Selectivity data for probe JNJ-4355 and control JNJ-78732576
Jump to control PDSP data
JNJ-4355
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| 5-HT1A | HTR1A | 47.84 | ||
| 5-HT1B | HTR1B | 2.80 | ||
| 5-HT1D | HTR1D | -6.42 | ||
| 5-HT2A | HTR2A | -0.64 | ||
| 5-HT2C | HTR2C | 1.66 | ||
| 5-HT3 | HTR3A | 6.57 | ||
| 5-HT5A | HTR5A | 28.46 | ||
| 5-HT6 | HTR6 | -22.49 | ||
| 5-HT7A | HTR7 | 20.10 | ||
| Alpha1A | ADRA1A | -11.84 | ||
| Alpha1B | ADRA1B | -1.94 | ||
| Alpha1D | ADRA1D | 2.28 | ||
| Alpha2A | ADRA2A | 21.53 | ||
| Alpha2B | ADRA2B | 6.60 | ||
| Alpha2C | ADRA2C | 3.84 | ||
| Beta1 | ADRB1 | -18.45 | ||
| Beta2 | ADRB2 | 4.71 | ||
| Beta3 | ADRB3 | 24.52 | ||
| GABAA/BZP | -20.56 | |||
| D1 | DRD1 | 10.45 | ||
| D2 | DRD2 | -6.66 | ||
| D3 | DRD3 | 13.50 | ||
| D4 | DRD4 | 2.70 | ||
| D5 | DRD5 | 26.20 | ||
| DAT | SLC6A3 | 49.53 | ||
| DOR | OPRD1 | 61.85 | 1344.93 | 5.87 |
| H1 | HRH1 | -0.28 | ||
| H3 | HRH3 | 4.96 | ||
| H4 | HRH4 | -14.62 | ||
| KOR | OPRK1 | 0.68 | ||
| M1 | CHRM1 | 4.67 | ||
| M2 | CHRM2 | -0.94 | ||
| M3 | CHRM3 | -0.43 | ||
| M4 | CHRM4 | -15.42 | ||
| M5 | CHRM5 | -9.51 | ||
| MOR | OPRM1 | -64.13 | > 10000.00 | < 5.00 |
| NET | SLC6A2 | 30.07 | ||
| GABA/PBR | 18.73 | |||
| SERT | SLC6A4 | 11.15 | ||
| Sigma 1 | TMEM97 | 20.64 | ||
| Sigma 2 | SIGMAR1 | 17.35 | ||
| 5-HT2B | HTR2B | -1.50 |
JNJ-78732576
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| 5-HT2B | HTR2B | 6.21 | ||
| 5-HT1A | HTR1A | 76.46 | 2242.33 | 5.65 |
| 5-HT1B | HTR1B | 23.04 | ||
| 5-HT1D | HTR1D | 31.41 | ||
| 5-HT2A | HTR2A | 10.64 | ||
| 5-HT2C | HTR2C | 7.75 | ||
| 5-HT3 | HTR3A | 8.89 | ||
| 5-HT5A | HTR5A | 54.49 | ||
| 5-HT6 | HTR6 | -22.12 | ||
| 5-HT7A | HTR7 | 18.98 | ||
| Alpha1A | ADRA1A | -4.41 | ||
| Alpha1B | ADRA1B | -0.92 | ||
| Alpha1D | ADRA1D | 1.09 | ||
| Alpha2A | ADRA2A | 6.61 | ||
| Alpha2B | ADRA2B | 29.52 | ||
| Alpha2C | ADRA2C | 7.00 | ||
| Beta1 | ADRB1 | -3.32 | ||
| Beta2 | ADRB2 | -3.65 | ||
| GABAA/BZP | -14.61 | |||
| D1 | DRD1 | 34.73 | ||
| D2 | DRD2 | -6.49 | ||
| D3 | DRD3 | 18.23 | ||
| D4 | DRD4 | 3.35 | ||
| D5 | DRD5 | 51.66 | ||
| DAT | SLC6A3 | 57.71 | 3723.97 average (n=2) | 5.45 |
| DOR | OPRD1 | 77.96 | 1359.25 | 5.87 |
| H1 | HRH1 | 10.85 | ||
| H3 | HRH3 | -6.18 | ||
| H4 | HRH4 | -20.76 | ||
| KOR | OPRK1 | 36.63 | ||
| M1 | CHRM1 | 1.89 | ||
| M2 | CHRM2 | 4.40 | ||
| M3 | CHRM3 | -1.43 | ||
| M4 | CHRM4 | -9.96 | ||
| M5 | CHRM5 | 2.15 | ||
| MOR | OPRM1 | 10.39 | ||
| NET | SLC6A2 | 58.91 | 2882.07 average (n=2) | 5.56 |
| GABA/PBR | 11.79 | |||
| SERT | SLC6A4 | 11.37 | ||
| Sigma 1 | TMEM97 | 30.74 | ||
| Sigma 2 | SIGMAR1 | 23.36 | ||
| Beta 3 | ADRB3 | 14.24 |
JNJ-4355
Cell activity was tested with various cell lines (AC50 = half-maximal activity concentration). Two different assays were used : CTG = Cell titer Glo assay (Promega), CasGlo= Caspase-Glo assay (Promega).
Conclusion: There is a high cell potency across a range of hematological cancers.
| Tumor type | Cell line | Species | Cell Proliferation AC50 [nM] | Assay |
|---|---|---|---|---|
| AML | EOL-1 | Homo sapiens | 2.10 | CTG |
| AML | NOMO-1 | Homo sapiens | 4.80 | CTG |
| AML | MOLM-13 | Homo sapiens | 10.00 | CTG |
| AML | MV4-11 | Homo sapiens | 14.00 | CTG |
| AML | THP-1 | Homo sapiens | 27.00 | CTG |
| AML | OCI-AML-2 | Homo sapiens | 48.00 | CTG |
| Lymphoma | SU-DHL-4 | Homo sapiens | 21.00 | CTG |
| Lymphoma | MINO | Homo sapiens | 73.00 | CTG |
| Myeloma | MOLP8 | Homo sapiens | 8.70 | CasGlo |
| Myeloma | KMS-12-PE | Homo sapiens | 69.00 | CasGlo |
| Myeloma | KMS-12-PE | Homo sapiens | 79.00 | CTG |
| Myeloma | KMS-12-PE MCL-1 KO | Homo sapiens | 30000.00 | CasGlo |
| Myeloma | KMS-12-PE Bax/Bak dKO | Homo sapiens | 30000.00 | CTG |