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Selectivity data for probe WM-1119 and control WM-2474


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WM-1119


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
Beta1 ADRB1 -0.13
Beta3 ADRB3 16.31
GABAA/BZP 75.65
GABAA 11.66
GABA/PBR 47.03
D4 DRD4 23.82
D5 DRD5 4.57
H4 HRH4 -2.44
KOR OPRK1 5.23
MOR OPRM1 3.45
5-HT1B HTR1B 13.62
Alpha1A ADRA1A 9.59
Alpha1B ADRA1B 7.18
Alpha1D ADRA1D 3.20
Alpha2A ADRA2A -14.88
Alpha2B ADRA2B -3.78
Alpha2C ADRA2C 10.19
M1 CHRM1 0.14
M2 CHRM2 15.93
M3 CHRM3 -17.57
M4 CHRM4 20.45
M5 CHRM5 -8.87
Sigma 2 TMEM97 19.95
5-HT1A HTR1A 16.03
5-HT1D HTR1D -0.66
5-HT1E HTR1E 13.84
5-HT2A HTR2A -7.37
5-HT2B HTR2B 2.94
5-HT6 HTR6 -20.19
5-HT7A HTR7 -3.75
D1 DRD1 -3.67
D2 DRD2 79.62 397.52 average (n=2) 6.41
D3 DRD3 4.97
5-HT2C HTR2C 6.46
5-HT3 HTR3A 32.85
5-HT5A HTR5A -9.77
Beta2 ADRB2 13.19
DAT SLC6A3 -27.13
DOR OPRD1 20.56
H1 HRH1 -8.33
H2 HRH2 5.32
H3 HRH3 -20.48
NET SLC6A2 -15.50
SERT SLC6A4 -16.72
Sigma 1 SIGMAR1 35.74

WM-2474


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
Alpha1B ADRA1B -3.44
5-HT1B HTR1B 11.01
5-HT1D HTR1D -15.02
5-HT1A HTR1A 23.05
M2 CHRM2 -5.57
5-HT2A HTR2A 11.82
5-HT2B HTR2B 40.09
Alpha1A ADRA1A 18.65
Alpha1D ADRA1D 17.43
Beta1 ADRB1 11.19
Beta2 ADRB2 10.38
D1 DRD1 8.58
D3 DRD3 -8.61
D5 DRD5 5.79
GABAA 4.55
H1 HRH1 -2.04
H2 HRH2 -5.93
H3 HRH3 15.52
H4 HRH4 -19.80
M1 CHRM1 43.34
M3 CHRM3 12.97
M4 CHRM4 -11.78
M5 CHRM5 -10.56
NET SLC6A2 -2.40
GABA/PBR -3.60
5-HT1E HTR1E 13.10
5-HT2C HTR2C 7.81
5-HT3 HTR3A 4.55
5-HT5A HTR5A -0.06
5-HT6 HTR6 2.65
5-HT7A HTR7 -1.87
Alpha2A ADRA2A 68.51 > 10000.00 average (n=2) < 5.00
Alpha2B ADRA2B 3.07
Alpha2C ADRA2C -5.42
Beta3 ADRB3 -12.02
GABAA/BZP 34.61
D2 DRD2 14.72
D4 DRD4 9.83
DAT SLC6A3 80.15 > 10000.00 average (n=2) < 5.00
DOR OPRD1 7.99
KOR OPRK1 -5.10
MOR OPRM1 26.08
SERT SLC6A4 6.15
Sigma 1 SIGMAR1 19.11
Sigma 2 TMEM97 40.13

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