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8RK64

Compound concentration: 10 µM

Receptor	HGNC target name	Inhibition [%] (Primary experimental value)	Ki [nM] (Secondary experimental value)	pKi
5-HT1B	HTR1B	1.57
5-HT1D	HTR1D	-0.37
GABAA		-1.06
5-HT1A	HTR1A	7.61
Sigma 2	TMEM97	-1.19
5-HT2A	HTR2A	30.02
5-HT2B	HTR2B	5.22
Alpha1A	ADRA1A	11.21
Alpha1B	ADRA1B	-12.04
Alpha1D	ADRA1D	12.21
Beta1	ADRB1	-7.19
Beta2	ADRB2	-0.70
Beta3	ADRB3	-3.31
D1	DRD1	-15.92
D3	DRD3	-2.14
D5	DRD5	7.55
H1	HRH1	7.45
H2	HRH2	0.58
H3	HRH3	-5.98
H4	HRH4	5.77
M1	CHRM1	7.58
M2	CHRM2	-0.45
M3	CHRM3	-1.04
M4	CHRM4	4.84
M5	CHRM5	-13.58
NET	SLC6A2	2.61
GABA/PBR		21.86
5-HT1E	HTR1E	2.35
5-HT2C	HTR2C	18.18
5-HT3	HTR3A	2.31
5-HT5A	HTR5A	11.84
5-HT6	HTR6	9.94
5-HT7A	HTR7	-0.16
Alpha2A	ADRA2A	-13.57
Alpha2B	ADRA2B	-1.02
Alpha2C	ADRA2C	14.70
GABAA/BZP		-2.35
D2	DRD2	0.55
D4	DRD4	4.26
DAT	SLC6A3	-2.33
DOR	OPRD1	8.43
KOR	OPRK1	0.19
MOR	OPRM1	12.61
SERT	SLC6A4	2.49
Sigma 1	SIGMAR1	69.03	3429.51 average (n=2)	5.47

JYQ88

Compound concentration: 10 µM

Receptor	HGNC target name	Inhibition [%] (Primary experimental value)	Ki [nM] (Secondary experimental value)	pKi
5-HT1B	HTR1B	6.13
5-HT1D	HTR1D	20.94
5-HT1A	HTR1A	12.11
M2	CHRM2	-12.03
Sigma 2	TMEM97	-18.70
5-HT2A	HTR2A	3.66
5-HT2B	HTR2B	5.55
Alpha1A	ADRA1A	3.73
Alpha1D	ADRA1D	0.34
Beta1	ADRB1	3.17
Beta2	ADRB2	-8.12
D1	DRD1	8.27
D3	DRD3	-11.67
D5	DRD5	-19.33
GABAA		34.17
H1	HRH1	0.43
H2	HRH2	3.43
H3	HRH3	-2.11
H4	HRH4	-10.88
M1	CHRM1	24.35
M3	CHRM3	-2.15
M4	CHRM4	-1.43
M5	CHRM5	2.94
NET	SLC6A2	3.51
GABA/PBR		5.64
5-HT1E	HTR1E	6.50
5-HT2C	HTR2C	6.22
5-HT3	HTR3A	0.95
5-HT5A	HTR5A	9.64
5-HT6	HTR6	8.14
5-HT7A	HTR7	-1.05
Alpha2A	ADRA2A	50.73	> 10000.00 average (n=2)	< 5.00
Alpha2B	ADRA2B	6.46
Alpha2C	ADRA2C	4.21
Beta3	ADRB3	-15.20
GABAA/BZP		28.73
D2	DRD2	4.82
D4	DRD4	5.53
DAT	SLC6A3	82.96	> 10000.00 average (n=2)	< 5.00
DOR	OPRD1	4.07
KOR	OPRK1	13.30
MOR	OPRM1	18.71
SERT	SLC6A4	7.66
Sigma 1	SIGMAR1	6.56
Alpha1B	ADRA1B	-7.50

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