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Selectivity data for probe BI-3802 and control BI-5273


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BI-3802


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT2B HTR2B -5.25
5-HT1A HTR1A 27.03
5-HT1B HTR1B 8.61
5-HT1D HTR1D 13.67
5-HT2A HTR2A -1.56
5-HT2C HTR2C 0.15
5-HT3 HTR3A 12.50
5-HT5A HTR5A 0.20
5-HT6 HTR6 -11.74
5-HT7A HTR7 15.46
Alpha1A ADRA1A -14.60
Alpha1B ADRA1B -0.36
Alpha1D ADRA1D -7.81
Alpha2A ADRA2A 5.49
Alpha2B ADRA2B 7.35
Alpha2C ADRA2C 6.50
Beta1 ADRB1 -14.44
Beta2 ADRB2 -8.13
Beta3 ADRB3 -4.02
GABAA/BZP 20.90
D1 DRD1 -4.07
D2 DRD2 -8.96
D3 DRD3 11.57
D4 DRD4 -9.60
D5 DRD5 1.96
DAT SLC6A3 12.59
DOR OPRD1 13.26
H1 HRH1 6.31
H3 HRH3 12.67
H4 HRH4 -0.56
KOR OPRK1 33.54
M1 CHRM1 -20.84
M2 CHRM2 -5.10
M3 CHRM3 -2.43
M4 CHRM4 -1.45
M5 CHRM5 -11.42
MOR OPRM1 24.53
NET SLC6A2 9.75
GABA/PBR -18.21
SERT SLC6A4 2.53
Sigma 1 TMEM97 19.92
Sigma 2 SIGMAR1 17.07

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BI-3802

Conclusion: Clean with the exception of HTR2B (agonist) (12 % ctrl).

Target protein HGNC name Species Cmp. conc. % Control Assay ID
COX-1 PTGS1 Homo sapiens 10 µM 90.0 Cerep_4173
COX-2 PTGS2 Homo sapiens 10 µM 88.0 Cerep_4186
5HT1A/H HTR1A Homo sapiens 10 µM 90.0 Cerep_131
5HT1B/R HTR1B Rattus norvegicus 10 µM 115.0 Cerep_132
5HT2AH_AGON HTR2A Homo sapiens 10 µM 112.0 Cerep_471
5HT2B/H AG HTR2B Homo sapiens 10 µM 12.0 Cerep_1333
5HT3/H HTR3A Homo sapiens 10 µM 101.0 Cerep_411
A2A/H ADORA2A Homo sapiens 10 µM 92.0 Cerep_4
ACE(HU_AMTCH400) ACHE Homo sapiens 10 µM 106.0 Old_Cerep_363
ALPHA1AH_ANTAG ADRA1A Homo sapiens 10 µM 110.0 Cerep_2338
ALPHA2A/HU ADRA2A Homo sapiens 10 µM 111.0 Cerep_13
ANDROGEN/H AR Homo sapiens 10 µM 103.0 Cerep_933
BETA1/HUM ADRB1 Homo sapiens 10 µM 99.0 Cerep_18
BETA2/HUM ADRB2 Homo sapiens 10 µM 101.0 Cerep_20
BZD/CENTR/R Rattus norvegicus 10 µM 97.0 Cerep_28
CA+/DHPSI/R Rattus norvegicus 10 µM 99.0 Old_Cerep_161
CB1/CENTR/H CNR1 Homo sapiens 10 µM 84.0 Cerep_4708
CB2/PERIPH/H CNR2 Homo sapiens 10 µM 96.0 Cerep_37
CCKA/H CCKAR Homo sapiens 10 µM 100.0 Old_Cerep_39
D1/H DRD1 Homo sapiens 10 µM 106.0 Cerep_44
D2SH_AGON DRD2 Homo sapiens 10 µM 115.0 Cerep_1322
DATRANS/HUM SLC6A3 Homo sapiens 10 µM 88.0 Old_Cerep_52
DELTA2/H OPRD1 Homo sapiens 10 µM 100.0 Cerep_114
ETA/H EDNRA Homo sapiens 10 µM 100.0 Cerep_54
GCORTICOID/H NR3C1 Homo sapiens 10 µM 99.0 Old_Cerep_469
H1/PYRIL/HS HRH1 Homo sapiens 10 µM 105.0 Cerep_870
H2/APT/HS HRH2 Homo sapiens 10 µM 110.0 Cerep_1208
HERG_DOFETILIDE KCNH2 Homo sapiens 10 µM 76.0 Cerep_4094
K+/VOLT/RA Rattus norvegicus 10 µM 105.0 Cerep_166
KAPPA/R OPRK1 Rattus norvegicus 10 µM 89.0 Cerep_1971
LCK_CE LCK Homo sapiens 10 µM 114.0 Old_Cerep_2906
M1/H CHRM1 Homo sapiens 10 µM 93.0 Cerep_91
M2/H CHRM2 Homo sapiens 10 µM 102.0 Cerep_93
M3/H CHRM3 Homo sapiens 10 µM 110.0 Cerep_95
MAO-A_ANTAG MAOA Rattus norvegicus 10 µM 89.0 Cerep_443
MU/H OPRM1 Homo sapiens 10 µM 81.0 Cerep_118
NA+/SITE2/R Rattus norvegicus 10 µM 114.0 Old_Cerep_169
NEUP/H SLC6A2 Homo sapiens 10 µM 99.0 Cerep_355
NMDA/R Rattus norvegicus 10 µM 78.0 Cerep_66
N_NEURO_A4B2 CHRNA4
 CHRNB2
 		Homo sapiens 10 µM 107.0 Cerep_3029
PDE3A PDE3A Homo sapiens 10 µM 95.0 Cerep_4072
PDE4D2 PDE4D Homo sapiens 10 µM 100.0 Cerep_4077
SLC6A4/H SCL6A4 Homo sapiens 10 µM 104.0 Cerep_439
V1A/HUM AVPR1A Homo sapiens 10 µM 85.0 Cerep_159
 

BI-5273

Conclusion: Clean panel.

Target protein HGNC name Species Cmp. conc. % Control Assay ID
5HT1B(H) HTR1B Homo sapiens 10 µM 95.0 Cerep_4376
CB1(HU)_AGON CNR1 Homo sapiens 10 µM 95.0 Cerep_4708
COX-1 PTGS1 Homo sapiens 10 µM 82.0 Cerep_4173
COX-2 PTGS2 Homo sapiens 10 µM 75.0 Cerep_4186
KAPPA(KOP)_HU OPRK1 Homo sapiens 10 µM 86.0 Cerep_4461
5HT1A/H HTR1A Homo sapiens 10 µM 97.0 Cerep_131
5HT2AH_AGON HTR2A Homo sapiens 10 µM 125.0 Cerep_471
5HT2B/H AG HTR2B Homo sapiens 10 µM 159.0 Cerep_1333
5HT3/H HTR3A Homo sapiens 10 µM 95.0 Cerep_411
A2A/H ADORA2A Homo sapiens 10 µM 107.0 Cerep_4
ACE(HU_AMTCH400) ACHE Homo sapiens 10 µM 111.0 Old_Cerep_363
ALPHA1AH_ANTAG ADRA1A Homo sapiens 10 µM 99.0 Cerep_2338
ALPHA2A/HU ADRA2A Homo sapiens 10 µM 104.0 Cerep_13
ANDROGEN/H AR Homo sapiens 10 µM 104.0 Cerep_933
BETA1/HUM ADRB1 Homo sapiens 10 µM 99.0 Cerep_18
BETA2/HUM ADRB2 Homo sapiens 10 µM 89.0 Cerep_20
BZD/CENTR/R Rattus norvegicus 10 µM 147.0 Cerep_28
CA+/DHPSI/R Rattus norvegicus 10 µM 104.0 Old_Cerep_161
CB2/PERIPH/H CNR2 Homo sapiens 10 µM 103.0 Cerep_37
CCKA/H CCKAR Homo sapiens 10 µM 137.0 Old_Cerep_39
D1/H DRD1 Homo sapiens 10 µM 92.0 Cerep_44
D2SH_AGON DRD2 Homo sapiens 10 µM 86.0 Cerep_1322
DATRANS/HUM SLC6A3 Homo sapiens 10 µM 100.0 Old_Cerep_52
DELTA2/H OPRD1 Homo sapiens 10 µM 97.0 Cerep_114
ETA/H EDNRA Homo sapiens 10 µM 111.0 Cerep_54
GCORTICOID/H NR3C1 Homo sapiens 10 µM 97.0 Old_Cerep_469
H1/PYRIL/HS HRH1 Homo sapiens 10 µM 86.0 Cerep_870
H2/APT/HS HRH2 Homo sapiens 10 µM 121.0 Cerep_1208
HERG_DOFETILIDE KCNH2 Homo sapiens 10 µM 95.0 Cerep_4094
K+/VOLT/RA Rattus norvegicus 10 µM 97.0 Cerep_166
LCK_CE LCK Homo sapiens 10 µM 87.0 Old_Cerep_2906
M1/H CHRM1 Homo sapiens 10 µM 128.0 Cerep_91
M2/H CHRM2 Homo sapiens 10 µM 111.0 Cerep_93
M3/H CHRM3 Homo sapiens 10 µM 111.0 Cerep_95
MAO-A_ANTAG MAOA Rattus norvegicus 10 µM 96.0 Cerep_443
MU/H OPRM1 Homo sapiens 10 µM 44.0 Cerep_118
NA+/SITE2/R Rattus norvegicus 10 µM 88.0 Old_Cerep_169
NEUP/H SLC6A2 Homo sapiens 10 µM 102.0 Cerep_355
NMDA/R Rattus norvegicus 10 µM 88.0 Cerep_66
N_NEURO_A4B2 CHRNA4
 CHRNB2
 		Homo sapiens 10 µM 106.0 Cerep_3029
PDE3A PDE3A Homo sapiens 10 µM 99.0 Cerep_4072
PDE4D2 PDE4D Homo sapiens 10 µM 87.0 Cerep_4077
SLC6A4/H SCL6A4 Homo sapiens 10 µM 91.0 Cerep_439
V1A/HUM AVPR1A Homo sapiens 10 µM 97.0 Cerep_159

BI-3802

Information about the assays can be found at the Thermo Fisher website: Z'-LYTE, Adapta and TR-FRET.

Conclusion: Clean panel

Target protein HGNC name Species % control at 1 µM Mode of action Assay
ABL1 ABL1 Homo sapiens 103.0 inhibitor fluorescence resonance energy transfer
AKT2 (PKB beta) AKT2 Homo sapiens 96.0 inhibitor Z´-LYTE
AMPK A1/B1/G1 (PRKA A1/B1/G1) PRKAA1
 PRKAB1
 PRKAG1
 		Homo sapiens 101.0 inhibitor fluorescence resonance energy transfer
AURKB (Aurora B) AURKB Homo sapiens 97.0 inhibitor fluorescence resonance energy transfer
CDK2/cyclin A CDK2 Homo sapiens 102.0 inhibitor Z´-LYTE
CHEK1 (CHK1) CHEK1 Homo sapiens 89.0 inhibitor Z´-LYTE
CHEK2 (CHK2) CHEK2 Homo sapiens 96.0 inhibitor Z´-LYTE
CLK1 CLK1 Homo sapiens 107.0 inhibitor Z´-LYTE
CSNK1A1 (CK1 alpha 1) CSNK1A1 Homo sapiens 93.0 inhibitor Z´-LYTE
EGFR (ErbB1) EGFR Homo sapiens 88.0 inhibitor Z´-LYTE
EPHA2 EPHA2 Homo sapiens 97.0 inhibitor Z´-LYTE
FGFR1 FGFR1 Homo sapiens 111.0 inhibitor fluorescence resonance energy transfer
GSK3B (GSK3 beta) GSK3B Homo sapiens 93.0 inhibitor fluorescence resonance energy transfer
IKBKB (IKK beta) IKBKB Homo sapiens 102.0 inhibitor Z´-LYTE
INSR INSR Homo sapiens 100.0 inhibitor Z´-LYTE
IRAK4 IRAK4 Homo sapiens 90.0 inhibitor Z´-LYTE
ITK ITK Homo sapiens 100.0 inhibitor Z´-LYTE
KDR (VEGFR2) KDR Homo sapiens 111.0 inhibitor fluorescence resonance energy transfer
LRRK2 - Adapta LRRK2 Homo sapiens 78.0 inhibitor Adapta
LYN A LYN Homo sapiens 104.0 inhibitor fluorescence resonance energy transfer
MAP2K1 (MEK1) MAP2K1 Homo sapiens 71.0 inhibitor Z´-LYTE
MAP2K2 (MEK2) MAP2K2 Homo sapiens 111.0 inhibitor Z´-LYTE
MAP2K6 (MKK6) MAP2K6 Homo sapiens 84.0 inhibitor Z´-LYTE
MAP3K8 (COT) MAP3K8 Homo sapiens 118.0 inhibitor Z´-LYTE
MAPK1 (ERK2) MAPK1 Homo sapiens 106.0 inhibitor Z´-LYTE
MAPK14 (p38 alpha) MAPK14 Homo sapiens 100.0 inhibitor Z´-LYTE
MAPK3 (ERK1) MAP3K3 Homo sapiens 105.0 inhibitor Z´-LYTE
MAPK8 (JNK1) MAPK8 Homo sapiens 120.0 inhibitor Z´-LYTE
MAPK9 (JNK2) MAPK9 Homo sapiens 110.0 inhibitor Z´-LYTE
MAPKAPK2 MAPKAPK2 Homo sapiens 102.0 inhibitor Z´-LYTE
MAPKAPK3 MAPKAPK3 Homo sapiens 97.0 inhibitor Z´-LYTE
MYLK2 (skMLCK) MYLK2 Homo sapiens 90.0 inhibitor Z´-LYTE
NEK1 NEK1 Homo sapiens 101.0 inhibitor Z´-LYTE
NTRK1 (TRKA) NTRK1 Homo sapiens 83.0 inhibitor Z´-LYTE
NTRK2 (TRKB) NTRK2 Homo sapiens 99.0 inhibitor Z´-LYTE
PAK4 PAK4 Homo sapiens 94.0 inhibitor Z´-LYTE
PDGFRA (PDGFR alpha) PDGFRA Homo sapiens 102.0 inhibitor fluorescence resonance energy transfer
PDK1 PDK1 Homo sapiens 98.0 inhibitor Z´-LYTE
PIK3CG (p110 gamma) PIK3CG Homo sapiens 95.0 inhibitor Adapta
PLK1 PLK1 Homo sapiens 92.0 inhibitor Z´-LYTE
PRKACA (PKA) PRKACA Homo sapiens 91.0 inhibitor Z´-LYTE
PRKCA (PKC alpha) PRKCA Homo sapiens 113.0 inhibitor Z´-LYTE
PTK2 (FAK) PTK2 Homo sapiens 106.0 inhibitor Z´-LYTE
RAF1 (cRAF) RAF1 Homo sapiens 94.0 inhibitor Z´-LYTE
RET RET Homo sapiens 101.0 inhibitor fluorescence resonance energy transfer
ROCK2 ROCK2 Homo sapiens 100.0 inhibitor Z´-LYTE
RPS6KA3 (RSK2) RPS6KA3 Homo sapiens 89.0 inhibitor Z´-LYTE
RPS6KA4 (MSK2) RPS6KA4 Homo sapiens 99.0 inhibitor Z´-LYTE
RPS6KA5 (MSK1) RPS6KA5 Homo sapiens 96.0 inhibitor Z´-LYTE
RPS6KB1 (p70S6K) RPS6KB1 Homo sapiens 97.0 inhibitor Z´-LYTE
SRC SRC Homo sapiens 105.0 inhibitor Z´-LYTE
SRPK2 SRPK2 Homo sapiens 106.0 inhibitor Z´-LYTE
STK3 (MST2) STK3 Homo sapiens 101.0 inhibitor Z´-LYTE
TBK1 TBK1 Homo sapiens 120.0 inhibitor Z´-LYTE