Selectivity data for probe (R)-ZINC-3573 and control (S)-ZINC-3573
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(R)-ZINC-3573
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| 5-HT2C | HTR2C | 2.22 | ||
| 5-HT3 | HTR3A | 76.60 | 2956.83 average (n=2) | 5.54 |
| 5-HT5A | HTR5A | 13.84 | ||
| Beta2 | ADRB2 | 14.38 | ||
| DAT | SLC6A3 | 74.32 | 1109.25 average (n=2) | 5.96 |
| DOR | OPRD1 | 34.28 | ||
| H1 | HRH1 | 39.34 | ||
| H2 | HRH2 | 31.91 | ||
| H3 | HRH3 | 38.64 | ||
| NET | SLC6A2 | 45.35 | ||
| SERT | SLC6A4 | 4.09 | ||
| 5-HT1A | HTR1A | 64.85 | 1621.89 average (n=2) | 5.80 |
| 5-HT1D | HTR1D | 58.43 | 1744.10 average (n=3) | 5.77 |
| 5-HT1E | HTR1E | 7.26 | ||
| 5-HT2A | HTR2A | 16.32 | ||
| 5-HT2B | HTR2B | 16.66 | ||
| 5-HT6 | HTR6 | 58.85 | 748.23 average (n=2) | 6.13 |
| 5-HT7A | HTR7 | 12.33 | ||
| D1 | DRD1 | 38.92 | ||
| D2 | DRD2 | 69.78 | 369.37 average (n=2) | 6.45 |
| D3 | DRD3 | 28.15 | ||
| 5-HT1B | HTR1B | 52.51 | 3243.00 average (n=2) | 5.50 |
| Alpha1A | ADRA1A | 21.80 | ||
| Alpha1B | ADRA1B | 10.17 | ||
| Alpha1D | ADRA1D | 20.45 | ||
| Alpha2A | ADRA2A | 32.86 | ||
| Alpha2B | ADRA2B | 11.31 | ||
| Alpha2C | ADRA2C | 40.45 | ||
| M1 | CHRM1 | 5.27 | ||
| M2 | CHRM2 | 20.13 | ||
| M3 | CHRM3 | 11.68 | ||
| M4 | CHRM4 | 28.79 | ||
| M5 | CHRM5 | -3.76 | ||
| Sigma 1 | SIGMAR1 | 28.62 | ||
| Sigma 2 | TMEM97 | 82.37 | 489.44 average (n=2) | 6.32 |
| D4 | DRD4 | 32.64 | ||
| D5 | DRD5 | 6.36 | ||
| H4 | HRH4 | 7.75 | ||
| KOR | OPRK1 | 13.56 | ||
| MOR | OPRM1 | 21.28 | ||
| GABAA/BZP | 54.94 | 1937.43 average (n=2) | 5.73 | |
| GABAA | 37.31 | |||
| GABA/PBR | 11.59 | |||
| Beta1 | ADRB1 | 30.73 | ||
| Beta3 | ADRB3 | 12.65 |
(S)-ZINC-3573
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| 5-HT2C | HTR2C | -3.16 | ||
| 5-HT3 | HTR3A | 64.51 | 3626.13 average (n=2) | 5.45 |
| 5-HT5A | HTR5A | 5.42 | ||
| Beta2 | ADRB2 | 27.43 | ||
| DOR | OPRD1 | 2.89 | ||
| H1 | HRH1 | 16.43 | ||
| H2 | HRH2 | 29.97 | ||
| H3 | HRH3 | 13.43 | ||
| M1 | CHRM1 | 42.75 | ||
| M3 | CHRM3 | 29.41 | ||
| M4 | CHRM4 | 34.36 | ||
| M5 | CHRM5 | 40.39 | ||
| SERT | SLC6A4 | 2.83 | ||
| Alpha1A | ADRA1A | 34.22 | ||
| Alpha1B | ADRA1B | 59.06 | 2293.60 average (n=2) | 5.68 |
| Alpha1D | ADRA1D | 33.49 | ||
| Alpha2A | ADRA2A | 40.25 | ||
| Alpha2B | ADRA2B | 9.93 | ||
| Alpha2C | ADRA2C | 16.42 | ||
| M2 | CHRM2 | 26.63 | ||
| Sigma 1 | SIGMAR1 | 22.00 | ||
| Sigma 2 | TMEM97 | 65.12 | 972.86 average (n=2) | 6.01 |
| 5-HT1A | HTR1A | 19.26 | ||
| 5-HT1B | HTR1B | 4.88 | ||
| 5-HT1D | HTR1D | 63.16 | 2961.88 average (n=2) | 5.54 |
| 5-HT1E | HTR1E | -16.38 | ||
| 5-HT2A | HTR2A | 23.50 | ||
| 5-HT2B | HTR2B | 33.26 | ||
| 5-HT6 | HTR6 | 69.10 | 1092.22 average (n=2) | 5.97 |
| 5-HT7A | HTR7 | 7.57 | ||
| D1 | DRD1 | -14.53 | ||
| D2 | DRD2 | 2.85 | ||
| D3 | DRD3 | 39.01 | ||
| D4 | DRD4 | 8.30 | ||
| D5 | DRD5 | 3.36 | ||
| DAT | SLC6A3 | -1.89 | ||
| H4 | HRH4 | 12.38 | ||
| KOR | OPRK1 | 6.22 | ||
| MOR | OPRM1 | 9.07 | ||
| NET | SLC6A2 | 2.02 | ||
| GABAA/BZP | 21.52 | |||
| GABAA | -12.49 | |||
| GABA/PBR | 2.83 | |||
| Beta1 | ADRB1 | 4.16 | ||
| Beta3 | ADRB3 | 18.95 |