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Selectivity data for probe BAY-707 and control BAY-604


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BAY-707


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1A HTR1A 69.80 > 10000.00 < 5.00
5-HT1B HTR1B -1.66
5-HT1D HTR1D -7.56
5-HT1E HTR1E 10.59
5-HT2A HTR2A -7.89
5-HT2B HTR2B 47.12
5-HT2C HTR2C -4.02
5-HT3 HTR3A -1.37
5-HT5A HTR5A -8.05
5-HT6 HTR6 -8.52
5-HT7A HTR7 -4.45
D1 DRD1 1.92
D2 DRD2 12.27
D3 DRD3 -7.82
D4 DRD4 -3.84
D5 DRD5 34.31
SERT SLC6A4 -17.27
NET SLC6A2 40.18
DAT SLC6A3 25.50
MOR OPRM1 24.84
DOR OPRD1 -0.04
KOR OPRK1 13.08
GABAA 28.21
H1 HRH1 4.94
H2 HRH2 1.31
H3 HRH3 40.48
H4 HRH4 0.03
Alpha1A ADRA1A 1.88
Alpha1B ADRA1B -2.40
Alpha2A ADRA2A 18.07
Alpha2B ADRA2B 34.39
Alpha2C ADRA2C 3.16
Beta1 ADRB1 -11.66
Beta2 ADRB2 -6.09
M1 CHRM1 21.68
M2 CHRM2 -1.26
M3 CHRM3 -11.60
M4 CHRM4 -13.82
M5 CHRM5 -4.95
Beta3 ADRB3 14.34
GABAA/BZP 57.31 1527.00 5.80
GABA/PBR 30.11
Alpha1D ADRA1D 8.58
Sigma 2 TMEM97 34.60
Sigma 1 SIGMAR1 24.30

BAY-604


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
GABA/PBR 17.17
Beta1 ADRB1 -10.13
Beta3 ADRB3 -9.19
GABAA/BZP 84.23 224.22 average (n=2) 6.72
DAT SLC6A3 -25.15
Alpha1A ADRA1A 3.94
Alpha1B ADRA1B 5.71
Alpha1D ADRA1D -8.10
Alpha2A ADRA2A 16.92
Alpha2B ADRA2B -2.44
5-HT1A HTR1A -1.88
5-HT1B HTR1B -8.46
5-HT2A HTR2A -1.68
5-HT2B HTR2B 2.79
5-HT6 HTR6 31.93
5-HT7A HTR7 -1.21
D2 DRD2 -1.89
D3 DRD3 12.13
5-HT1D HTR1D -0.31
5-HT1E HTR1E 9.36
5-HT2C HTR2C 46.24
5-HT3 HTR3A 18.55
5-HT5A HTR5A -16.79
Beta2 ADRB2 27.31
D1 DRD1 14.19
DOR OPRD1 2.73
H1 HRH1 26.01
H2 HRH2 -3.91
H3 HRH3 -6.16
M1 CHRM1 11.90
M2 CHRM2 7.19
M3 CHRM3 38.05
M4 CHRM4 5.75
M5 CHRM5 -0.90
SERT SLC6A4 -11.38
Sigma 1 SIGMAR1 24.46
Sigma 2 TMEM97 30.40
D4 DRD4 77.62 735.98 average (n=2) 6.15
D5 DRD5 -20.58
H4 HRH4 5.51
KOR OPRK1 14.59
MOR OPRM1 0.08
NET SLC6A2 5.35
Alpha2C ADRA2C -1.28
GABAA -1.39

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