Selectivity data for probe BI-5121 and control BI-6199
Coming soon
BI-5121
Conclusion: Clean with the closest off-target OPRK1 with 45 % control at 10 µM.
| Target protein | HGNC name | Species | % control at 10 µM | % control at 30 µM | % control at 3 µM | % control at 1 µM | % control at 0.3 µM | Mode of action | Assay |
|---|---|---|---|---|---|---|---|---|---|
| 5HT1A/H | HTR1A | Hono sapiens | 89.0 | Radioactive Assay | |||||
| 5HT1B/R | HTR1B | Rattus norvegicus | 112.0 | inhibitor | Radioactive Assay | ||||
| 5HT2AH_AGON | HTR2A | Homo sapiens | 106.0 | agonist | Scintillation counting | ||||
| 5HT2B/H AG | HTR2B | Homo sapiens | 111.0 | agonist | Radioactive Assay | ||||
| 5HT3/H | HTR3A | Homo sapiens | 100.0 | inhibitor | Radioactive Assay | ||||
| A2A/H | ADORA2A | Homo sapiens | 113.0 | antagonist | Radioligand Binding | ||||
| ACE(HU_AMTCH400) | ACHE | Homo sapiens | 103.0 | Photometry | |||||
| ALPHA1AH_ANTAG | ADRA1A | Homo sapiens | 99.0 | antagonist | Scintillation counting | ||||
| ALPHA2A/HU | ADRA2A | Homo sapiens | 98.0 | inhibitor | Radioactive Assay | ||||
| ANDROGEN/H | AR | Homo sapiens | 105.0 | Radioactive Assay | |||||
| BETA1/HUM | ADRB1 | Homo sapiens | 96.0 | Radioactive Assay | |||||
| BETA2/HUM | ADRB2 | Homo sapiens | 91.0 | antagonist | Radioactive Assay | ||||
| BZD/CENTR/R | Rattus norvegicus | 101.0 | Radioactive Assay | ||||||
| CA+/PAASITE | CACNA1C | Rattus norvegicus | 76.0 | inhibitor | Radioactive Assay | ||||
| CB1/CENTR/H | CNR1 | Homo sapiens | 117.0 | Radioactive Assay | |||||
| CB2/PERIPH/H | CNR2 | Homo sapiens | 130.0 | Radioactive Assay | |||||
| CCKA/H | CCKAR | Homo sapiens | 102.0 | Radioactive Assay | |||||
| COX-1 | PTGS1 | Homo sapiens | 99.0 | inhibitor | Fluorimetry | ||||
| COX-2 | PTGS2 | Homo sapiens | 132.0 | inhibitor | Fluorimetry | ||||
| D1/H | DRD1 | Homo sapiens | 120.0 | antagonist | Radioactive Assay | ||||
| D2L/H | DRD2 | Homo sapiens | 84.0 | agonist | Radioactive Assay | ||||
| DATRANS/HUM | SLC6A3 | Homo sapiens | 88.0 | inhibitor | Radioactive Assay | ||||
| DELTA2/H | OPRD1 | Homo sapiens | 88.0 | inhibitor | Radioactive Assay | ||||
| ETA/H | EDNRA | Homo sapiens | 103.0 | Radioactive Assay | |||||
| GCORTICOID/H | NR3C1 | Homo sapiens | 102.0 | inhibitor | Radioactive Assay | ||||
| H1/PYRIL/HS | HRH1 | Homo sapiens | 113.0 | Radioactive Assay | |||||
| H2/APT/HS | HRH2 | Homo sapiens | 108.0 | antagonist | Radioactive Assay | ||||
| HERG_DOFETILIDE | KCNH2 | Homo sapiens | 110.0 | inhibitor | Scintillation counting | ||||
| K+/VOLT/RA | KCNV1 | Rattus norvegicus | 99.0 | inhibitor | Radioactive Assay | ||||
| KAPPA(KOP)ANTAG | OPRK1 | Homo sapiens | 85.0 | 87.00 | 86.00 | 83.00 | 99.00 | antagonist | Scintillation counting |
| KAPPA/R | OPRK1 | Rattus norvegicus | 45.0 | inhibitor | Radioactive Assay | ||||
| LCK_CE | LCK | Homo sapiens | 107.0 | inhibitor | lanthanide chelation excitation | ||||
| M1/H | CHRM1 | Homo sapiens | 100.0 | Radioactive Assay | |||||
| M2/H | CHRM2 | Homo sapiens | 103.0 | antagonist | Radioactive Assay | ||||
| M3/H | CHRM3 | Homo sapiens | 93.0 | Radioactive Assay | |||||
| MAO-A_ANTAG | MAOA | Rattus norvegicus | 103.0 | antagonist | Scintillation counting | ||||
| MU/H | OPRM1 | Homo sapiens | 70.0 | inhibitor | Radioactive Assay | ||||
| NA+/SITE2/R | SCN1B | Rattus norvegicus | 100.0 | Radioactive Assay | |||||
| NEUP/H | SLC6A2 | Homo sapiens | 99.0 | inhibitor | Radioactive Assay | ||||
| NMDA/R | Rattus norvegicus | 102.0 | inhibitor | Radioactive Assay | |||||
| N_NEURO_A4B2 |
CHRNA4 CHRNB2 |
110.0 | agonist | Radioligand Binding | |||||
| PDE3A | PDE3A | 100.0 | inhibitor | HTRF-homogeneous time resolved fluoresce | |||||
| PDE4D2 | PDE4D | 106.0 | inhibitor | Scintillation counting | |||||
| SLC6A4/H | SLC6A4 | Homo sapiens | 100.0 | antagonist | Scintillation counting | ||||
| V1A/HUM | AVPR1A | Homo sapiens | 93.0 | inhibitor | Radioactive Assay | ||||
| 5HT2C/HU | HTR2C | Homo sapiens | 81.0 | Radioactive Assay | |||||
| A1/HU | ADORA1 | Homo sapiens | 100.0 | Radioactive Assay | |||||
| ALPHA1B/R | ADRA1B | Rattus norvegicus | 118.0 | Radioactive Assay | |||||
| ALPHA1D/H | ADRA1D | Homo sapiens | 96.0 | Others | |||||
| ALPHA2B/H | ADRA2B | Homo sapiens | 105.0 | ||||||
| AMPA/RA | GRIA1 | Rattus norvegicus | 85.0 | ||||||
| ANGIOCONVENZ | ACE | Oryctolagus cuniculus | 86.0 | inhibitor | Photometry | ||||
| AT1/HU | AGTR1 | Homo sapiens | 109.0 | Radioligand Binding | |||||
| ATP NA+/K+PI | ATP1A1 | Sus scrofa | 94.0 | inhibitor | Spectrofluorimetry | ||||
| ATRANS | Cavia porcellus | 97.0 | Radioactive Assay | ||||||
| B2/H | BDKRB2 | Homo sapiens | 102.0 | antagonist | Radioligand Binding | ||||
| CA+/N/RA | CACNA1B | Rattus norvegicus | 98.0 | Radioactive Assay | |||||
| CCK2 | CCKBR | Homo sapiens | 96.0 | Radioligand Binding | |||||
| CCR1 | CCR1 | Homo sapiens | 105.0 | Radioligand Binding | |||||
| CXCR2/H | CXCR2 | Homo sapiens | 103.0 | Radioactive Assay | |||||
| CYSLT1_HS | CYSLTR1 | Homo sapiens | 100.0 | Radioactive Assay | |||||
| ERALPHA/H | ESR1 | Homo sapiens | 95.0 | Radioactive Assay | |||||
| GABAACL+ | GABRA1 | Rattus norvegicus | 109.0 | Radioactive Assay | |||||
| GABAA_RO | GABRR1 | Homo sapiens | 92.0 | Radioactive Assay | |||||
| GABATRANS/RA | SLC6A1 | Rattus norvegicus | 101.0 | Radioactive Assay | |||||
| GABA_B1A | GABRB1 | Homo sapiens | 82.0 | Radioactive Assay | |||||
| GLYCINSTRS | GLRA1 | Rattus norvegicus | 106.0 | Radioactive Assay | |||||
| K+/KATP/HA | KCNJ1 | Mullus auratus | 99.0 | Radioactive Assay | |||||
| KAINATE/R | GRIK1 | Rattus norvegicus | 96.0 | Radioactive Assay | |||||
| M4/HU | CHRM4 | Homo sapiens | 98.0 | Radioactive Assay | |||||
| MAOB | MAOB | Homo sapiens | 91.0 | inhibitor | FI - fluorescence intensity | ||||
| MC1_HS | MC1R | Homo sapiens | 99.0 | Radioactive Assay | |||||
| MC4/H | MC4R | Homo sapiens | 95.0 | Radioactive Assay | |||||
| MGLU5 | GRM5 | Homo sapiens | 83.0 | Radioactive Assay | |||||
| NACH/H | CHRNA1 | Homo sapiens | 105.0 | Radioligand Binding | |||||
| NACH_BS_N/H |
CHRNA1 CHRNB1 |
Homo sapiens | 98.0 | Radioactive Assay | |||||
| NK1/HU | TACR1 | Homo sapiens | 97.0 | Radioligand Binding | |||||
| NMDAGLSI/RA | GRIN1 | Rattus norvegicus | 96.0 | inhibitor | Scintillation counting | ||||
| NMDAPHSI/R | GRIN2A | Rattus norvegicus | 96.0 | inhibitor | Radioactive Assay | ||||
| ORL1/HU | OPRL1 | Homo sapiens | 97.0 | Others | |||||
| PAF/H | PTAFR | Homo sapiens | 103.0 | Radioactive Assay | |||||
| PEPCATHEPSG | CTSG | Homo sapiens | 103.0 | inhibitor | FI - fluorescence intensity | ||||
| PKC | Homo sapiens | 80.0 | inhibitor | Radioactive Assay | |||||
| PPARGHU | PPARG | Homo sapiens | 101.0 | activator | Radioligand Binding | ||||
| PROGESTERONE_PR-B | PGR | Homo sapiens | 111.0 | inhibitor | Radioligand Binding | ||||
| PTK_INSULIN | PTK2B | Bos taurus | 107.0 | Scintillation counting | |||||
| Y1/HU | NPY1R | Homo sapiens | 99.0 | Radioactive Assay |
BI-6199
Conclusion: Clean with the closest off-target OPRK1 with 44 % control at 10 µM.
| Target protein | HGNC name | Species | % control at 10 µM | Mode of action | Assay |
|---|---|---|---|---|---|
| 5HT1A/H | HTR1A | Homo sapiens | 89.0 | Radioactive Assay | |
| 5HT1B(H) | HTR1B | Homo sapiens | 92.0 | antagonist | Scintillation counting |
| 5HT2AH_AGON | HTR2A | Homo sapiens | 102.0 | agonist | Scintillation counting |
| 5HT2B/H AG | HTR2B | Homo sapiens | 77.0 | agonist | Radioactive Assay |
| 5HT3/H | HTR3A | Homo sapiens | 107.0 | inhibitor | Radioactive Assay |
| A2A/H | ADORA2A | Homo sapiens | 99.0 | antagonist | Radioligand Binding |
| ACE(HU_AMTCH400) | ACHE | Homo sapiens | 103.0 | Photometry | |
| ALPHA1AH_ANTAG | ADRA1A | Homo sapiens | 113.0 | antagonist | Scintillation counting |
| ALPHA2A/HU | ADRA2A | Homo sapiens | 106.0 | inhibitor | Radioactive Assay |
| ANDROGEN/H | AR | Homo sapiens | 97.0 | Radioactive Assay | |
| BETA1/HUM | ADRB1 | Homo sapiens | 99.0 | Radioactive Assay | |
| BETA2/HUM | ADRB2 | Homo sapiens | 103.0 | antagonist | Radioactive Assay |
| BZD/CENTR/R | Rattus norvegicus | 103.0 | Radioactive Assay | ||
| CA+/DHPSI/R | CACNA1C | Rattus norvegicus | 109.0 | inhibitor | Radioactive Assay |
| CB1(HU)_AGON | CNR1 | Homo sapiens | 138.0 | agonist | Scintillation counting |
| CB2/PERIPH/H | CNR2 | Homo sapiens | 105.0 | Radioactive Assay | |
| CCKA/H | CCKAR | Homo sapiens | 89.0 | Radioactive Assay | |
| COX-1 | PTGS1 | Homo sapiens | 83.0 | inhibitor | Fluorimetry |
| COX-2 | PTGS2 | Homo sapiens | 106.0 | inhibitor | Fluorimetry |
| D1/H | DRD1 | Homo sapiens | 98.0 | antagonist | Radioactive Assay |
| D2SH_AGON | DRD2 | Homo sapiens | 100.0 | agonist | Scintillation counting |
| DATRANS/HUM | SLC6A3 | Homo sapiens | 113.0 | inhibitor | Radioactive Assay |
| DELTA2/H | OPRD1 | Homo sapiens | 96.0 | inhibitor | Radioactive Assay |
| ETA/H | EDNRA | Homo sapiens | 103.0 | Radioactive Assay | |
| GCORTICOID/H | NR3C1 | Homo sapiens | 95.0 | inhibitor | Radioactive Assay |
| H1/PYRIL/HS | HRH1 | Homo sapiens | 98.0 | Radioactive Assay | |
| H2/APT/HS | HRH2 | Homo sapiens | 113.0 | antagonist | Radioactive Assay |
| HERG_DOFETILIDE | KCNH2 | Homo sapiens | 121.0 | inhibitor | Scintillation counting |
| K+/VOLT/RA | KCNV1 | Rattus norvegicus | 109.0 | inhibitor | Radioactive Assay |
| KAPPA(KOP)_HU | OPRK1 | Homo sapiens | 44.0 | inhibitor | Radioactive Assay |
| LCK_CE | LCK | Homo sapiens | 103.0 | inhibitor | lanthanide chelation excitation |
| M1/H | CHRM1 | Homo sapiens | 94.0 | Radioactive Assay | |
| M2/H | CHRM2 | Homo sapiens | 95.0 | antagonist | Radioactive Assay |
| M3/H | CHRM3 | Homo sapiens | 110.0 | Radioactive Assay | |
| MAO-A_ANTAG | MAOA | Homo sapiens | 102.0 | antagonist | Scintillation counting |
| MU/H | OPRM1 | Homo sapiens | 105.0 | inhibitor | Radioactive Assay |
| NA+/SITE2/R | SCN1B | Rattus norvegicus | 122.0 | Radioactive Assay | |
| NEUP/H | SLC6A2 | Homo sapiens | 112.0 | inhibitor | Radioactive Assay |
| NMDA/R | Rattus norvegicus | 88.0 | inhibitor | Radioactive Assay | |
| N_NEURO_A4B2 |
CHRNA4 CHRNB2 |
Homo sapiens | 99.0 | agonist | Radioligand Binding |
| PDE3A | PDE3A | Homo sapiens | 119.0 | inhibitor | HTRF-homogeneous time resolved fluoresce |
| PDE4D2 | PDE4D | Homo sapiens | 99.0 | inhibitor | Scintillation counting |
| SLC6A4/H | SLC6A4 | Homo sapiens | 104.0 | antagonist | Scintillation counting |
| V1A/HUM | AVPR1A | Homo sapiens | 90.0 | inhibitor | Radioactive Assay |