Selectivity data for probe BI-113823 and control BI-5832
Coming soon
BI-113823
Conclusion: The data are from Panlabs. Closest off-targets are SIGMAR1 (70 % inh.), TMEM97 (55 % inh.)
| Target protein | HGNC name | Species | % control at 10 µM | Mode of action | Assay |
|---|---|---|---|---|---|
| 5HT1A/HU | HTR1A | Homo sapiens | 99.0 | Radioactive Assay | |
| 5HT3/HU | HTR3A | Homo sapiens | 91.0 | Others | |
| 5HTTRANS/HU | SLC6A4 | Homo sapiens | 108.0 | Radioactive Assay | |
| A1/HU | ADORA1 | Homo sapiens | 99.0 | Radioactive Assay | |
| A2A/HU | ADORA2A | Homo sapiens | 97.0 | ||
| A3/H | ADORA3 | Homo sapiens | 101.0 | ||
| ALPHA1A/R | ADRA1A | Rattus norvegicus | 118.0 | Others | |
| ALPHA1B/R | ADRA1B | Rattus norvegicus | 96.0 | Radioactive Assay | |
| ALPHA1D/H | ADRA1D | Homo sapiens | 96.0 | Others | |
| ALPHA2A/H | ADRA2A | Homo sapiens | 85.0 | Radioactive Assay | |
| AT1/HU | AGTR1 | Homo sapiens | 115.0 | Radioligand Binding | |
| B1/H | BDKRB1 | Homo sapiens | 22.0 | Radioactive Assay | |
| B2/HU | BDKRB2 | Homo sapiens | 108.0 | Radioactive Assay | |
| BETA1/HU | ADRB1 | Homo sapiens | 105.0 | Radioactive Assay | |
| BETA2/HU | ADRB2 | Homo sapiens | 103.0 | Radioactive Assay | |
| CA+/DILSI/RA | CACNA1C | Rattus norvegicus | 86.0 | Radioactive Assay | |
| CA+/N/RA | CACNA1B | Rattus norvegicus | 100.0 | Radioactive Assay | |
| CYSLT1_HS | CYSLTR1 | Homo sapiens | 95.0 | Radioactive Assay | |
| D1/HU | DRD1 | Homo sapiens | 97.0 | Radioactive Assay | |
| D2S/HU | DRD2 | Homo sapiens | 105.0 | Radioligand Binding | |
| D3/HU | DRD3 | Homo sapiens | 86.0 | Radioactive Assay | |
| D4.2/H | DRD4 | Homo sapiens | 101.0 | Radioactive Assay | |
| DATRANS/H | SLC6A3 | Homo sapiens | 103.0 | inhibitor | Radioactive Assay |
| DELTA/HU | OPRD1 | Homo sapiens | 86.0 | Radioactive Assay | |
| EGF/HU | EGFR | Homo sapiens | 125.0 | Radioactive Assay | |
| EP4/H | PTGER4 | Homo sapiens | 93.0 | Radioactive Assay | |
| ERALPHA/H | ESR1 | Homo sapiens | 104.0 | Radioactive Assay | |
| ETA/HU | EDNRA | Homo sapiens | 96.0 | Radioactive Assay | |
| ETB/HUM | EDNRB | Homo sapiens | 104.0 | Radioactive Assay | |
| GABAACENTR | GABRA1 | Rattus norvegicus | 96.0 | Radioactive Assay | |
| GABATRANS/RA | SLC6A1 | Rattus norvegicus | 119.0 | Radioactive Assay | |
| GABA_B1A | GABRB1 | Homo sapiens | 98.0 | Radioactive Assay | |
| GLUCOCORTICO | NR3C1 | Homo sapiens | 103.0 | Radioactive Assay | |
| GPR103 | QRFPR | Homo sapiens | 105.0 | Radioactive Assay | |
| H1/H | HRH1 | Homo sapiens | 85.0 | Radioactive Assay | |
| H2/H | HRH2 | Homo sapiens | 93.0 | Radioactive Assay | |
| H3/H | HRH3 | Homo sapiens | 77.0 | Radioactive Assay | |
| I2/CENTR/R | GNAI2 | Rattus norvegicus | 60.0 | Radioactive Assay | |
| IL-1ALPHA/M | IL1R1 | Mus musculus | 79.0 | Others | |
| K+/HERG | KCNH2 | Homo sapiens | 70.0 | Radioactive Assay | |
| K+/KATP/HA | KCNJ1 | Cricetinae | 90.0 | Radioactive Assay | |
| KAINATE/R | GRIK1 | Rattus norvegicus | 93.0 | Radioactive Assay | |
| KAPPA/HU | OPRK1 | Homo sapiens | 99.0 | Radioactive Assay | |
| M1/HU | CHRM1 | Homo sapiens | 88.0 | Radioactive Assay | |
| M2/HU | CHRM2 | Homo sapiens | 61.0 | Radioactive Assay | |
| M3/HU | CHRM3 | Homo sapiens | 84.0 | Radioactive Assay | |
| MT1/H | MTNR1A | Homo sapiens | 97.0 | Radioactive Assay | |
| MU/HU | OPRM1 | Homo sapiens | 91.0 | Radioactive Assay | |
| NA+/SITE2/RA | SCN1B | Rattus norvegicus | 82.0 | Radioactive Assay | |
| NACH/H | CHRNA1 | Homo sapiens | 100.0 | Radioligand Binding | |
| NACH_BS_N/H |
CHRNA1 CHRNB1 |
Homo sapiens | 96.0 | Radioactive Assay | |
| NETRANS/H | SLC6A2 | Homo sapiens | 114.0 | Radioactive Assay | |
| NK1/HU | TACR1 | Homo sapiens | 109.0 | Radioactive Assay | |
| NMDAAGSI/RA | Rattus norvegicus | 92.0 | agonist | Radioactive Assay | |
| NMDAGLSI/RA | GRIN1 | Rattus norvegicus | 93.0 | inhibitor | Scintillation counting |
| NMDAPHSI/R | GRIN2A | Rattus norvegicus | 111.0 | Radioactive Assay | |
| P2X/RB | P2RX1 | Oryctolagus cuniculus | 100.0 | Radioactive Assay | |
| P2Y/RAT | P2RY1 | Rattus norvegicus | 108.0 | Radioactive Assay | |
| PAF/H | PTAFR | Homo sapiens | 87.0 | Radioactive Assay | |
| PHORBOLE/M | PRKCA | Mus musculus | 102.0 | inhibitor | Radioactive Assay |
| ROLIPRAM/R | PDE4A | Rattus norvegicus | 84.0 | Radioligand Binding | |
| SIGMA1/HU | SIGMAR1 | Homo sapiens | 30.0 | Radioactive Assay | |
| SIGMA2/R | TMEM97 | Rattus norvegicus | 45.0 | Radioactive Assay | |
| TESTOST/RA | AR | Rattus norvegicus | 96.0 | Others | |
| THYROID HORM | THRA | Homo sapiens | 84.0 | Radioactive Assay | |
| Y1/HU | NPY1R | Homo sapiens | 109.0 | Radioactive Assay | |
| Y2/HU | NPY2R | Homo sapiens | 111.0 | Radioactive Assay |
BI-5832
The data are from Cerep.
Conclusion: Clean panel except for OPRK1 (58 % inh.)
| Target protein | HGNC name | Species | Cmp. conc. | % Control | Assay ID |
|---|---|---|---|---|---|
| 5HT1B(H) | HTR1B | Homo sapiens | 10 µM | 92.0 | Cerep_4376 |
| CB1(HU)_AGON | CNR1 | Homo sapiens | 10 µM | 137.0 | Cerep_4708 |
| COX-1 | PTGS1 | Homo sapiens | 10 µM | 85.0 | Cerep_4173 |
| COX-2 | PTGS2 | Homo sapiens | 10 µM | 98.0 | Cerep_4186 |
| KAPPA(KOP)_HU | OPRK1 | Homo sapiens | 10 µM | 42.0 | Cerep_4461 |
| 5HT1A/H | HTR1A | Homo sapiens | 10 µM | 99.0 | Cerep_131 |
| 5HT2AH_AGON | HTR2A | Homo sapiens | 10 µM | 108.0 | Cerep_471 |
| 5HT2B/H AG | HTR2B | Homo sapiens | 10 µM | 81.0 | Cerep_1333 |
| 5HT3/H | HTR3A | Homo sapiens | 10 µM | 93.0 | Cerep_411 |
| A2A/H | ADORA2A | Homo sapiens | 10 µM | 124.0 | Cerep_4 |
| ACE(HU_AMTCH400) | ACE | Homo sapiens | 10 µM | 97.0 | Cerep_3441 |
| ALPHA1AH_ANTAG | ADRA1A | Homo sapiens | 10 µM | 91.0 | Cerep_2338 |
| ALPHA2A/HU | ADRA2A | Homo sapiens | 10 µM | 90.0 | Cerep_13 |
| ANDROGEN/H | AR | Homo sapiens | 10 µM | 90.0 | Cerep_933 |
| BETA1/HUM | ADRB1 | Homo sapiens | 10 µM | 97.0 | Cerep_18 |
| BETA2/HUM | ADRB2 | Homo sapiens | 10 µM | 101.0 | Cerep_20 |
| BZD/CENTR/R | Rattus norvegicus | 10 µM | 105.0 | Cerep_28 | |
| CA+/DHPSI/R | Rattus norvegicus | 10 µM | 120.0 | Cerep_161 | |
| CB2/PERIPH/H | CNR2 | Homo sapiens | 10 µM | 106.0 | Cerep_37 |
| CCKA/H | CCKAR | Homo sapiens | 10 µM | 85.0 | Cerep_39 |
| D1/H | DRD1 | Homo sapiens | 10 µM | 94.0 | Cerep_44 |
| D2SH_AGON | DRD2 | Homo sapiens | 10 µM | 97.0 | Cerep_1322 |
| DATRANS/HUM | SLC6A3 | Homo sapiens | 10 µM | 98.0 | Cerep_52 |
| DELTA2/H | OPRD1 | Homo sapiens | 10 µM | 87.0 | Cerep_114 |
| ETA/H | EDNRA | Homo sapiens | 10 µM | 109.0 | Cerep_54 |
| GCORTICOID/H | NR3C1 | Homo sapiens | 10 µM | 102.0 | Cerep_469 |
| H1/PYRIL/HS | HRH1 | Homo sapiens | 10 µM | 104.0 | Cerep_870 |
| H2/APT/HS | HRH2 | Homo sapiens | 10 µM | 113.0 | Cerep_1208 |
| HERG_DOFETILIDE | KCNH2 | Homo sapiens | 10 µM | 63.0 | Cerep_4094 |
| K+/VOLT/RA | Rattus norvegicus | 10 µM | 98.0 | Cerep_166 | |
| LCK_CE | LCK | Homo sapiens | 10 µM | 94.0 | Old_Cerep_2906 |
| M1/H | CHRM1 | Homo sapiens | 10 µM | 89.0 | Cerep_91 |
| M2/H | CHRM2 | Homo sapiens | 10 µM | 67.0 | Cerep_93 |
| M3/H | CHRM3 | Homo sapiens | 10 µM | 92.0 | Cerep_95 |
| MAO-A_ANTAG | MAOA | Rattus norvegicus | 10 µM | 106.0 | Cerep_443 |
| MU/H | OPRM1 | Homo sapiens | 10 µM | 96.0 | Cerep_118 |
| NA+/SITE2/R | Rattus norvegicus | 10 µM | 87.0 | Old_Cerep_169 | |
| NEUP/H | SLC6A2 | Homo sapiens | 10 µM | 93.0 | Cerep_355 |
| NMDA/R | Rattus norvegicus | 10 µM | 112.0 | Cerep_66 | |
| N_NEURO_A4B2 |
CHRNA4 CHRNB2 |
Homo sapiens | 10 µM | 98.0 | Cerep_3029 |
| PDE3A | PDE3A | Homo sapiens | 10 µM | 105.0 | Cerep_4072 |
| PDE4D2 | PDE4D | Homo sapiens | 10 µM | 104.0 | Cerep_4077 |
| SLC6A4/H | SCL6A4 | Homo sapiens | 10 µM | 103.0 | Cerep_439 |
| V1A/HUM | AVPR1A | Homo sapiens | 10 µM | 87.0 | Cerep_159 |