Selectivity data for probe KISS1-305 and control KISS1-543
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KISS1-305
Compound concentration: 1 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| 5-HT1A | HTR1A | 18.50 | ||
| 5-HT1B | HTR1B | 29.29 | ||
| 5-HT1D | HTR1D | 10.42 | ||
| 5-HT1E | HTR1E | 24.15 | ||
| 5-HT2A | HTR2A | -11.23 | ||
| 5-HT2B | HTR2B | 1.13 | ||
| 5-HT2C | HTR2C | 12.84 | ||
| 5-HT3 | HTR3A | -18.89 | ||
| 5-HT5A | HTR5A | 20.12 | ||
| 5-HT6 | HTR6 | 4.93 | ||
| 5-HT7A | HTR7 | -2.33 | ||
| D1 | DRD1 | -7.58 | ||
| D2 | DRD2 | 0.86 | ||
| D3 | DRD3 | -8.85 | ||
| D4 | DRD4 | -13.47 | ||
| D5 | DRD5 | 0.51 | ||
| SERT | SLC6A4 | 8.84 | ||
| NET | SLC6A2 | 5.40 | ||
| DAT | SLC6A3 | 12.03 | ||
| MOR | OPRM1 | -4.62 | ||
| DOR | OPRD1 | -32.27 | 47.50 average (n=2) | 7.35 |
| KOR | OPRK1 | -6.31 | ||
| H1 | HRH1 | 19.90 | ||
| H2 | HRH2 | 4.38 | ||
| H4 | HRH4 | 10.43 | ||
| Alpha1A | ADRA1A | -9.06 | ||
| Alpha1B | ADRA1B | -7.65 | ||
| Alpha2A | ADRA2A | 8.60 | ||
| Alpha2B | ADRA2B | 17.64 | ||
| Alpha2C | ADRA2C | 4.19 | ||
| Beta1 | ADRB1 | 0.56 | ||
| Beta2 | ADRB2 | 1.39 | ||
| M1 | CHRM1 | 2.17 | ||
| M2 | CHRM2 | 25.09 | ||
| M3 | CHRM3 | 10.65 | ||
| M4 | CHRM4 | 13.83 | ||
| M5 | CHRM5 | 14.89 | ||
| Beta3 | ADRB3 | 7.10 | ||
| GABAA/BZP | 13.58 | |||
| GABA/PBR | 31.45 | |||
| Alpha1D | ADRA1D | 13.91 | ||
| Sigma 2 | TMEM97 | -5.31 | ||
| Sigma 1 | SIGMAR1 | 3.72 | ||
| GABAA | 1.39 | |||
| H3 | HRH3 | 43.30 |
KISS1-543
Compound concentration: 1 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| GABAA | 15.48 | |||
| H3 | HRH3 | 12.51 | ||
| 5-HT1A | HTR1A | 30.92 | ||
| 5-HT1B | HTR1B | 30.97 | ||
| 5-HT1D | HTR1D | 12.38 | ||
| 5-HT1E | HTR1E | 27.88 | ||
| 5-HT2A | HTR2A | 16.91 | ||
| 5-HT2B | HTR2B | 11.34 | ||
| 5-HT2C | HTR2C | -2.67 | ||
| 5-HT3 | HTR3A | -8.29 | ||
| 5-HT5A | HTR5A | 16.33 | ||
| 5-HT6 | HTR6 | -0.51 | ||
| 5-HT7A | HTR7 | -6.69 | ||
| D1 | DRD1 | -0.60 | ||
| D2 | DRD2 | 9.67 | ||
| D3 | DRD3 | -3.90 | ||
| D4 | DRD4 | -9.83 | ||
| D5 | DRD5 | 29.20 | ||
| SERT | SLC6A4 | -0.41 | ||
| NET | SLC6A2 | -1.33 | ||
| DAT | SLC6A3 | 10.44 | ||
| MOR | OPRM1 | -7.85 | ||
| DOR | OPRD1 | -18.29 | ||
| KOR | OPRK1 | -5.75 | ||
| H1 | HRH1 | -16.98 | ||
| H2 | HRH2 | 3.31 | ||
| H4 | HRH4 | -3.39 | ||
| Alpha1A | ADRA1A | -12.48 | ||
| Alpha1B | ADRA1B | -2.08 | ||
| Alpha2A | ADRA2A | 10.17 | ||
| Alpha2B | ADRA2B | 14.49 | ||
| Alpha2C | ADRA2C | -0.48 | ||
| Beta1 | ADRB1 | 3.41 | ||
| Beta2 | ADRB2 | -2.89 | ||
| M1 | CHRM1 | 15.10 | ||
| M2 | CHRM2 | 40.72 | ||
| M3 | CHRM3 | 24.67 | ||
| M4 | CHRM4 | 18.48 | ||
| M5 | CHRM5 | 12.26 | ||
| Beta3 | ADRB3 | 2.70 | ||
| GABAA/BZP | 12.35 | |||
| GABA/PBR | 15.58 | |||
| Alpha1D | ADRA1D | 9.13 | ||
| Sigma 2 | TMEM97 | -8.74 | ||
| Sigma 1 | SIGMAR1 | 0.21 |