Selectivity data for probe JNJ-39758979 and control JNJ-39668551
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JNJ-39758979
Shown are data from PMID: 24549371 (Supplementary Table 1) .
Conclusion: Clean panel. Ki for CHRM1, CHRM2, CHRM3, CHRM4 was > 10 µM in a follow up assay.
| Target protein | HGNC name | Species | % inhibition at 1 µM | Ki [nM] |
|---|---|---|---|---|
| alpha 1 (non-selective) | < 10.0 | |||
| alpha 2 (non-selective) | 18.0 | |||
| beta 1 (h) | ADRB1 | Homo sapiens | < 10.0 | |
| NE transporter (h) | SLC6A2 | Homo sapiens | 10.0 | |
| BZD (central) | < 10.0 | |||
| A2A (h) | ADORA2A | Homo sapiens | < 10.0 | |
| A3 (h) | ADORA3 | Homo sapiens | < 10.0 | |
| A1 (h) | ADORA1 | Homo sapiens | < 10.0 | |
| B2 (h) | ADRB2 | Homo sapiens | < 10.0 | |
| CCKA (h) (CCK1) | CCKAR | Homo sapiens | < 10.0 | |
| D1 (h) | DRD1 | Homo sapiens | < 10.0 | |
| D2 (h) | DRD2 | Homo sapiens | < 10.0 | |
| DA transporter (h) | SLC6A3 | Homo sapiens | 18.0 | |
| ETA (h) | EDNRA | Homo sapiens | 15.0 | |
| GABA (non-selective) | < 10.0 | |||
| GAL2 (h) | GALR2 | Homo sapiens | < 10.0 | |
| IL-8B (h) (CXCR2) | CXCR2 | Homo sapiens | < 10.0 | |
| CCR1 (h) | CCR1 | Homo sapiens | < 10.0 | |
| H1 (h) | HRH1 | Homo sapiens | < 10.0 | |
| H2 (h) | HRH2 | Homo sapiens | < 10.0 | |
| MC4 (h) | MC4R | Homo sapiens | < 10.0 | |
| MT1 | < 10.0 | |||
| M1 (h) | CHRM1 | Homo sapiens | 19.0 | > 10.00 |
| M2 (h) | CHRM2 | Homo sapiens | < 10.0 | > 10.00 |
| M3 (h) | CHRM3 | Homo sapiens | 64.0 | > 10.00 |
| NK2 (h) | TACR2 | Homo sapiens | < 10.0 | |
| NK3 (h) | TACR3 | Homo sapiens | < 10.0 | |
| Y1 (h) | NPY1R | Homo sapiens | < 10.0 | |
| Y2 (h) | NPY2R | Homo sapiens | < 10.0 | |
| NT1 (h) (NTS1) | NTSR1 | Homo sapiens | < 10.0 | |
| delta (h) | OPRD1 | Homo sapiens | < 10.0 | |
| kappa (h) | OPRK1 | Homo sapiens | < 10.0 | |
| mu (h) | OPRM1 | Homo sapiens | < 10.0 | |
| ORL1 (h) | OPRL1 | Homo sapiens | < 10.0 | |
| 5-HT1A (h) | HTR1A | Homo sapiens | < 10.0 | |
| 5-HT1B | HTR1B | < 10.0 | ||
| 5-HT2A (h) | HTR2A | Homo sapiens | < 10.0 | |
| 5-HT3 (h) | HTR3A | Homo sapiens | < 10.0 | |
| 5-HT5A (h) (5-ht5a) | HTR5A | Homo sapiens | < 10.0 | |
| 5-HT6 (h) (5-ht6) | HTR6 | Homo sapiens | < 10.0 | |
| 5-HT7 (h) | HTR7 | Homo sapiens | < 10.0 | |
| sst (non-selective) | < 10.0 | |||
| VIP1 (h) (VPAC1) | VIPR1 | Homo sapiens | < 10.0 | |
| V1A (h) | AVPR1A | Homo sapiens | < 10.0 | |
| Ca2+ channel | < 10.0 | |||
| K+V channel | < 10.0 | |||
| SK+Ca channel | < 10.0 | |||
| Na+ channel (site 2) | < 10.0 | |||
| Cl- channel | < 10.0 |
JNJ-39758979
Shown are data from PMID: 24549371 (Supplementary Table 2) .
Conclusion: Clean panel.
| Target protein | HGNC name | Species | % inhibition |
|---|---|---|---|
| Abl(h) | ABL1 | Homo sapiens | -2.0 |
| ALK(h) | ALK | Homo sapiens | 12.0 |
| AMPK(r) | Rattus sp. | 1.0 | |
| Aurora-A(h) | AURKA | Homo sapiens | -14.0 |
| Axl(h) | AXL | Homo sapiens | -11.0 |
| BTK(h) | BTK | Homo sapiens | -9.0 |
| CaMKI(h) | CAMK1 | Homo sapiens | 3.0 |
| CaMKII(r) | Rattus sp. | -18.0 | |
| CDK2/cyclinA(h) | CDK2 | Homo sapiens | -3.0 |
| CHK1(h) | CHEK1 | Homo sapiens | -18.0 |
| CHK2(h) | CHEK2 | Homo sapiens | 4.0 |
| CK1δ(h) | CSNK1D | Homo sapiens | 1.0 |
| CK2(h) | Homo sapiens | 4.0 | |
| CLK3(h) | CLK3 | Homo sapiens | 9.0 |
| c-RAF(h) | RAF1 | Homo sapiens | -5.0 |
| CSK(h) | CSK | Homo sapiens | -9.0 |
| cSRC(h) | SRC | Homo sapiens | -5.0 |
| DAPK1(h) | DAPK1 | Homo sapiens | -3.0 |
| DCAMKL2(h) | DCLK2 | Homo sapiens | 1.0 |
| DDR2(h) | DDR2 | Homo sapiens | -8.0 |
| DYRK2(h) | DYRK2 | Homo sapiens | -20.0 |
| EGFR(h) | EGFR | Homo sapiens | 2.0 |
| EphA1(h) | EPHA1 | Homo sapiens | -6.0 |
| FAK(h) | PTK2 | Homo sapiens | -1.0 |
| Fer(h) | FER | Homo sapiens | -8.0 |
| FGFR1(h) | FGFR1 | Homo sapiens | -13.0 |
| Flt3(h) | FLT3 | Homo sapiens | -12.0 |
| GSK3α(h) | GSK3A | Homo sapiens | 8.0 |
| GSK3β(h) | GSK3B | Homo sapiens | 0.0 |
| IGF-1R(h) | IGF1R | Homo sapiens | -27.0 |
| IKKα(h) | CHUK | Homo sapiens | -18.0 |
| IRAK1(h) | IRAK1 | Homo sapiens | -6.0 |
| IRAK4(h) | IRAK4 | Homo sapiens | -5.0 |
| JAK2(h) | JAK2 | Homo sapiens | -7.0 |
| JNK1α1(h) | MAPK8 | Homo sapiens | 10.0 |
| LIMK1(h) | LIMK1 | Homo sapiens | -10.0 |
| LKB1(h) | STK11 | Homo sapiens | 0.0 |
| MAPKAP-K2(h) | MAPKAPK2 | Homo sapiens | -11.0 |
| Met(h) | MET | Homo sapiens | -15.0 |
| MLK1(h) | MAP3K9 | Homo sapiens | 6.0 |
| MSK1(h) | RPS6KA5 | Homo sapiens | 6.0 |
| MSSK1(h) | SRPK1 | Homo sapiens | -1.0 |
| MuSK(h) | MUSK | Homo sapiens | -9.0 |
| NEK2(h) | NEK2 | Homo sapiens | -10.0 |
| p70S6K(h) | RPS6KB1 | Homo sapiens | 8.0 |
| PDK1(h) | PDK1 | Homo sapiens | -4.0 |
| Pim-1(h) | PIM1 | Homo sapiens | 3.0 |
| PKA(h) | PRKACA | Homo sapiens | -2.0 |
| PKBα(h) | AKT1 | Homo sapiens | -7.0 |
| PKBβ(h) | AKT2 | Homo sapiens | -5.0 |
| PKBγ(h) | AKT3 | Homo sapiens | -3.0 |
| PKCα(h) | PRKCA | Homo sapiens | 23.0 |
| PKD2(h) | PRKD2 | Homo sapiens | 8.0 |
| PKG1α(h) | PRKG1 | Homo sapiens | -2.0 |
| Plk3(h) | PLK3 | Homo sapiens | -5.0 |
| Ret(h) | RET | Homo sapiens | -6.0 |
| Ros(h) | ROS1 | Homo sapiens | 6.0 |
| SAPK2a(h) | MAPK14 | Homo sapiens | -12.0 |
| SGK(h) | SGK1 | Homo sapiens | 7.0 |
| STK33(h) | STK33 | Homo sapiens | -4.0 |
| Syk(h) | SYK | Homo sapiens | 3.0 |
| Tie2(h) | TEK | Homo sapiens | 12.0 |
| TrkA(h) | NTRK1 | Homo sapiens | 13.0 |
| TSSK1(h) | TSSK1B | Homo sapiens | 16.0 |
| WNK2(h) | WNK2 | Homo sapiens | -5.0 |
| VRK2(h) | VRK2 | Homo sapiens | -2.0 |