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Selectivity data for probe BAY-3153 and control BAY-173


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BAY-3153


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1B HTR1B -2.86
5-HT1D HTR1D -2.08
5-HT1E HTR1E -15.99
5-HT2B HTR2B 10.50
Alpha1A ADRA1A 16.97
Alpha1B ADRA1B -12.09
H1 HRH1 11.15
H2 HRH2 27.73
D3 DRD3 1.58
D4 DRD4 15.47
D5 DRD5 2.54
DAT SLC6A3 3.92
M2 CHRM2 8.64
M3 CHRM3 8.61
M4 CHRM4 -3.29
Sigma 1 SIGMAR1 84.98 1828.52 5.74
5-HT2C HTR2C 4.08
5-HT3 HTR3A -1.97
5-HT6 HTR6 -8.16
Alpha1D ADRA1D 7.09
Alpha2A ADRA2A -10.96
Alpha2B ADRA2B -19.91
Alpha2C ADRA2C 2.17
Beta2 ADRB2 -4.63
D1 DRD1 40.33
D2 DRD2 7.26
DOR OPRD1 10.33
KOR OPRK1 53.60 3005.38 5.52
MOR OPRM1 5.82
SERT SLC6A4 33.43
H4 HRH4 -13.92
5-HT7A HTR7 -15.45
Beta1 ADRB1 -26.17
Beta3 ADRB3 -5.38
GABAA/BZP -6.17
H3 HRH3 17.30
M5 CHRM5 -4.29
NET SLC6A2 1.24
GABA/PBR 54.19 1805.09 5.74
5-HT1A HTR1A -9.03
GABAA 18.57
5-HT2A HTR2A 6.74
5-HT5A HTR5A 1.70
Sigma 2 TMEM97 83.60 1476.05 5.83

BAY-173


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
M1 SLC6A3 -3.85
5-HT2A HTR2A 7.31
5-HT5A HTR5A -1.82
Sigma 2 TMEM97 76.48 2169.70 5.66
5-HT1A HTR1A -16.00
GABAA 20.02
5-HT1D HTR1D -7.50
5-HT7A HTR7 -13.85
Beta1 ADRB1 6.12
Beta3 ADRB3 -9.84
GABAA/BZP 0.65
D1 DRD1 -16.49
H3 HRH3 9.39
M5 CHRM5 -1.65
NET SLC6A2 -4.52
GABA/PBR -8.33
H4 HRH4 -3.31
5-HT1B HTR1B -6.45
5-HT1E HTR1E -25.43
5-HT2B HTR2B 14.76
Alpha1A ADRA1A 7.02
Alpha1B ADRA1B 0.94
H1 HRH1 14.28
H2 HRH2 8.13
D3 DRD3 2.75
D4 DRD4 51.55 > 10000.00 < 5.00
D5 DRD5 6.84
M2 CHRM2 1.89
M3 CHRM3 24.07
M4 CHRM4 -6.12
Sigma 1 SIGMAR1 69.54 8245.18 5.08
5-HT2C HTR2C -2.02
5-HT3 HTR3A -7.03
Alpha1D ADRA1D -7.34
Alpha2A ADRA2A 11.34
Alpha2B ADRA2B -34.32 > 10000.00 < 5.00
Alpha2C ADRA2C 14.45
Beta2 ADRB2 -7.55
D2 DRD2 -16.50
DOR OPRD1 -14.99
KOR OPRK1 18.73
MOR OPRM1 4.45
SERT SLC6A4 70.26 1460.83 5.84
5-HT6 HTR6 5.38

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