Selectivity data for probe JNJ-54119936 and control JNJ-53721590
Jump to control PDSP data
JNJ-54119936
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| 5-HT1B | HTR1B | 8.87 | ||
| 5-HT1D | HTR1D | 5.90 | ||
| 5-HT1A | HTR1A | 16.62 | ||
| Sigma 2 | TMEM97 | 65.81 | 636.66 average (n=2) | 6.22 |
| 5-HT2A | HTR2A | 6.87 | ||
| 5-HT2B | HTR2B | 18.70 | ||
| Alpha1A | ADRA1A | 10.28 | ||
| Alpha1B | ADRA1B | -4.69 | ||
| Alpha1D | ADRA1D | 6.64 | ||
| Beta1 | ADRB1 | 15.25 | ||
| Beta2 | ADRB2 | 15.56 | ||
| D1 | DRD1 | 19.87 | ||
| D3 | DRD3 | -2.36 | ||
| D5 | DRD5 | 33.89 | ||
| GABAA | -28.84 | |||
| H1 | HRH1 | 38.04 | ||
| H2 | HRH2 | -0.99 | ||
| H3 | HRH3 | 0.46 | ||
| H4 | HRH4 | -21.19 | ||
| M1 | CHRM1 | 5.40 | ||
| M2 | CHRM2 | 1.16 | ||
| M3 | CHRM3 | 0.49 | ||
| M4 | CHRM4 | 8.86 | ||
| M5 | CHRM5 | -16.10 | ||
| NET | SLC6A2 | 21.70 | ||
| GABA/PBR | 35.60 | |||
| 5-HT1E | HTR1E | -18.69 | ||
| 5-HT2C | HTR2C | 21.18 | ||
| 5-HT3 | HTR3A | 9.28 | ||
| 5-HT5A | HTR5A | -0.46 | ||
| 5-HT6 | HTR6 | 8.80 | ||
| 5-HT7A | HTR7 | -2.29 | ||
| Alpha2A | ADRA2A | 20.77 | ||
| Alpha2B | ADRA2B | 54.57 | 9223.59 | 5.04 |
| Alpha2C | ADRA2C | 39.78 | ||
| Beta3 | ADRB3 | 39.39 | ||
| GABAA/BZP | 10.34 | |||
| D2 | DRD2 | 12.52 | ||
| D4 | DRD4 | -5.45 | ||
| DAT | SLC6A3 | 21.04 | ||
| DOR | OPRD1 | 7.18 | ||
| KOR | OPRK1 | -6.00 | ||
| MOR | OPRM1 | 25.56 | ||
| SERT | SLC6A4 | 5.62 | ||
| Sigma 1 | SIGMAR1 | 101.54 | 3125.58 average (n=2) | 5.52 |
JNJ-54119936
The screen was perfomred at Cerep Inc. (Redmond, WA, USA). For some data the average of two measurements is shown.
Conclusion: Clean panel
| Target protein | HGNC name | Species | % inhibition at 10 µM | % inhibition at 1 µM |
|---|---|---|---|---|
| A2a (h) | ADORA2A | Homo sapiens | 21.0 | 18.00 |
| A3 (h) | ADORA3 | Homo sapiens | 25.0 | 45.00 |
| AT1 (h) | AGTR1 | Homo sapiens | 11.0 | |
| D1 (h) | DRD1 | Homo sapiens | 16.0 | |
| D2S (h) | DRD2 | Homo sapiens | 10.00 | |
| ETA (h) | EDNRA | Homo sapiens | 12.0 | |
| GABA (non selective) | 12.00 | |||
| CXCR2 (h) | CXCR2 | Homo sapiens | 10.00 | |
| CCR1 (h) | CCR1 | Homo sapiens | 17.00 | |
| H1 (h) | HRH1 | Homo sapiens | 10.00 | |
| MC4 (h) | MC4R | Homo sapiens | 14.0 | |
| MT1 (ML1A) (h) | MTNR1A | Homo sapiens | 20.0 | |
| M1 (h) | CHRM1 | Homo sapiens | 21.0 | 12.00 |
| M3 (h) | CHRM3 | Homo sapiens | 19.0 | 21.00 |
| NK2 (h) | TACR2 | Homo sapiens | 23.0 | |
| NK3 (h) | TACR3 | Homo sapiens | 22.0 | 18.00 |
| Delta2 (h) | OPRD1 | Homo sapiens | 11.0 | |
| Kappa (KOP) (h) | OPRK1 | Homo sapiens | 12.0 | |
| Mu (h) | OPRM1 | Homo sapiens | 15.0 | |
| 5-HT3 (h) | HTR3A | Homo sapiens | 18.0 | |
| 5-HT5A (h) | HTR5A | Homo sapiens | 23.0 | 13.00 |
| 5-HT6 (h) | HTR6 | Homo sapiens | 22.0 | 20.00 |
| K+ channel (Volt-dependent) | 15.0 | |||
| Cl- channel | 44.0 | 21.00 | ||
| norepinephrine transporter (h) | SLC6A2 | Homo sapiens | 16.0 | 34.00 |
| dopamine transporter (h) | SLC6A3 | Homo sapiens | 30.0 | 18.00 |
| 5-HT transporter (h) | SLC6A4 | Homo sapiens | 13.0 |
JNJ-54119936
The transcriptional cellular reporter assays were performed at Indigo Biosciences Inc. Assays are described here.
Conclusion: Clean panel.
| Target protein | HGNC name | Species | % inhibition at 3 µM | % inhibition at 1 µM | % inhibition at 0.3 µM |
|---|---|---|---|---|---|
| PPARalpha | PPARA | Homo sapiens | -25.6 | -16.22 | 1.34 |
| PPARdelta | PPARD | Homo sapiens | 0.3 | -5.27 | -3.53 |
| PPARgamma | PPARG | Homo sapiens | -6.0 | -12.50 | -0.89 |
| LXRalpha | NR1H3 | Homo sapiens | -37.1 | -23.39 | -3.25 |
| LXRbeta | NR1H2 | Homo sapiens | 11.0 | 8.98 | 5.39 |
| CAR | NR1I3 | Homo sapiens | 2.4 | -0.75 | -0.12 |
| FXR | NR1H4 | Homo sapiens | -16.8 | 5.23 | -8.50 |
| GR | NR3C1 | Homo sapiens | 12.6 | 2.23 | 4.11 |
| ERalpha | ESR1 | Homo sapiens | -3.0 | 0.61 | -1.20 |
| ERbeta | ESR2 | Homo sapiens | 14.8 | 7.87 | 1.77 |
| TRalpha | THRA | Homo sapiens | -29.2 | -26.67 | -5.63 |
| TRbeta | THRB | Homo sapiens | -31.1 | -15.50 | 1.13 |
| VDR | VDR | Homo sapiens | -21.1 | -0.28 | -6.97 |
| PXR | NR1I2 | Homo sapiens | 1.0 | -26.42 | -7.63 |
| RXRalpha | RXRA | Homo sapiens | -59.2 | -30.15 | -12.18 |
JNJ-54119936
The selectivity screen was performed at 10 µM compound and 100 µM ATP using the z’-lite assay format.
Conclusion: Clean panel.
| Target protein | HGNC name | Species | % inhibition at 10 µM |
|---|---|---|---|
| Alk4 | ACVR1B | Homo sapiens | -5.0 |
| PKBalpha | AKT1 | Homo sapiens | -5.0 |
| Aurora_A | AURKA | Homo sapiens | 9.0 |
| Aurora_B | AURKB | Homo sapiens | 21.0 |
| Blk | BLK | Homo sapiens | 0.0 |
| CaMKIdelta | CAMK1D | Homo sapiens | 7.0 |
| CaMKIIalpha | CAMK2A | Homo sapiens | 14.0 |
| CaMKIIbeta | CAMK2B | Homo sapiens | 7.0 |
| CDK1/cyclinB | CDK1 | Homo sapiens | 0.0 |
| CDK5/p35 | CDK5 | Homo sapiens | -2.0 |
| CHK1 | CHEK1 | Homo sapiens | 2.0 |
| CHK2 | CHEK2 | Homo sapiens | 6.0 |
| CLK2 | CLK2 | Homo sapiens | 4.0 |
| CK1epsilon | CSNK1E | Homo sapiens | 0.0 |
| CK2alpha1 | CSNK2A1 | Homo sapiens | 2.0 |
| CK2alpha2 | CSNK2A2 | Homo sapiens | 4.0 |
| ZIPK | DAPK3 | Homo sapiens | 10.0 |
| EGFR | EGFR | Homo sapiens | -4.0 |
| EphA2 | EPHA2 | Homo sapiens | 6.0 |
| FGFR1 | FGFR1 | Homo sapiens | -2.0 |
| Flt3 | FLT3 | Homo sapiens | 4.0 |
| GRK4 | GRK4 | Homo sapiens | -14.0 |
| GSK3alpha | GSK3A | Homo sapiens | -4.0 |
| GSK3beta | GSK3B | Homo sapiens | 3.0 |
| IGF-1R | IGF1R | Homo sapiens | 6.0 |
| IKKbeta | IKBKB | Homo sapiens | 6.0 |
| INSR | INSR | Homo sapiens | 3.0 |
| IRAK4 | IRAK4 | Homo sapiens | 6.0 |
| JAK2 | JAK2 | Homo sapiens | 6.0 |
| JAK3 | JAK3 | Homo sapiens | 2.0 |
| ERK2 | MAPK1 | Homo sapiens | 13.0 |
| p38gamma | MAPK12 | Homo sapiens | 2.0 |
| p38delta | MAPK13 | Homo sapiens | 14.0 |
| ERK1 | MAPK3 | Homo sapiens | 10.0 |
| NEK2 | NEK2 | Homo sapiens | 3.0 |
| TrkC | NTRK3 | Homo sapiens | 3.0 |
| PAK3 | PAK3 | Homo sapiens | 6.0 |
| PAK4 | PAK4 | Homo sapiens | 4.0 |
| PDGFRbeta | PDGFRB | Homo sapiens | 5.0 |
| Pim2 | PIM2 | Homo sapiens | 1.0 |
| Plk1 | PLK1 | Homo sapiens | -1.0 |
| Plk3 | PLK3 | Homo sapiens | 3.0 |
| PKA | PRKACA | Homo sapiens | 1.0 |
| PKCalpha | PRKCA | Homo sapiens | 4.0 |
| PKCbetaI | PRKCB | Homo sapiens | 1.0 |
| Ret | RET | Homo sapiens | 3.0 |
| ROCK_I | ROCK1 | Homo sapiens | 4.0 |
| Rsk3 | RPS6KA2 | Homo sapiens | 11.0 |
| SRC | SRC | Homo sapiens | 4.0 |
| ZAP_70 | ZAP70 | Homo sapiens | 5.0 |
JNJ-54119936
The transcriptional cellular reporter assays were performed in-house at Janssen using protocols from commercial kits from Indigo Biosciences Inc. Assays are described here. Some values were calculated from the 3.3 µM dose from dose response curves.
Conclusion: Clean panel
| Target protein | HGNC name | Species | % inhibition at 3 µM | IC50 [nM] |
|---|---|---|---|---|
| PPARalpha | PPARA | Homo sapiens | 17.0 | ~ 5000.00 |
| PPARdelta | PPARD | Homo sapiens | 37.3 | 5900.00 |
| PPARgamma | PPARG | Homo sapiens | 28.2 | 5400.00 |
| LXRalpha | NR1H3 | Homo sapiens | 31.0 | 6400.00 |
| LXRbeta | NR1H2 | Homo sapiens | 10.0 | ~ 5000.00 |
| CAR | NR1I3 | Homo sapiens | 31.2 | 8400.00 |
| FXR | NR1H4 | Homo sapiens | 33.0 | 5800.00 |
| GR | NR3C1 | Homo sapiens | 13.0 | ~ 6000.00 |
| ERalpha | ESR1 | Homo sapiens | 16.8 | |
| ERbeta | ESR2 | Homo sapiens | 31.2 |