Selectivity data for probe BI-1915 and control BI-1920
Coming soon
BI-1915
Conclusion: Clean panel.
| Target protein | HGNC name | Species | Cmp. conc. | % Control | Assay ID |
|---|---|---|---|---|---|
| K+/VOLT/RA | Rattus norvegicus | 10 µM | 109.0 | Cerep_166 | |
| LCK_CE | LCK | Homo sapiens | 10 µM | 96.5 | Old_Cerep_2906 |
| M1/H | CHRM1 | Homo sapiens | 10 µM | 105.0 | Cerep_91 |
| M2/H | CHRM2 | Homo sapiens | 10 µM | 105.5 | Cerep_93 |
| 5HT1B(H) | HTR1B | Homo sapiens | 10 µM | 92.5 | Cerep_4376 |
| CB1(HU)_AGON | CNR1 | Homo sapiens | 10 µM | 116.0 | Cerep_4708 |
| COX-1 | PTGS1 | Homo sapiens | 10 µM | 112.0 | Cerep_4173 |
| COX-2 | PTGS2 | Homo sapiens | 10 µM | 104.0 | Cerep_4186 |
| KAPPA(KOP)_HU | OPRK1 | Homo sapiens | 10 µM | 84.5 | Cerep_4461 |
| 5HT1A/H | HTR1A | Homo sapiens | 10 µM | 103.5 | Cerep_131 |
| 5HT2AH_AGON | HTR2A | Homo sapiens | 10 µM | 103.5 | Cerep_471 |
| 5HT2B/H AG | HTR2B | Homo sapiens | 10 µM | 118.0 | Cerep_1333 |
| 5HT3/H | HTR3A | Homo sapiens | 10 µM | 100.5 | Cerep_411 |
| A2A/H | ADORA2A | Homo sapiens | 10 µM | 102.5 | Cerep_4 |
| ACE(HU_AMTCH400) | ACE | Homo sapiens | 10 µM | 98.5 | Cerep_3441 |
| ALPHA1AH_ANTAG | ADRA1A | Homo sapiens | 10 µM | 110.0 | Cerep_2338 |
| ALPHA2A/HU | ADRA2A | Homo sapiens | 10 µM | 97.0 | Cerep_13 |
| ANDROGEN/H | AR | Homo sapiens | 10 µM | 107.0 | Cerep_933 |
| BETA1/HUM | ADRB1 | Homo sapiens | 10 µM | 101.0 | Cerep_18 |
| BETA2/HUM | ADRB2 | Homo sapiens | 10 µM | 103.0 | Cerep_20 |
| BZD/CENTR/R | Rattus norvegicus | 10 µM | 113.5 | Cerep_28 | |
| CA+/DHPSI/R | Rattus norvegicus | 10 µM | 106.5 | Cerep_161 | |
| CB2/PERIPH/H | CNR2 | Homo sapiens | 10 µM | 105.5 | Cerep_37 |
| CCKA/H | CCKAR | Homo sapiens | 10 µM | 88.0 | Cerep_39 |
| D1/H | DRD1 | Homo sapiens | 10 µM | 94.0 | Cerep_44 |
| D2SH_AGON | DRD2 | Homo sapiens | 10 µM | 106.0 | Cerep_1322 |
| DATRANS/HUM | SLC6A3 | Homo sapiens | 10 µM | 98.5 | Cerep_52 |
| DELTA2/H | OPRD1 | Homo sapiens | 10 µM | 92.5 | Cerep_114 |
| ETA/H | EDNRA | Homo sapiens | 10 µM | 105.5 | Cerep_54 |
| GCORTICOID/H | NR3C1 | Homo sapiens | 10 µM | 102.5 | Cerep_469 |
| H1/PYRIL/HS | HRH1 | Homo sapiens | 10 µM | 101.0 | Cerep_870 |
| H2/APT/HS | HRH2 | Homo sapiens | 10 µM | 105.5 | Cerep_1208 |
| HERG_DOFETILIDE | KCNH2 | Homo sapiens | 10 µM | 100.0 | Cerep_4094 |
| M3/H | CHRM3 | Homo sapiens | 10 µM | 106.5 | Cerep_95 |
| MAO-A_ANTAG | MAOA | Rattus norvegicus | 10 µM | 107.5 | Cerep_443 |
| MU/H | OPRM1 | Homo sapiens | 10 µM | 81.0 | Cerep_118 |
| NA+/SITE2/R | Rattus norvegicus | 10 µM | 93.5 | Old_Cerep_169 | |
| NEUP/H | SLC6A2 | Homo sapiens | 10 µM | 103.0 | Cerep_355 |
| NMDA/R | Rattus norvegicus | 10 µM | 106.0 | Cerep_66 | |
| N_NEURO_A4B2 |
CHRNA4 CHRNB2 |
Homo sapiens | 10 µM | 114.0 | Cerep_3029 |
| PDE3A | PDE3A | Homo sapiens | 10 µM | 103.0 | Cerep_4072 |
| PDE4D2 | PDE4D | Homo sapiens | 10 µM | 100.5 | Cerep_4077 |
| SLC6A4/H | SCL6A4 | Homo sapiens | 10 µM | 105.5 | Cerep_439 |
| V1A/HUM | AVPR1A | Homo sapiens | 10 µM | 92.5 | Cerep_159 |
BI-1920
Conclusion: Clean panel.
| Target protein | HGNC name | Species | Cmp. conc. | % Control | Assay ID |
|---|---|---|---|---|---|
| 5HT1B(H) | HTR1B | Homo sapiens | 10 µM | 61.0 | Cerep_4376 |
| CB1(HU)_AGON | CNR1 | Homo sapiens | 10 µM | 112.0 | Cerep_4708 |
| COX-1 | PTGS1 | Homo sapiens | 10 µM | 108.0 | Cerep_4173 |
| COX-2 | PTGS2 | Homo sapiens | 10 µM | 90.0 | Cerep_4186 |
| KAPPA(KOP)_HU | OPRK1 | Homo sapiens | 10 µM | 96.0 | Cerep_4461 |
| 5HT1A/H | HTR1A | Homo sapiens | 10 µM | 97.0 | Cerep_131 |
| 5HT2AH_AGON | HTR2A | Homo sapiens | 10 µM | 123.0 | Cerep_471 |
| 5HT2B/H AG | HTR2B | Homo sapiens | 10 µM | 117.0 | Cerep_1333 |
| 5HT3/H | HTR3A | Homo sapiens | 10 µM | 97.0 | Cerep_411 |
| A2A/H | ADORA2A | Homo sapiens | 10 µM | 87.0 | Cerep_4 |
| ACE(HU_AMTCH400) | ACE | Homo sapiens | 10 µM | 105.0 | Cerep_3441 |
| ALPHA1AH_ANTAG | ADRA1A | Homo sapiens | 10 µM | 104.0 | Cerep_2338 |
| ALPHA2A/HU | ADRA2A | Homo sapiens | 10 µM | 80.0 | Cerep_13 |
| ANDROGEN/H | AR | Homo sapiens | 10 µM | 110.0 | Cerep_933 |
| BETA1/HUM | ADRB1 | Homo sapiens | 10 µM | 97.0 | Cerep_18 |
| BETA2/HUM | ADRB2 | Homo sapiens | 10 µM | 92.0 | Cerep_20 |
| BZD/CENTR/R | Rattus norvegicus | 10 µM | 111.0 | Cerep_28 | |
| CA+/DHPSI/R | Rattus norvegicus | 10 µM | 115.0 | Cerep_161 | |
| CB2/PERIPH/H | CNR2 | Homo sapiens | 10 µM | 109.0 | Cerep_37 |
| CCKA/H | CCKAR | Homo sapiens | 10 µM | 96.0 | Cerep_39 |
| D1/H | DRD1 | Homo sapiens | 10 µM | 105.0 | Cerep_44 |
| D2SH_AGON | DRD2 | Homo sapiens | 10 µM | 107.0 | Cerep_1322 |
| DATRANS/HUM | SLC6A3 | Homo sapiens | 10 µM | 105.0 | Cerep_52 |
| DELTA2/H | OPRD1 | Homo sapiens | 10 µM | 106.0 | Cerep_114 |
| ETA/H | EDNRA | Homo sapiens | 10 µM | 112.0 | Cerep_54 |
| GCORTICOID/H | NR3C1 | Homo sapiens | 10 µM | 105.0 | Cerep_469 |
| H1/PYRIL/HS | HRH1 | Homo sapiens | 10 µM | 106.0 | Cerep_870 |
| H2/APT/HS | HRH2 | Homo sapiens | 10 µM | 92.0 | Cerep_1208 |
| HERG_DOFETILIDE | KCNH2 | Homo sapiens | 10 µM | 98.0 | Cerep_4094 |
| K+/VOLT/RA | Rattus norvegicus | 10 µM | 110.0 | Cerep_166 | |
| LCK_CE | LCK | Homo sapiens | 10 µM | 99.0 | Old_Cerep_2906 |
| M1/H | CHRM1 | Homo sapiens | 10 µM | 108.0 | Cerep_91 |
| M2/H | CHRM2 | Homo sapiens | 10 µM | 125.0 | Cerep_93 |
| M3/H | CHRM3 | Homo sapiens | 10 µM | 112.0 | Cerep_95 |
| MAO-A_ANTAG | MAOA | Rattus norvegicus | 10 µM | 105.0 | Cerep_443 |
| MU/H | OPRM1 | Homo sapiens | 10 µM | 96.0 | Cerep_118 |
| NA+/SITE2/R | Rattus norvegicus | 10 µM | 94.0 | Old_Cerep_169 | |
| NEUP/H | SLC6A2 | Homo sapiens | 10 µM | 120.0 | Cerep_355 |
| NMDA/R | Rattus norvegicus | 10 µM | 92.0 | Cerep_66 | |
| N_NEURO_A4B2 |
CHRNA4 CHRNB2 |
Homo sapiens | 10 µM | 98.0 | Cerep_3029 |
| PDE3A | PDE3A | Homo sapiens | 10 µM | 88.0 | Cerep_4072 |
| PDE4D2 | PDE4D | Homo sapiens | 10 µM | 105.0 | Cerep_4077 |
| SLC6A4/H | SCL6A4 | Homo sapiens | 10 µM | 106.0 | Cerep_439 |
| V1A/HUM | AVPR1A | Homo sapiens | 10 µM | 94.0 | Cerep_159 |
BI-1915
The compound was tested in single-dose duplicate at 10 µM. The protease activities were monitored as a time-course measurement of the increase in fluorescence signal from fluorescently-labeled peptide substrate, and initial linear portion of slope (signal/min) was analyzed. No compound exhibited fluorescent background that could interfere with the assay.
Conclusion: Clean panel except for Papain with 12.43 % enzyme activity.
| Target protein | HGNC name | Species | Cmp. conc. | Mean [% Enzyme Activity] | First measurement | Second measurement | Assay ID |
|---|---|---|---|---|---|---|---|
| Caspase 1 | CASP1 | Homo sapiens | 10 µM | 96.8 | 97.34 | 96.26 | ReactionBiology_Caspase1 |
| Caspase 2 | CASP2 | Homo sapiens | 10 µM | 96.3 | 95.30 | 97.26 | ReactionBiology_Caspase2 |
| Caspase 3 | CASP3 | Homo sapiens | 10 µM | 106.3 | 105.87 | 106.80 | ReactionBiology_Caspase3 |
| Caspase 4 | CASP4 | Homo sapiens | 10 µM | 92.6 | 105.87 | 106.80 | ReactionBiology_Caspase4 |
| Caspase 5 | CASP5 | Homo sapiens | 10 µM | 99.1 | 98.41 | 99.80 | ReactionBiology_Caspase5 |
| Caspase 6 | CASP6 | Homo sapiens | 10 µM | 97.2 | 97.78 | 96.59 | ReactionBiology_Caspase6 |
| Caspase 7 | CASP7 | Homo sapiens | 10 µM | 102.5 | 104.18 | 100.85 | ReactionBiology_Caspase7 |
| Caspase 8 | CASP8 | Homo sapiens | 10 µM | 94.9 | 94.82 | 94.90 | ReactionBiology_Caspase8 |
| Caspase 9 | CASP9 | Homo sapiens | 10 µM | 99.5 | 96.56 | 102.36 | ReactionBiology_Caspase9 |
| Caspase 10 | CASP10 | Homo sapiens | 10 µM | 102.4 | 102.10 | 102.79 | ReactionBiology_Caspase10 |
| Caspase 11 | Mus musculus | 10 µM | 99.6 | 99.88 | 99.28 | ReactionBiology_Caspase11 | |
| Chymase | CMA1 | Homo sapiens | 10 µM | 87.1 | 84.94 | 89.23 | ReactionBiology_Chymase |
| Chymotrypsin | CTRC | Homo sapiens | 10 µM | 102.0 | 100.94 | 102.99 | ReactionBiology_Chymotrypsin |
| Elastase | ELANE | Homo sapiens | 10 µM | 96.9 | 96.08 | 97.64 | ReactionBiology_Elastase |
| Kallikrein 1 | KLK1 | Homo sapiens | 10 µM | 97.1 | 97.92 | 96.22 | ReactionBiology_Kallikrein1 |
| Kallikrein 12 | KLK12 | Homo sapiens | 10 µM | 98.9 | 98.69 | 99.15 | ReactionBiology_Kallikrein12 |
| Kallikrein 13 | KLK13 | Homo sapiens | 10 µM | 97.2 | 97.75 | 96.56 | ReactionBiology_Kallikrein13 |
| Kallikrein 14 | KLK14 | Homo sapiens | 10 µM | 98.5 | 98.08 | 98.91 | ReactionBiology_Kallikrein14 |
| Matriptase 2 | TMPRSS6 | Homo sapiens | 10 µM | 101.6 | 101.88 | 101.23 | ReactionBiology_Matriptase2 |
| MMP1 | MMP1 | Homo sapiens | 10 µM | 96.2 | 97.33 | 95.02 | ReactionBiology_MMP1 |
| MMP2 | MMP2 | Homo sapiens | 10 µM | 102.1 | 101.70 | 102.41 | ReactionBiology_MMP2 |
| MMP3 | MMP3 | Homo sapiens | 10 µM | 99.7 | 95.61 | 103.86 | ReactionBiology_MMP3 |
| MMP7 | MMP7 | Homo sapiens | 10 µM | 97.0 | 97.88 | 96.09 | ReactionBiology_MMP7 |
| MMP8 | MMP8 | Homo sapiens | 10 µM | 99.9 | 99.83 | 99.87 | ReactionBiology_MMP8 |
| MMP9 | MMP9 | Homo sapiens | 10 µM | 90.0 | 88.05 | 91.99 | ReactionBiology_MMP9 |
| MMP10 | MMP10 | Homo sapiens | 10 µM | 98.1 | 97.87 | 98.24 | ReactionBiology_MMP10 |
| MMP12 | MMP12 | Homo sapiens | 10 µM | 95.9 | 96.06 | 95.82 | ReactionBiology_MMP12 |
| MMP13 | MMP13 | Homo sapiens | 10 µM | 97.0 | 96.82 | 97.12 | ReactionBiology_MMP13 |
| MMP14 | MMP14 | Homo sapiens | 10 µM | 96.3 | 96.61 | 96.05 | ReactionBiology_MMP14 |
| Neprilysin | MME | Homo sapiens | 10 µM | 97.2 | 97.83 | 96.61 | ReactionBiology_Neprilysin |
| Papain | Carica papaya | 10 µM | 12.4 | 11.93 | 12.93 | ReactionBiology_Papain | |
| Plasma Kallikrein | KLKB1 | Homo sapiens | 10 µM | 102.6 | 102.35 | 102.81 | ReactionBiology_PlasmaKallikrein |
| Plasmin | PLG | Homo sapiens | 10 µM | 97.9 | 97.50 | 98.34 | ReactionBiology_Plasmin |
| Proteinase A | Bacillus licheniformis | 10 µM | 94.1 | 94.57 | 93.69 | ReactionBiology_ProteinaseA | |
| Proteinase K | Parengyodontium album | 10 µM | 98.8 | 98.24 | 99.43 | ReactionBiology_ProteinaseK | |
| SARS-CoV2-Plpro | 10 µM | 97.4 | 97.82 | 97.02 | ReactionBiology_SARS-CoV2-Plpro | ||
| TACE | ADAM17 | Homo sapiens | 10 µM | 98.1 | 97.40 | 98.89 | ReactionBiology_TACE |
| Thrombin a | F2 | Homo sapiens | 10 µM | 94.9 | 94.84 | 94.98 | ReactionBiology_Thrombina |
| TMPRS11D | TMPRSS11D | Homo sapiens | 10 µM | 95.6 | 95.49 | 95.70 | ReactionBiology_TMPRS11D |
| Trypsin | PRSS1 | Homo sapiens | 10 µM | 103.3 | 99.79 | 106.87 | ReactionBiology_Trypsin |
| Tryptase b2 | TPSB2 | Homo sapiens | 10 µM | 99.6 | 100.86 | 98.43 | ReactionBiology_Tryptaseb2 |
| Tryptase g1 | TPSG1 | Homo sapiens | 10 µM | 102.0 | 101.05 | 102.89 | ReactionBiology_Tryptaseg1 |
| Urokinase | PLAU | Homo sapiens | 10 µM | 102.3 | 103.27 | 101.23 | ReactionBiology_Urokinase |
BI-1920
Conclusion: Clean panel.
| Target protein | HGNC name | Species | Cmp. conc. | Mean [% Enzyme Activity] | First measurement | Second measurement | Assay ID |
|---|---|---|---|---|---|---|---|
| Caspase 1 | CASP1 | Homo sapiens | 10 µM | 101.4 | 101.4 | 101.3 | ReactionBiology_Caspase1 |
| Caspase 2 | CASP2 | Homo sapiens | 10 µM | 107.1 | 107.5 | 106.8 | ReactionBiology_Caspase2 |
| Caspase 3 | CASP3 | Homo sapiens | 10 µM | 103.1 | 101.7 | 104.5 | ReactionBiology_Caspase3 |
| Caspase 4 | CASP4 | Homo sapiens | 10 µM | 106.9 | 105.3 | 108.5 | ReactionBiology_Caspase4 |
| Caspase 5 | CASP5 | Homo sapiens | 10 µM | 102.3 | 102.5 | 102.1 | ReactionBiology_Caspase5 |
| Caspase 6 | CASP6 | Homo sapiens | 10 µM | 99.3 | 98.8 | 99.7 | ReactionBiology_Caspase6 |
| Caspase 7 | CASP7 | Homo sapiens | 10 µM | 108.8 | 107.6 | 109.9 | ReactionBiology_Caspase7 |
| Caspase 8 | CASP8 | Homo sapiens | 10 µM | 102.0 | 101.5 | 102.4 | ReactionBiology_Caspase8 |
| Caspase 9 | CASP9 | Homo sapiens | 10 µM | 108.8 | 109.1 | 108.5 | ReactionBiology_Caspase9 |
| Caspase 10 | CASP10 | Homo sapiens | 10 µM | 95.1 | 94.7 | 95.6 | ReactionBiology_Caspase10 |
| Caspase 11 | Mus musculus | 10 µM | 105.1 | 101.6 | 108.5 | ReactionBiology_Caspase11 | |
| Chymase | CMA1 | Homo sapiens | 10 µM | 102.8 | 101.6 | 104.1 | ReactionBiology_Chymase |
| Chymotrypsin | CTRC | Homo sapiens | 10 µM | 106.7 | 104.6 | 108.7 | ReactionBiology_Chymotrypsin |
| Elastase | ELANE | Homo sapiens | 10 µM | 99.9 | 100.8 | 99.0 | ReactionBiology_Elastase |
| Kallikrein 1 | KLK1 | Homo sapiens | 10 µM | 98.0 | 97.8 | 98.3 | ReactionBiology_Kallikrein1 |
| Kallikrein 12 | KLK12 | Homo sapiens | 10 µM | 97.5 | 96.9 | 98.0 | ReactionBiology_Kallikrein12 |
| Kallikrein 13 | KLK13 | Homo sapiens | 10 µM | 98.5 | 98.7 | 98.3 | ReactionBiology_Kallikrein13 |
| Kallikrein 14 | KLK14 | Homo sapiens | 10 µM | 101.5 | 101.8 | 101.3 | ReactionBiology_Kallikrein14 |
| Matriptase 2 | TMPRSS6 | Homo sapiens | 10 µM | 103.4 | 103.2 | 103.6 | ReactionBiology_Matriptase2 |
| MMP1 | MMP1 | Homo sapiens | 10 µM | 92.6 | 95.3 | 89.9 | ReactionBiology_MMP1 |
| MMP2 | MMP2 | Homo sapiens | 10 µM | 93.3 | 94.3 | 92.2 | ReactionBiology_MMP2 |
| MMP3 | MMP3 | Homo sapiens | 10 µM | 101.4 | 100.8 | 102.0 | ReactionBiology_MMP3 |
| MMP7 | MMP7 | Homo sapiens | 10 µM | 103.9 | 101.5 | 106.3 | ReactionBiology_MMP7 |
| MMP8 | MMP8 | Homo sapiens | 10 µM | 99.2 | 100.5 | 97.9 | ReactionBiology_MMP8 |
| MMP9 | MMP9 | Homo sapiens | 10 µM | 99.3 | 99.7 | 98.9 | ReactionBiology_MMP9 |
| MMP10 | MMP10 | Homo sapiens | 10 µM | 101.0 | 102.7 | 99.3 | ReactionBiology_MMP10 |
| MMP12 | MMP12 | Homo sapiens | 10 µM | 95.9 | 96.4 | 95.4 | ReactionBiology_MMP12 |
| MMP13 | MMP13 | Homo sapiens | 10 µM | 103.8 | 104.4 | 103.3 | ReactionBiology_MMP13 |
| MMP14 | MMP14 | Homo sapiens | 10 µM | 94.4 | 95.2 | 93.6 | ReactionBiology_MMP14 |
| Neprilysin | MME | Homo sapiens | 10 µM | 103.8 | 101.2 | 106.3 | ReactionBiology_Neprilysin |
| Papain | Carica papaya | 10 µM | 93.8 | 93.8 | 93.9 | ReactionBiology_Papain | |
| Plasma Kallikrein | KLKB1 | Homo sapiens | 10 µM | 91.3 | 91.8 | 90.9 | ReactionBiology_PlasmaKallikrein |
| Plasmin | PLG | Homo sapiens | 10 µM | 101.9 | 102.2 | 101.7 | ReactionBiology_Plasmin |
| Proteinase A | Bacillus licheniformis | 10 µM | 99.6 | 99.2 | 100.0 | ReactionBiology_ProteinaseA | |
| Proteinase K | Parengyodontium album | 10 µM | 103.3 | 102.1 | 104.5 | ReactionBiology_ProteinaseK | |
| SARS-CoV2-Plpro | 10 µM | 102.0 | 103.2 | 100.7 | ReactionBiology_SARS-CoV2-Plpro | ||
| TACE | ADAM17 | Homo sapiens | 10 µM | 92.8 | 92.3 | 93.3 | ReactionBiology_TACE |
| Thrombin a | F2 | Homo sapiens | 10 µM | 104.0 | 102.2 | 105.8 | ReactionBiology_Thrombina |
| TMPRS11D | TMPRSS11D | Homo sapiens | 10 µM | 101.8 | 100.0 | 103.5 | ReactionBiology_TMPRS11D |
| Trypsin | PRSS1 | Homo sapiens | 10 µM | 100.2 | 100.9 | 99.6 | ReactionBiology_Trypsin |
| Tryptase b2 | TPSB2 | Homo sapiens | 10 µM | 93.9 | 96.8 | 91.1 | ReactionBiology_Tryptaseb2 |
| Tryptase g1 | TPSG1 | Homo sapiens | 10 µM | 94.8 | 95.3 | 94.3 | ReactionBiology_Tryptaseg1 |
| Urokinase | PLAU | Homo sapiens | 10 µM | 104.6 | 105.8 | 103.4 | ReactionBiology_Urokinase |