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Selectivity data for probe TP-008 and control Al11


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TP-008


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1A HTR1A 22.86
5-HT1B HTR1B 19.51
5-HT1D HTR1D 5.53
5-HT1E HTR1E -5.81
5-HT2A HTR2A -0.87
5-HT2B HTR2B 70.48 1881.00 5.73
5-HT2C HTR2C 15.52
5-HT3 HTR3A -6.36
5-HT5A HTR5A 16.77
5-HT6 HTR6 -4.28
5-HT7A HTR7 3.97
D1 DRD1 12.87
D2 DRD2 -5.48
D3 DRD3 2.27
D4 DRD4 5.41
D5 DRD5 -12.68
SERT SLC6A4 3.84
NET SLC6A2 -16.56
DAT SLC6A3 87.59 > 10000.00 < 5.00
MOR OPRM1 13.66
DOR OPRD1 -4.16
KOR OPRK1 -0.98
GABAA 27.31
H1 HRH1 0.85
H2 HRH2 6.53
H3 HRH3 30.52
H4 HRH4 26.65
Alpha1A ADRA1A -2.17
Alpha1B ADRA1B 3.76
Alpha2A ADRA2A -0.77
Alpha2B ADRA2B 18.06
Alpha2C ADRA2C -5.16
Beta1 ADRB1 -17.89
Beta2 ADRB2 13.88
M1 CHRM1 -3.81
M2 CHRM2 2.23
M3 CHRM3 -7.48
M4 CHRM4 -3.08
M5 CHRM5 -5.69
Beta3 ADRB3 3.94
GABAA/BZP 31.78
GABA/PBR -8.98
Alpha1D ADRA1D -12.85
Sigma 2 TMEM97 -2.75
Sigma 1 SIGMAR1 50.00 > 10000.00 < 5.00

Al11


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT2C HTR2C 10.20
5-HT3 HTR3A 19.85
5-HT5A HTR5A -0.66
Beta2 ADRB2 16.70
DOR OPRD1 17.46
H1 HRH1 -2.43
H2 HRH2 -19.72
H3 HRH3 -8.16
M3 CHRM3 -5.28
M4 CHRM4 3.09
M5 CHRM5 1.56
SERT SLC6A4 14.28
Sigma 1 SIGMAR1 13.22
5-HT1A HTR1A 11.97
5-HT1B HTR1B -7.07
5-HT1D HTR1D -22.63
5-HT1E HTR1E -22.11
5-HT2A HTR2A 11.15
5-HT2B HTR2B 72.03 1591.74 average (n=2) 5.81
5-HT6 HTR6 14.14
5-HT7A HTR7 12.06
D1 DRD1 -2.08
D2 DRD2 -1.99
D3 DRD3 -17.02
Alpha1A ADRA1A 0.25
Alpha1B ADRA1B 5.45
Alpha1D ADRA1D 2.71
Alpha2A ADRA2A 3.10
Alpha2B ADRA2B 17.31
Alpha2C ADRA2C 17.90
M1 CHRM1 -1.17
M2 CHRM2 14.42
Sigma 2 TMEM97 41.64
D4 DRD4 -1.38
D5 DRD5 6.12
DAT SLC6A3 -4.34
H4 HRH4 -20.13
KOR OPRK1 13.51
MOR OPRM1 47.40
NET SLC6A2 -13.54
GABAA/BZP 50.22 2746.00 5.56
GABAA -14.29
GABA/PBR 27.09
Beta1 ADRB1 25.75
Beta3 ADRB3 9.94

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