Selectivity data for probe Borussertib and control RL2578
Jump to control PDSP data
Borussertib
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| H2 | HRH2 | 65.13 | 949.61 average (n=2) | 6.09 |
| Beta3 | ADRB3 | 9.68 | ||
| 5-HT1B | HTR1B | 35.62 | ||
| 5-HT1D | HTR1D | 12.11 | ||
| 5-HT1A | HTR1A | 14.98 | ||
| 5-HT1E | HTR1E | 18.03 | ||
| 5-HT2A | HTR2A | -6.26 | ||
| 5-HT2B | HTR2B | -2.56 | ||
| 5-HT2C | HTR2C | -8.03 | ||
| 5-HT3 | HTR3A | 30.24 | ||
| 5-HT5A | HTR5A | 19.41 | ||
| 5-HT6 | HTR6 | -3.73 | ||
| 5-HT7A | HTR7 | -21.35 | ||
| Alpha1A | ADRA1A | 72.24 | 2655.83 | 5.58 |
| Alpha1B | ADRA1B | 52.26 | 4244.24 | 5.37 |
| Alpha1D | ADRA1D | 22.14 | ||
| Alpha2A | ADRA2A | 9.04 | ||
| Alpha2B | ADRA2B | 4.03 | ||
| Alpha2C | ADRA2C | -7.20 | ||
| Beta1 | ADRB1 | -0.86 | ||
| Beta2 | ADRB2 | 18.34 | ||
| GABAA/BZP | 12.30 | |||
| D1 | DRD1 | 19.20 | ||
| D2 | DRD2 | 22.72 | ||
| D3 | DRD3 | 20.85 | ||
| D4 | DRD4 | 10.04 | ||
| D5 | DRD5 | 28.83 | ||
| DAT | SLC6A3 | 59.74 | 3655.95 | 5.44 |
| DOR | OPRD1 | 24.10 | ||
| H1 | HRH1 | 23.78 | ||
| H3 | HRH3 | 6.51 | ||
| H4 | HRH4 | 31.28 | ||
| KOR | OPRK1 | 48.69 | ||
| M1 | CHRM1 | -8.04 | ||
| M2 | CHRM2 | 3.07 | ||
| M3 | CHRM3 | 5.83 | ||
| M4 | CHRM4 | -7.81 | ||
| M5 | CHRM5 | 11.78 | ||
| MOR | OPRM1 | 32.37 | ||
| NET | SLC6A2 | 4.49 | ||
| GABA/PBR | 72.26 | 57.32 | 7.24 | |
| SERT | SLC6A4 | 2.16 | ||
| Sigma 1 | SIGMAR1 | 17.83 | ||
| Sigma 2 | TMEM97 | 24.77 |
Borussertib
Results are averages from duplicated measurements performed at the apparent ATP KM of each individual kinase using the activity based Z’LYTE kinase assay of the SelectScreen Kinase Profiling Services (LifeTechnologies). Shown are supplementary data from PMID: 26110718 (Table S1) . (Assay conditions)
Conclusion: The only off-target is AKT3 with 83 % inhibition.
| Target protein | HGNC name | Species | % Inhibition at 1 µM |
|---|---|---|---|
| ABL1 | ABL1 | Homo sapiens | 2.0 |
| ACVR1B (ALK4) | ACVR1B | Homo sapiens | -13.0 |
| AKT1 (PKB alpha) | AKT1 | Homo sapiens | 98.0 |
| AKT2 (PKB beta) | AKT2 | Homo sapiens | 96.0 |
| AKT3 (PKB gamma) | AKT3 | Homo sapiens | 83.0 |
| ALK | ALK | Homo sapiens | -2.0 |
| AMPK A1/B1/G1 | PRKAA1 | Homo sapiens | 14.0 |
| AMPK A2/B1/G1 | PRKAA2 | Homo sapiens | 20.0 |
| AURKA (Aurora A) | AURKA | Homo sapiens | 15.0 |
| AURKB (Aurora B) | AURKB | Homo sapiens | 7.0 |
| BMX | BMX | Homo sapiens | 7.0 |
| BRSK1 (SAD1) | BRSK1 | Homo sapiens | 7.0 |
| BTK | BTK | Homo sapiens | 6.0 |
| CAMK1D (CaMKI delta) | CAMK1D | Homo sapiens | 9.0 |
| CAMK4 (CaMKIV) | CAMK4 | Homo sapiens | 12.0 |
| CDC42 BPA (MRCKA) | CDC42BPA | Homo sapiens | 2.0 |
| CDC42 BPB (MRCKB) | CDC42BPB | Homo sapiens | 1.0 |
| CDK1/cyclin B | CDK1 | Homo sapiens | 3.0 |
| CDK2/cyclin A | CDK2 | Homo sapiens | 1.0 |
| CHEK1 (CHK1) | CHEK1 | Homo sapiens | -4.0 |
| CHEK2 (CHK2) | CHEK2 | Homo sapiens | 4.0 |
| DCAMKL2 (DCK2) | DCLK2 | Homo sapiens | -2.0 |
| DNA-PK | PRKDC | Homo sapiens | 0.0 |
| EGFR (ErbB1) | EGFR | Homo sapiens | 2.0 |
| EPHA2 | EPHA2 | Homo sapiens | -12.0 |
| EPHB4 | EPHA4 | Homo sapiens | 7.0 |
| ERBB2 (HER2) | ERBB2 | Homo sapiens | -3.0 |
| FGFR1 | FGFR1 | Homo sapiens | 25.0 |
| FLT3 | FLT3 | Homo sapiens | 17.0 |
| FRAP1 (mTOR) | MTOR | Homo sapiens | -9.0 |
| GRK4 | GRK4 | Homo sapiens | 8.0 |
| GRK5 | GRK5 | Homo sapiens | -2.0 |
| GRK6 | GRK6 | Homo sapiens | 2.0 |
| GRK7 | GRK7 | Homo sapiens | -6.0 |
| GSK3B (GSK3 beta) | GSK3B | Homo sapiens | 20.0 |
| IGF1R | IGF1R | Homo sapiens | -4.0 |
| ITK | ITK | Homo sapiens | -1.0 |
| JAK2 | JAK2 | Homo sapiens | -8.0 |
| JAK3 | JAK3 | Homo sapiens | -11.0 |
| KIT | KIT | Homo sapiens | 8.0 |
| LCK | LCK | Homo sapiens | 8.0 |
| MAP4K5 (KHS1) | MAP4K5 | Homo sapiens | 37.0 |
| MAPK1 (ERK2) | MAPK1 | Homo sapiens | 3.0 |
| MAPK14 (p38 alpha) Direct | MAPK14 | Homo sapiens | -1.0 |
| MAPK3 (ERK1) | MAPK3 | Homo sapiens | -3.0 |
| MAPKAPK2 | MAPKAPK2 | Homo sapiens | 30.0 |
| MAPKAPK3 | MAPKAPK3 | Homo sapiens | 17.0 |
| MARK1 (MARK) | MARK1 | Homo sapiens | -7.0 |
| MARK2 | MARK2 | Homo sapiens | -2.0 |
| MELK | MELK | Homo sapiens | 30.0 |
| MET (cMet) | MET | Homo sapiens | -2.0 |
| MKNK1 (MNK1) | MINK1 | Homo sapiens | 8.0 |
| NEK1 | NEK1 | Homo sapiens | 8.0 |
| NTRK2 (TRKB) | NTRK2 | Homo sapiens | -15.0 |
| PAK1 | PAK1 | Homo sapiens | -9.0 |
| PAK4 | PAK4 | Homo sapiens | 7.0 |
| PASK | PASK | Homo sapiens | 15.0 |
| PDGFRA (PDGFR alpha) | PDGFRA | Homo sapiens | -12.0 |
| PDK1 Direct | PDK1 | Homo sapiens | -4.0 |
| PIM1 | PIM1 | Homo sapiens | 0.0 |
| PKN1 (PRK1) | PKN1 | Homo sapiens | -4.0 |
| PLK1 | PLK1 | Homo sapiens | -3.0 |
| PRKACA (PKA) | PRKACA | Homo sapiens | -3.0 |
| PRKCA (PKC alpha) | PRKCA | Homo sapiens | 10.0 |
| PRKCB1 (PKC beta I) | PRKCB | Homo sapiens | -7.0 |
| PRKCB2 (PKC beta II) | PRKCB | Homo sapiens | 9.0 |
| PRKCD (PKC delta) | PRKCD | Homo sapiens | -8.0 |
| PRKCE (PKC epsilon) | PRKCE | Homo sapiens | -1.0 |
| PRKCG (PKC gamma) | PRKCG | Homo sapiens | 17.0 |
| PRKCH (PKC eta) | PRKCH | Homo sapiens | -2.0 |
| PRKCI (PKC iota) | PRKCI | Homo sapiens | 6.0 |
| PRKCN (PKD3) | PRKD3 | Homo sapiens | 14.0 |
| PRKCQ (PKC theta) | PRKCQ | Homo sapiens | 35.0 |
| PRKCZ (PKC zeta) | PRKCZ | Homo sapiens | -1.0 |
| PRKD1 (PKC mu) | PRKD1 | Homo sapiens | 10.0 |
| PRKD2 (PKD2) | PRKD2 | Homo sapiens | 5.0 |
| PRKG1 | PRKG1 | Homo sapiens | 5.0 |
| PRKG2 (PKG2) | PRKG2 | Homo sapiens | 2.0 |
| PRKX | PRKX | Homo sapiens | 3.0 |
| PTK2 (FAK) | PTK2 | Homo sapiens | 4.0 |
| RET | RET | Homo sapiens | 7.0 |
| ROCK1 | ROCK1 | Homo sapiens | 9.0 |
| ROCK2 | ROCK2 | Homo sapiens | -3.0 |
| RPS6KA1 (RSK1) | RPS6KA1 | Homo sapiens | 12.0 |
| RPS6KA2 (RSK3) | RPS6KA2 | Homo sapiens | 14.0 |
| RPS6KA3 (RSK2) | RPS6KA3 | Homo sapiens | 21.0 |
| RPS6KA4 (MSK2) | RPS6KA4 | Homo sapiens | 8.0 |
| RPS6KA5 (MSK1) | RPS6KA5 | Homo sapiens | 2.0 |
| RPS6KA6 (RSK4) | RPS6KA6 | Homo sapiens | 14.0 |
| RPS6KB1 (p70S6K) | RPS6KB1 | Homo sapiens | 2.0 |
| SGK (SGK1) | SGK1 | Homo sapiens | 20.0 |
| SGK2 | SGK2 | Homo sapiens | 6.0 |
| SGKL (SGK3) | SGK3 | Homo sapiens | 2.0 |
| SRC | SRC | Homo sapiens | 10.0 |
| STK3 (MST2) | STK3 | Homo sapiens | 1.0 |
| STK4 (MST1) | STK4 | Homo sapiens | -1.0 |
| SYK | SYK | Homo sapiens | -3.0 |
| TBK1 | TBK1 | Homo sapiens | 6.0 |
| TEK (Tie2) | TEK | Homo sapiens | 13.0 |
| TXK | TXK | Homo sapiens | 8.0 |