1000
MAP2K7 MKK7 85.0 1000
MKNK1 MKNK1 94.0 1000
MKNK2 MKNK2 76.0 1000
MYLK3 MLCK 85.0 1000
MAP3K9 MLK1 100.0 1000
MAP3K10 MLK2 73.0 1000
MAP3K11 MLK3 91.0 1000
CDC42BPA MRCKA 98.0 1000
CDC42BPB MRCKB 80.0 1000
STK4 MST1 100.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 97.0 1000
STK24 MST3 100.0 1000
STK26 MST4 100.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 100.0 1000
MYLK MYLK 88.0 1000
MYLK2 MYLK2 77.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 79.0 1000
STK38L NDR2 67.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 91.0 1000
NEK11 NEK11 84.0 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 69.0 1000
NEK4 NEK4 100.0 1000
NEK5 NEK5 95.0 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 100.0 1000
NEK9 NEK9 95.0 1000
MAP3K14 NIK 68.0 1000
NIM1K NIM1 76.0 1000
NLK NLK 77.0 1000
OXSR1 OSR1 65.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 100.0 1000
MAPK13 p38-delta 97.0 1000
MAPK12 p38-gamma 96.0 1000
PAK1 PAK1 98.0 1000
PAK2 PAK2 94.0 1000
PAK3 PAK3 91.0 1000
PAK4 PAK4 95.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 83.0 1000
CDK17 PCTK2 88.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 83.0 1000
PDGFRB PDGFRB 87.0 1000
PDPK1 PDPK1 85.0 1000
CDPK1 PFCDPK1(P.falciparum) 93.0 1000
PK5 PFPK5(P.falciparum) 95.0 1000
CDK15 PFTAIRE2 100.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 99.0 1000
PIK3C2G PIK3C2G 97.0 1000
PIK3CA PIK3CA(Q546K) 81.0 1000
PIK3CB PIK3CB 97.0 1000
PIK3CD PIK3CD 100.0 1000
PIK3CG PIK3CG 64.0 1000
PI4KB PIK4CB 71.0 1000
PIKFYVE PIKFYVE 72.0 1000
PIM1 PIM1 100.0 1000
PIM2 PIM2 89.0 1000
PIM3 PIM3 89.0 1000
PIP5K1A PIP5K1A 89.0 1000
PIP5K1C PIP5K1C 100.0 1000
PIP4K2B PIP5K2B 60.0 1000
PIP4K2C PIP5K2C 100.0 1000
PRKACA PKAC-alpha 99.0 1000
PRKACB PKAC-beta 100.0 1000
PKMYT1 PKMYT1 92.0 1000
PKN1 PKN1 98.0 1000
PKN2 PKN2 100.0 1000
PKNB PKNB(M.tuberculosis) 84.0 1000
PLK1 PLK1 82.0 1000
PLK2 PLK2 92.0 1000
PLK3 PLK3 84.0 1000
PLK4 PLK4 100.0 1000
PRKCD PRKCD 75.0 1000
PRKCE PRKCE 99.0 1000
PRKCH PRKCH 87.0 1000
PRKCI PRKCI 91.0 1000
PRKCQ PRKCQ 89.0 1000
PRKD1 PRKD1 100.0 1000
PRKD2 PRKD2 100.0 1000
PRKD3 PRKD3 100.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 85.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 100.0 1000
PRPF4B PRP4 90.0 1000
PTK2B PYK2 83.0 1000
SIK3 QSK 100.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 83.0 1000
RIOK3 RIOK3 100.0 1000
RIPK1 RIPK1 93.0 1000
RIPK2 RIPK2 83.0 1000
RIPK4 RIPK4 52.0 1000
DSTYK RIPK5 89.0 1000
ROCK1 ROCK1 81.0 1000
ROCK2 ROCK2 95.0 1000
ROS1 ROS1 87.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 88.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 72.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 84.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KB1 S6K1 100.0 1000
SBK1 SBK1 75.0 1000
SGK1 SGK 54.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 88.0 1000
SGK3 SGK3 72.0 1000
SIK1 SIK 90.0 1000
SIK2 SIK2 88.0 1000
SLK SLK 83.0 1000
NUAK2 SNARK 77.0 1000
SNRK SNRK 100.0 1000
SRC SRC 90.0 1000
SRMS SRMS 88.0 1000
SRPK1 SRPK1 100.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 99.0 1000
STK33 STK33 100.0 1000
STK35 STK35 85.0 1000
STK36 STK36 100.0 1000
STK39 STK39 100.0 1000
SYK SYK 82.0 1000
MAP3K7 TAK1 81.0 1000
TAOK1 TAOK1 97.0 1000
TAOK2 TAOK2 95.0 1000
TAOK3 TAOK3 82.0 1000
TBK1 TBK1 84.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 100.0 1000
TGFBR1 TGFBR1 89.0 1000
TGFBR2 TGFBR2 95.0 1000
TIE1 TIE1 100.0 1000
TEK TIE2 100.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 87.0 1000
TNK1 TNK1 100.0 1000
TNK2 TNK2 87.0 1000
TNNI3K TNNI3K 98.0 1000
NTRK1 TRKA 41.0 1000
NTRK2 TRKB 89.0 1000
NTRK3 TRKC 82.0 1000
TRPM6 TRPM6 98.0 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) 68.0 1000
TYRO3 TYRO3 70.0 1000
ULK1 ULK1 64.0 1000
ULK2 ULK2 100.0 1000
ULK3 ULK3 55.0 1000
KDR VEGFR2 84.0 1000
PIK3C3 VPS34 96.0 1000
VRK2 VRK2 97.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 79.0 1000
WNK2 WNK2 59.0 1000
WNK3 WNK3 63.0 1000
WNK4 WNK4 100.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 67.0 1000
STK32C YANK3 100.0 1000
YES1 YES 85.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 73.0 1000
MAP3K20 ZAK 93.0 1000
ZAP70 ZAP70 100.0 1000

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A-485

Ligand profiling has been performed at 10 µM probe concentration. Shown are supplementary data from PMID: 28953875 .

Conclusion: A-485 displays substantial binding (>90%) to dopamine and serotonin transporters at 10 μM.

Target protein HGNC name Species % inhibition at 10 µM Mode of action
5-HT transporter (h) SLC6A4 Homo sapiens 99.0 antagonist
dopamine transporter (h) SLC6A3 Homo sapiens 94.0 antagonist
5-HT2B (h) HTR2B Homo sapiens 73.0 agonist
BZD (peripheral) 72.0 antagonist
CB2 (h) CNR2 Homo sapiens 67.0 agonist
Cl- channel (GABA-gated) 47.0 antagonist
A3 (h) ADORA3 Homo sapiens 40.0 agonist
alpha 1A (h) ADRA1A Homo sapiens 29.0 antagonist
kappa (KOP) OPRK1 28.0 agonist
MAO-A MAOA 28.0 antagonist
EP2 (h) PTGER2 Homo sapiens 27.0 agonist
CB1 (h) CNR1 Homo sapiens 25.0 agonist
KATP channel 24.0 antagonist
H1 (h) HRH1 Homo sapiens 22.0 antagonist
NK1 (h) TACR1 Homo sapiens 21.0 agonist
Na+ channel (site 2) 19.0 antagonist
AT1 (h) AGTR1 Homo sapiens 18.0 antagonist
NK2 (h) TACR2 Homo sapiens 18.0 agonist
beta 1 (h) ADRB1 Homo sapiens 17.0 agonist
5-HT7 (h) HTR7 Homo sapiens 16.0 agonist
5-HT1A (h) HTR1A Homo sapiens 15.0 agonist
PCP PRCP 15.0 antagonist
5-HT2A (h) HTR2A Homo sapiens 14.0 antagonist
M4 (h) CHRM4 Homo sapiens 14.0 antagonist
D2S (h) DRD2 Homo sapiens 13.0 antagonist
GR (h) NR3C1 Homo sapiens 13.0 agonist
AT2 (h) AGTR2 Homo sapiens 12.0 agonist
MT2 (ML1B) (h) MTNR1B Homo sapiens 12.0 agonist
mu (MOP) (h) OPRM1 Homo sapiens 12.0 agonist
norepinephrine transporter (h) SLC6A2 Homo sapiens 12.0 antagonist
P2X 12.0 agonist
alpha 2A (h) ADRA2A Homo sapiens 11.0 antagonist
delta (DOP) (h) OPRD1 Homo sapiens 11.0 agonist
5-HT4e (h) HTR4 Homo sapiens 10.0 antagonist
PPARgamma (h) PPARG Homo sapiens 10.0 agonist
V1a (h) AVPR1A Homo sapiens 10.0 agonist
A1 (h) ADORA1 Homo sapiens 9.0 antagonist
beta 2 (h) ADRB2 Homo sapiens 8.0 agonist
M5 (h) CHRM5 Homo sapiens 8.0 antagonist
A2A (h) ADORA2A Homo sapiens 7.0 agonist
UT (h) UTS2R Homo sapiens 6.0 agonist
Estrogen ER alpha (h) ESR1 Homo sapiens 5.0 agonist
alpha 1B (h) ADRA1B Homo sapiens 4.0 antagonist
NMDA 4.0 antagonist
ETA (h) EDNRA Homo sapiens 3.0 agonist
Ca2+ channel (L, diltiazem site) (benzothiazepines) 2.0 antagonist
SKCa channel 2.0 antagonist
TNF-alpha (h) TNF Homo sapiens 1.0 agonist
5-HT3 (h) HTR3A Homo sapiens 0.0 antagonist
B2 (h) BDKRB2 Homo sapiens 0.0 agonist
CGRP (h) CALCA Homo sapiens 0.0 agonist
5-HT2C (h) HTR2C Homo sapiens -2.0 antagonist
M1 (h) CHRM1 Homo sapiens -2.0 antagonist
sigma (non-selective) (h) Homo sapiens -3.0 agonist
alpha 2B (h) ADRA2B Homo sapiens -4.0 antagonist
AR (h) AR Homo sapiens -4.0 agonist
D1 (h) DRD1 Homo sapiens -4.0 antagonist
motilin (h) MLNR Homo sapiens -4.0 agonist
M2 (h) CHRM2 Homo sapiens -5.0 antagonist
M3 (h) CHRM3 Homo sapiens -5.0 antagonist
VPAC1 (VIP1) (h) VIPR1 Homo sapiens -5.0 agonist
5-HT1B HTR1B -6.0 antagonist
Ca2+ channel (L, dihydropyridine site) -9.0 antagonist
H2 (h) HRH2 Homo sapiens -9.0 antagonist
BZD (central) -11.0 agonist
Y1 (h) NPY1R Homo sapiens -16.0 agonist
ETB (h) EDNRB Homo sapiens -19.0 agonist
CCK1 (CCKA) (h) CCKAR Homo sapiens -22.0 agonist
A2B (h) ADORA2B Homo sapiens -30.0 antagonist
GABAA1 (h) (alpha 1, beta2, gamma 2) Homo sapiens -31.0 agonist
COX2(h) PTGS2 Homo sapiens 11.0
acetylcholinesterase (h) ACHE Homo sapiens -1.0
ATPase (Na+/K+) -1.0
ACE (h) ACE Homo sapiens -13.0
COX1(h) PTGS1 Homo sapiens -16.0
MAO-B (h) recombinant enzyme MAOB Homo sapiens -20.0
PDE3A (h) PDE3A Homo sapiens -34.0
MYST3 (HAT) KAT6A 5.6
MYST4 (HAT) KAT6B 1.4
PCAF (HAT) KAT2B 1.0
HAT1 (HAT) HAT1 -1.9
TIP60 (HAT) TIP60 -1.9
GCN5L2 (HAT) KAT2A -31.2
 

A-486

Conclusion: Clean panel.

Target protein HGNC name Species % inhibition at 10 µM Mode of action
5-HT transporter (h) SLC6A4 Homo sapiens 40.0 antagonist
dopamine transporter (h) SLC6A3 Homo sapiens 27.0 antagonist
5-HT2B (h) HTR2B Homo sapiens 5.0 agonist
CB2 (h) CNR2 Homo sapiens 4.0 agonist
Cl- channel (GABA-gated) 41.0 antagonist
alpha 1A (h) ADRA1A Homo sapiens 16.0 antagonist
kappa (KOP) OPRK1 12.0 agonist
MAO-A MAOA 7.0 antagonist
EP2 (h) PTGER2 Homo sapiens 10.0 agonist
CB1 (h) CNR1 Homo sapiens 22.0 agonist
KATP channel 19.0 antagonist
H1 (h) HRH1 Homo sapiens 7.0 antagonist
NK1 (h) TACR1 Homo sapiens 12.0 agonist
Na+ channel (site 2) -5.0 antagonist
AT1 (h) AGTR1 Homo sapiens 17.0 antagonist
NK2 (h) TACR2 Homo sapiens 12.0 agonist
beta 1 (h) ADRB1 Homo sapiens 6.0 agonist
5-HT7 (h) HTR7 Homo sapiens 6.0 agonist
5-HT1A (h) HTR1A Homo sapiens 8.0 agonist
PCP PRCP -17.0 antagonist
5-HT2A (h) HTR2A Homo sapiens 8.0 antagonist
M4 (h) CHRM4 Homo sapiens 6.0 antagonist
D2S (h) DRD2 Homo sapiens -3.0 antagonist
GR (h) NR3C1 Homo sapiens 16.0 agonist
AT2 (h) AGTR2 Homo sapiens 2.0 agonist
MT2 (ML1B) (h) MTNR1B Homo sapiens 8.0 agonist
mu (MOP) (h) OPRM1 Homo sapiens 7.0 agonist
norepinephrine transporter (h) SLC6A2 Homo sapiens 4.0 antagonist
P2X -5.0 agonist
alpha 2A (h) ADRA2A Homo sapiens -7.0 antagonist
delta (DOP) (h) OPRD1 Homo sapiens 1.0 agonist
5-HT4e (h) HTR4 Homo sapiens 9.0 antagonist
PPARgamma (h) PPARG Homo sapiens 1.0 agonist
V1a (h) AVPR1A Homo sapiens 23.0 agonist
A1 (h) ADORA1 Homo sapiens -16.0 antagonist
beta 2 (h) ADORA3 Homo sapiens 1.0 agonist
M5 (h) CHRM5 Homo sapiens -8.0 antagonist
A2A (h) ADORA2A Homo sapiens -1.0 agonist
UT (h) UTS2R Homo sapiens 21.0 agonist
Estrogen ER alpha (h) ESR1 Homo sapiens -10.0 agonist
alpha 1B (h) ADRA1B Homo sapiens -6.0 antagonist
NMDA Homo sapiens 2.0 antagonist
ETA (h) EDNRA Homo sapiens -1.0 agonist
Ca2+ channel (L, diltiazem site) (benzothiazepines) Homo sapiens -5.0 antagonist
SKCa channel -7.0 antagonist
TNF-alpha (h) TNF Homo sapiens 1.0 agonist
5-HT3 (h) HTR3A Homo sapiens 4.0 antagonist
B2 (h) BDKRB2 Homo sapiens -12.0 agonist
5-HT2C (h) HTR2C Homo sapiens -7.0 antagonist
M1 (h) CHRM1 Homo sapiens -8.0 antagonist
sigma (non-selective) (h) Homo sapiens 7.0 agonist
alpha 2B (h) ADRA2B Homo sapiens 4.0 antagonist
AR (h) AR Homo sapiens 4.0 agonist
D1 (h) DRD1 Homo sapiens -5.0 antagonist
motilin (h) MLNR Homo sapiens 41.0 agonist
M2 (h) CHRM2 Homo sapiens -8.0 antagonist
M3 (h) CHRM3 Homo sapiens 0.0 antagonist
VPAC1 (VIP1) (h) VIPR1 Homo sapiens -8.0 agonist
5-HT1B HTR1B -9.0 antagonist
Ca2+ channel (L, dihydropyridine site) -3.0 antagonist
H2 (h) HRH2 Homo sapiens 6.0 antagonist
BZD (central) -17.0 agonist
Y1 (h) NPY1R Homo sapiens -10.0 agonist
ETB (h) EDNRB Homo sapiens 8.0 agonist
CCK1 (CCKA) (h) CCKAR Homo sapiens 1.0 agonist
A2B (h) ADORA2B Homo sapiens 1.0 antagonist
GABAA1 (h) (alpha 1,beta 2,gamma 2) Homo sapiens 0.0 agonist
Calcitonin Gene-Related Peptide CGRP1 CALCA -10.0
COX2(h) PTGS2 Homo sapiens -37.0
acetylcholinesterase (h) ACHE Homo sapiens 8.0
ATPase (Na+/K+) -1.0
ACE (h) ACE Homo sapiens -26.0
COX1(h) PTGS1 Homo sapiens -5.0
MAO-B (h) recombinant enzyme MAOB Homo sapiens 0.0
PDE3A (h) PDE3A Homo sapiens -1.0

A-485

EC50 values are determined for the proliferation inhibition of cancer cell lines. Shown are supplementary data from PMID: 28953875 . Abbreviations of the tumor types:

  • NSCLC: non small cell lung cancer
  • SCLC: small cell lung cancer
  • TNBC: triple negative breast cancer
  • MCL: mantle cell lymphoma
  • MM: multiple myeloma
  • NHL: non hodgkin's lymphoma
  • AML: acute myeloid leukemia
  • Misc: miscellaneous

Conclusion: A-485 inhibits most MM cell lines and some of the AML and NHLcell lines. It is less sensitive to solid tumor lines such as melanoma, SCLC and TNBC.

Tumor type Cell line Species Cell Proliferation EC50 [µM] Time [day]
NSCLC H23 Homo sapiens 1.79 3
NSCLC H1373 Homo sapiens 2.34 3
NSCLC H1693 Homo sapiens 2.37 3
NSCLC H522 Homo sapiens 3.52 3
NSCLC HCC4006 Homo sapiens 4.64 3
NSCLC H2444 Homo sapiens 5.92 3
NSCLC H727 Homo sapiens 6.63 3
NSCLC H838 Homo sapiens 6.99 3
NSCLC H661 Homo sapiens 7.66 3
NSCLC Calu 6 Homo sapiens 8.57 3
NSCLC H441 Homo sapiens 10.00 3
NSCLC H596 Homo sapiens 10.00 3
NSCLC HCC2935 Homo sapiens 10.00 3
Prostate VCaP Homo sapiens 0.04 5
Prostate LnCaP -FGC Homo sapiens 0.26 5
Prostate 22Rv1 Homo sapiens 0.32 5
Prostate PC-3 Homo sapiens 2.05 5
Prostate DU-145 Homo sapiens 10.00 5
Melanoma CHL1 Homo sapiens 0.37 5
Melanoma SKMEL1 Homo sapiens 0.57 5
Melanoma SKMEL5 Homo sapiens 0.91 5
Melanoma WM2664 Homo sapiens 1.91 5
Melanoma Colo679 Homo sapiens 2.26 5
Melanoma MeWo Homo sapiens 2.43 5
Melanoma Malme3M Homo sapiens 2.69 5
Melanoma HT-144 Homo sapiens 3.08 5
Melanoma Hs695T Homo sapiens 3.57 5
Melanoma G361 Homo sapiens 3.77 5
Melanoma Hs294T Homo sapiens 9.00 5
Melanoma A375 Homo sapiens 10.00 5
Melanoma SKMEL24 Homo sapiens 10.00 5
Melanoma SKMEL2 Homo sapiens 10.00 5
SCLC H146 Homo sapiens 0.40 4
SCLC H209 Homo sapiens 0.40 4
SCLC H211 Homo sapiens 1.50 4
SCLC H69 Homo sapiens 10.00 4
SCLC H1048 Homo sapiens 10.00 4
SCLC H510A Homo sapiens 10.00 4
SCLC H1836 Homo sapiens 10.00 4
SCLC H1417 Homo sapiens 10.00 4
SCLC H128 Homo sapiens 10.00 4
SCLC H187 Homo sapiens 10.00 4
SCLC H1930 Homo sapiens 10.00 4
SCLC H2081 Homo sapiens 10.00 4
SCLC Cor-L47 Homo sapiens 10.00 4
TNBC BT-20 Homo sapiens 0.34 5
TNBC MDA_MB_468 Homo sapiens 0.38 5
TNBC EMT6 (mouse) Mus musculus 0.50 5
TNBC DU4475 Homo sapiens 0.67 5
TNBC MDA_MB_453 Homo sapiens 1.87 5
TNBC HCC1806 Homo sapiens 2.95 5
TNBC MDA_MB_157 Homo sapiens 4.59 5
TNBC HCC1599 Homo sapiens 4.85 5
TNBC HCC1143 Homo sapiens 10.00 5
TNBC HCC1937 Homo sapiens 10.00 5
TNBC MDA_MB_436 Homo sapiens 10.00 5
TNBC HCC1395 Homo sapiens 10.00 5
TNBC MDA_MB_231 Homo sapiens 10.00 5
TNBC CAL_120 Homo sapiens 10.00 5
TNBC 4T1 (mouse) Mus musculus 10.00 5
TNBC HCC70 Homo sapiens 10.00 5
TNBC HCC38 Homo sapiens 10.00 5
TNBC HCC1187 Homo sapiens 10.00 5
MCL Granta 519 Homo sapiens 3.28 3
MCL JVM-2 Homo sapiens 10.00 3
MM RPMI-8226 Homo sapiens 0.16 3
MM MM1.s Homo sapiens 0.18 3
MM KMS-11 Homo sapiens 0.24 3
MM H929 Homo sapiens 0.33 3
MM L-363 Homo sapiens 0.51 3
MM OPM-2 Homo sapiens 0.62 3
MM AMO-1 Homo sapiens 1.09 3
NHL Karpas422 Homo sapiens 0.25 3
NHL BJAB Homo sapiens 0.28 3
NHL OCI Ly18 Homo sapiens 0.32 3
NHL K1106 Homo sapiens 0.41 3
NHL Daudi Homo sapiens 0.43 3
NHL Raji Homo sapiens 0.46 3
NHL NuDUL1 Homo sapiens 0.48 3
NHL CA46 Homo sapiens 0.48 3
NHL Toledo Homo sapiens 0.49 3
NHL OCI Ly3 Homo sapiens 0.49 3
NHL NuDHL1 Homo sapiens 0.53 3
NHL Mino Homo sapiens 0.53 3
NHL SuDHL8 Homo sapiens 0.54 3
NHL ULA Homo sapiens 0.55 3
NHL RCK8 Homo sapiens 0.59 3
NHL U2973 Homo sapiens 0.66 3
NHL SuDHL4 Homo sapiens 0.72 3
NHL SuDHL16 Homo sapiens 0.73 3
NHL SuDHL6 Homo sapiens 0.75 3
NHL DoHH2 Homo sapiens 0.75 3
NHL SuDHL5 Homo sapiens 0.76 3
NHL DB Homo sapiens 0.77 3
NHL Pfeiffer Homo sapiens 0.86 3
NHL SuDHL10 Homo sapiens 0.92 3
NHL Ramos Homo sapiens 0.93 3
NHL OCI Ly1 Homo sapiens 0.94 3
NHL SuDHL2 Homo sapiens 0.95 3
NHL RL Homo sapiens 1.05 3
NHL GA10 Homo sapiens 1.06 3
NHL WSU-NHL Homo sapiens 1.06 3
NHL U2940 Homo sapiens 1.33 3
NHL Sc1 Homo sapiens 1.69 3
NHL OCI Ly7 Homo sapiens 1.81 3
NHL U2932 Homo sapiens 2.46 3
NHL REC1 Homo sapiens 10.00 3
NHL Farage Homo sapiens 10.00 3
NHL HT Homo sapiens 10.00 3
AML Kasumi-1 Homo sapiens 0.29 3
AML MOLM-13 Homo sapiens 0.35 3
AML SKM-1 Homo sapiens 1.34 3
AML SET-2 Homo sapiens 2.01 3
AML OCI-AML2 Homo sapiens 2.03 3
AML HEL Homo sapiens 3.09 3
AML THP-1 Homo sapiens 3.51 3
AML OCI-AML5 Homo sapiens 4.86 3
AML HL-60 Homo sapiens 10.00 3
AML EOL-1 Homo sapiens 10.00 3
AML U937 Homo sapiens 10.00 3
Misc K562 Homo sapiens 1.27 3
Misc Jurkat Homo sapiens 4.03 3
Misc MOLT-4 Homo sapiens 10.00 3
Misc KARPAS-299 Homo sapiens 10.00 3