Selectivity data for probe BI-1942
Jump to control PDSP data
BI-1942
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| 5-HT1E | HTR1E | -9.73 | ||
| 5-HT2C | HTR2C | 1.02 | ||
| 5-HT3 | HTR3A | 0.31 | ||
| 5-HT5A | HTR5A | 5.71 | ||
| 5-HT6 | HTR6 | 12.18 | ||
| 5-HT7A | HTR7 | 27.18 | ||
| Alpha2A | ADRA2A | 19.55 | ||
| Alpha2B | ADRA2B | 0.56 | ||
| Alpha2C | ADRA2C | 13.76 | ||
| GABAA/BZP | 3.50 | |||
| D2 | DRD2 | 0.91 | ||
| D4 | DRD4 | -1.40 | ||
| DAT | SLC6A3 | -18.20 | ||
| DOR | OPRD1 | 9.83 | ||
| KOR | OPRK1 | 95.88 | 4948.48 average (n=2) | 5.32 |
| MOR | OPRM1 | 2.82 | ||
| SERT | SLC6A4 | 4.96 | ||
| Sigma 1 | SIGMAR1 | -15.94 | ||
| 5-HT2A | HTR2A | 0.22 | ||
| 5-HT2B | HTR2B | 5.53 | ||
| Alpha1A | ADRA1A | 0.23 | ||
| Alpha1B | ADRA1B | -5.58 | ||
| Alpha1D | ADRA1D | 12.08 | ||
| Beta1 | ADRB1 | 10.38 | ||
| Beta2 | ADRB2 | 10.49 | ||
| Beta3 | ADRB3 | -6.54 | ||
| D1 | DRD1 | 20.31 | ||
| D3 | DRD3 | 11.07 | ||
| D5 | DRD5 | 22.16 | ||
| H1 | HRH1 | 14.14 | ||
| H2 | HRH2 | -4.71 | ||
| H3 | HRH3 | 3.32 | ||
| H4 | HRH4 | -5.56 | ||
| M1 | CHRM1 | 8.69 | ||
| M2 | CHRM2 | 12.00 | ||
| M3 | CHRM3 | 23.82 | ||
| M4 | CHRM4 | 9.09 | ||
| M5 | CHRM5 | 8.73 | ||
| NET | SLC6A2 | 31.52 | ||
| GABA/PBR | 12.23 | |||
| 5-HT1A | HTR1A | 8.83 | ||
| Sigma 2 | TMEM97 | -9.50 | ||
| GABAA | 6.86 | |||
| 5-HT1B | HTR1B | 5.01 | ||
| 5-HT1D | HTR1D | 52.91 | 1130.61 average (n=2) | 5.95 |
BI-1942
Conclusion: The only off-target is CTSG with -2 % Ctrl at 10 µM.
| 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 | 114.0 | Cerep_4708 |
| CHYMASE | CMA1 | Homo sapiens | 10 µM | -1.0 | Cerep_5646 |
| COX-1 | PTGS1 | Homo sapiens | 10 µM | 134.0 | Cerep_4173 |
| COX-2 | PTGS2 | Homo sapiens | 10 µM | 101.0 | Cerep_4186 |
| KAPPA(KOP)_HU | OPRK1 | Homo sapiens | 10 µM | 89.0 | Cerep_4461 |
| THROMBIN | F2 | Homo sapiens | 10 µM | 102.0 | Cerep_3751 |
| 5HT1A/H | HTR1A | Homo sapiens | 10 µM | 79.0 | Cerep_131 |
| 5HT2AH_AGON | HTR2A | Homo sapiens | 10 µM | 87.0 | Cerep_471 |
| 5HT2B/H AG | HTR2B | Homo sapiens | 10 µM | 100.0 | Cerep_1333 |
| 5HT3/H | HTR3A | Homo sapiens | 10 µM | 97.0 | Cerep_411 |
| A2A/H | ADORA2A | Homo sapiens | 10 µM | 98.0 | Cerep_4 |
| ACE(HU) | ACE | Homo sapiens | 10 µM | 127.0 | Cerep_3441 |
| ACE(HU_AMTCH400) | ACHE | Homo sapiens | 10 µM | 99.0 | Old_Cerep_363 |
| ACE-2(HU) | ACE2 | Homo sapiens | 10 µM | 127.0 | Cerep_1954 |
| ALPHA1AH_ANTAG | ADRA1A | Homo sapiens | 10 µM | 103.0 | Cerep_2338 |
| ALPHA2A/HU | ADRA2A | Homo sapiens | 10 µM | 90.0 | Cerep_13 |
| ANDROGEN/H | AR | Homo sapiens | 10 µM | 115.0 | Cerep_933 |
| BACE-1 | BACE1 | Homo sapiens | 10 µM | 106.0 | Cerep_701 |
| BETA1/HUM | ADRB1 | Homo sapiens | 10 µM | 105.0 | Cerep_18 |
| BETA2/HUM | ADRB2 | Homo sapiens | 10 µM | 93.0 | Cerep_20 |
| BZD/CENTR/R | Rattus norvegicus | 10 µM | 129.0 | Cerep_28 | |
| CA+/DHPSI/R | Rattus norvegicus | 10 µM | 108.0 | Old_Cerep_161 | |
| CASPASE-1(H) | CASP1 | Homo sapiens | 10 µM | 103.0 | Cerep_3251 |
| CASPASE-10(H) | CASP10 | Homo sapiens | 10 µM | 111.0 | Cerep_910 |
| CASPASE-2(H) | CASP2 | Homo sapiens | 10 µM | 156.0 | Cerep_681 |
| CASPASE-3 | CASP3 | Homo sapiens | 10 µM | 97.0 | Cerep_774 |
| CASPASE-6_CE | CASP6 | Homo sapiens | 10 µM | 99.0 | Cerep_908 |
| CASPASE-7(H) | CASP7 | Homo sapiens | 10 µM | 101.0 | Cerep_909 |
| CASPASE8_CE | CASP8 | Homo sapiens | 10 µM | 88.0 | Cerep_668 |
| CATHEPSB(H) | CTSB | Homo sapiens | 10 µM | 98.0 | Cerep_178 |
| CATHEPSG(H) | CTSG | Homo sapiens | 10 µM | -2.0 | Cerep_179 |
| CATHEPSIN-L | CTSL | Homo sapiens | 10 µM | 99.0 | Cerep_802 |
| CATHEPSIND | CTSD | Homo sapiens | 10 µM | 118.0 | Cerep_650 |
| CATHEPSINE | CTSE | Mus musculus | 10 µM | 106.0 | Cerep_1001 |
| CATHEPSINX(H) | CTSZ | Homo sapiens | 10 µM | 98.0 | Cerep_931 |
| CATHEPSIN_C_CE | CTSS | Homo sapiens | 10 µM | 92.0 | Cerep_803 |
| CB2/PERIPH/H | CNR2 | Homo sapiens | 10 µM | 109.0 | Cerep_37 |
| CCKA/H | CCKAR | Homo sapiens | 10 µM | 98.0 | Old_Cerep_39 |
| D1/H | DRD1 | Homo sapiens | 10 µM | 96.0 | Cerep_44 |
| D2SH_AGON | DRD2 | Homo sapiens | 10 µM | 108.0 | Cerep_1322 |
| DATRANS/HUM | SLC6A3 | Homo sapiens | 10 µM | 101.0 | Old_Cerep_52 |
| DELTA2/H | OPRD1 | Homo sapiens | 10 µM | 95.0 | Cerep_114 |
| DIPEPTIDYLPEPTIDASE | DPP4 | Homo sapiens | 10 µM | 107.0 | Cerep_2942 |
| ECE(H) | ECE1 | Homo sapiens | 10 µM | 82.0 | Cerep_184 |
| ELASTASE(H) | ELANE | Homo sapiens | 10 µM | 101.0 | Cerep_183 |
| ETA/H | EDNRA | Homo sapiens | 10 µM | 106.0 | Cerep_54 |
| GCORTICOID/H | NR3C1 | Homo sapiens | 10 µM | 107.0 | Old_Cerep_469 |
| H1/PYRIL/HS | HRH1 | Homo sapiens | 10 µM | 100.0 | Cerep_870 |
| H2/APT/HS | HRH2 | Homo sapiens | 10 µM | 114.0 | Cerep_1208 |
| HERG_DOFETILIDE | KCNH2 | Homo sapiens | 10 µM | 105.0 | Cerep_4094 |
| HIV-1/H | HIV-1 protease | Human immunodeficiency virus 1 | 10 µM | 111.0 | Cerep_346 |
| K+/VOLT/RA | Rattus norvegicus | 10 µM | 104.0 | Cerep_166 | |
| LCK_CE | LCK | Homo sapiens | 10 µM | 103.0 | Old_Cerep_2906 |
| M1/H | CHRM1 | Homo sapiens | 10 µM | 112.0 | Cerep_91 |
| M2/H | CHRM2 | Homo sapiens | 10 µM | 104.0 | Cerep_93 |
| M3/H | CHRM3 | Homo sapiens | 10 µM | 98.0 | Cerep_95 |
| MAO-A_ANTAG | MAOA | Rattus norvegicus | 10 µM | 86.0 | Cerep_443 |
| MMP-12 | MMP12 | Homo sapiens | 10 µM | 104.0 | Cerep_511 |
| MMP-13 (H) | MMP13 | Homo sapiens | 10 µM | 109.0 | Cerep_632 |
| MMP-2 (H) | MMP2 | Homo sapiens | 10 µM | 103.0 | Old_Cerep_43 |
| MMP-3 (H) | MMP3 | Homo sapiens | 10 µM | 90.0 | Old_Cerep_42 |
| MMP-7 (H) | MMP7 | Homo sapiens | 10 µM | 100.0 | Cerep_502 |
| MMP-8(H) | MMP8 | Homo sapiens | 10 µM | 107.0 | Cerep_643 |
| MMP-9 (H) | MMP9 | Homo sapiens | 10 µM | 124.0 | Old_Cerep_41 |
| MMP1 (H) | MMP1 | Homo sapiens | 10 µM | 97.0 | Cerep_510 |
| MT1-MMP(H)(MMP-14) | MMP14 | Homo sapiens | 10 µM | 134.0 | Cerep_670 |
| MU/H | OPRM1 | Homo sapiens | 10 µM | 96.0 | Cerep_118 |
| NA+/SITE2/R | Rattus norvegicus | 10 µM | 97.0 | Old_Cerep_169 | |
| NEUP/H | SLC6A2 | Homo sapiens | 10 µM | 102.0 | Cerep_355 |
| NMDA/R | Rattus norvegicus | 10 µM | 113.0 | Cerep_66 | |
| N_NEURO_A4B2 |
CHRNA4 CHRNB2 |
Homo sapiens | 10 µM | 103.0 | Cerep_3029 |
| PAR1(H)AGON | F2R | Homo sapiens | 10 µM | 100.0 | Old_Cerep_46 |
| PAR1(H)ANTAG | F2R | Homo sapiens | 10 µM | 120.0 | Old_Cerep_47 |
| PDE3A | PDE3A | Homo sapiens | 10 µM | 94.0 | Cerep_4072 |
| PDE4D2 | PDE4D | Homo sapiens | 10 µM | 106.0 | Cerep_4077 |
| SLC6A4/H | SCL6A4 | Homo sapiens | 10 µM | 86.0 | Cerep_439 |
| TACE | ADAM17 | Homo sapiens | 10 µM | 88.0 | Cerep_702 |
| TRYPSIN_CE | Homo sapiens | 10 µM | 108.0 | Cerep_3742 | |
| TRYPTASE_H | Homo sapiens | 10 µM | 102.0 | Old_Cerep_40 | |
| V1A/HUM | AVPR1A | Homo sapiens | 10 µM | 101.0 | Cerep_159 |