Selectivity data for probe TP-040 and control TP-040n
Jump to control PDSP data
TP-040
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| GABAA | 2.33 | |||
| 5-HT1E | HTR1E | 3.36 | ||
| 5-HT2C | HTR2C | 89.24 | 373.79 average (n=2) | 6.44 |
| 5-HT3 | HTR3A | 27.73 | ||
| 5-HT5A | HTR5A | 23.96 | ||
| 5-HT6 | HTR6 | 32.15 | ||
| 5-HT7A | HTR7 | 34.61 | ||
| Alpha2A | ADRA2A | 12.79 | ||
| Alpha2B | ADRA2B | 56.30 | 2570.64 average (n=2) | 5.59 |
| Alpha2C | ADRA2C | 51.76 | 3432.79 average (n=2) | 5.47 |
| Beta3 | ADRB3 | -18.26 | ||
| GABAA/BZP | 67.44 | 511.70 average (n=2) | 6.30 | |
| D2 | DRD2 | 4.96 | ||
| D4 | DRD4 | 3.89 | ||
| DAT | SLC6A3 | 20.61 | ||
| DOR | OPRD1 | 4.65 | ||
| KOR | OPRK1 | 36.63 | ||
| MOR | OPRM1 | 10.84 | ||
| SERT | SLC6A4 | 5.83 | ||
| Sigma 1 | SIGMAR1 | 36.59 | ||
| 5-HT2A | HTR2A | 33.84 | ||
| 5-HT2B | HTR2B | 81.84 | 699.39 average (n=2) | 6.16 |
| Alpha1A | ADRA1A | 15.44 | ||
| Alpha1B | ADRA1B | -5.62 | ||
| Alpha1D | ADRA1D | 25.10 | ||
| Beta1 | ADRB1 | 3.97 | ||
| Beta2 | ADRB2 | -3.61 | ||
| D1 | DRD1 | -8.84 | ||
| D3 | DRD3 | 47.01 | ||
| D5 | DRD5 | 5.03 | ||
| H1 | HRH1 | 40.15 | ||
| H2 | HRH2 | 28.57 | ||
| H3 | HRH3 | 35.13 | ||
| H4 | HRH4 | -31.32 | ||
| M1 | CHRM1 | 17.24 | ||
| M2 | CHRM2 | 7.21 | ||
| M3 | CHRM3 | 7.48 | ||
| M4 | CHRM4 | 20.62 | ||
| M5 | CHRM5 | 25.06 | ||
| NET | SLC6A2 | 75.75 | 1935.54 average (n=2) | 5.72 |
| GABA/PBR | 17.91 | |||
| 5-HT1A | HTR1A | 29.99 | ||
| Sigma 2 | TMEM97 | 33.65 | ||
| 5-HT1B | HTR1B | 24.39 | ||
| 5-HT1D | HTR1D | 81.86 | 417.50 average (n=2) | 6.20 |
TP-040n
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| Alpha1B | ADRA1B | 22.14 | ||
| 5-HT1E | HTR1E | 19.53 | ||
| 5-HT2C | HTR2C | 94.84 | 266.79 average (n=2) | 6.59 |
| 5-HT3 | HTR3A | 22.40 | ||
| 5-HT5A | HTR5A | 59.81 | 6131.61 average (n=2) | 5.29 |
| 5-HT6 | HTR6 | 80.39 | 606.40 average (n=2) | 6.22 |
| 5-HT7A | HTR7 | 92.37 | 334.53 average (n=2) | 6.48 |
| Alpha2A | ADRA2A | 34.59 | ||
| Alpha2B | ADRA2B | 98.03 | 475.35 average (n=2) | 6.37 |
| Alpha2C | ADRA2C | 96.85 | 414.29 average (n=2) | 6.39 |
| GABAA/BZP | 22.89 | |||
| D2 | DRD2 | 20.55 | ||
| D4 | DRD4 | 13.01 | ||
| DAT | SLC6A3 | 98.00 | 864.98 average (n=2) | 6.08 |
| DOR | OPRD1 | 8.02 | ||
| KOR | OPRK1 | 23.72 | ||
| MOR | OPRM1 | 25.94 | ||
| SERT | SLC6A4 | 35.77 | ||
| Sigma 1 | SIGMAR1 | 98.80 | 125.10 average (n=2) | 6.91 |
| 5-HT2A | HTR2A | 72.87 | 757.58 average (n=2) | 6.16 |
| 5-HT2B | HTR2B | 91.72 | 290.75 average (n=2) | 6.55 |
| Alpha1A | ADRA1A | 19.16 | ||
| Alpha1D | ADRA1D | 25.99 | ||
| Beta1 | ADRB1 | 6.05 | ||
| Beta2 | ADRB2 | -3.49 | ||
| Beta3 | ADRB3 | 2.45 | ||
| D1 | DRD1 | 26.47 | ||
| D3 | DRD3 | 22.62 | ||
| D5 | DRD5 | -20.80 | ||
| GABAA | 34.64 | |||
| H1 | HRH1 | 41.58 | ||
| H2 | HRH2 | 95.59 | 148.82 average (n=2) | 6.84 |
| H3 | HRH3 | 86.19 | 99.57 average (n=4) | 7.03 |
| H4 | HRH4 | 82.84 | 703.07 average (n=2) | 6.16 |
| M1 | CHRM1 | 18.60 | ||
| M3 | CHRM3 | -3.28 | ||
| M4 | CHRM4 | 25.87 | ||
| M5 | CHRM5 | 6.46 | ||
| NET | SLC6A2 | 93.82 | 3112.25 average (n=2) | 5.52 |
| GABA/PBR | -0.34 | |||
| 5-HT1A | HTR1A | 26.74 | ||
| M2 | CHRM2 | -1.51 | ||
| Sigma 2 | TMEM97 | 77.15 | 1463.21 average (n=2) | 5.84 |
| 5-HT1B | HTR1B | 45.86 | ||
| 5-HT1D | HTR1D | 53.24 | 2037.31 average (n=2) | 5.74 |