Selectivity data for probe BI-2540 and control BI-2439
Coming soon
BI-2540
Conclusion: Clean panel
| Target protein | HGNC name | Species | Cmp. conc. | % Control | Assay ID |
|---|---|---|---|---|---|
| 5HT1B(H) | HTR1B | Homo sapiens | 10 µM | 90.0 | Cerep_4376 |
| CB1(HU)_AGON | CNR1 | Homo sapiens | 10 µM | 125.0 | Cerep_4708 |
| COX-1 | PTGS1 | Homo sapiens | 10 µM | 110.0 | Cerep_4173 |
| COX-2 | PTGS2 | Homo sapiens | 10 µM | 84.0 | Cerep_4186 |
| KAPPA(KOP)_HU | OPRK1 | Homo sapiens | 10 µM | 103.0 | Cerep_4461 |
| 5HT1A/H | HTR1A | Homo sapiens | 10 µM | 94.0 | Cerep_131 |
| 5HT2AH_AGON | HTR2A | Homo sapiens | 10 µM | 110.0 | Cerep_471 |
| 5HT2B/H AG | HTR2B | Homo sapiens | 10 µM | 103.0 | Cerep_1333 |
| 5HT3/H | HTR3A | Homo sapiens | 10 µM | 100.0 | Cerep_411 |
| A2A/H | ADORA2A | Homo sapiens | 10 µM | 82.0 | Cerep_4 |
| ACE(HU_AMTCH400) | ACHE | Homo sapiens | 10 µM | 110.0 | Old_Cerep_363 |
| ALPHA1AH_ANTAG | ADRA1A | Homo sapiens | 10 µM | 97.0 | Cerep_2338 |
| ALPHA2A/HU | ADRA2A | Homo sapiens | 10 µM | 79.0 | Cerep_13 |
| ANDROGEN/H | AR | Homo sapiens | 10 µM | 105.0 | Cerep_933 |
| BETA1/HUM | ADRB1 | Homo sapiens | 10 µM | 101.0 | Cerep_18 |
| BETA2/HUM | ADRB2 | Homo sapiens | 10 µM | 96.0 | Cerep_20 |
| BZD/CENTR/R | Rattus norvegicus | 10 µM | 127.0 | Cerep_28 | |
| CA+/DHPSI/R | Rattus norvegicus | 10 µM | 96.0 | Old_Cerep_161 | |
| CB2/PERIPH/H | CNR2 | Homo sapiens | 10 µM | 100.0 | Cerep_37 |
| CCKA/H | CCKAR | Homo sapiens | 10 µM | 108.0 | Old_Cerep_39 |
| D1/H | DRD1 | Homo sapiens | 10 µM | 100.0 | Cerep_44 |
| D2SH_AGON | DRD2 | Homo sapiens | 10 µM | 96.0 | Cerep_1322 |
| DATRANS/HUM | SLC6A3 | Homo sapiens | 10 µM | 92.0 | Old_Cerep_52 |
| DELTA2/H | OPRD1 | Homo sapiens | 10 µM | 78.0 | Cerep_114 |
| ETA/H | EDNRA | Homo sapiens | 10 µM | 113.0 | Cerep_54 |
| GCORTICOID/H | NR3C1 | Homo sapiens | 10 µM | 103.0 | Old_Cerep_469 |
| H1/PYRIL/HS | HRH1 | Homo sapiens | 10 µM | 96.0 | Cerep_870 |
| H2/APT/HS | HRH2 | Homo sapiens | 10 µM | 111.0 | Cerep_1208 |
| HERG_DOFETILIDE | KCNH2 | Homo sapiens | 10 µM | 94.0 | Cerep_4094 |
| K+/VOLT/RA | Rattus norvegicus | 10 µM | 103.0 | Cerep_166 | |
| LCK_CE | LCK | Homo sapiens | 10 µM | 88.0 | Old_Cerep_2906 |
| M1/H | CHRM1 | Homo sapiens | 10 µM | 113.0 | Cerep_91 |
| M2/H | CHRM2 | Homo sapiens | 10 µM | 111.0 | Cerep_93 |
| M3/H | CHRM3 | Homo sapiens | 10 µM | 101.0 | Cerep_95 |
| MAO-A_ANTAG | MAOA | Rattus norvegicus | 10 µM | 104.0 | Cerep_443 |
| MU/H | OPRM1 | Homo sapiens | 10 µM | 99.0 | Cerep_118 |
| NA+/SITE2/R | Rattus norvegicus | 10 µM | 89.0 | Old_Cerep_169 | |
| NEUP/H | SLC6A2 | Homo sapiens | 10 µM | 98.0 | Cerep_355 |
| NMDA/R | Rattus norvegicus | 10 µM | 87.0 | Cerep_66 | |
| N_NEURO_A4B2 |
CHRNA4 CHRNB2 |
Homo sapiens | 10 µM | 102.0 | Cerep_3029 |
| PDE3A | PDE3A | Homo sapiens | 10 µM | 103.0 | Cerep_4072 |
| PDE4D2 | PDE4D | Homo sapiens | 10 µM | 93.0 | Cerep_4077 |
| SLC6A4/H | SCL6A4 | Homo sapiens | 10 µM | 110.0 | Cerep_439 |
| V1A/HUM | AVPR1A | Homo sapiens | 10 µM | 107.0 | Cerep_159 |
BI-2439
Conclusion: Closest off-targets are PTGS1 with 80 % inhibition, PDE4D with 65 % inhibition and OPRD1 with 52 % inhibition.
| Target protein | HGNC name | Species | Cmp. conc. | % Control | Assay ID |
|---|---|---|---|---|---|
| 5HT1B(H) | HTR1B | Homo sapiens | 10 µM | 100.0 | Cerep_4376 |
| CB1(HU)_AGON | CNR1 | Homo sapiens | 10 µM | 120.0 | Cerep_4708 |
| COX-1 | PTGS1 | Homo sapiens | 10 µM | 20.0 | Cerep_4173 |
| COX-2 | PTGS2 | Homo sapiens | 10 µM | 83.0 | Cerep_4186 |
| KAPPA(KOP)_HU | OPRK1 | Homo sapiens | 10 µM | 85.0 | Cerep_4461 |
| 5HT1A/H | HTR1A | Homo sapiens | 10 µM | 100.0 | Cerep_131 |
| 5HT2AH_AGON | HTR2A | Homo sapiens | 10 µM | 117.0 | Cerep_471 |
| 5HT2B/H AG | HTR2B | Homo sapiens | 10 µM | 111.0 | Cerep_1333 |
| 5HT3/H | HTR3A | Homo sapiens | 10 µM | 100.0 | Cerep_411 |
| A2A/H | ADORA2A | Homo sapiens | 10 µM | 85.0 | Cerep_4 |
| ACE(HU_AMTCH400) | ACHE | Homo sapiens | 10 µM | 116.0 | Old_Cerep_363 |
| ALPHA1AH_ANTAG | ADRA1A | Homo sapiens | 10 µM | 96.0 | Cerep_2338 |
| ALPHA2A/HU | ADRA2A | Homo sapiens | 10 µM | 89.0 | Cerep_13 |
| ANDROGEN/H | AR | Homo sapiens | 10 µM | 106.0 | Cerep_933 |
| BETA1/HUM | ADRB1 | Homo sapiens | 10 µM | 97.0 | Cerep_18 |
| BETA2/HUM | ADRB2 | Homo sapiens | 10 µM | 98.0 | Cerep_20 |
| BZD/CENTR/R | Rattus norvegicus | 10 µM | 102.0 | Cerep_28 | |
| CA+/DHPSI/R | Rattus norvegicus | 10 µM | 68.0 | Old_Cerep_161 | |
| CB2/PERIPH/H | CNR2 | Homo sapiens | 10 µM | 107.0 | Cerep_37 |
| CCKA/H | CCKAR | Homo sapiens | 10 µM | 50.0 | Old_Cerep_39 |
| D1/H | DRD1 | Homo sapiens | 10 µM | 93.0 | Cerep_44 |
| D2SH_AGON | DRD2 | Homo sapiens | 10 µM | 114.0 | Cerep_1322 |
| DATRANS/HUM | SLC6A3 | Homo sapiens | 10 µM | 79.0 | Old_Cerep_52 |
| DELTA2/H | OPRD1 | Homo sapiens | 10 µM | 48.0 | Cerep_114 |
| ETA/H | EDNRA | Homo sapiens | 10 µM | 115.0 | Cerep_54 |
| GCORTICOID/H | NR3C1 | Homo sapiens | 10 µM | 94.0 | Old_Cerep_469 |
| H1/PYRIL/HS | HRH1 | Homo sapiens | 10 µM | 94.0 | Cerep_870 |
| H2/APT/HS | HRH2 | Homo sapiens | 10 µM | 112.0 | Cerep_1208 |
| HERG_DOFETILIDE | KCNH2 | Homo sapiens | 10 µM | 96.0 | Cerep_4094 |
| K+/VOLT/RA | Rattus norvegicus | 10 µM | 103.0 | Cerep_166 | |
| LCK_CE | LCK | Homo sapiens | 10 µM | 96.0 | Old_Cerep_2906 |
| M1/H | CHRM1 | Homo sapiens | 10 µM | 115.0 | Cerep_91 |
| M2/H | CHRM2 | Homo sapiens | 10 µM | 115.0 | Cerep_93 |
| M3/H | CHRM3 | Homo sapiens | 10 µM | 109.0 | Cerep_95 |
| MAO-A_ANTAG | MAOA | Rattus norvegicus | 10 µM | 102.0 | Cerep_443 |
| MU/H | OPRM1 | Homo sapiens | 10 µM | 92.0 | Cerep_118 |
| NA+/SITE2/R | Rattus norvegicus | 10 µM | 97.0 | Old_Cerep_169 | |
| NEUP/H | SLC6A2 | Homo sapiens | 10 µM | 109.0 | Cerep_355 |
| NMDA/R | Rattus norvegicus | 10 µM | 104.0 | Cerep_66 | |
| N_NEURO_A4B2 |
CHRNA4 CHRNB2 |
Homo sapiens | 10 µM | 104.0 | Cerep_3029 |
| PDE3A | PDE3A | Homo sapiens | 10 µM | 116.0 | Cerep_4072 |
| PDE4D2 | PDE4D | Homo sapiens | 10 µM | 35.0 | Cerep_4077 |
| SLC6A4/H | SCL6A4 | Homo sapiens | 10 µM | 105.0 | Cerep_439 |
| V1A/HUM | AVPR1A | Homo sapiens | 10 µM | 98.0 | Cerep_159 |