Selectivity data for probe GSK973 and control GSK943
Jump to control PDSP data
GSK973
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| Beta1 | ADRB1 | 6.03 | ||
| Beta3 | ADRB3 | 15.50 | ||
| GABAA/BZP | 30.17 | |||
| GABAA | 4.07 | |||
| GABA/PBR | 9.06 | |||
| D4 | DRD4 | 81.57 | 982.65 average (n=2) | 6.03 |
| D5 | DRD5 | 28.26 | ||
| DAT | SLC6A3 | -16.94 | ||
| H4 | HRH4 | 9.36 | ||
| KOR | OPRK1 | 1.22 | ||
| MOR | OPRM1 | -5.14 | ||
| NET | SLC6A2 | 0.32 | ||
| Alpha1A | ADRA1A | -4.55 | ||
| Alpha1B | ADRA1B | 1.49 | ||
| Alpha1D | ADRA1D | 3.51 | ||
| Alpha2A | ADRA2A | 1.67 | ||
| Alpha2B | ADRA2B | 12.48 | ||
| Alpha2C | ADRA2C | 8.26 | ||
| M1 | CHRM1 | -14.72 | ||
| M2 | CHRM2 | -5.52 | ||
| M3 | CHRM3 | 11.21 | ||
| Sigma 2 | TMEM97 | 14.29 | ||
| 5-HT1A | HTR1A | 8.96 | ||
| 5-HT1B | HTR1B | -0.10 | ||
| 5-HT1D | HTR1D | -5.14 | ||
| 5-HT1E | HTR1E | -12.78 | ||
| 5-HT2A | HTR2A | 13.40 | ||
| 5-HT2B | HTR2B | 28.25 | ||
| 5-HT6 | HTR6 | 16.77 | ||
| 5-HT7A | HTR7 | 13.57 | ||
| D1 | DRD1 | 9.70 | ||
| D2 | DRD2 | 60.90 | 967.00 average (n=2) | 6.09 |
| D3 | DRD3 | 81.79 | 257.47 average (n=2) | 6.59 |
| 5-HT2C | HTR2C | 22.16 | ||
| 5-HT3 | HTR3A | 20.18 | ||
| 5-HT5A | HTR5A | 12.51 | ||
| Beta2 | ADRB2 | 17.94 | ||
| DOR | OPRD1 | 2.46 | ||
| H1 | HRH1 | -26.88 | ||
| H2 | HRH2 | -3.94 | ||
| H3 | HRH3 | -9.57 | ||
| M4 | CHRM4 | 2.78 | ||
| M5 | CHRM5 | 2.23 | ||
| SERT | SLC6A4 | 27.25 | ||
| Sigma 1 | SIGMAR1 | 28.35 |
GSK943
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| 5-HT2C | HTR2C | -11.01 | ||
| 5-HT3 | HTR3A | 10.62 | ||
| 5-HT5A | HTR5A | -11.19 | ||
| Beta2 | ADRB2 | 9.35 | ||
| DOR | OPRD1 | 17.07 | ||
| H1 | HRH1 | -1.58 | ||
| H2 | HRH2 | 4.49 | ||
| H3 | HRH3 | -5.65 | ||
| M1 | CHRM1 | 12.05 | ||
| M2 | CHRM2 | -7.30 | ||
| M3 | CHRM3 | 12.58 | ||
| M4 | CHRM4 | 6.19 | ||
| M5 | CHRM5 | 18.00 | ||
| SERT | SLC6A4 | -14.21 | ||
| Sigma 1 | SIGMAR1 | 10.21 | ||
| Alpha1A | ADRA1A | 7.39 | ||
| Alpha1B | ADRA1B | -0.98 | ||
| Alpha1D | ADRA1D | -7.87 | ||
| Alpha2A | ADRA2A | 13.75 | ||
| Alpha2B | ADRA2B | 22.80 | ||
| Alpha2C | ADRA2C | 7.66 | ||
| Sigma 2 | TMEM97 | 35.62 | ||
| 5-HT1A | HTR1A | 14.87 | ||
| 5-HT1B | HTR1B | -8.28 | ||
| 5-HT1D | HTR1D | -8.07 | ||
| 5-HT1E | HTR1E | 0.03 | ||
| 5-HT2A | HTR2A | 11.62 | ||
| 5-HT2B | HTR2B | -14.09 | ||
| 5-HT6 | HTR6 | -1.21 | ||
| 5-HT7A | HTR7 | 1.31 | ||
| D1 | DRD1 | -6.73 | ||
| D2 | DRD2 | -10.18 | ||
| D3 | DRD3 | 4.11 | ||
| D4 | DRD4 | 17.72 | ||
| D5 | DRD5 | -7.16 | ||
| DAT | SLC6A3 | -18.75 | ||
| H4 | HRH4 | -13.26 | ||
| KOR | OPRK1 | 41.06 | ||
| MOR | OPRM1 | 4.77 | ||
| NET | SLC6A2 | -37.31 | ||
| GABAA/BZP | 74.23 | 473.91 average (n=2) | 6.33 | |
| GABAA | 14.53 | |||
| GABA/PBR | -12.51 | |||
| Beta1 | ADRB1 | 6.93 | ||
| Beta3 | ADRB3 | 31.02 |
GSK973
A panel of bromodomain containing proteins (BCP) was screened in a dose-response format in duplicate.
Conclusion: GSK973 is selective for the BD2 domain of BET proteins (pKd > 8). Closest hits among other BCPs: TAF1 BD2 (pKd = 6.4), TAF1L BD2 (pKd = 5.7) and BRD9 (pKd = 5.7).
| Target protein | HGNC name | Species | pKd |
|---|---|---|---|
| ATAD2A | ATAD2 | Homo sapiens | < 4.5 |
| ATAD2B | ATAD2B | Homo sapiens | < 4.5 |
| BAZ2A | BAZ2A | Homo sapiens | 5.5 |
| BAZ2B | BAZ2B | Homo sapiens | 5.1 |
| BRD1 | BRD1 | Homo sapiens | < 4.5 |
| BRD7 | BRD7 | Homo sapiens | < 4.5 |
| BRD8 (1) | BRD8 | Homo sapiens | < 4.5 |
| BRD8 (2) | BRD8 | Homo sapiens | < 4.5 |
| BRD9 | BRD9 | Homo sapiens | 5.7 |
| BRPF1 | BRPF1 | Homo sapiens | < 4.5 |
| BRPF3 | BRPF3 | Homo sapiens | < 4.5 |
| CECR2 | CECR2 | Homo sapiens | 5.5 |
| CREBBP | CREBBP | Homo sapiens | 4.6 |
| EP300 | EP300 | Homo sapiens | < 4.5 |
| FALZ | BPTF | Homo sapiens | < 4.5 |
| GCN5L2 | KAT2A | Homo sapiens | 4.7 |
| PBRM1 (2) | PBRM1 | Homo sapiens | 4.7 |
| PBRM1 (5) | PBRM1 | Homo sapiens | 5.0 |
| PCAF | KAT2B | Homo sapiens | < 4.5 |
| SMARCA2 | SMARCA2 | Homo sapiens | 4.8 |
| SMARCA4 | SMARCA4 | Homo sapiens | 4.8 |
| TAF1 (2) | TAF1 | Homo sapiens | 6.4 |
| TAF1L (2) | TAF1L | Homo sapiens | 5.7 |
| TRIM24 (PHD, BD) | TRIM24 | Homo sapiens | 4.5 |
| TRIM33 (PHD,BD) | TRIM33 | Homo sapiens | < 4.5 |
| WDR9 (2) | BRWD1 | Homo sapiens | < 4.5 |
| BRD2 (BD1) | BRD2 | Homo sapiens | 5.3 |
| BRD2 (BD2) | BRD2 | Homo sapiens | 8.3 |
| BRD3 (BD1) | BRD3 | Homo sapiens | 5.2 |
| BRD3 (BD2) | BRD3 | Homo sapiens | 8.5 |
| BRD4 (BD1) | BRD4 | Homo sapiens | 5.6 |
| BRD4 (BD2) | BRD4 | Homo sapiens | 8.7 |
| BRDT (BD1) | BRDT | Homo sapiens | 5.4 |
| BRDT (BD2) | BRDT | Homo sapiens | 8.3 |