Selectivity data for probe JNJ-65355394 and control JNJ-73924149
Jump to control PDSP data
JNJ-65355394
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| 5-HT1B | HTR1B | -2.53 | ||
| 5-HT1D | HTR1D | 11.61 | ||
| 5-HT1A | HTR1A | 22.23 | ||
| Alpha1B | ADRA1B | -5.20 | ||
| Sigma 2 | TMEM97 | 19.00 | ||
| 5-HT2A | HTR2A | -2.94 | ||
| 5-HT2B | HTR2B | 6.70 | ||
| Alpha1A | ADRA1A | 2.36 | ||
| Alpha1D | ADRA1D | 8.30 | ||
| Beta1 | ADRB1 | 3.29 | ||
| Beta2 | ADRB2 | -5.16 | ||
| D1 | DRD1 | -19.74 | ||
| D3 | DRD3 | 10.31 | ||
| D5 | DRD5 | 7.69 | ||
| GABAA | -8.39 | |||
| H1 | HRH1 | 44.02 | ||
| H2 | HRH2 | 3.45 | ||
| H3 | HRH3 | 10.75 | ||
| H4 | HRH4 | -44.60 | ||
| M1 | CHRM1 | 6.18 | ||
| M2 | CHRM2 | 9.54 | ||
| M3 | CHRM3 | 8.40 | ||
| M4 | CHRM4 | -5.53 | ||
| M5 | CHRM5 | -10.83 | ||
| NET | SLC6A2 | 12.69 | ||
| GABA/PBR | 5.69 | |||
| 5-HT1E | HTR1E | -10.98 | ||
| 5-HT2C | HTR2C | 15.17 | ||
| 5-HT3 | HTR3A | 6.87 | ||
| 5-HT5A | HTR5A | 18.67 | ||
| 5-HT6 | HTR6 | 14.28 | ||
| 5-HT7A | HTR7 | 9.60 | ||
| Alpha2A | ADRA2A | 8.68 | ||
| Alpha2B | ADRA2B | 44.84 | ||
| Alpha2C | ADRA2C | 31.91 | ||
| Beta3 | ADRB3 | -19.87 | ||
| GABAA/BZP | 8.07 | |||
| D2 | DRD2 | 0.63 | ||
| D4 | DRD4 | 3.53 | ||
| DAT | SLC6A3 | 13.39 | ||
| DOR | OPRD1 | 11.76 | ||
| KOR | OPRK1 | 75.14 | 773.30 average (n=2) | 6.13 |
| MOR | OPRM1 | 12.75 | ||
| SERT | SLC6A4 | 7.21 | ||
| Sigma 1 | SIGMAR1 | 46.46 |
JNJ-73924149
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| Alpha1B | ADRA1B | -3.57 | ||
| 5-HT1B | HTR1B | 4.01 | ||
| 5-HT1D | HTR1D | 14.51 | ||
| 5-HT1A | HTR1A | 12.34 | ||
| M2 | CHRM2 | 8.65 | ||
| Sigma 2 | TMEM97 | 59.64 | 1399.16 average (n=2) | 5.87 |
| 5-HT2A | HTR2A | 6.45 | ||
| 5-HT2B | HTR2B | 17.95 | ||
| Alpha1A | ADRA1A | -1.89 | ||
| Alpha1D | ADRA1D | 7.45 | ||
| Beta1 | ADRB1 | 4.41 | ||
| Beta2 | ADRB2 | -8.10 | ||
| Beta3 | ADRB3 | -8.59 | ||
| D1 | DRD1 | 10.68 | ||
| D3 | DRD3 | -11.44 | ||
| D5 | DRD5 | -30.39 | ||
| GABAA | 43.57 | |||
| H1 | HRH1 | 44.17 | ||
| H2 | HRH2 | -13.19 | ||
| H3 | HRH3 | 27.07 | ||
| H4 | HRH4 | -0.60 | ||
| M1 | CHRM1 | 25.44 | ||
| M3 | CHRM3 | -9.98 | ||
| M4 | CHRM4 | 8.78 | ||
| M5 | CHRM5 | -6.15 | ||
| NET | SLC6A2 | 17.82 | ||
| GABA/PBR | 11.18 | |||
| 5-HT1E | HTR1E | 0.93 | ||
| 5-HT2C | HTR2C | 16.29 | ||
| 5-HT3 | HTR3A | 20.71 | ||
| 5-HT5A | HTR5A | 17.82 | ||
| 5-HT6 | HTR6 | 25.62 | ||
| 5-HT7A | HTR7 | 2.58 | ||
| Alpha2A | ADRA2A | 31.69 | ||
| Alpha2B | ADRA2B | 59.06 | 3691.26 average (n=2) | 5.44 |
| Alpha2C | ADRA2C | 36.54 | ||
| GABAA/BZP | 43.54 | |||
| D2 | DRD2 | 8.04 | ||
| D4 | DRD4 | 6.82 | ||
| DAT | SLC6A3 | 81.93 | 5284.45 | 5.28 |
| DOR | OPRD1 | 8.67 | ||
| KOR | OPRK1 | 17.86 | ||
| MOR | OPRM1 | 27.31 | ||
| SERT | SLC6A4 | 52.27 | 2614.09 average (n=2) | 5.59 |
| Sigma 1 | SIGMAR1 | 101.04 | 63.33 average (n=2) | 7.20 |
JNJ-65355394
The panel was screened at 10 µM except for hERG (0.1 µM) and rCaCH-nitrendipine (0.3 µM).
Conclusion: Closest off-targets are OPRK1 (77.85 % effect) and ADRA2A (69.05 % effect).
| Target protein | HGNC name | Species | Cmp. conc. | % Effect | Assay ID |
|---|---|---|---|---|---|
| cML1 | MTNR1A | Cricetinae | 10 µM | 11.5 | Old_Cerep_1538 |
| h5HT2A | HTR2A | Homo sapiens | 10 µM | 4.1 | Cerep_471 |
| hAT1 | AGTR1 | Homo sapiens | 10 µM | -3.1 | Cerep_24 |
| hBCXCR2 | CXCR2 | Homo sapiens | 10 µM | 0.9 | Cerep_419 |
| hCCR1 | CCR1 | Homo sapiens | 10 µM | -1.9 | Cerep_361 |
| hD2S | DRD2 | Homo sapiens | 10 µM | 10.5 | Cerep_46 |
| hERG | KCNH2 | Homo sapiens | 10 µM | 10.0 | Cerep_4094 |
| hGAL2 | GALR2 | Homo sapiens | 10 µM | 1.4 | Cerep_410 |
| hMC4 | MC4R | Homo sapiens | 10 µM | 1.3 | Cerep_420 |
| hNPY1 | NPY1R | Homo sapiens | 10 µM | -7.4 | Cerep_106 |
| hNPY2 | NPY2R | Homo sapiens | 10 µM | -2.7 | Cerep_107 |
| hORL1 | OPRL1 | Homo sapiens | 10 µM | -5.7 | Cerep_358 |
| hVPAC1 | VIPR1 | Homo sapiens | 10 µM | -10.1 | Cerep_157 |
| r5HT1B | HTR1B | Rattus norvegicus | 10 µM | -9.7 | Cerep_132 |
| rCaCH (D888) | Rattus norvegicus | 10 µM | 4.9 | Cerep_163 | |
| rCaCH (nitrendipine) | Rattus norvegicus | 10 µM | 14.0 | Cerep_161 | |
| rNaCH | Rattus norvegicus | 10 µM | 1.6 | Old_Cerep_169 | |
| rOP2 | OPRK1 | Homo sapiens | 10 µM | 77.9 | Cerep_4461 |
| hA1 | ADORA1 | Homo sapiens | 10 µM | -13.2 | Cerep_2 |
| hA2A | ADORA2A | Homo sapiens | 10 µM | 4.9 | Cerep_4 |
| hA3 | ADORA3 | Homo sapiens | 10 µM | 16.0 | Cerep_6 |
| rAa1 |
ADRA1A ADRA1B ADRA1D |
Rattus norvegicus | 10 µM | 19.5 | Cerep_8 |
| rAa2 |
ADRA2A ADRA2B ADRA2C |
Rattus norvegicus | 10 µM | 69.1 | Cerep_11 |
| hAb1 | ADRB1 | Homo sapiens | 10 µM | 11.2 | Cerep_18 |
| rBZD | Rattus norvegicus | 10 µM | -16.6 | Cerep_28 | |
| hBK2 | BDKRB2 | Homo sapiens | 10 µM | 10.8 | Cerep_33 |
| hCCKA | CCKAR | Homo sapiens | 10 µM | -22.0 | Cerep_39 |
| hD1 | DRD1 | Homo sapiens | 10 µM | 20.1 | Cerep_44 |
| hDAT | SLC6A3 | Homo sapiens | 10 µM | 19.3 | Cerep_52 |
| hETA | EDNRA | Homo sapiens | 10 µM | 3.6 | Cerep_54 |
| rGABA | Rattus norvegicus | 10 µM | -9.8 | Cerep_57 | |
| hM1 | CHRM1 | Homo sapiens | 10 µM | 32.5 | Cerep_91 |
| hM2 | CHRM2 | Homo sapiens | 10 µM | 25.4 | Cerep_93 |
| hM3 | CHRM3 | Homo sapiens | 10 µM | 45.6 | Cerep_95 |
| hNK2 | TACR2 | Homo sapiens | 10 µM | 4.5 | Cerep_102 |
| hNK3 | TACR3 | Homo sapiens | 10 µM | 7.0 | Cerep_104 |
| hNT1 | NTSR1 | Homo sapiens | 10 µM | 4.2 | Cerep_109 |
| hOP1 | OPRD1 | Homo sapiens | 10 µM | 20.4 | Cerep_114 |
| hOP3 | OPRM1 | Homo sapiens | 10 µM | 55.4 | Cerep_118 |
| h5HT1A | HTR1A | Homo sapiens | 10 µM | 9.5 | Cerep_131 |
| h5HT5A | HTR5A | Homo sapiens | 10 µM | -7.7 | Cerep_140 |
| h5HT6 | HTR6 | Homo sapiens | 10 µM | 14.2 | Cerep_142 |
| h5HT7 | HTR7 | Homo sapiens | 10 µM | -1.7 | Cerep_144 |
| mSST | Mus musculus | 10 µM | 4.2 | Cerep_149 | |
| hV1a | AVPR1A | Homo sapiens | 10 µM | 7.7 | Cerep_159 |
| rKCH | Rattus norvegicus | 10 µM | 1.0 | Cerep_166 | |
| rSKCaCH | Rattus norvegicus | 10 µM | 35.4 | Cerep_167 | |
| rCLCH | Rattus norvegicus | 10 µM | -5.7 | Old_Cerep_170 | |
| hNET | SLC6A2 | Homo sapiens | 10 µM | 5.8 | Cerep_355 |
| h5HT3 | HTR3A | Homo sapiens | 10 µM | 1.9 | Cerep_411 |
| h5HTT | SCL6A4 | Homo sapiens | 10 µM | -7.1 | Cerep_439 |
| hH1 | HRH1 | Homo sapiens | 10 µM | 5.7 | Cerep_870 |
| hH2 | HRH2 | Homo sapiens | 10 µM | 11.5 | Cerep_1208 |
| h5HT2B | HTR2B | Homo sapiens | 10 µM | 6.3 | Cerep_1333 |