Selectivity data for probe JNJ-42226314 and control JNJ-8034


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JNJ-42226314


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT2B HTR2B 8.47
5-HT1A HTR1A 11.58
5-HT1B HTR1B 6.33
5-HT1D HTR1D 18.18
5-HT2A HTR2A 7.06
5-HT2C HTR2C -27.14
5-HT3 HTR3A 19.29
5-HT5A HTR5A 17.68
5-HT6 HTR6 -9.24
5-HT7A HTR7 12.78
Alpha1A ADRA1A -2.02
Alpha1B ADRA1B -6.82
Alpha1D ADRA1D 9.02
Alpha2A ADRA2A 14.15
Alpha2B ADRA2B 9.63
Alpha2C ADRA2C 4.03
Beta1 ADRB1 -2.68
Beta2 ADRB2 -2.21
Beta3 ADRB3 0.70
GABAA/BZP -17.47
D1 DRD1 -13.44
D2 DRD2 -9.71
D3 DRD3 1.99
D4 DRD4 0.01
D5 DRD5 -0.29
DAT SLC6A3 25.23
DOR OPRD1 9.83
H1 HRH1 4.93
H3 HRH3 19.38
H4 HRH4 -8.52
KOR OPRK1 11.10
M1 CHRM1 -17.37
M2 CHRM2 -3.14
M3 CHRM3 54.66
M4 CHRM4 1.62
M5 CHRM5 -7.30
MOR OPRM1 14.51
NET SLC6A2 8.01
GABA/PBR -0.52
SERT SLC6A4 8.15
Sigma 1 TMEM97 27.58
Sigma 2 SIGMAR1 27.59

JNJ-8034


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1A HTR1A 18.14
5-HT1B HTR1B 35.00
5-HT1D HTR1D 22.73
5-HT2A HTR2A 8.77
5-HT2C HTR2C 2.58
5-HT3 HTR3A 9.93
5-HT5A HTR5A 11.51
5-HT6 HTR6 16.97
5-HT7A HTR7 12.36
Alpha1A ADRA1A -6.90
Alpha1B ADRA1B -7.67
Alpha1D ADRA1D 10.41
Alpha2A ADRA2A 23.28
Alpha2B ADRA2B 22.99
Alpha2C ADRA2C 16.60
Beta1 ADRB1 -6.07
Beta2 ADRB2 0.18
Beta3 ADRB3 23.60
GABAA/BZP 36.51
D1 DRD1 -10.63
D2 DRD2 8.15
D3 DRD3 11.13
D4 DRD4 16.01
D5 DRD5 -21.93
DAT SLC6A3 43.50
DOR OPRD1 38.98
H1 HRH1 29.88
H3 HRH3 41.25
H4 HRH4 -7.89
KOR OPRK1 24.25
M1 CHRM1 -10.95
M2 CHRM2 -3.68
M3 CHRM3 48.91
M4 CHRM4 -10.57
M5 CHRM5 -4.46
MOR OPRM1 49.06
NET SLC6A2 3.51
GABA/PBR 37.98
SERT SLC6A4 22.30
Sigma 1 TMEM97 37.13
Sigma 2 SIGMAR1 43.57
5-HT2B HTR2B 8.86

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JNJ-42226314

A fluorescence assay using purified enzyme and chromogenic substrate was deployed. JNJ-42226314 was used at 10 µM. Data are from PMID: 32527545 (Table 4).

Conclusion: Clean panel.

Target protein HGNC name Species % Inhibition at 10 µM
Tryptase Homo sapiens 2.0
Elastase ELANE Homo sapiens 4.0
Plasmin PLG Homo sapiens 4.0
Chymotrypsin Homo sapiens -3.0
TPA PLAT Homo sapiens 6.0
Kallikrein KLK1 Homo sapiens 4.0
Thrombin F2 Homo sapiens -1.0
Chymase CMA1 Homo sapiens 11.0
Cathepsin G CTSG Homo sapiens 13.0
Proteinase 3 PRTN3 Homo sapiens 7.0
Factor VIIa F7 Homo sapiens -5.0
Urokinase PLAU Homo sapiens 2.0
Streptokinase Homo sapiens 1.0
Trypsin PRSS1 Homo sapiens -10.0
Factor Xa F10 Homo sapiens 0.0
 

JNJ-42226314

Radiometric assay using cell lysate and radiolabeled substrate was deployed for endocannabinoid related proteins. Cell-based fluorescence assay using BODIPY FL containing PLA1-specific substrate was used for lipases.

Conclusion: Closest hit is hFAAH with IC50 > 4 µM

Target protein HGNC name Species IC50 [µM]
hFAAH FAAH Homo sapiens 4.0
hABHD6 ABHD6 Homo sapiens > 10.0
hABHD12 ABHD12 Homo sapiens > 10.0
Endothelial lipase LIPG Homo sapiens > 30.0
Hepatic lipase LIPC Homo sapiens > 30.0
Lipoprotein lipase LPL Homo sapiens > 30.0