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Selectivity data for probe BI-5524 and control BI-5525


Coming soon

BI-5524

Conclusion: Clean panel.

Target protein HGNC name Species Cmp. conc. % Control @10µM % Control @30µM Assay ID
5HT1A/H HTR1A Homo sapiens 10 µM 72.0 Cerep_131
5HT1B/R HTR1B Rattus norvegicus 10 µM 136.0 Cerep_132
5HT2A/H HTR2A Homo sapiens 10 µM 69.0 Cerep_471
5HT2B/H AG HTR2B Homo sapiens 10 µM 130.0 Cerep_1333
5HT2C/H HTR2C Homo sapiens 10 µM 94.0 Cerep_1003
5HT3/H HTR3A Homo sapiens 10 µM 108.0 Cerep_411
5HT5A/H HTR5A Homo sapiens 10 µM 98.0 Cerep_140
5HT6/H HTR6 Homo sapiens 10 µM 93.0 Cerep_142
5HT7/H HTR7 Homo sapiens 10 µM 102.0 Cerep_144
5HTTRANS/H SCL6A4 Homo sapiens 10 µM 108.0 Cerep_439
A1/H ADORA1 Homo sapiens 10 µM 107.0 102.00 Cerep_2
A2A/H ADORA2A Homo sapiens 10 µM 100.0 83.00 Cerep_4
A3/H ADORA3 Homo sapiens 10 µM 92.0 80.00 Cerep_6
ALPHA1/NS/R ADRA1A
ADRA1B
ADRA1D
Rattus norvegicus 10 µM 97.0 103.00 Cerep_8
ALPHA2/NS/R ADRA2A
ADRA2B
ADRA2C
Rattus norvegicus 10 µM 93.0 98.00 Cerep_11
AT1/H AGTR1 Homo sapiens 10 µM 116.0 92.00 Cerep_24
AT2/H AGTR2 Homo sapiens 10 µM 92.0 114.00 Cerep_26
B2/HUM BDKRB2 Homo sapiens 10 µM 107.0 97.00 Cerep_33
BETA1/HUM ADRB1 Homo sapiens 10 µM 100.0 100.00 Cerep_18
BETA2/HUM ADRB2 Homo sapiens 10 µM 87.0 92.00 Cerep_20
BOMBESIN/NS Rattus norvegicus 10 µM 129.0 118.00 Cerep_30
BZD/CENTR/R Rattus norvegicus 10 µM 119.0 116.00 Cerep_28
BZD/PERIPH/R Rattus norvegicus 10 µM 100.0 93.00 Old_Cerep_10
CA+/VERSI/R Rattus norvegicus 10 µM 102.0 Cerep_163
CB1/CENTR/H CNR1 Homo sapiens 10 µM 87.0 93.00 Cerep_4708
CCKA/H CCKAR Homo sapiens 10 µM 89.0 89.00 Cerep_39
CCKB/H CCKBR Homo sapiens 10 µM 106.0 Cerep_41
CCR1/H CCR1 Homo sapiens 10 µM 89.0 Cerep_361
CGRP/H CALCRL Homo sapiens 10 µM 108.0 113.00 Cerep_373
CL-CHANNEL/R Rattus norvegicus 10 µM 90.0 Old_Cerep_16
D1/H DRD1 Homo sapiens 10 µM 96.0 Cerep_44
D2S/H DRD2 Homo sapiens 10 µM 89.0 Cerep_1322
D3/H DRD3 Homo sapiens 10 µM 96.0 Cerep_48
D4.4/H DRD4 Homo sapiens 10 µM 98.0 Cerep_49
D5/H DRD5 Homo sapiens 10 µM 103.0 Cerep_50
DATRANS/HUM SLC6A3 Homo sapiens 10 µM 110.0 Cerep_52
DELTA2/H OPRD1 Homo sapiens 10 µM 101.0 Cerep_114
EP2(H) PTGER2 Homo sapiens 10 µM 93.0 Cerep_1955
EP4/H AG PTGER4 Homo sapiens 10 µM 77.0 Cerep_441
ETA/H EDNRA Homo sapiens 10 µM 99.0 Cerep_54
ETB/H EDNRB Homo sapiens 10 µM 92.0 Cerep_56
GABA/NS/R Rattus norvegicus 10 µM 103.0 Cerep_60
GAL1/H GALR1 Homo sapiens 10 µM 121.0 Cerep_62
GAL2/H GALR2 Homo sapiens 10 µM 114.0 Cerep_410
GCORTICOID/H NR3C1 Homo sapiens 10 µM 107.0 Cerep_469
H1/PYRIL/HS HRH1 Homo sapiens 10 µM 108.0 Cerep_870
H2/APT/HS HRH2 Homo sapiens 10 µM 114.0 Cerep_1208
IL8B/CXCR2/H CXCR2 Homo sapiens 10 µM 105.0 Cerep_419
K+/CA+/R Rattus norvegicus 10 µM 97.0 Cerep_167
K+/VOLT/RA Rattus norvegicus 10 µM 102.0 Cerep_166
KAPPA/R OPRK1 Rattus norvegicus 10 µM 65.0 Cerep_1971
M1/H CHRM1 Homo sapiens 10 µM 103.0 Cerep_91
M2/H CHRM2 Homo sapiens 10 µM 121.0 Cerep_93
M3/H CHRM3 Homo sapiens 10 µM 84.0 Cerep_95
M4/H CHRM4 Homo sapiens 10 µM 95.0 Cerep_96
M5/H CHRM5 Homo sapiens 10 µM 92.0 Cerep_97
MC4/HU MC4R Homo sapiens 10 µM 92.0 Cerep_420
MT1 (ML1A) MTNR1A Homo sapiens 10 µM 105.0 Cerep_1538
MU/H OPRM1 Homo sapiens 10 µM 82.0 Cerep_118
NA+/SITE2/R Rattus norvegicus 10 µM 84.0 Old_Cerep_169
NEUP/H SLC6A2 Homo sapiens 10 µM 98.0 Cerep_355
NK1/HUM TACR1 Homo sapiens 10 µM 115.0 Cerep_100
NK2/H TACR2 Homo sapiens 10 µM 103.0 Cerep_102
NK3/H TACR3 Homo sapiens 10 µM 102.0 Cerep_104
NT1/H NTSR1 Homo sapiens 10 µM 114.0 Cerep_109
ORL1/H OPRL1 Homo sapiens 10 µM 95.0 Cerep_358
P2X/R Rattus norvegicus 10 µM 103.0 Old_Cerep_127
P2Y/RA Rattus norvegicus 10 µM 88.0 Cerep_128
PACAP/HU ADCYAP1R1 Homo sapiens 10 µM 122.0 Cerep_1518
PCP/R Rattus norvegicus 10 µM 104.0 Old_Cerep_32
PDGF/M Mus musculus 10 µM 103.0 Cerep_70
PGI2/H PTGIR Homo sapiens 10 µM 123.0 Cerep_2230
PPARG/H AG PPARG Homo sapiens 10 µM 111.0 Cerep_641
SIGMA/NS Homo sapiens 10 µM 72.0 Cerep_3500
SOMATOS/M Mus musculus 10 µM 114.0 Cerep_149
TNFALPHA/H TNFRSF1A Homo sapiens 10 µM 115.0 Cerep_76
V1A/HUM AVPR1A Homo sapiens 10 µM 102.0 Cerep_159
VIP1/VPAC1/H VIPR1 Homo sapiens 10 µM 111.0 Cerep_157
Y1/HUM NPY1R Homo sapiens 10 µM 107.0 Cerep_106
Y2/H NPY2R Homo sapiens 10 µM 113.0 Cerep_107
 

BI-5525

Conclusion: Clean panel.

Target protein HGNC name Species Cmp. conc. % Control Assay ID
5HT1B(H) HTR1B Homo sapiens 10 µM 86.0 Cerep_4376
CB1(HU)_AGON CNR1 Homo sapiens 10 µM 88.0 Cerep_4708
COX-1 PTGS1 Homo sapiens 10 µM 105.0 Cerep_4173
COX-2 PTGS2 Homo sapiens 10 µM 101.0 Cerep_4186
KAPPA(KOP)_HU OPRK1 Homo sapiens 10 µM 94.0 Cerep_4461
5HT1A/H HTR1A Homo sapiens 10 µM 91.0 Cerep_131
5HT2AH_AGON HTR2A Homo sapiens 10 µM 111.0 Cerep_471
5HT2B/H AG HTR2B Homo sapiens 10 µM 97.0 Cerep_1333
5HT3/H HTR3A Homo sapiens 10 µM 81.0 Cerep_411
A2A/H ADORA2A Homo sapiens 10 µM 109.0 Cerep_4
ACE(HU_AMTCH400) ACE Homo sapiens 10 µM 98.0 Cerep_3441
ALPHA1AH_ANTAG ADRA1A Homo sapiens 10 µM 102.0 Cerep_2338
ALPHA2A/HU ADRA2A Homo sapiens 10 µM 98.0 Cerep_13
ANDROGEN/H AR Homo sapiens 10 µM 101.0 Cerep_933
BETA1/HUM ADRB1 Homo sapiens 10 µM 89.0 Cerep_18
BETA2/HUM ADRB2 Homo sapiens 10 µM 101.0 Cerep_20
BZD/CENTR/R Rattus norvegicus 10 µM 101.0 Cerep_28
CA+/DHPSI/R Rattus norvegicus 10 µM 104.0 Cerep_161
CB2/PERIPH/H CNR2 Homo sapiens 10 µM 83.0 Cerep_37
CCKA/H CCKAR Homo sapiens 10 µM 97.0 Cerep_39
D1/H DRD1 Homo sapiens 10 µM 100.0 Cerep_44
D2SH_AGON DRD2 Homo sapiens 10 µM 99.0 Cerep_1322
DATRANS/HUM SLC6A3 Homo sapiens 10 µM 98.0 Cerep_52
DELTA2/H OPRD1 Homo sapiens 10 µM 100.0 Cerep_114
ETA/H EDNRA Homo sapiens 10 µM 95.0 Cerep_54
GCORTICOID/H NR3C1 Homo sapiens 10 µM 96.0 Cerep_469
H1/PYRIL/HS HRH1 Homo sapiens 10 µM 101.0 Cerep_870
H2/APT/HS HRH2 Homo sapiens 10 µM 105.0 Cerep_1208
HERG_DOFETILIDE KCNH2 Homo sapiens 10 µM 96.0 Cerep_4094
K+/VOLT/RA Rattus norvegicus 10 µM 101.0 Cerep_166
LCK_CE LCK Homo sapiens 10 µM 92.0 Old_Cerep_2906
M1/H CHRM1 Homo sapiens 10 µM 114.0 Cerep_91
M2/H CHRM2 Homo sapiens 10 µM 103.0 Cerep_93
M3/H CHRM3 Homo sapiens 10 µM 95.0 Cerep_95
MAO-A_ANTAG MAOA Rattus norvegicus 10 µM 101.0 Cerep_443
MU/H OPRM1 Homo sapiens 10 µM 104.0 Cerep_118
NA+/SITE2/R Rattus norvegicus 10 µM 101.0 Old_Cerep_169
NEUP/H SLC6A2 Homo sapiens 10 µM 95.0 Cerep_355
NMDA/R Rattus norvegicus 10 µM 96.0 Cerep_66
N_NEURO_A4B2 CHRNA4
CHRNB2
Homo sapiens 10 µM 115.0 Cerep_3029
PDE3A PDE3A Homo sapiens 10 µM 97.0 Cerep_4072
PDE4D2 PDE4D Homo sapiens 10 µM 114.0 Cerep_4077
SLC6A4/H SCL6A4 Homo sapiens 10 µM 105.0 Cerep_439
V1A/HUM AVPR1A Homo sapiens 10 µM 99.0 Cerep_159

BI-5524

The compound was tested in single-dose duplicate at 1 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.

Target protein HGNC name Species Cmp. conc. Mean [% Enzyme Activity] First measurement Second measurement Assay ID
Caspase 1 CASP1 Homo sapiens 1 µM 98.3 97.97 98.70 ReactionBiology_Caspase1
Caspase 2 CASP2 Homo sapiens 1 µM 99.4 99.55 99.21 ReactionBiology_Caspase2
Caspase 3 CASP3 Homo sapiens 1 µM 97.4 95.99 98.90 ReactionBiology_Caspase3
Caspase 4 CASP4 Homo sapiens 1 µM 94.2 92.09 96.33 ReactionBiology_Caspase4
Caspase 5 CASP5 Homo sapiens 1 µM 106.3 105.83 106.78 ReactionBiology_Caspase5
Caspase 6 CASP6 Homo sapiens 1 µM 101.1 101.34 100.95 ReactionBiology_Caspase6
Caspase 7 CASP7 Homo sapiens 1 µM 106.6 106.62 106.65 ReactionBiology_Caspase7
Caspase 8 CASP8 Homo sapiens 1 µM 102.8 102.21 103.41 ReactionBiology_Caspase8
Caspase 9 CASP9 Homo sapiens 1 µM 98.8 98.95 98.69 ReactionBiology_Caspase9
Caspase 10 CASP10 Homo sapiens 1 µM 107.8 108.50 107.02 ReactionBiology_Caspase10
Caspase 11 Mus musculus 1 µM 97.8 96.68 98.86 ReactionBiology_Caspase11
Chymase CMA1 Homo sapiens 1 µM 85.5 88.74 82.31 ReactionBiology_Chymase
Chymotrypsin CTRC Homo sapiens 1 µM 102.9 105.90 99.97 ReactionBiology_Chymotrypsin
Elastase ELANE Homo sapiens 1 µM -0.5 -0.57 -0.35 ReactionBiology_Elastase
Kallikrein 1 KLK1 Homo sapiens 1 µM 101.5 101.58 101.44 ReactionBiology_Kallikrein1
Kallikrein 12 KLK12 Homo sapiens 1 µM 99.3 99.05 99.57 ReactionBiology_Kallikrein12
Kallikrein 13 KLK13 Homo sapiens 1 µM 98.4 98.98 97.78 ReactionBiology_Kallikrein13
Kallikrein 14 KLK14 Homo sapiens 1 µM 99.5 99.47 99.62 ReactionBiology_Kallikrein14
Matriptase 2 TMPRSS6 Homo sapiens 1 µM 95.4 96.28 94.47 ReactionBiology_Matriptase2
MMP1 MMP1 Homo sapiens 1 µM 96.6 96.18 97.08 ReactionBiology_MMP1
MMP2 MMP2 Homo sapiens 1 µM 97.2 95.58 98.88 ReactionBiology_MMP2
MMP3 MMP3 Homo sapiens 1 µM 94.5 94.34 94.66 ReactionBiology_MMP3
MMP7 MMP7 Homo sapiens 1 µM 100.3 99.27 101.27 ReactionBiology_MMP7
MMP8 MMP8 Homo sapiens 1 µM 99.5 99.12 99.87 ReactionBiology_MMP8
MMP9 MMP9 Homo sapiens 1 µM 97.0 98.55 95.47 ReactionBiology_MMP9
MMP10 MMP10 Homo sapiens 1 µM 100.5 99.77 101.29 ReactionBiology_MMP10
MMP12 MMP12 Homo sapiens 1 µM 101.0 100.53 101.52 ReactionBiology_MMP12
MMP13 MMP13 Homo sapiens 1 µM 100.8 100.64 100.87 ReactionBiology_MMP13
MMP14 MMP14 Homo sapiens 1 µM 98.0 97.34 98.74 ReactionBiology_MMP14
Neprilysin MME Homo sapiens 1 µM 97.5 98.94 96.10 ReactionBiology_Neprilysin
Papain Carica papaya 1 µM 93.3 97.88 88.82 ReactionBiology_Papain
Plasma Kallikrein KLKB1 Homo sapiens 1 µM 95.7 96.15 95.19 ReactionBiology_PlasmaKallikrein
Plasmin PLG Homo sapiens 1 µM 97.9 98.81 97.02 ReactionBiology_Plasmin
Proteinase A Bacillus licheniformis 1 µM 99.3 99.75 98.92 ReactionBiology_ProteinaseA
Proteinase K Parengyodontium album 1 µM 97.5 97.00 98.03 ReactionBiology_ProteinaseK
SARS-CoV2-Plpro 1 µM 104.5 104.92 104.13 ReactionBiology_SARS-CoV2-Plpro
TACE ADAM17 Homo sapiens 1 µM 104.6 110.14 99.02 ReactionBiology_TACE
Thrombin a F2 Homo sapiens 1 µM 102.4 103.07 101.75 ReactionBiology_Thrombina
TMPRS11D TMPRSS11D Homo sapiens 1 µM 91.5 90.01 93.00 ReactionBiology_TMPRS11D
Trypsin PRSS1 Homo sapiens 1 µM 102.4 100.22 104.53 ReactionBiology_Trypsin
Tryptase b2 TPSB2 Homo sapiens 1 µM 93.9 91.91 95.96 ReactionBiology_Tryptaseb2
Tryptase g1 TPSG1 Homo sapiens 1 µM 103.4 104.35 102.51 ReactionBiology_Tryptaseg1
Urokinase PLAU Homo sapiens 1 µM 101.9 101.18 102.68 ReactionBiology_Urokinase
 

BI-5525

Conclusion: Clean panel.

Target protein HGNC name Species Cmp. conc. Mean [% Enzyme Activity] First measurement Second measurement Assay ID
Caspase 1 CASP1 Homo sapiens 1 µM 97.2 97.3 97.0 ReactionBiology_Caspase1
Caspase 2 CASP2 Homo sapiens 1 µM 98.0 98.1 97.8 ReactionBiology_Caspase2
Caspase 3 CASP3 Homo sapiens 1 µM 98.5 97.7 99.2 ReactionBiology_Caspase3
Caspase 4 CASP4 Homo sapiens 1 µM 93.9 91.6 96.2 ReactionBiology_Caspase4
Caspase 5 CASP5 Homo sapiens 1 µM 99.1 102.5 95.8 ReactionBiology_Caspase5
Caspase 6 CASP6 Homo sapiens 1 µM 102.1 101.5 102.6 ReactionBiology_Caspase6
Caspase 7 CASP7 Homo sapiens 1 µM 106.3 104.9 107.7 ReactionBiology_Caspase7
Caspase 8 CASP8 Homo sapiens 1 µM 96.3 95.3 97.3 ReactionBiology_Caspase8
Caspase 9 CASP9 Homo sapiens 1 µM 92.6 92.2 93.0 ReactionBiology_Caspase9
Caspase 10 CASP10 Homo sapiens 1 µM 100.0 101.6 98.4 ReactionBiology_Caspase10
Caspase 11 Mus musculus 1 µM 100.5 100.5 100.6 ReactionBiology_Caspase11
Chymase CMA1 Homo sapiens 1 µM 86.6 88.6 84.7 ReactionBiology_Chymase
Chymotrypsin CTRC Homo sapiens 1 µM 101.3 101.1 101.4 ReactionBiology_Chymotrypsin
Elastase ELANE Homo sapiens 1 µM 8.3 8.3 8.3 ReactionBiology_Elastase
Kallikrein 1 KLK1 Homo sapiens 1 µM 102.0 103.4 100.6 ReactionBiology_Kallikrein1
Kallikrein 12 KLK12 Homo sapiens 1 µM 97.6 98.8 96.3 ReactionBiology_Kallikrein12
Kallikrein 13 KLK13 Homo sapiens 1 µM 101.5 100.9 102.1 ReactionBiology_Kallikrein13
Kallikrein 14 KLK14 Homo sapiens 1 µM 104.3 105.4 103.2 ReactionBiology_Kallikrein14
Matriptase 2 TMPRSS6 Homo sapiens 1 µM 100.8 99.3 102.2 ReactionBiology_Matriptase2
MMP1 MMP1 Homo sapiens 1 µM 99.7 99.7 99.6 ReactionBiology_MMP1
MMP2 MMP2 Homo sapiens 1 µM 101.6 100.8 102.5 ReactionBiology_MMP2
MMP3 MMP3 Homo sapiens 1 µM 100.3 100.0 100.6 ReactionBiology_MMP3
MMP7 MMP7 Homo sapiens 1 µM 102.6 103.0 102.1 ReactionBiology_MMP7
MMP8 MMP8 Homo sapiens 1 µM 100.3 100.0 100.6 ReactionBiology_MMP8
MMP9 MMP9 Homo sapiens 1 µM 97.7 97.6 97.7 ReactionBiology_MMP9
MMP10 MMP10 Homo sapiens 1 µM 97.4 97.0 97.8 ReactionBiology_MMP10
MMP12 MMP12 Homo sapiens 1 µM 99.5 99.1 99.8 ReactionBiology_MMP12
MMP13 MMP13 Homo sapiens 1 µM 98.8 99.5 98.0 ReactionBiology_MMP13
MMP14 MMP14 Homo sapiens 1 µM 96.9 97.6 96.3 ReactionBiology_MMP14
Neprilysin MME Homo sapiens 1 µM 94.0 94.2 93.7 ReactionBiology_Neprilysin
Papain Carica papaya 1 µM 92.5 93.0 92.0 ReactionBiology_Papain
Plasma Kallikrein KLKB1 Homo sapiens 1 µM 94.8 95.1 94.5 ReactionBiology_PlasmaKallikrein
Plasmin PLG Homo sapiens 1 µM 98.6 98.2 99.0 ReactionBiology_Plasmin
Proteinase A Bacillus licheniformis 1 µM 98.5 98.0 99.0 ReactionBiology_ProteinaseA
Proteinase K Parengyodontium album 1 µM 100.7 99.9 101.5 ReactionBiology_ProteinaseK
SARS-CoV2-Plpro 1 µM 100.8 100.9 100.7 ReactionBiology_SARS-CoV2-Plpro
TACE ADAM17 Homo sapiens 1 µM 100.3 100.7 99.9 ReactionBiology_TACE
Thrombin a F2 Homo sapiens 1 µM 96.5 96.5 96.5 ReactionBiology_Thrombina
TMPRS11D TMPRSS11D Homo sapiens 1 µM 95.4 96.5 94.3 ReactionBiology_TMPRS11D
Trypsin PRSS1 Homo sapiens 1 µM 99.1 103.9 94.3 ReactionBiology_Trypsin
Tryptase b2 TPSB2 Homo sapiens 1 µM 93.8 93.4 94.2 ReactionBiology_Tryptaseb2
Tryptase g1 TPSG1 Homo sapiens 1 µM 96.2 93.1 99.2 ReactionBiology_Tryptaseg1
Urokinase PLAU Homo sapiens 1 µM 102.2 104.2 100.3 ReactionBiology_Urokinase