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JNJ-65355394

Compound concentration: 10 µM

Receptor	HGNC target name	Inhibition [%] (Primary experimental value)	Ki [nM] (Secondary experimental value)	pKi
5-HT1B	HTR1B	-2.53
5-HT1D	HTR1D	11.61
5-HT1A	HTR1A	22.23
Alpha1B	ADRA1B	-5.20
Sigma 2	TMEM97	19.00
5-HT2A	HTR2A	-2.94
5-HT2B	HTR2B	6.70
Alpha1A	ADRA1A	2.36
Alpha1D	ADRA1D	8.30
Beta1	ADRB1	3.29
Beta2	ADRB2	-5.16
D1	DRD1	-19.74
D3	DRD3	10.31
D5	DRD5	7.69
GABAA		-8.39
H1	HRH1	44.02
H2	HRH2	3.45
H3	HRH3	10.75
H4	HRH4	-44.60
M1	CHRM1	6.18
M2	CHRM2	9.54
M3	CHRM3	8.40
M4	CHRM4	-5.53
M5	CHRM5	-10.83
NET	SLC6A2	12.69
GABA/PBR		5.69
5-HT1E	HTR1E	-10.98
5-HT2C	HTR2C	15.17
5-HT3	HTR3A	6.87
5-HT5A	HTR5A	18.67
5-HT6	HTR6	14.28
5-HT7A	HTR7	9.60
Alpha2A	ADRA2A	8.68
Alpha2B	ADRA2B	44.84
Alpha2C	ADRA2C	31.91
Beta3	ADRB3	-19.87
GABAA/BZP		8.07
D2	DRD2	0.63
D4	DRD4	3.53
DAT	SLC6A3	13.39
DOR	OPRD1	11.76
KOR	OPRK1	75.14	773.30 average (n=2)	6.13
MOR	OPRM1	12.75
SERT	SLC6A4	7.21
Sigma 1	SIGMAR1	46.46

JNJ-73924149

Compound concentration: 10 µM

Receptor	HGNC target name	Inhibition [%] (Primary experimental value)	Ki [nM] (Secondary experimental value)	pKi
Alpha1B	ADRA1B	-3.57
5-HT1B	HTR1B	4.01
5-HT1D	HTR1D	14.51
5-HT1A	HTR1A	12.34
M2	CHRM2	8.65
Sigma 2	TMEM97	59.64	1399.16 average (n=2)	5.87
5-HT2A	HTR2A	6.45
5-HT2B	HTR2B	17.95
Alpha1A	ADRA1A	-1.89
Alpha1D	ADRA1D	7.45
Beta1	ADRB1	4.41
Beta2	ADRB2	-8.10
Beta3	ADRB3	-8.59
D1	DRD1	10.68
D3	DRD3	-11.44
D5	DRD5	-30.39
GABAA		43.57
H1	HRH1	44.17
H2	HRH2	-13.19
H3	HRH3	27.07
H4	HRH4	-0.60
M1	CHRM1	25.44
M3	CHRM3	-9.98
M4	CHRM4	8.78
M5	CHRM5	-6.15
NET	SLC6A2	17.82
GABA/PBR		11.18
5-HT1E	HTR1E	0.93
5-HT2C	HTR2C	16.29
5-HT3	HTR3A	20.71
5-HT5A	HTR5A	17.82
5-HT6	HTR6	25.62
5-HT7A	HTR7	2.58
Alpha2A	ADRA2A	31.69
Alpha2B	ADRA2B	59.06	3691.26 average (n=2)	5.44
Alpha2C	ADRA2C	36.54
GABAA/BZP		43.54
D2	DRD2	8.04
D4	DRD4	6.82
DAT	SLC6A3	81.93	5284.45	5.28
DOR	OPRD1	8.67
KOR	OPRK1	17.86
MOR	OPRM1	27.31
SERT	SLC6A4	52.27	2614.09 average (n=2)	5.59
Sigma 1	SIGMAR1	101.04	63.33 average (n=2)	7.20

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JNJ-65355394

The panel was screened at 10 µM except for hERG (0.1 µM) and rCaCH-nitrendipine (0.3 µM).

Conclusion: Closest off-targets are OPRK1 (77.85 % effect) and ADRA2A (69.05 % effect).

Target protein	HGNC name	Species	Cmp. conc.	% Effect	Assay ID
cML1	MTNR1A	Cricetinae	10 µM	11.5	Old_Cerep_1538
h5HT2A	HTR2A	Homo sapiens	10 µM	4.1	Cerep_471
hAT1	AGTR1	Homo sapiens	10 µM	-3.1	Cerep_24
hBCXCR2	CXCR2	Homo sapiens	10 µM	0.9	Cerep_419
hCCR1	CCR1	Homo sapiens	10 µM	-1.9	Cerep_361
hD2S	DRD2	Homo sapiens	10 µM	10.5	Cerep_46
hERG	KCNH2	Homo sapiens	10 µM	10.0	Cerep_4094
hGAL2	GALR2	Homo sapiens	10 µM	1.4	Cerep_410
hMC4	MC4R	Homo sapiens	10 µM	1.3	Cerep_420
hNPY1	NPY1R	Homo sapiens	10 µM	-7.4	Cerep_106
hNPY2	NPY2R	Homo sapiens	10 µM	-2.7	Cerep_107
hORL1	OPRL1	Homo sapiens	10 µM	-5.7	Cerep_358
hVPAC1	VIPR1	Homo sapiens	10 µM	-10.1	Cerep_157
r5HT1B	HTR1B	Rattus norvegicus	10 µM	-9.7	Cerep_132
rCaCH (D888)		Rattus norvegicus	10 µM	4.9	Cerep_163
rCaCH (nitrendipine)		Rattus norvegicus	10 µM	14.0	Cerep_161
rNaCH		Rattus norvegicus	10 µM	1.6	Old_Cerep_169
rOP2	OPRK1	Homo sapiens	10 µM	77.9	Cerep_4461
hA1	ADORA1	Homo sapiens	10 µM	-13.2	Cerep_2
hA2A	ADORA2A	Homo sapiens	10 µM	4.9	Cerep_4
hA3	ADORA3	Homo sapiens	10 µM	16.0	Cerep_6
rAa1	ADRA1A ADRA1B ADRA1D	Rattus norvegicus	10 µM	19.5	Cerep_8
rAa2	ADRA2A ADRA2B ADRA2C	Rattus norvegicus	10 µM	69.1	Cerep_11
hAb1	ADRB1	Homo sapiens	10 µM	11.2	Cerep_18
rBZD		Rattus norvegicus	10 µM	-16.6	Cerep_28
hBK2	BDKRB2	Homo sapiens	10 µM	10.8	Cerep_33
hCCKA	CCKAR	Homo sapiens	10 µM	-22.0	Cerep_39
hD1	DRD1	Homo sapiens	10 µM	20.1	Cerep_44
hDAT	SLC6A3	Homo sapiens	10 µM	19.3	Cerep_52
hETA	EDNRA	Homo sapiens	10 µM	3.6	Cerep_54
rGABA		Rattus norvegicus	10 µM	-9.8	Cerep_57
hM1	CHRM1	Homo sapiens	10 µM	32.5	Cerep_91
hM2	CHRM2	Homo sapiens	10 µM	25.4	Cerep_93
hM3	CHRM3	Homo sapiens	10 µM	45.6	Cerep_95
hNK2	TACR2	Homo sapiens	10 µM	4.5	Cerep_102
hNK3	TACR3	Homo sapiens	10 µM	7.0	Cerep_104
hNT1	NTSR1	Homo sapiens	10 µM	4.2	Cerep_109
hOP1	OPRD1	Homo sapiens	10 µM	20.4	Cerep_114
hOP3	OPRM1	Homo sapiens	10 µM	55.4	Cerep_118
h5HT1A	HTR1A	Homo sapiens	10 µM	9.5	Cerep_131
h5HT5A	HTR5A	Homo sapiens	10 µM	-7.7	Cerep_140
h5HT6	HTR6	Homo sapiens	10 µM	14.2	Cerep_142
h5HT7	HTR7	Homo sapiens	10 µM	-1.7	Cerep_144
mSST		Mus musculus	10 µM	4.2	Cerep_149
hV1a	AVPR1A	Homo sapiens	10 µM	7.7	Cerep_159
rKCH		Rattus norvegicus	10 µM	1.0	Cerep_166
rSKCaCH		Rattus norvegicus	10 µM	35.4	Cerep_167
rCLCH		Rattus norvegicus	10 µM	-5.7	Old_Cerep_170
hNET	SLC6A2	Homo sapiens	10 µM	5.8	Cerep_355
h5HT3	HTR3A	Homo sapiens	10 µM	1.9	Cerep_411
h5HTT	SCL6A4	Homo sapiens	10 µM	-7.1	Cerep_439
hH1	HRH1	Homo sapiens	10 µM	5.7	Cerep_870
hH2	HRH2	Homo sapiens	10 µM	11.5	Cerep_1208
h5HT2B	HTR2B	Homo sapiens	10 µM	6.3	Cerep_1333