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Selectivity data for probe GSK789 and control GSK791


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GSK789


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT2C HTR2C 14.02
5-HT3 HTR3A 31.79
5-HT5A HTR5A 24.15
Beta2 ADRB2 19.83
DOR OPRD1 40.94
H1 HRH1 -0.72
H2 HRH2 -1.12
H3 HRH3 -9.93
M4 CHRM4 17.14
M5 CHRM5 16.34
SERT SLC6A4 17.70
5-HT1A HTR1A 17.27
5-HT1B HTR1B 3.37
5-HT1D HTR1D -6.42
5-HT1E HTR1E -38.65
5-HT2A HTR2A -5.01
5-HT2B HTR2B 9.16
5-HT6 HTR6 -37.35
5-HT7A HTR7 -15.88
D1 DRD1 27.26
D2 DRD2 -4.38
D3 DRD3 9.01
Alpha1A ADRA1A 25.24
Alpha1B ADRA1B 11.83
Alpha1D ADRA1D 36.58
Alpha2A ADRA2A -3.97
Alpha2B ADRA2B -0.37
Alpha2C ADRA2C 8.58
M1 CHRM1 -9.42
M2 CHRM2 0.27
M3 CHRM3 -10.96
Sigma 1 SIGMAR1 22.61
Sigma 2 TMEM97 9.26
D4 DRD4 97.93 1013.12 average (n=2) 6.00
D5 DRD5 33.17
DAT SLC6A3 28.51
H4 HRH4 15.90
KOR OPRK1 28.06
MOR OPRM1 27.04
NET SLC6A2 30.53
GABAA/BZP 24.74
GABAA 14.77
GABA/PBR 3.90
Beta1 ADRB1 1.68
Beta3 ADRB3 13.80

GSK791


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
Beta1 ADRB1 2.98
Beta3 ADRB3 35.12
GABAA/BZP 86.29 2539.22 5.60
GABAA 14.94
GABA/PBR -8.18
D4 DRD4 17.42
D5 DRD5 35.43
DAT SLC6A3 8.66
H4 HRH4 -23.90
KOR OPRK1 34.94
MOR OPRM1 24.29
NET SLC6A2 32.42
5-HT1A HTR1A 16.91
5-HT1B HTR1B 1.93
5-HT1D HTR1D 33.11
5-HT1E HTR1E 9.79
5-HT2A HTR2A 2.71
5-HT2B HTR2B 24.26
5-HT6 HTR6 -15.62
5-HT7A HTR7 -22.02
D1 DRD1 21.21
D2 DRD2 -10.92
D3 DRD3 15.52
Alpha1A ADRA1A 10.06
Alpha1B ADRA1B 1.98
Alpha1D ADRA1D 7.87
Alpha2A ADRA2A 9.80
Alpha2B ADRA2B 28.51
Alpha2C ADRA2C 10.75
Sigma 2 TMEM97 44.11
5-HT2C HTR2C 3.86
5-HT3 HTR3A 1.04
5-HT5A HTR5A 10.08
Beta2 ADRB2 4.04
DOR OPRD1 21.99
H1 HRH1 11.68
H2 HRH2 21.58
H3 HRH3 -2.09
M1 CHRM1 11.99
M2 CHRM2 5.25
M3 CHRM3 28.89
M4 CHRM4 -3.00
M5 CHRM5 7.44
SERT SLC6A4 13.85
Sigma 1 SIGMAR1 -20.77

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GSK789

A panel of bromodomain containing proteins (BCP) was screened in a dose-response format in duplicate.

Conclusion: GSK789 is selective for the BD1 domain of BET proteins with the exception of the following two hits: TAF1 BD2 (pKd = 7.3) and TAF1L BD2 (pKd = 6.4).

Target protein HGNC name Species pKd
ATAD2A ATAD2 Homo sapiens 4.8
ATAD2B ATAD2B Homo sapiens 4.8
BAZ2A BAZ2A Homo sapiens 4.8
BAZ2B BAZ2B Homo sapiens < 4.5
BRD1 BRD1 Homo sapiens < 4.5
BRD2 (BD1) BRD2 Homo sapiens 7.7
BRD2 (BD2) BRD2 Homo sapiens 4.6
BRD3 (BD1) BRD3 Homo sapiens 7.8
BRD3 (BD2) BRD3 Homo sapiens 4.7
BRD4 (BD1) BRD4 Homo sapiens 7.7
BRD4 (BD2) BRD4 Homo sapiens 4.5
BRD7 BRD7 Homo sapiens < 4.6
BRD8 (BD1) BRD8 Homo sapiens < 4.5
BRD8 (BD2) BRD8 Homo sapiens < 4.5
BRD9 BRD9 Homo sapiens < 4.5
BRDT (BD1) BRDT Homo sapiens 7.7
BRDT (1,2) BRDT Homo sapiens 7.0
BRDT (BD2) BRDT Homo sapiens 4.7
BRPF1 BRPF1 Homo sapiens < 4.5
BRPF3 BRPF3 Homo sapiens < 4.5
CECR2 CECR2 Homo sapiens < 4.5
CREBBP CREBBP Homo sapiens < 4.5
EP300 EP300 Homo sapiens 4.6
FALZ BPTF Homo sapiens < 4.5
GCN5L2 KAT2A Homo sapiens < 4.5
PBRM1 (BD2) PBRM1 Homo sapiens < 4.5
PBRM1(5) PBRM1 Homo sapiens 5.0
PCAF KAT2B Homo sapiens < 4.5
SMARCA2 SMARCA2 Homo sapiens < 4.5
SMARCA4 SMARCA4 Homo sapiens < 4.5
TAF1 (BD2) TAF1 Homo sapiens 7.3
TAF1L (BD2) TAF1L Homo sapiens 6.4
TRIM24 (TIF1alpha) (BD) TRIM24 Homo sapiens 4.7
TRIM24 (TIF1alpha) (PHD & BD) TRIM24 Homo sapiens < 4.5
TRIM33 (TIF1gamma) (PHD & BD) TRIM33 Homo sapiens < 4.5
WDR9 (BD2) BRWD1 Homo sapiens < 4.5