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Selectivity data for probe JNJ-54082730 and control JNJ-54103985


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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.
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Jump to control KinomeScan data

JNJ-54082730


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 90.0 1000
ABL1 ABL1-phosphorylated 99.0 1000
ABL2 ABL2 95.0 1000
ACVR1 ACVR1 100.0 1000
ACVR1B ACVR1B 100.0 1000
ACVR2A ACVR2A 94.0 1000
ACVR2B ACVR2B 96.0 1000
ACVRL1 ACVRL1 98.0 1000
COQ8A ADCK3 89.0 1000
COQ8B ADCK4 90.0 1000
AKT1 AKT1 96.0 1000
AKT2 AKT2 100.0 1000
AKT3 AKT3 80.0 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 98.0 1000
MAP3K5 ASK1 100.0 1000
MAP3K6 ASK2 100.0 1000
AURKA AURKA 100.0 1000
AURKB AURKB 100.0 1000
AURKC AURKC 100.0 1000
AXL AXL 89.0 1000
BMP2K BIKE 100.0 1000
BLK BLK 100.0 1000
BMPR1A BMPR1A 96.0 1000
BMPR1B BMPR1B 100.0 1000
BMPR2 BMPR2 100.0 1000
BMX BMX 95.0 1000
BRAF BRAF(V600E) 100.0 1000
PTK6 BRK 72.0 1000
BRSK1 BRSK1 84.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 100.0 1000
BUB1 BUB1 100.0 1000
CAMK1 CAMK1 100.0 1000
PNCK CAMK1B 100.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 90.0 1000
CAMK2A CAMK2A 96.0 1000
CAMK2B CAMK2B 100.0 1000
CAMK2D CAMK2D 93.0 1000
CAMK2G CAMK2G 100.0 1000
CAMK4 CAMK4 100.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 100.0 1000
CASK CASK 100.0 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 97.0 1000
CDK13 CDC2L5 100.0 1000
CDK19 CDK11 100.0 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 96.0 1000
CDK4 CDK4-cyclinD3 93.0 1000
CDK5 CDK5 100.0 1000
CDK7 CDK7 100.0 1000
CDK8 CDK8 86.0 1000
CDK9 CDK9 100.0 1000
CDKL1 CDKL1 60.0 1000
CDKL2 CDKL2 100.0 1000
CDKL3 CDKL3 100.0 1000
CDKL5 CDKL5 100.0 1000
CHEK1 CHEK1 100.0 1000
CHEK2 CHEK2 84.0 1000
CIT CIT 91.0 1000
CLK1 CLK1 100.0 1000
CLK2 CLK2 88.0 1000
CLK3 CLK3 100.0 1000
CLK4 CLK4 100.0 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 100.0 1000
CSNK1A1L CSNK1A1L 100.0 1000
CSNK1D CSNK1D 97.0 1000
CSNK1E CSNK1E 97.0 1000
CSNK1G1 CSNK1G1 100.0 1000
CSNK1G2 CSNK1G2 100.0 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 100.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 100.0 1000
DAPK1 DAPK1 91.0 1000
DAPK2 DAPK2 100.0 1000
DAPK3 DAPK3 90.0 1000
DCLK1 DCAMKL1 20.0 1000
DCLK2 DCAMKL2 87.0 1000
DCLK3 DCAMKL3 100.0 1000
DDR1 DDR1 100.0 1000
DDR2 DDR2 82.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 82.0 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 100.0 1000
EPHA1 EPHA1 93.0 1000
EPHA2 EPHA2 86.0 1000
EPHA3 EPHA3 100.0 1000
EPHA4 EPHA4 100.0 1000
EPHA5 EPHA5 97.0 1000
EPHA6 EPHA6 100.0 1000
EPHA7 EPHA7 100.0 1000
EPHA8 EPHA8 100.0 1000
EPHB1 EPHB1 100.0 1000
EPHB2 EPHB2 96.0 1000
EPHB3 EPHB3 100.0 1000
EPHB4 EPHB4 100.0 1000
EPHB6 EPHB6 100.0 1000
ERBB2 ERBB2 99.0 1000
ERBB3 ERBB3 100.0 1000
ERBB4 ERBB4 98.0 1000
MAPK3 ERK1 100.0 1000
MAPK1 ERK2 100.0 1000
MAPK6 ERK3 97.0 1000
MAPK4 ERK4 85.0 1000
MAPK7 ERK5 91.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 100.0 1000
PTK2 FAK 100.0 1000
FER FER 93.0 1000
FES FES 100.0 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 79.0 1000
FGFR3 FGFR3(G697C) 85.0 1000
FGFR4 FGFR4 100.0 1000
FGR FGR 100.0 1000
FLT1 FLT1 98.0 1000
FLT3 FLT3-autoinhibited 100.0 1000
FLT4 FLT4 100.0 1000
FRK FRK 92.0 1000
FYN FYN 100.0 1000
GAK GAK 100.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 84.0 1000
GRK1 GRK1 84.0 1000
GRK2 GRK2 100.0 1000
GRK3 GRK3 100.0 1000
GRK4 GRK4 96.0 1000
GRK7 GRK7 100.0 1000
GSK3A GSK3A 91.0 1000
GSK3B GSK3B 100.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 98.0 1000
HIPK1 HIPK1 81.0 1000
HIPK2 HIPK2 100.0 1000
HIPK3 HIPK3 100.0 1000
HIPK4 HIPK4 98.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 100.0 1000
CILK1 ICK 100.0 1000
IGF1R IGF1R 100.0 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 96.0 1000
IRAK1 IRAK1 100.0 1000
IRAK3 IRAK3 96.0 1000
IRAK4 IRAK4 100.0 1000
ITK ITK 98.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 60.0 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 95.0 1000
KIT KIT-autoinhibited 82.0 1000
LATS1 LATS1 100.0 1000
LATS2 LATS2 100.0 1000
LCK LCK 99.0 1000
LIMK1 LIMK1 100.0 1000
LIMK2 LIMK2 100.0 1000
STK11 LKB1 93.0 1000
STK10 LOK 100.0 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 100.0 1000
MAP3K15 MAP3K15 100.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 96.0 1000
MAP3K4 MAP3K4 96.0 1000
MAP4K2 MAP4K2 100.0 1000
MAP4K3 MAP4K3 100.0 1000
MAP4K4 MAP4K4 96.0 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 86.0 1000
MAPKAPK5 MAPKAPK5 100.0 1000
MARK1 MARK1 100.0 1000
MARK2 MARK2 97.0 1000
MARK3 MARK3 100.0 1000
MARK4 MARK4 100.0 1000
MAST1 MAST1 83.0 1000
MAP2K1 MEK1 100.0 1000
MAP2K2 MEK2 100.0 1000
MAP2K3 MEK3 100.0 1000
MAP2K4 MEK4 100.0 1000
MAP2K5 MEK5 97.0 1000
MAP2K6 MEK6 100.0 1000
MELK MELK 100.0 1000
MERTK MERTK 88.0 1000
MET MET(Y1235D) 92.0 1000
MINK1 MINK 81.0 1000
MAP2K7 MKK7 100.0 1000
MKNK1 MKNK1 100.0 1000
MKNK2 MKNK2 100.0 1000
MYLK3 MLCK 100.0 1000
MAP3K9 MLK1 100.0 1000
MAP3K10 MLK2 100.0 1000
MAP3K11 MLK3 97.0 1000
CDC42BPA MRCKA 90.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 100.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 89.0 1000
STK24 MST3 92.0 1000
STK26 MST4 100.0 1000
MTOR MTOR 82.0 1000
MUSK MUSK 100.0 1000
MYLK MYLK 88.0 1000
MYLK2 MYLK2 100.0 1000
MYLK4 MYLK4 91.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 72.0 1000
STK38L NDR2 100.0 1000
NEK1 NEK1 96.0 1000
NEK10 NEK10 100.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 97.0 1000
NEK4 NEK4 100.0 1000
NEK5 NEK5 100.0 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 96.0 1000
NEK9 NEK9 100.0 1000
MAP3K14 NIK 100.0 1000
NIM1K NIM1 100.0 1000
NLK NLK 94.0 1000
OXSR1 OSR1 100.0 1000
MAPK14 p38-alpha 87.0 1000
MAPK11 p38-beta 100.0 1000
MAPK13 p38-delta 100.0 1000
MAPK12 p38-gamma 98.0 1000
PAK1 PAK1 90.0 1000
PAK2 PAK2 83.0 1000
PAK3 PAK3 100.0 1000
PAK4 PAK4 96.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 98.0 1000
CDK16 PCTK1 100.0 1000
CDK17 PCTK2 98.0 1000
CDK18 PCTK3 84.0 1000
PDGFRA PDGFRA 98.0 1000
PDGFRB PDGFRB 100.0 1000
PDPK1 PDPK1 96.0 1000
CDPK1 PFCDPK1(P.falciparum) 100.0 1000
PK5 PFPK5(P.falciparum) 93.0 1000
CDK15 PFTAIRE2 100.0 1000
CDK14 PFTK1 91.0 1000
PHKG1 PHKG1 80.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 100.0 1000
PIK3C2G PIK3C2G 100.0 1000
PIK3CA PIK3CA(Q546K) 83.0 1000
PIK3CB PIK3CB 97.0 1000
PIK3CD PIK3CD 100.0 1000
PIK3CG PIK3CG 100.0 1000
PI4KB PIK4CB 100.0 1000
PIKFYVE PIKFYVE 98.0 1000
PIM1 PIM1 95.0 1000
PIM2 PIM2 98.0 1000
PIM3 PIM3 88.0 1000
PIP5K1A PIP5K1A 99.0 1000
PIP5K1C PIP5K1C 100.0 1000
PIP4K2B PIP5K2B 84.0 1000
PIP4K2C PIP5K2C 90.0 1000
PRKACA PKAC-alpha 99.0 1000
PRKACB PKAC-beta 78.0 1000
PKMYT1 PKMYT1 100.0 1000
PKN1 PKN1 64.0 1000
PKN2 PKN2 95.0 1000
PKNB PKNB(M.tuberculosis) 95.0 1000
PLK1 PLK1 100.0 1000
PLK2 PLK2 100.0 1000
PLK3 PLK3 69.0 1000
PLK4 PLK4 100.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 91.0 1000
PRKCH PRKCH 100.0 1000
PRKCI PRKCI 72.0 1000
PRKCQ PRKCQ 65.0 1000
PRKD1 PRKD1 100.0 1000
PRKD2 PRKD2 100.0 1000
PRKD3 PRKD3 83.0 1000
PRKG1 PRKG1 78.0 1000
PRKG2 PRKG2 95.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 92.0 1000
PRPF4B PRP4 100.0 1000
PTK2B PYK2 100.0 1000
SIK3 QSK 100.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 82.0 1000
RIOK1 RIOK1 96.0 1000
RIOK2 RIOK2 100.0 1000
RIOK3 RIOK3 100.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 100.0 1000
RIPK4 RIPK4 100.0 1000
DSTYK RIPK5 100.0 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 100.0 1000
ROS1 ROS1 95.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 98.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 80.0 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 86.0 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 100.0 1000
SIK2 SIK2 98.0 1000
SLK SLK 98.0 1000
NUAK2 SNARK 100.0 1000
SNRK SNRK 100.0 1000
SRC SRC 100.0 1000
SRMS SRMS 100.0 1000
SRPK1 SRPK1 100.0 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 99.0 1000
STK39 STK39 100.0 1000
SYK SYK 96.0 1000
MAP3K7 TAK1 100.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 100.0 1000
TAOK3 TAOK3 100.0 1000
TBK1 TBK1 65.0 1000
TEC TEC 96.0 1000
TESK1 TESK1 94.0 1000
TGFBR1 TGFBR1 100.0 1000
TGFBR2 TGFBR2 97.0 1000
TIE1 TIE1 90.0 1000
TEK TIE2 100.0 1000
TLK1 TLK1 82.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 100.0 1000
TNK1 TNK1 100.0 1000
TNK2 TNK2 100.0 1000
TNNI3K TNNI3K 100.0 1000
NTRK1 TRKA 100.0 1000
NTRK2 TRKB 100.0 1000
NTRK3 TRKC 100.0 1000
TRPM6 TRPM6 100.0 1000
TSSK1B TSSK1B 98.0 1000
TSSK3 TSSK3 62.0 1000
TTK TTK 94.0 1000
TXK TXK 85.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 100.0 1000
ULK2 ULK2 100.0 1000
ULK3 ULK3 100.0 1000
KDR VEGFR2 100.0 1000
PIK3C3 VPS34 100.0 1000
VRK2 VRK2 100.0 1000
WEE1 WEE1 95.0 1000
WEE2 WEE2 97.0 1000
WNK1 WNK1 100.0 1000
WNK2 WNK2 100.0 1000
WNK3 WNK3 100.0 1000
WNK4 WNK4 100.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 81.0 1000
YES1 YES 92.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 100.0 1000
MAP3K20 ZAK 97.0 1000
ZAP70 ZAP70 100.0 1000

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JNJ-54082730

The panel was screened with 10 µM compound.

Conclusion: Clean panel.

Target protein HGNC name Species Cmp. conc. Mean [% control specific binding] First measurement Second measurement Reference compound name Reference compound IC50 [nM] Assay ID
A1 (h) ADORA1 Homo sapiens 10 µM 107.2 106.20 108.30 DPCPX 0.70 Cerep_2
A2A (h) ADORA2A Homo sapiens 10 µM 55.1 59.40 50.90 NECA 26.00 Cerep_4
A3 (h) ADORA3 Homo sapiens 10 µM 104.3 104.40 104.10 IB-MECA 0.24 Cerep_6
Alpha1 (non-selective) ADRA1A
 ADRA1B
 ADRA1D
 		Rattus norvegicus 10 µM 103.8 107.30 100.30 prazosin 0.22 Cerep_8
Alpha2 (non-selective) ADRA2A
 ADRA2B
 ADRA2C
 		Rattus norvegicus 10 µM 103.7 96.40 111.10 yohimbine 22.00 Cerep_11
Beta1 (h) ADRB1 Homo sapiens 10 µM 96.8 94.00 99.60 atenolol 299.00 Cerep_18
AT1 (h) AGTR1 Homo sapiens 10 µM 104.0 107.80 100.20 saralasin 0.57 Cerep_24
BZD (central) Rattus norvegicus 10 µM 105.0 101.30 108.80 diazepam 11.00 Old_Cerep_37
B2 (h) BDKRB2 Homo sapiens 10 µM 103.1 100.80 105.40 NPC 567 21.00 Cerep_33
CCK1 (CCKA) (h) CCKAR Homo sapiens 10 µM 103.5 100.90 106.00 CCK-8s 0.08 Cerep_39
D1 (h) DRD1 Homo sapiens 10 µM 99.2 94.00 104.40 SCH 23390 0.23 Cerep_44
D2S (h) DRD2 Homo sapiens 10 µM 104.4 109.30 99.60 (+)butaclamol 1.40 Cerep_46
ETA (h) EDNRA Homo sapiens 10 µM 102.4 119.20 85.70 endothelin-1 0.06 Cerep_54
GABA (non-selective) Rattus norvegicus 10 µM 100.4 104.90 96.00 GABA 26.00 Cerep_57
GAL2 (h) GALR2 Homo sapiens 10 µM 94.0 105.60 82.30 galanin 27.00 Cerep_410
CXCR2 (IL-8B) (h) CXCR2 Homo sapiens 10 µM 109.0 110.40 107.50 IL-8 28.00 Cerep_419
CCR1 (h) CCR1 Homo sapiens 10 µM 89.6 87.10 92.20 MIP-1a 29.00 Cerep_361
H1 (h) HRH1 Homo sapiens 10 µM 105.6 104.50 106.60 pyrilamine 30.00 Cerep_870
H2 (h) HRH2 Homo sapiens 10 µM 103.4 109.40 97.40 cimetidine 31.00 Cerep_1208
MC4 (h) MC4R Homo sapiens 10 µM 111.0 115.90 106.10 NDP-a-MSH 32.00 Cerep_420
MT1 (ML1A) (h) MTNR1A Homo sapiens 10 µM 108.6 114.10 103.10 melatonin 33.00 Cerep_1538
M1 (h) CHRM1 Homo sapiens 10 µM 92.8 91.40 94.30 pirenzepine 34.00 Cerep_91
M2 (h) CHRM2 Homo sapiens 10 µM 114.8 129.10 100.50 methoctramine 35.00 Cerep_93
M3 (h) CHRM3 Homo sapiens 10 µM 102.7 105.90 99.50 4-DAMP 36.00 Cerep_95
NK2 (h) TACR2 Homo sapiens 10 µM 102.1 109.10 95.20 [Nleu10]-NKA (4-10) 37.00 Cerep_102
NK3 (h) TACR3 Homo sapiens 10 µM 99.8 106.80 92.80 SB 222200 38.00 Cerep_104
Y1 (h) NPY1R Homo sapiens 10 µM 108.3 112.10 104.60 NPY 39.00 Cerep_106
Y2 (h) NPY2R Homo sapiens 10 µM 108.6 108.90 108.30 NPY 40.00 Cerep_107
NTS1 (NT1) (h) NTSR1 Homo sapiens 10 µM 110.9 110.70 111.20 neurotensin 41.00 Cerep_109
delta 2 (DOP) (h) OPRD1 Homo sapiens 10 µM 90.2 92.50 87.90 DPDPE 42.00 Cerep_114
kappa (h) (KOP) OPRK1 Homo sapiens 10 µM 91.0 87.60 94.50 U 50488 43.00 Cerep_4461
mu (MOP) (h) OPRM1 Homo sapiens 10 µM 96.0 98.90 93.10 DAMGO 44.00 Cerep_118
NOP (ORL1) (h) OPRL1 Homo sapiens 10 µM 103.1 102.20 103.90 nociceptin 45.00 Cerep_358
5-HT1A (h) HTR1A Homo sapiens 10 µM 99.0 101.60 96.50 8-OH-DPAT 46.00 Cerep_131
5-HT1B(h) HTR1B Homo sapiens 10 µM 101.6 106.80 96.40 serotonin 47.00 Cerep_4376
5-HT2A (h) HTR2A Homo sapiens 10 µM 107.8 108.70 107.00 ketanserin 48.00 Cerep_135
5-HT2B (h) HTR2B Homo sapiens 10 µM 117.8 106.20 129.40 (±)DOI 49.00 Cerep_1333
5-HT3 (h) HTR3A Homo sapiens 10 µM 102.9 102.20 103.60 MDL 72222 50.00 Cerep_411
5-HT5a (h) HTR5A Homo sapiens 10 µM 95.3 93.10 97.50 serotonin 51.00 Cerep_140
5-HT6 (h) HTR6 Homo sapiens 10 µM 100.1 99.40 100.80 serotonin 52.00 Cerep_142
5-HT7 (h) HTR7 Homo sapiens 10 µM 104.6 108.00 101.20 serotonin 53.00 Cerep_144
sst (non-selective) Mus musculus 10 µM 121.8 127.10 116.50 somatostatin-14 54.00 Cerep_149
VPAC1 (VIP1) (h) VIPR1 Homo sapiens 10 µM 110.6 106.30 115.00 VIP 55.00 Cerep_157
V1a (h) AVPR1A Homo sapiens 10 µM 97.3 98.50 96.10 [d(CH2)51,Tyr(Me)2]-AVP 56.00 Cerep_159
Ca2+ channel (L, verapamil site) (phenylalkylamine) Rattus norvegicus 10 µM 96.6 99.60 93.70 D 600 57.00 Cerep_163
KV channel Rattus norvegicus 10 µM 93.6 95.10 92.10 a-dendrotoxin 58.00 Cerep_166
SKCa channel Rattus norvegicus 10 µM 100.6 120.90 80.30 apamin 59.00 Cerep_167
Cl- channel (GABA-gated) Rattus norvegicus 10 µM 101.6 103.00 100.20 picrotoxinin 60.00 Old_Cerep_16
norepinephrine transporter (h) SLC6A2 Homo sapiens 10 µM 99.0 95.30 102.80 protriptyline 61.00 Cerep_355
dopamine transporter (h) SLC6A3 Homo sapiens 10 µM 107.5 108.50 106.60 BTCP 62.00 Cerep_52
5-HT transporter (h) SCL6A4 Homo sapiens 10 µM 117.2 120.70 113.70 imipramine 63.00 Cerep_439
 

JNJ-54082730

Scintillation proximity assay was used.

Conclusion: Closest off-target in the PDE family is PDE20A2 with IC50 = 99 nM (47 fold) .

Target protein HGNC name Species IC50 [µM] Ki [nM] number of experiments 95% Confidence Interval [nM]
hPDE10A2 PDE10A Homo sapiens 0.1 30.00 93.00 90 - 109
hPDE3 PDE3A
 PDE3B
 		Homo sapiens 6.6 3320.00 42.00 6100 -7200
hPDE1B1 PDE1B Homo sapiens > 10.0 1.00
hPDE4D3 PDE4D Homo sapiens > 10.0 1.00
hPDE5A3 PDE5A Homo sapiens > 10.0 1.00
bovine retina PDE6 PDE6A
 PDE6B
 PDE6G
 		Bos taurus > 10.0 1.00
hPDE7A1 PDE7A Homo sapiens > 10.0 1.00
hPDE8A1 PDE8A Homo sapiens > 10.0 1.00
hPDE9A PDE9A Homo sapiens > 10.0 1.00