Selectivity data for probe BI 605906 and control BI-5026
Jump to control PDSP data
BI 605906
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| 5-HT1B | HTR1B | 3.43 | ||
| 5-HT1D | HTR1D | 26.95 | ||
| GABAA | 32.62 | |||
| 5-HT1A | HTR1A | 14.43 | ||
| Sigma 2 | TMEM97 | 34.49 | ||
| 5-HT2A | HTR2A | 6.10 | ||
| 5-HT2B | HTR2B | 13.36 | ||
| Alpha1A | ADRA1A | 18.88 | ||
| Alpha1B | ADRA1B | -0.02 | ||
| Alpha1D | ADRA1D | 36.74 | ||
| Beta1 | ADRB1 | -8.38 | ||
| Beta2 | ADRB2 | 8.96 | ||
| Beta3 | ADRB3 | 17.99 | ||
| D1 | DRD1 | 25.69 | ||
| D3 | DRD3 | 51.50 | 428.07 average (n=3) | 6.54 |
| D5 | DRD5 | 2.13 | ||
| H1 | HRH1 | 9.22 | ||
| H2 | HRH2 | -16.70 | ||
| H3 | HRH3 | 0.20 | ||
| H4 | HRH4 | -1.66 | ||
| M1 | CHRM1 | 8.33 | ||
| M2 | CHRM2 | 8.00 | ||
| M3 | CHRM3 | 21.10 | ||
| M4 | CHRM4 | 13.31 | ||
| M5 | CHRM5 | -10.33 | ||
| NET | SLC6A2 | 8.84 | ||
| GABA/PBR | 51.87 | 2622.51 average (n=2) | 5.59 | |
| 5-HT1E | HTR1E | 1.69 | ||
| 5-HT2C | HTR2C | -5.41 | ||
| 5-HT3 | HTR3A | -5.46 | ||
| 5-HT5A | HTR5A | 6.16 | ||
| 5-HT6 | HTR6 | 8.77 | ||
| 5-HT7A | HTR7 | 13.71 | ||
| Alpha2A | ADRA2A | -12.44 | ||
| Alpha2B | ADRA2B | 9.66 | ||
| Alpha2C | ADRA2C | 13.65 | ||
| GABAA/BZP | 8.92 | |||
| D2 | DRD2 | 69.76 | 341.44 average (n=2) | 6.48 |
| D4 | DRD4 | 44.56 | ||
| DAT | SLC6A3 | 2.35 | ||
| DOR | OPRD1 | 3.97 | ||
| KOR | OPRK1 | 8.09 | ||
| MOR | OPRM1 | 5.18 | ||
| SERT | SLC6A4 | 8.94 | ||
| Sigma 1 | SIGMAR1 | 8.89 |
BI-5026
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| Alpha1B | ADRA1B | -7.86 | ||
| 5-HT1E | HTR1E | 2.45 | ||
| 5-HT2C | HTR2C | 11.57 | ||
| 5-HT3 | HTR3A | 10.29 | ||
| 5-HT5A | HTR5A | 5.35 | ||
| 5-HT6 | HTR6 | 24.19 | ||
| 5-HT7A | HTR7 | 2.32 | ||
| Alpha2A | ADRA2A | 12.98 | ||
| Alpha2B | ADRA2B | 3.36 | ||
| Alpha2C | ADRA2C | 2.96 | ||
| Beta3 | ADRB3 | -18.58 | ||
| GABAA/BZP | 13.53 | |||
| D2 | DRD2 | 1.12 | ||
| D4 | DRD4 | 4.15 | ||
| DAT | SLC6A3 | 80.47 | 4270.71 | 5.37 |
| DOR | OPRD1 | 8.58 | ||
| KOR | OPRK1 | 9.53 | ||
| MOR | OPRM1 | 22.41 | ||
| SERT | SLC6A4 | 18.09 | ||
| Sigma 1 | SIGMAR1 | 31.52 | ||
| 5-HT2A | HTR2A | -1.79 | ||
| 5-HT2B | HTR2B | 47.51 | ||
| Alpha1A | ADRA1A | 22.83 | ||
| Alpha1D | ADRA1D | 7.27 | ||
| Beta1 | ADRB1 | -41.21 | ||
| Beta2 | ADRB2 | 6.22 | ||
| D1 | DRD1 | 1.22 | ||
| D3 | DRD3 | -12.53 | ||
| D5 | DRD5 | -19.74 | ||
| GABAA | 3.61 | |||
| H1 | HRH1 | 24.46 | ||
| H2 | HRH2 | -1.35 | ||
| H3 | HRH3 | -1.10 | ||
| H4 | HRH4 | -16.67 | ||
| M1 | CHRM1 | 0.25 | ||
| M2 | CHRM2 | 13.37 | ||
| M3 | CHRM3 | 7.05 | ||
| M4 | CHRM4 | 3.63 | ||
| M5 | CHRM5 | -6.93 | ||
| NET | SLC6A2 | 1.70 | ||
| GABA/PBR | 27.87 | |||
| 5-HT1A | HTR1A | 40.62 | ||
| Sigma 2 | TMEM97 | 70.59 | 7307.71 average (n=2) | 5.14 |
| 5-HT1B | HTR1B | -10.69 | ||
| 5-HT1D | HTR1D | 6.70 |
BI 605906
Conclusion: Results for all other targets >50 % Ctrl except for human PDE3A with 31 % Ctrl at 10 µM.
| Target protein | HGNC name | Species | % control at 10 µM | % control at 30 µM | % control at 3 µM | % control at 1 µM | % control at 100 µM | Mode of action | Assay |
|---|---|---|---|---|---|---|---|---|---|
| 12-LO | ALOX12 | Homo sapiens | 96.0 | Fluorimetry | |||||
| 15LO | ALOX15 | Oryctolagus cuniculus | 79.0 | inhibitor | absorption of electromagnetic radiation | ||||
| 5HT1/R | Rattus norvegicus | 119.0 | 107.00 | Radioactive Assay | |||||
| 5HT2/R | Rattus norvegicus | 97.0 | 95.00 | Radioactive Assay | |||||
| 5HT3/HU | HTR3A | Homo sapiens | 84.0 | Others | |||||
| 5HT4/GPIG | HTR4 | Cavia porcellus | 98.0 | Radioactive Assay | |||||
| 5HTTRANS/HU | SLC6A4 | Homo sapiens | 108.0 | Radioactive Assay | |||||
| 5LO | ALOX5 | Homo sapiens | 53.0 | inhibitor | Enzyme Immunoassay | ||||
| A1/HU | ADORA1 | Homo sapiens | 77.00 | Radioactive Assay | |||||
| ACHOLINEST | ACHE | Homo sapiens | 87.0 | inhibitor | Photometry | ||||
| ALPHA1/R | Rattus norvegicus | 109.0 | 93.00 | Others | |||||
| ALPHA2/R | Rattus norvegicus | 103.0 | 102.00 | Others | |||||
| ANF/GP | NPPA | Cavia porcellus | 100.00 | Radioactive Assay | |||||
| ANGIOCONVENZ | ACE | Oryctolagus cuniculus | 98.0 | inhibitor | Photometry | ||||
| AT1 | AGTR1 | Homo sapiens | 104.0 | 72.00 | Others | ||||
| ATP NA+/K+PI | ATP1A1 | Sus scrofa | 105.0 | inhibitor | Spectrofluorimetry | ||||
| B1/H | BDKRB1 | Homo sapiens | 93.0 | 108.00 | Radioactive Assay | ||||
| BETA/R | ADRB2 | Rattus norvegicus | 86.0 | 94.00 | Radioactive Assay | ||||
| CA+/DHPSI/RA | CACNA1C | Rattus norvegicus | 91.0 | 77.00 | 94.00 | 104.00 | 41.50 | Radioactive Assay | |
| CA+/DILSI/RA | CACNA1C | Rattus norvegicus | 101.0 | 87.00 | 111.00 | 99.00 | 45.00 | Radioactive Assay | |
| CA+/N/RA | CACNA1B | Rattus norvegicus | 86.0 | Radioactive Assay | |||||
| CA+/PAASITE | CACNA1C | Rattus norvegicus | 99.0 | 70.00 | Radioactive Assay | ||||
| CANHYDRASE | CA6 | Homo sapiens | 86.0 | inhibitor | absorption of electromagnetic radiation | ||||
| CB2/H | CNR2 | Homo sapiens | 91.0 | Radioactive Assay | |||||
| CGRP/HU | CALCA | Homo sapiens | 99.0 | 96.00 | Radioactive Assay | ||||
| CHYMASE | CMA1 | Homo sapiens | 93.0 | inhibitor | Spectrofluorimetry | ||||
| CNOS | NOS3 | Rattus norvegicus | 102.0 | inhibitor | Radioactive Assay | ||||
| COX-1 | PTGS1 | Homo sapiens | 105.0 | inhibitor | Enzyme Immunoassay | ||||
| COX-2 | PTGS2 | Homo sapiens | 82.0 | inhibitor | Enzyme Immunoassay | ||||
| D1/HU | DRD1 | Homo sapiens | 101.0 | Radioactive Assay | |||||
| D2L/H | DRD2 | Homo sapiens | 100.0 | Radioactive Assay | |||||
| D3/HU | DRD3 | Homo sapiens | 105.0 | Radioactive Assay | |||||
| D4.2/H | DRD4 | Homo sapiens | 95.0 | Radioactive Assay | |||||
| DATRANS/H | SLC6A3 | Homo sapiens | 105.0 | inhibitor | Radioactive Assay | ||||
| ECE-1 (HU) | ECE1 | Homo sapiens | 82.0 | inhibitor | FI - fluorescence intensity | ||||
| ELASTASEPMN | ELANE | Homo sapiens | 98.0 | absorption of electromagnetic radiation | |||||
| ENOS_MDS | NOS3 | Bos taurus | 100.0 | Radioactive Assay | |||||
| ETA/HU | EDNRA | Homo sapiens | 101.00 | Radioactive Assay | |||||
| GABAB/RA | GABRB1 | Rattus norvegicus | 113.0 | inhibitor | Radioactive Assay | ||||
| H1/H | HRH1 | Homo sapiens | 95.0 | Radioactive Assay | |||||
| H2/H | HRH2 | Homo sapiens | 94.0 | Radioactive Assay | |||||
| HMGCOARED | HMGCR | Rattus norvegicus | 85.0 | inhibitor | Radioactive Assay | ||||
| INOS | NOS2 | Mus musculus | 108.0 | absorption of electromagnetic radiation | |||||
| K+/KA/R | KCNA1 | Rattus norvegicus | 97.0 | Radioactive Assay | |||||
| K+/KATP/HA | KCNJ1 | Cricetinae | 110.0 | Radioactive Assay | |||||
| LTA4HYD | LTA4H | Cavia porcellus | 93.0 | inhibitor | Radioactive Assay | ||||
| LTC4SYN | LTC4S | Cavia porcellus | 93.0 | inhibitor | Radioactive Assay | ||||
| MAOA | MAOA | Homo sapiens | 68.0 | inhibitor | FI - fluorescence intensity | ||||
| MMP-13 | MMP13 | Homo sapiens | 90.0 | FI - fluorescence intensity | |||||
| MU-CALPAIN | CAPN1 | Homo sapiens | 97.0 | inhibitor | FI - fluorescence intensity | ||||
| MUSCARIN/NS | Rattus norvegicus | 99.0 | Radioactive Assay | ||||||
| NACH/H | CHRNA1 | Homo sapiens | 101.0 | Radioligand Binding | |||||
| NETRANS/H | SLC6A2 | Homo sapiens | 112.0 | Radioactive Assay | |||||
| PDE-III/HU | PDE3A | Homo sapiens | 31.0 | inhibitor | Radioactive Assay | ||||
| PDE-IV/HU | PDE4A | Homo sapiens | 68.0 | inhibitor | Radioactive Assay | ||||
| PEPCATHEPSG | CTSG | Homo sapiens | 106.0 | inhibitor | FI - fluorescence intensity | ||||
| PEP_MMP-1 | MMP1 | Homo sapiens | 94.0 | inhibitor | absorption of electromagnetic radiation | ||||
| PLA2 | PLA2G2A | Sus scrofa | 96.0 | inhibitor | Radioactive Assay | ||||
| RENIN (HU) | REN | Homo sapiens | 100.0 | inhibitor | FI - fluorescence intensity | ||||
| THRO SYN(HU) | TBXAS1 | Homo sapiens | 86.0 | Enzyme Immunoassay | |||||
| UROTENSIN_II | UTS2 | Homo sapiens | 107.0 | inhibitor | Radioactive Assay | ||||
| VASOPRE_V1A | AVPR1A | Homo sapiens | 99.0 | 89.00 | Radioactive Assay |
BI 605906
Conclusion: Closest off-targets at 1 µM are AAK1 with 13 % Ctrl, GAK with 7 % Ctrl and IRAK3 with 24 % Ctrl
| Target protein | HGNC name | Species | % control at 1 µM | % control at 10 µM | % control at 20 µM | % control at 0.001 µM | Mode of action | Assay |
|---|---|---|---|---|---|---|---|---|
| AAK1 | AAK1 | Homo sapiens | 13.0 | 4.00 | 101.00 | inhibitor | LanthaScreen | |
| ACVR2A | ACVR2A | Homo sapiens | 108.0 | inhibitor | LanthaScreen | |||
| ACVRL1 (ALK1) | ACVRL1 | Homo sapiens | 64.0 | inhibitor | LanthaScreen | |||
| ADCK3 | COQ8A | Homo sapiens | 67.0 | inhibitor | LanthaScreen | |||
| AMPK (A1/B1/G2) |
PRKAA1 PRKAB1 PRKAG2 |
Homo sapiens | 89.0 | inhibitor | LanthaScreen | |||
| AMPK (A1/B1/G3) |
PRKAA1 PRKAB1 PRKAG3 |
Homo sapiens | 84.0 | inhibitor | LanthaScreen | |||
| AMPK (A1/B2/G1) |
PRKAA1 PRKAB2 PRKAG1 |
Homo sapiens | 91.0 | inhibitor | LanthaScreen | |||
| AMPK (A1/B2/G3) |
PRKAA1 PRKAB2 PRKAG3 |
Homo sapiens | 91.0 | inhibitor | Z´-LYTE | |||
| AMPK (A2/B1/G2) |
PRKAA2 PRKAB1 PRKAG2 |
Homo sapiens | 88.0 | inhibitor | Z´-LYTE | |||
| AMPK (A2/B1/G3) |
PRKAA2 PRKAB1 PRKAG3 |
Homo sapiens | 89.0 | inhibitor | Z´-LYTE | |||
| AMPK (A2/B2/G1) |
PRKAA2 PRKAB2 PRKAG1 |
Homo sapiens | 88.0 | inhibitor | LanthaScreen | |||
| AMPK (A2/B2/G2) |
PRKAA2 PRKAB2 PRKAG2 |
Homo sapiens | 88.0 | inhibitor | LanthaScreen | |||
| AMPK (A2/B2/G3) |
PRKAA2 PRKAB2 PRKAG3 |
Homo sapiens | 99.0 | inhibitor | Z´-LYTE | |||
| ANKK1 | ANKK1 | Homo sapiens | 95.0 | inhibitor | LanthaScreen | |||
| BMPR1B (ALK6) | BMPR1B | Homo sapiens | 74.0 | inhibitor | LanthaScreen | |||
| BMPR2 | BMPR2 | Homo sapiens | 65.0 | inhibitor | LanthaScreen | |||
| BRSK2 | BRSK2 | Homo sapiens | 102.0 | inhibitor | LanthaScreen | |||
| CAMK1G | CAMK1G | Homo sapiens | 90.0 | inhibitor | Z´-LYTE | |||
| CAMK2G (CAMKII GA | CAMK2G | Homo sapiens | 90.0 | inhibitor | LanthaScreen | |||
| CASK | CASK | Homo sapiens | 52.0 | inhibitor | LanthaScreen | |||
| CDC42 BPG (MRCKG) | CDC42BPG | Homo sapiens | 111.0 | inhibitor | Z´-LYTE | |||
| CDC7/DBF4 |
CDC7 DBF4 |
Homo sapiens | 88.0 | inhibitor | LanthaScreen | |||
| CDK11 (INACTIVE) | CDK19 | Homo sapiens | 87.0 | inhibitor | LanthaScreen | |||
| CDK11/CYCLIN C |
CDK19 CCNC |
Homo sapiens | 83.0 | inhibitor | LanthaScreen | |||
| CDK13/CYCLIN K |
CDK13 CCNK |
Homo sapiens | 85.0 | inhibitor | LanthaScreen | |||
| CDK14 (PFTK1)/CYC |
CDK14 CYCS |
Homo sapiens | 70.0 | inhibitor | LanthaScreen | |||
| CDK16 (PCTK1)/CYC |
CDK16 CYCS |
Homo sapiens | 87.0 | inhibitor | LanthaScreen | |||
| CDK17/CYCLIN Y |
CDK17 CCNY |
Homo sapiens | 88.0 | inhibitor | Z´-LYTE | |||
| CDK18/CYCLIN Y |
CDK18 CCNY |
Homo sapiens | 96.0 | inhibitor | Z´-LYTE | |||
| CDK2/CYCLIN A1 |
CDK2 CCNA1 |
Homo sapiens | 80.0 | inhibitor | LanthaScreen | |||
| CDK2/CYCLIN E1 |
CDK2 CCNE1 |
Homo sapiens | 94.0 | inhibitor | LanthaScreen | |||
| CDK2/CYCLIN O |
CDK2 CCNO |
Homo sapiens | 81.0 | inhibitor | LanthaScreen | |||
| CDK3/CYCLIN E1 |
CDK3 CCNE1 |
Homo sapiens | 78.0 | inhibitor | LanthaScreen | |||
| CDK4/CYCLIN D1 |
CDK4 CCND1 |
Homo sapiens | 99.0 | inhibitor | Adapta | |||
| CDK4/CYCLIN D3 |
CDK4 CCND3 |
Homo sapiens | 97.0 | inhibitor | Adapta | |||
| CDK5 (INACTIVE) | CDK5 | Homo sapiens | 83.0 | inhibitor | LanthaScreen | |||
| CDK6/CYCLIN D1 |
CDK6 CCND1 |
Homo sapiens | 100.0 | inhibitor | Adapta | |||
| CDK9 (INACTIVE) | CDK9 | Homo sapiens | 91.0 | inhibitor | LanthaScreen | |||
| CDKL5 | CDKL5 | Homo sapiens | 103.0 | inhibitor | Z´-LYTE | |||
| CSNK1A1L | CSNK1A1L | Homo sapiens | 84.0 | inhibitor | Z´-LYTE | |||
| DAPK2 | DAPK2 | Homo sapiens | 79.0 | inhibitor | LanthaScreen | |||
| DCAMKL1 (DCLK1) | DCLK1 | Homo sapiens | 99.0 | inhibitor | Z´-LYTE | |||
| DYRK2 | DYRK2 | Homo sapiens | 62.0 | inhibitor | LanthaScreen | |||
| EIF2AK2 | EIF2AK2 | Homo sapiens | 96.0 | inhibitor | LanthaScreen | |||
| EPHA6 | EPHA6 | Homo sapiens | 91.0 | inhibitor | LanthaScreen | |||
| ERN1 | ERN1 | Homo sapiens | 82.0 | inhibitor | LanthaScreen | |||
| ERN2 | ERN2 | Homo sapiens | 102.0 | inhibitor | LanthaScreen | |||
| FLT3 ITD | FLT3 | Homo sapiens | 101.0 | inhibitor | LanthaScreen | |||
| FYN A | FYN | Homo sapiens | 97.0 | inhibitor | LanthaScreen | |||
| GAK | GAK | Homo sapiens | 7.0 | 6.00 | 99.00 | inhibitor | LanthaScreen | |
| GRK1 | GRK1 | Homo sapiens | 87.0 | inhibitor | LanthaScreen | |||
| HUNK | HUNK | Homo sapiens | 97.0 | inhibitor | LanthaScreen | |||
| ICK | CILK1 | Homo sapiens | 96.0 | inhibitor | LanthaScreen | |||
| IRAK3 | IRAK3 | Homo sapiens | 24.0 | 14.00 | 93.00 | inhibitor | LanthaScreen | |
| KSR2 | KSR2 | Homo sapiens | 92.0 | inhibitor | Z´-LYTE | |||
| LATS2 | LATS2 | Homo sapiens | 88.0 | inhibitor | LanthaScreen | |||
| MAP2K4 | MAP2K4 | Homo sapiens | 79.0 | inhibitor | LanthaScreen | |||
| MAP2K5 | MAP2K5 | Homo sapiens | 107.0 | inhibitor | LanthaScreen | |||
| MAP3K19 (YSK4) | MAP3K19 | Homo sapiens | 98.0 | inhibitor | Z´-LYTE | |||
| MAP4K1 (HPK1) | MAP4K1 | Homo sapiens | 82.0 | inhibitor | LanthaScreen | |||
| MAP4K3 (GLK) | MAP4K3 | Homo sapiens | 93.0 | inhibitor | LanthaScreen | |||
| MAPK15 (ERK7) | MAPK15 | Homo sapiens | 103.0 | inhibitor | LanthaScreen | |||
| MAPK7 (ERK5) | MAPK7 | Homo sapiens | 98.0 | inhibitor | Z´-LYTE | |||
| MARK3 | MARK3 | Homo sapiens | 90.0 | inhibitor | Z´-LYTE | |||
| MASTL | MASTL | Homo sapiens | 85.0 | inhibitor | LanthaScreen | |||
| MLK4 | MAP3K21 | Homo sapiens | 97.0 | inhibitor | LanthaScreen | |||
| MYLK4 | MYLK4 | Homo sapiens | 83.0 | inhibitor | LanthaScreen | |||
| MYO3A | MYO3A | Homo sapiens | 92.0 | inhibitor | LanthaScreen | |||
| MYO3B (MYO3 BETA) | MYO3B | Homo sapiens | 90.0 | inhibitor | LanthaScreen | |||
| NEK8 | NEK8 | Homo sapiens | 95.0 | inhibitor | LanthaScreen | |||
| NIM1K | NIM1K | Homo sapiens | 93.0 | inhibitor | Z´-LYTE | |||
| NUAK2 | NUAK2 | Homo sapiens | 86.0 | inhibitor | LanthaScreen | |||
| PEAK1 | PEAK1 | Homo sapiens | 94.0 | inhibitor | Z´-LYTE | |||
| PI4K2A | PI4K2A | Homo sapiens | 92.0 | inhibitor | Adapta | |||
| PI4K2B | PIP4K2B | Homo sapiens | 102.0 | inhibitor | Adapta | |||
| PIK3C2G | PIK3C2G | Homo sapiens | 90.0 | inhibitor | Adapta | |||
| PIK3CA/PIK3R3 | PIK3CA | Homo sapiens | 103.0 | inhibitor | Adapta | |||
| PIK3CAE545K/PIK3R1 |
PIK3CA PIK3R1 |
Homo sapiens | 100.0 | inhibitor | Adapta | |||
| PIK3CB/PIK3R2 | PIK3CB | Homo sapiens | 112.0 | inhibitor | Adapta | |||
| PIM3 | PIM3 | Homo sapiens | 103.0 | inhibitor | Z´-LYTE | |||
| PIP4K2A | PIP4K2A | Homo sapiens | 115.0 | inhibitor | Adapta | |||
| PIP5K1A | PIP5K1A | Homo sapiens | 83.0 | inhibitor | Adapta | |||
| PIP5K1B | PIP5K1B | Homo sapiens | 108.0 | inhibitor | Adapta | |||
| PIP5K1C | PIP5K1C | Homo sapiens | 96.0 | inhibitor | Adapta | |||
| PKMYT1 | PKMYT1 | Homo sapiens | 90.0 | inhibitor | LanthaScreen | |||
| PKN2 | PKN2 | Homo sapiens | 86.0 | inhibitor | LanthaScreen | |||
| PLK4 | PLK4 | Homo sapiens | 89.0 | inhibitor | LanthaScreen | |||
| PRKACB (PRKAC BET | PRKACB | Homo sapiens | 77.0 | inhibitor | LanthaScreen | |||
| PRKACG (PRKAC GAM | PRKACG | Homo sapiens | 103.0 | inhibitor | LanthaScreen | |||
| RIPK3 | RIPK3 | Homo sapiens | 100.0 | inhibitor | LanthaScreen | |||
| RPS6KB2 (P70S6KB) | RPS6KB2 | Homo sapiens | 86.0 | inhibitor | Z´-LYTE | |||
| SBK1 | SBK1 | Homo sapiens | 98.0 | inhibitor | Z´-LYTE | |||
| SIK1 | SIK1 | Homo sapiens | 92.0 | inhibitor | LanthaScreen | |||
| SIK3 | SIK3 | Homo sapiens | 79.0 | inhibitor | LanthaScreen | |||
| STK17B (DRAK2) | STK17B | Homo sapiens | 97.0 | inhibitor | LanthaScreen | |||
| STK32B (YANK2) | STK32B | Homo sapiens | 96.0 | inhibitor | LanthaScreen | |||
| STK32C (YANK3) | STK32C | Homo sapiens | 99.0 | inhibitor | LanthaScreen | |||
| STK38 (NDR) | STK38 | Homo sapiens | 83.0 | inhibitor | LanthaScreen | |||
| STK38L (NDR2) | STK38L | Homo sapiens | 125.0 | inhibitor | LanthaScreen | |||
| STK39 (STLK3) | STK39 | Homo sapiens | 88.0 | inhibitor | LanthaScreen | |||
| TAOK1 | TAOK1 | Homo sapiens | 88.0 | inhibitor | LanthaScreen | |||
| TESK1 | TESK1 | Homo sapiens | 92.0 | inhibitor | LanthaScreen | |||
| TESK2 | TESK2 | Homo sapiens | 90.0 | inhibitor | LanthaScreen | |||
| TGFBR2 | TGFBR2 | Homo sapiens | 87.0 | inhibitor | LanthaScreen | |||
| TLK1 | TLK1 | Homo sapiens | 91.0 | inhibitor | LanthaScreen | |||
| TLK2 | TLK2 | Homo sapiens | 98.0 | inhibitor | LanthaScreen | |||
| TNIK | TNIK | Homo sapiens | 99.0 | inhibitor | LanthaScreen | |||
| TNK1 | TNK1 | Homo sapiens | 92.0 | inhibitor | Z´-LYTE | |||
| ULK1 | ULK1 | Homo sapiens | 94.0 | inhibitor | LanthaScreen | |||
| ULK2 | ULK2 | Homo sapiens | 93.0 | inhibitor | LanthaScreen | |||
| ULK3 | ULK3 | Homo sapiens | 95.0 | inhibitor | LanthaScreen | |||
| VRK2 | VRK2 | Homo sapiens | 82.0 | inhibitor | LanthaScreen | |||
| WNK1 | WNK1 | Homo sapiens | 99.0 | inhibitor | LanthaScreen | |||
| WNK3 | WNK3 | Homo sapiens | 102.0 | inhibitor | LanthaScreen | |||
| ABL1 | ABL1 | Homo sapiens | 95.0 | 77.00 | inhibitor | fluorescence resonance energy transfer | ||
| ABL2 | ABL2 | Homo sapiens | 91.0 | inhibitor | Z´-LYTE | |||
| ACVR1 | ACVR1 | Homo sapiens | 79.0 | inhibitor | LanthaScreen | |||
| ACVR1B | ACVR1B | Homo sapiens | 96.0 | 105.00 | inhibitor | Z´-LYTE | ||
| ACVR2B | ACVR2B | Homo sapiens | 91.0 | inhibitor | LanthaScreen | |||
| ADRBK1 | GRK2 | Homo sapiens | 95.0 | inhibitor | Z´-LYTE | |||
| ADRBK2 | GRK3 | Homo sapiens | 96.0 | inhibitor | Z´-LYTE | |||
| AKT1 | AKT1 | Homo sapiens | 99.0 | 96.00 | inhibitor | Z´-LYTE | ||
| AKT2 | AKT2 | Homo sapiens | 95.0 | inhibitor | Z´-LYTE | |||
| AKT3 | AKT3 | Homo sapiens | 91.0 | inhibitor | Z´-LYTE | |||
| ALK | ALK | Homo sapiens | 80.0 | 74.00 | inhibitor | fluorescence resonance energy transfer | ||
| AMPK A1B1G1 |
PRKAA1 PRKAB1 PRKAG1 |
Homo sapiens | 95.0 | 80.00 | inhibitor | fluorescence resonance energy transfer | ||
| AMPK A2B1G1 |
PRKAA2 PRKAB1 PRKAG1 |
Homo sapiens | 88.0 | inhibitor | Z´-LYTE | |||
| AURKB | AURKB | Homo sapiens | 98.0 | inhibitor | fluorescence resonance energy transfer | |||
| AURKC | AURKC | Homo sapiens | 95.0 | inhibitor | Z´-LYTE | |||
| AXL | AXL | Homo sapiens | 98.0 | 85.00 | inhibitor | Z´-LYTE | ||
| BLK | BLK | Homo sapiens | 88.0 | inhibitor | Z´-LYTE | |||
| BMPR1A(ALK3) | BMPR1A | Homo sapiens | 100.0 | inhibitor | LanthaScreen | |||
| BMX | BMX | Homo sapiens | 88.0 | inhibitor | Z´-LYTE | |||
| BRAF | BRAF | Homo sapiens | 72.0 | inhibitor | Z´-LYTE | |||
| BRAF V599E | BRAF | Homo sapiens | 34.00 | inhibitor | Z´-LYTE | |||
| BRSK1 | BRSK1 | Homo sapiens | 92.0 | inhibitor | Z´-LYTE | |||
| BTK | BTK | Homo sapiens | 85.0 | 96.00 | inhibitor | Z´-LYTE | ||
| CAMK1D | CAMK1D | Homo sapiens | 98.0 | inhibitor | Z´-LYTE | |||
| CAMK1_A | CAMK1 | Homo sapiens | 109.0 | inhibitor | Adapta | |||
| CAMK2A | CAMK2A | Homo sapiens | 100.0 | inhibitor | Z´-LYTE | |||
| CAMK2B | CAMK2B | Homo sapiens | 99.0 | inhibitor | Z´-LYTE | |||
| CAMK2D | CAMK2D | Homo sapiens | 96.0 | inhibitor | fluorescence resonance energy transfer | |||
| CAMK4 | CAMK4 | Homo sapiens | 103.0 | inhibitor | Z´-LYTE | |||
| CAMKK1 | CAMKK1 | Homo sapiens | 93.0 | inhibitor | LanthaScreen | |||
| CAMKK2 | CAMKK2 | Homo sapiens | 93.0 | inhibitor | LanthaScreen | |||
| CDC42 BPA | CDC42BPA | Homo sapiens | 95.0 | inhibitor | Z´-LYTE | |||
| CDC42 BPB | CDC42BPB | Homo sapiens | 103.0 | inhibitor | Z´-LYTE | |||
| CDK1/CYCLINB | CDK1 | Homo sapiens | 92.0 | 94.00 | inhibitor | fluorescence resonance energy transfer | ||
| CDK2/CYCLINA | CDK2 | Homo sapiens | 90.0 | inhibitor | Z´-LYTE | |||
| CDK5/P25 | CDK5 | Homo sapiens | 99.0 | inhibitor | Z´-LYTE | |||
| CDK5/P35 | CDK5 | Homo sapiens | 97.0 | inhibitor | Z´-LYTE | |||
| CDK7CYCLIN | CDK7 | Homo sapiens | 99.0 | inhibitor | Adapta | |||
| CDK8_CYCLINC | CDK8 | Homo sapiens | 82.0 | inhibitor | LanthaScreen | |||
| CDK9CYCLIN | CDK9 | Homo sapiens | 86.0 | inhibitor | Adapta | |||
| CDK9_CYCLINK | CDK9 | Homo sapiens | 88.0 | inhibitor | LanthaScreen | |||
| CHEK1 | CHEK1 | Homo sapiens | 95.0 | 89.00 | inhibitor | Z´-LYTE | ||
| CHEK2 | CHEK2 | Homo sapiens | 79.0 | inhibitor | Z´-LYTE | |||
| CHUK_IKKA | CHUK | Homo sapiens | 67.0 | 27.00 | inhibitor | Adapta | ||
| CLK1 | CLK1 | Homo sapiens | 92.0 | inhibitor | Z´-LYTE | |||
| CLK2 | CLK2 | Homo sapiens | 91.0 | inhibitor | Z´-LYTE | |||
| CLK3 | CLK3 | Homo sapiens | 102.0 | inhibitor | Z´-LYTE | |||
| CLK4 | CLK4 | Homo sapiens | 69.0 | inhibitor | LanthaScreen | |||
| CSF1R | CSF1R | Homo sapiens | 58.0 | 14.00 | inhibitor | Z´-LYTE | ||
| CSK | CSK | Homo sapiens | 96.0 | 84.00 | inhibitor | Z´-LYTE | ||
| CSNK1A1 | CSNK1A1 | Homo sapiens | 98.0 | inhibitor | Z´-LYTE | |||
| CSNK1D | CSNK1D | Homo sapiens | 100.0 | inhibitor | Z´-LYTE | |||
| CSNK1E | CSNK1E | Homo sapiens | 75.0 | inhibitor | Z´-LYTE | |||
| CSNK1G1 | CSNK1G1 | Homo sapiens | 102.0 | inhibitor | Z´-LYTE | |||
| CSNK1G2 | CSNK1G2 | Homo sapiens | 96.0 | 94.00 | inhibitor | Z´-LYTE | ||
| CSNK1G3 | CSNK1G3 | Homo sapiens | 99.0 | inhibitor | Z´-LYTE | |||
| CSNK2A1 | CSNK2A1 | Homo sapiens | 92.0 | 107.00 | inhibitor | Z´-LYTE | ||
| CSNK2A2 | CSNK2A2 | Homo sapiens | 87.0 | inhibitor | Z´-LYTE | |||
| DAPK1 | DAPK1 | Homo sapiens | 100.0 | inhibitor | Adapta | |||
| DAPK3 | DAPK3 | Homo sapiens | 101.0 | inhibitor | Z´-LYTE | |||
| DCAMKL2 | DCLK2 | Homo sapiens | 101.0 | inhibitor | Z´-LYTE | |||
| DDR1 | DDR1 | Homo sapiens | 84.0 | inhibitor | LanthaScreen | |||
| DDR2 | DDR2 | Homo sapiens | 99.0 | inhibitor | LanthaScreen | |||
| DMPK | DMPK | Homo sapiens | 95.0 | inhibitor | LanthaScreen | |||
| DNA-PK | PRKDC | Homo sapiens | 90.0 | inhibitor | Z´-LYTE | |||
| DYRK1A | DYRK1A | Homo sapiens | 91.0 | inhibitor | Z´-LYTE | |||
| DYRK1B | DYRK1B | Homo sapiens | 95.0 | 91.00 | inhibitor | Z´-LYTE | ||
| DYRK3 | DYRK3 | Homo sapiens | 92.0 | inhibitor | Z´-LYTE | |||
| DYRK4 | DYRK4 | Homo sapiens | 97.0 | inhibitor | Z´-LYTE | |||
| EEF2K | EEF2K | Homo sapiens | 98.0 | inhibitor | Z´-LYTE | |||
| EGFR | EGFR | Homo sapiens | 99.0 | 90.00 | inhibitor | Z´-LYTE | ||
| EPHA1 | EPHA1 | Homo sapiens | 82.0 | inhibitor | Z´-LYTE | |||
| EPHA2 | EPHA2 | Homo sapiens | 93.0 | 63.00 | inhibitor | Z´-LYTE | ||
| EPHA3 | EPHA3 | Homo sapiens | 85.0 | inhibitor | LanthaScreen | |||
| EPHA4 | EPHA4 | Homo sapiens | 93.0 | inhibitor | Z´-LYTE | |||
| EPHA5 | EPHA5 | Homo sapiens | 94.0 | inhibitor | Z´-LYTE | |||
| EPHA7 | EPHA7 | Homo sapiens | 87.0 | inhibitor | LanthaScreen | |||
| EPHA8 | EPHA8 | Homo sapiens | 85.0 | inhibitor | Z´-LYTE | |||
| EPHB1 | EPHB1 | Homo sapiens | 85.0 | inhibitor | Z´-LYTE | |||
| EPHB2 | EPHB2 | Homo sapiens | 89.0 | inhibitor | Z´-LYTE | |||
| EPHB3 | EPHB3 | Homo sapiens | 99.0 | inhibitor | Z´-LYTE | |||
| EPHB4 | EPHB4 | Homo sapiens | 90.0 | inhibitor | Z´-LYTE | |||
| ERBB2 | ERBB2 | Homo sapiens | 96.0 | 86.00 | inhibitor | Z´-LYTE | ||
| ERBB4 | ERBB4 | Homo sapiens | 94.0 | inhibitor | Z´-LYTE | |||
| FER | FER | Homo sapiens | 95.0 | inhibitor | fluorescence resonance energy transfer | |||
| FES | FES | Homo sapiens | 91.0 | inhibitor | fluorescence resonance energy transfer | |||
| FGFR1 | FGFR1 | Homo sapiens | 84.0 | 91.00 | inhibitor | fluorescence resonance energy transfer | ||
| FGFR2 | FGFR2 | Homo sapiens | 94.0 | inhibitor | Z´-LYTE | |||
| FGFR3 | FGFR3 | Homo sapiens | 96.0 | inhibitor | Z´-LYTE | |||
| FGFR4 | FGFR4 | Homo sapiens | 96.0 | inhibitor | Z´-LYTE | |||
| FGR | FGR | Homo sapiens | 78.0 | inhibitor | Z´-LYTE | |||
| FLT1 | FLT1 | Homo sapiens | 100.0 | inhibitor | Z´-LYTE | |||
| FLT3 | FLT3 | Homo sapiens | 71.0 | 38.00 | inhibitor | fluorescence resonance energy transfer | ||
| FLT4 | FLT4 | Homo sapiens | 97.0 | inhibitor | Z´-LYTE | |||
| FRAP1 (MTOR) | MTOR | Homo sapiens | 99.0 | 98.00 | inhibitor | fluorescence resonance energy transfer | ||
| FRK | FRK | Homo sapiens | 92.0 | inhibitor | Z´-LYTE | |||
| FYN | FYN | Homo sapiens | 89.0 | inhibitor | Z´-LYTE | |||
| GRK4 | GRK4 | Homo sapiens | 100.0 | inhibitor | Z´-LYTE | |||
| GRK5 | GRK5 | Homo sapiens | 96.0 | inhibitor | Z´-LYTE | |||
| GRK6 | GRK6 | Homo sapiens | 93.0 | inhibitor | Z´-LYTE | |||
| GRK7 | GRK7 | Homo sapiens | 101.0 | inhibitor | Z´-LYTE | |||
| GSG2 | HASPIN | Homo sapiens | 70.0 | inhibitor | Adapta | |||
| GSK3A | GSK3A | Homo sapiens | 99.0 | inhibitor | Z´-LYTE | |||
| GSK3B | GSK3B | Homo sapiens | 93.0 | 87.00 | inhibitor | fluorescence resonance energy transfer | ||
| HCK | HCK | Homo sapiens | 90.0 | inhibitor | Z´-LYTE | |||
| HIPK1 | HIPK1 | Homo sapiens | 101.0 | inhibitor | Z´-LYTE | |||
| HIPK2 | HIPK2 | Homo sapiens | 81.0 | inhibitor | Z´-LYTE | |||
| HIPK3 | HIPK3 | Homo sapiens | 95.0 | inhibitor | Z´-LYTE | |||
| HIPK4 | HIPK4 | Homo sapiens | 77.0 | inhibitor | Z´-LYTE | |||
| IGF1R | IGF1R | Homo sapiens | 95.0 | 99.00 | inhibitor | Z´-LYTE | ||
| IKBKB | IKBKB | Homo sapiens | 13.5 | -1.50 | inhibitor | Z´-LYTE | ||
| IKBKE | IKBKE | Homo sapiens | 98.0 | 98.00 | inhibitor | Z´-LYTE | ||
| INSR | INSR | Homo sapiens | 94.0 | 93.00 | inhibitor | Z´-LYTE | ||
| INSRR | INSRR | Homo sapiens | 92.0 | inhibitor | Z´-LYTE | |||
| IRAK1 | IRAK1 | Homo sapiens | 89.0 | inhibitor | Adapta | |||
| IRAK4 | IRAK4 | Homo sapiens | 100.0 | 90.00 | inhibitor | Z´-LYTE | ||
| ITK | ITK | Homo sapiens | 107.0 | inhibitor | Z´-LYTE | |||
| JAK1 | JAK1 | Homo sapiens | 98.0 | inhibitor | Z´-LYTE | |||
| JAK2 | JAK2 | Homo sapiens | 94.0 | inhibitor | Z´-LYTE | |||
| JAK2 JH1 JH2 | JAK2 | Homo sapiens | 94.0 | inhibitor | Z´-LYTE | |||
| JAK3 | JAK3 | Homo sapiens | 92.0 | 95.00 | inhibitor | Z´-LYTE | ||
| KDR | KDR | Homo sapiens | 98.0 | 79.00 | inhibitor | fluorescence resonance energy transfer | ||
| KIT | KIT | Homo sapiens | 89.0 | 83.00 | inhibitor | Z´-LYTE | ||
| LCK | LCK | Homo sapiens | 68.0 | 67.00 | inhibitor | fluorescence resonance energy transfer | ||
| LIMK1 | LIMK1 | Homo sapiens | 97.0 | inhibitor | LanthaScreen | |||
| LIMK2 | LIMK2 | Homo sapiens | 95.0 | inhibitor | LanthaScreen | |||
| LRRK2 | LRRK2 | Homo sapiens | 62.0 | inhibitor | Adapta | |||
| LRRK2_FL | LRRK2 | Homo sapiens | 62.0 | inhibitor | Adapta | |||
| LTK | LTK | Homo sapiens | 99.0 | inhibitor | fluorescence resonance energy transfer | |||
| LYN A | LYN | Homo sapiens | 82.0 | inhibitor | fluorescence resonance energy transfer | |||
| LYN B | LYN | Homo sapiens | 78.0 | inhibitor | Z´-LYTE | |||
| MAP2K1 | MAP2K1 | Homo sapiens | 76.0 | 80.00 | inhibitor | Z´-LYTE | ||
| MAP2K2 | MAP2K2 | Homo sapiens | 91.0 | inhibitor | Z´-LYTE | |||
| MAP2K6 | MAP2K6 | Homo sapiens | 75.0 | inhibitor | Z´-LYTE | |||
| MAP3K10 | MAP3K10 | Homo sapiens | 98.0 | inhibitor | LanthaScreen | |||
| MAP3K11 | MAP3K11 | Homo sapiens | 95.0 | inhibitor | LanthaScreen | |||
| MAP3K14 | MAP3K14 | Homo sapiens | 100.0 | inhibitor | LanthaScreen | |||
| MAP3K2 | MAP3K2 | Homo sapiens | 92.0 | inhibitor | LanthaScreen | |||
| MAP3K3 | MAP3K3 | Homo sapiens | 98.0 | inhibitor | LanthaScreen | |||
| MAP3K5 | MAP3K5 | Homo sapiens | 99.0 | inhibitor | LanthaScreen | |||
| MAP3K7_K7IP1 | MAP3K7 | Homo sapiens | 101.0 | inhibitor | LanthaScreen | |||
| MAP3K8 | MAP3K8 | Homo sapiens | 90.0 | inhibitor | Z´-LYTE | |||
| MAP3K9 | MAP3K9 | Homo sapiens | 108.0 | inhibitor | Z´-LYTE | |||
| MAP4K2 | MAP4K2 | Homo sapiens | 99.0 | inhibitor | Z´-LYTE | |||
| MAP4K4 | MAP4K4 | Homo sapiens | 95.0 | 89.00 | inhibitor | Z´-LYTE | ||
| MAP4K5 | MAP4K5 | Homo sapiens | 101.0 | inhibitor | Z´-LYTE | |||
| MAPK1 | MAPK1 | Homo sapiens | 92.0 | 101.00 | inhibitor | Z´-LYTE | ||
| MAPK10 | MAPK10 | Homo sapiens | 101.0 | inhibitor | Z´-LYTE | |||
| MAPK11 | MAPK11 | Homo sapiens | 98.0 | inhibitor | Z´-LYTE | |||
| MAPK12 | MAPK12 | Homo sapiens | 99.0 | inhibitor | Z´-LYTE | |||
| MAPK13 | MAPK13 | Homo sapiens | 94.0 | inhibitor | Z´-LYTE | |||
| MAPK14 | MAPK14 | Homo sapiens | 92.0 | 60.00 | inhibitor | Z´-LYTE | ||
| MAPK14P38A | MAPK14 | Homo sapiens | 89.0 | inhibitor | Z´-LYTE | |||
| MAPK3 | MAPK3 | Homo sapiens | 100.0 | inhibitor | Z´-LYTE | |||
| MAPK8 | MAPK8 | Homo sapiens | 91.0 | 100.00 | inhibitor | Z´-LYTE | ||
| MAPK9 | MAPK9 | Homo sapiens | 98.0 | inhibitor | Z´-LYTE | |||
| MAPKAPK2 | MAPKAPK2 | Homo sapiens | 93.0 | 87.00 | inhibitor | Z´-LYTE | ||
| MAPKAPK3 | MAPKAPK3 | Homo sapiens | 93.0 | inhibitor | Z´-LYTE | |||
| MAPKAPK5 | MAPKAPK5 | Homo sapiens | 92.0 | inhibitor | Z´-LYTE | |||
| MARK1 | MARK1 | Homo sapiens | 91.0 | inhibitor | Z´-LYTE | |||
| MARK2 | MARK2 | Homo sapiens | 90.0 | 87.00 | inhibitor | Z´-LYTE | ||
| MARK4 | MARK4 | Homo sapiens | 100.0 | inhibitor | Z´-LYTE | |||
| MATK | MATK | Homo sapiens | 101.0 | inhibitor | Z´-LYTE | |||
| MELK | MELK | Homo sapiens | 103.0 | inhibitor | fluorescence resonance energy transfer | |||
| MERTK | MERTK | Homo sapiens | 93.0 | inhibitor | Z´-LYTE | |||
| MET | MET | Homo sapiens | 103.0 | 90.00 | inhibitor | fluorescence resonance energy transfer | ||
| MINK1 | MINK1 | Homo sapiens | 96.0 | inhibitor | Z´-LYTE | |||
| MKNK1 | MKNK1 | Homo sapiens | 107.0 | inhibitor | Z´-LYTE | |||
| MKNK2 (MNK2) | MKNK2 | Homo sapiens | 68.0 | inhibitor | LanthaScreen | |||
| MST1R | MST1R | Homo sapiens | 105.0 | inhibitor | fluorescence resonance energy transfer | |||
| MST4 | STK26 | Homo sapiens | 109.0 | inhibitor | Z´-LYTE | |||
| MUSK | MUSK | Homo sapiens | 84.0 | inhibitor | Z´-LYTE | |||
| MYLK | MYLK | Homo sapiens | 91.0 | inhibitor | LanthaScreen | |||
| MYLK2 | MYLK2 | Homo sapiens | 98.0 | inhibitor | Z´-LYTE | |||
| NEK1 | NEK1 | Homo sapiens | 92.0 | 30.00 | inhibitor | Z´-LYTE | ||
| NEK2 | NEK2 | Homo sapiens | 93.0 | inhibitor | Z´-LYTE | |||
| NEK4 | NEK4 | Homo sapiens | 89.0 | inhibitor | Z´-LYTE | |||
| NEK6 | NEK6 | Homo sapiens | 95.0 | inhibitor | Z´-LYTE | |||
| NEK9 | NEK9 | Homo sapiens | 99.0 | inhibitor | Z´-LYTE | |||
| NLK | NLK | Homo sapiens | 93.0 | inhibitor | LanthaScreen | |||
| NTRK1 | NTRK1 | Homo sapiens | 81.0 | 83.00 | inhibitor | Z´-LYTE | ||
| NTRK2 | NTRK2 | Homo sapiens | 95.0 | inhibitor | Z´-LYTE | |||
| NTRK3 | NTRK3 | Homo sapiens | 84.0 | inhibitor | Z´-LYTE | |||
| NUAK1 | NUAK1 | Homo sapiens | 84.0 | inhibitor | Adapta | |||
| PAK1 | PAK1 | Homo sapiens | 98.0 | inhibitor | Z´-LYTE | |||
| PAK2 | PAK2 | Homo sapiens | 95.0 | inhibitor | Z´-LYTE | |||
| PAK3 | PAK3 | Homo sapiens | 101.0 | inhibitor | Z´-LYTE | |||
| PAK4 | PAK4 | Homo sapiens | 95.0 | 80.00 | inhibitor | Z´-LYTE | ||
| PAK6 | PAK6 | Homo sapiens | 105.0 | inhibitor | Z´-LYTE | |||
| PAK7 | PAK5 | Homo sapiens | 93.0 | inhibitor | Z´-LYTE | |||
| PASK | PASK | Homo sapiens | 106.0 | inhibitor | Z´-LYTE | |||
| PDGFRA | PDGFRA | Homo sapiens | 93.0 | inhibitor | fluorescence resonance energy transfer | |||
| PDGFRB | PDGFRB | Homo sapiens | 89.0 | 87.00 | inhibitor | Z´-LYTE | ||
| PDK1 | PDK1 | Homo sapiens | 89.0 | 101.00 | inhibitor | Z´-LYTE | ||
| PDK1DIRECT | PDK1 | Homo sapiens | 82.0 | inhibitor | Z´-LYTE | |||
| PHKG1 | PHKG1 | Homo sapiens | 103.0 | inhibitor | Z´-LYTE | |||
| PHKG2 | PHKG2 | Homo sapiens | 99.0 | 97.00 | inhibitor | Z´-LYTE | ||
| PI4KA | PI4KA | Homo sapiens | 84.0 | inhibitor | Adapta | |||
| PI4KB | PI4KB | Homo sapiens | 92.0 | inhibitor | Adapta | |||
| PIK3C2A | PIK3C2A | Homo sapiens | 97.0 | inhibitor | Adapta | |||
| PIK3C2B | PIK3C2B | Homo sapiens | 101.0 | inhibitor | Adapta | |||
| PIK3C3 | PIK3C3 | Homo sapiens | 91.0 | inhibitor | Adapta | |||
| PIK3CAPIK3R1 |
PIK3CA PIK3R1 |
Homo sapiens | 103.0 | inhibitor | Adapta | |||
| PIK3CBPIK3RI |
PIK3CB PIK3R1 |
Homo sapiens | 124.0 | inhibitor | Adapta | |||
| PIK3CDPIK3R1 |
PIK3CD PIK3R1 |
Homo sapiens | 87.0 | inhibitor | Adapta | |||
| PIK3CG | PIK3CG | Homo sapiens | 102.0 | inhibitor | Adapta | |||
| PIM1 | PIM1 | Homo sapiens | 90.0 | 99.00 | inhibitor | Z´-LYTE | ||
| PIM2 | PIM2 | Homo sapiens | 99.0 | inhibitor | Z´-LYTE | |||
| PKN1 | PKN1 | Homo sapiens | 87.0 | inhibitor | Z´-LYTE | |||
| PLK1 | PLK1 | Homo sapiens | 94.0 | 109.00 | inhibitor | Z´-LYTE | ||
| PLK2 | PLK2 | Homo sapiens | 96.0 | inhibitor | Z´-LYTE | |||
| PLK3 | PLK3 | Homo sapiens | 93.0 | inhibitor | Z´-LYTE | |||
| PRKACA | PRKACA | Homo sapiens | 98.0 | 71.00 | inhibitor | Z´-LYTE | ||
| PRKCA | PRKCA | Homo sapiens | 85.0 | inhibitor | Z´-LYTE | |||
| PRKCB1 | PRKCB | Homo sapiens | 89.0 | 102.00 | inhibitor | Z´-LYTE | ||
| PRKCB2 | PRKCB | Homo sapiens | 99.0 | inhibitor | Z´-LYTE | |||
| PRKCD | PRKCD | Homo sapiens | 109.0 | inhibitor | Z´-LYTE | |||
| PRKCE | PRKCE | Homo sapiens | 127.0 | inhibitor | Z´-LYTE | |||
| PRKCG | PRKCG | Homo sapiens | 102.0 | inhibitor | Z´-LYTE | |||
| PRKCH | PRKCH | Homo sapiens | 100.0 | inhibitor | Z´-LYTE | |||
| PRKCI | PRKCI | Homo sapiens | 105.0 | inhibitor | Z´-LYTE | |||
| PRKCN | PRKD3 | Homo sapiens | 91.0 | inhibitor | Z´-LYTE | |||
| PRKCQ | PRKCQ | Homo sapiens | 101.0 | inhibitor | Z´-LYTE | |||
| PRKCZ | PRKCZ | Homo sapiens | 112.0 | inhibitor | Z´-LYTE | |||
| PRKD1 | PRKD1 | Homo sapiens | 83.0 | inhibitor | Z´-LYTE | |||
| PRKD2 | PRKD2 | Homo sapiens | 95.0 | inhibitor | Z´-LYTE | |||
| PRKG1 | PRKG1 | Homo sapiens | 97.0 | inhibitor | Z´-LYTE | |||
| PRKG2 | PRKG2 | Homo sapiens | 108.0 | inhibitor | Z´-LYTE | |||
| PRKX | PRKX | Homo sapiens | 96.0 | inhibitor | Z´-LYTE | |||
| PTK2 | PTK2 | Homo sapiens | 87.0 | inhibitor | Z´-LYTE | |||
| PTK2B | PTK2B | Homo sapiens | 91.0 | 70.00 | inhibitor | Z´-LYTE | ||
| PTK6 | PTK6 | Homo sapiens | 98.0 | inhibitor | Z´-LYTE | |||
| RAF1 | RAF1 | Homo sapiens | 78.0 | inhibitor | Z´-LYTE | |||
| RET | RET | Homo sapiens | 60.0 | 32.00 | inhibitor | fluorescence resonance energy transfer | ||
| RIPK2 | RIPK2 | Homo sapiens | 94.0 | inhibitor | LanthaScreen | |||
| ROCK1 | ROCK1 | Homo sapiens | 88.0 | 47.00 | inhibitor | Z´-LYTE | ||
| ROCK2 | ROCK2 | Homo sapiens | 96.0 | inhibitor | Z´-LYTE | |||
| ROS1 | ROS1 | Homo sapiens | 94.0 | inhibitor | fluorescence resonance energy transfer | |||
| RPS6KA1 | RPS6KA1 | Homo sapiens | 94.0 | inhibitor | fluorescence resonance energy transfer | |||
| RPS6KA2 | RPS6KA2 | Homo sapiens | 96.0 | inhibitor | Z´-LYTE | |||
| RPS6KA3 | RPS6KA3 | Homo sapiens | 94.0 | 95.00 | inhibitor | Z´-LYTE | ||
| RPS6KA4 | RPS6KA4 | Homo sapiens | 96.0 | inhibitor | Z´-LYTE | |||
| RPS6KA5 | RPS6KA5 | Homo sapiens | 102.0 | inhibitor | Z´-LYTE | |||
| RPS6KA6 | RPS6KA6 | Homo sapiens | 98.0 | inhibitor | Z´-LYTE | |||
| RPS6KB1 | RPS6KB1 | Homo sapiens | 94.0 | 66.00 | inhibitor | Z´-LYTE | ||
| SGK | SGK1 | Homo sapiens | 97.0 | inhibitor | Z´-LYTE | |||
| SGK2 | SGK2 | Homo sapiens | 99.0 | inhibitor | Z´-LYTE | |||
| SGKL | SGK3 | Homo sapiens | 96.0 | inhibitor | Z´-LYTE | |||
| SLK | SLK | Homo sapiens | 99.0 | inhibitor | LanthaScreen | |||
| SNF1LK2 | SIK2 | Homo sapiens | 84.0 | inhibitor | Z´-LYTE | |||
| SPHK1 | SPHK1 | Homo sapiens | 81.0 | inhibitor | Adapta | |||
| SRC | SRC | Homo sapiens | 79.0 | 92.00 | inhibitor | Z´-LYTE | ||
| SRC N1 | SRC | Homo sapiens | 88.0 | inhibitor | Z´-LYTE | |||
| SRMS | SRMS | Homo sapiens | 99.0 | inhibitor | Z´-LYTE | |||
| SRPK1 | SRPK1 | Homo sapiens | 99.0 | inhibitor | Z´-LYTE | |||
| SRPK2 | SRPK2 | Homo sapiens | 103.0 | inhibitor | Z´-LYTE | |||
| STK16 | STK16 | Homo sapiens | 91.0 | inhibitor | LanthaScreen | |||
| STK17A | STK17A | Homo sapiens | 80.0 | inhibitor | LanthaScreen | |||
| STK22B | TSSK2 | Homo sapiens | 91.0 | inhibitor | Z´-LYTE | |||
| STK22D | TSSK3 | Homo sapiens | 79.0 | inhibitor | Z´-LYTE | |||
| STK23 | SRPK3 | Homo sapiens | 99.0 | inhibitor | Z´-LYTE | |||
| STK24 | STK24 | Homo sapiens | 101.0 | inhibitor | Z´-LYTE | |||
| STK25 | STK25 | Homo sapiens | 100.0 | inhibitor | Z´-LYTE | |||
| STK3 | STK3 | Homo sapiens | 103.0 | inhibitor | Z´-LYTE | |||
| STK33 | STK33 | Homo sapiens | 88.0 | inhibitor | LanthaScreen | |||
| STK4 | STK4 | Homo sapiens | 102.0 | inhibitor | Z´-LYTE | |||
| STK6 | AURKA | Homo sapiens | 93.0 | 38.00 | inhibitor | Z´-LYTE | ||
| SYK | SYK | Homo sapiens | 94.0 | 97.00 | inhibitor | Z´-LYTE | ||
| TAOK2 | TAOK2 | Homo sapiens | 101.0 | inhibitor | Z´-LYTE | |||
| TAOK3 | TAOK3 | Homo sapiens | 93.0 | inhibitor | LanthaScreen | |||
| TBK1 | TBK1 | Homo sapiens | 96.0 | inhibitor | Z´-LYTE | |||
| TEC | TEC | Homo sapiens | 96.0 | inhibitor | LanthaScreen | |||
| TEK | TEK | Homo sapiens | 93.0 | 82.00 | inhibitor | Z´-LYTE | ||
| TGFBR1 | TGFBR1 | Homo sapiens | 94.0 | inhibitor | LanthaScreen | |||
| TNK2 | TNK2 | Homo sapiens | 97.0 | inhibitor | LanthaScreen | |||
| TTK | TTK | Homo sapiens | 75.0 | inhibitor | LanthaScreen | |||
| TXK | TXK | Homo sapiens | 93.0 | inhibitor | Z´-LYTE | |||
| TYK2 | TYK2 | Homo sapiens | 93.0 | inhibitor | Z´-LYTE | |||
| TYRO3 | TYRO3 | Homo sapiens | 94.0 | inhibitor | Z´-LYTE | |||
| WEE1 | WEE1 | Homo sapiens | 82.0 | inhibitor | LanthaScreen | |||
| WNK2 | WNK2 | Homo sapiens | 86.0 | inhibitor | LanthaScreen | |||
| YES1 | YES1 | Homo sapiens | 74.0 | inhibitor | Z´-LYTE | |||
| ZAK | MAP3K20 | Homo sapiens | 97.0 | inhibitor | LanthaScreen | |||
| ZAP70 | ZAP70 | Homo sapiens | 95.0 | inhibitor | Z´-LYTE |
BI-5026
Conclusion: Clean panel
| Target protein | HGNC name | Species | % control at 10 µM | Mode of action | Assay |
|---|---|---|---|---|---|
| CHUK_IKKA | CHUK | Homo sapiens | 105.0 | inhibitor | Adapta |
| IKBKB | IKBKB | Homo sapiens | 91.0 | inhibitor | Z´-LYTE |
| IKBKE | IKBKE | Homo sapiens | 76.0 | inhibitor | Z´-LYTE |
BI 605906
Conclusion: Closest hit is MAP2K1 with 19.3 % Ctrl at 10 µM. But it was not a hit in the Invitrogen Lab (UK) kinase screen with 80 % Ctrl at 10 µM.
| Target protein | HGNC name | Species | % control at 10 µM | Mode of action | Assay |
|---|---|---|---|---|---|
| AMPK | PRKAA1 | Rattus norvegicus | 79.2 | ||
| Aurora B | AURKB | Homo sapiens | 60.9 | inhibitor | Others |
| Calmodulin dependent kinase 1, CAMK-1 | CAMK1 | Homo sapiens | 78.4 | inhibitor | Radioactive Assay |
| CDK2/cyclin A | CDK2 | Homo sapiens | 78.0 | inhibitor | Radioactive Assay |
| CHK1 | CHEK1 | Homo sapiens | 90.2 | Radioactive Assay | |
| Checkpoint kinase-2, CHK2 | CHEK2 | Homo sapiens | 49.7 | Radioactive Assay | |
| CK1 | CSNK1A1 | Rattus norvegicus | 68.6 | Radioactive Assay | |
| CK2 | CSNK2A1 | Homo sapiens | 89.4 | Radioactive Assay | |
| CSK | CSK | Homo sapiens | 78.3 | Radioactive Assay | |
| DYRK 1a | DYRK1A | Rattus norvegicus | 74.9 | inhibitor | Radioactive Assay |
| Elongation factor kinase, EF2K | EEF2K | Homo sapiens | 66.2 | activator | Radioactive Assay |
| mitogen-activated protein kinase 8, ERK8 | MAPK15 | Homo sapiens | 63.2 | Radioactive Assay | |
| GSK3b | GSK3B | Homo sapiens | 74.4 | Radioactive Assay | |
| JNK1alpha1/SAPK1c | MAPK8 | Homo sapiens | 93.8 | inhibitor | Radioactive Assay |
| c-Jun N-terminal kinase 3, JNK3 alpha 1 | MAPK10 | Homo sapiens | 72.4 | inhibitor | Radioactive Assay |
| MAPK2/ERK2 | MAPK1 | Mus musculus | 90.1 | inhibitor | Radioactive Assay |
| MAPK-activated protein kinase-1b, MAPKAP-K1b | RPS6KA3 | Homo sapiens | 78.2 | inhibitor | Radioactive Assay |
| MAPK-activated protein kinase-3, MAPKAP-K3 | MAPKAPK3 | Homo sapiens | 90.2 | Radioactive Assay | |
| MAPKAP-K1a | RPS6KA1 | Rattus norvegicus | 77.5 | inhibitor | Radioactive Assay |
| MAPKAP-K2 | MAPKAPK2 | Homo sapiens | 94.5 | inhibitor | Radioactive Assay |
| Microtubile affinity regulating kinase (C-TAK1), MARK3 | MARK3 | Homo sapiens | 63.8 | Radioactive Assay | |
| MKK1 | MAP2K1 | Oryctolagus cuniculus | 19.3 | inhibitor | Radioactive Assay |
| MAP kinase interacting Kinase 1, MNK1 | MKNK1 | Homo sapiens | 93.8 | inhibitor | Radioactive Assay |
| MAP kinase interacting Kinase 2, MNK2 alpha | MKNK2 | Homo sapiens | 67.2 | inhibitor | Radioactive Assay |
| MSK1 | RPS6KA5 | Homo sapiens | 86.6 | inhibitor | Radioactive Assay |
| Mammalian sterile 20-like 2 (KRS1 or Ser/Thr protein kinase 3), MST2 | STK3 | Homo sapiens | 91.0 | inhibitor | Radioactive Assay |
| NEK2A | NEK2 | Homo sapiens | 74.8 | Radioactive Assay | |
| NIMA-related protein kinase 6 | NEK6 | Homo sapiens | 83.3 | Radioactive Assay | |
| NIMA related Protein Kinase 7, NEK7 | NEK7 | Homo sapiens | 104.0 | Radioactive Assay | |
| PBK | PBK | Homo sapiens | 100.0 | Radioactive Assay | |
| PDK1 | PDK1 | Homo sapiens | 89.1 | Radioactive Assay | |
| PIM2 | PIM2 | Homo sapiens | 101.0 | inhibitor | Radioactive Assay |
| PKA (rec) | Homo sapiens | 61.7 | inhibitor | Radioactive Assay | |
| protein kinase B beta, deltaPH-PKBbeta (S474D) | AKT2 | Homo sapiens | 98.1 | inhibitor | Radioactive Assay |
| PKBdeltaPH (AKT1 without PH domain) | AKT1 | Homo sapiens | 75.6 | inhibitor | Radioactive Assay |
| PKCa | PRKCA | Homo sapiens | 66.9 | inhibitor | Radioactive Assay |
| Protein kinase D1, PKD1 | PKD1 | Homo sapiens | 93.5 | inhibitor | Radioactive Assay |
| Polo like kinase 1 (Ser/Thr protein kinase 13), PLK1 | PLK1 | Homo sapiens | 86.8 | inhibitor | Radioactive Assay |
| PRAK | MAPKAPK5 | Homo sapiens | 61.1 | inhibitor | Radioactive Assay |
| PKC like Kinase 2, PRK2 | PKN2 | Homo sapiens | 46.4 | Radioactive Assay | |
| ROCK-II | ROCK2 | Rattus norvegicus | 40.1 | inhibitor | Radioactive Assay |
| S6K1/p70S6K | RPS6KB1 | Homo sapiens | 56.3 | Radioactive Assay | |
| SAPK2a/p38 | MAPK14 | Homo sapiens | 85.3 | Radioactive Assay | |
| SGK | SGK1 | Homo sapiens | 101.0 | Radioactive Assay | |
| Smooth muscle Myosin Light Chain Kinase, smMLCK | MYLK | Homo sapiens | 57.7 | Radioactive Assay | |
| Src | SRC | Gallus gallus | 73.8 | ||
| Serine Arginine Protein Kinase, SRPK1 | SRPK1 | Homo sapiens | 73.3 | inhibitor | Radioactive Assay |
BI-5026
Conclusion: Clean panel.
| Target protein | HGNC name | Species | Cmp. conc. | % Control | Assay ID |
|---|---|---|---|---|---|
| 5HT1B(H) | HTR1B | Homo sapiens | 10 µM | 109.0 | Cerep_4376 |
| CB1(HU)_AGON | CNR1 | Homo sapiens | 10 µM | 101.0 | Cerep_4708 |
| COX-1 | PTGS1 | Homo sapiens | 10 µM | 110.0 | Cerep_4173 |
| COX-2 | PTGS2 | Homo sapiens | 10 µM | 92.0 | Cerep_4186 |
| KAPPA(KOP)_HU | OPRK1 | Homo sapiens | 10 µM | 97.0 | Cerep_4461 |
| 5HT1A/H | HTR1A | Homo sapiens | 10 µM | 97.0 | Cerep_131 |
| 5HT2AH_AGON | HTR2A | Homo sapiens | 10 µM | 103.0 | Cerep_471 |
| 5HT2B/H AG | HTR2B | Homo sapiens | 10 µM | 41.0 | Cerep_1333 |
| 5HT3/H | HTR3A | Homo sapiens | 10 µM | 94.0 | Cerep_411 |
| A2A/H | ADORA2A | Homo sapiens | 10 µM | 93.0 | Cerep_4 |
| ACE(HU_AMTCH400) | ACHE | Homo sapiens | 10 µM | 111.0 | Old_Cerep_363 |
| ALPHA1AH_ANTAG | ADRA1A | Homo sapiens | 10 µM | 94.0 | Cerep_2338 |
| ALPHA2A/HU | ADRA2A | Homo sapiens | 10 µM | 93.0 | Cerep_13 |
| ANDROGEN/H | AR | Homo sapiens | 10 µM | 103.0 | Cerep_933 |
| BETA1/HUM | ADRB1 | Homo sapiens | 10 µM | 102.0 | Cerep_18 |
| BETA2/HUM | ADRB2 | Homo sapiens | 10 µM | 101.0 | Cerep_20 |
| BZD/CENTR/R | Rattus norvegicus | 10 µM | 119.0 | Cerep_28 | |
| CA+/DHPSI/R | Rattus norvegicus | 10 µM | 102.0 | Old_Cerep_161 | |
| CB2/PERIPH/H | CNR2 | Homo sapiens | 10 µM | 98.0 | Cerep_37 |
| CCKA/H | CCKAR | Homo sapiens | 10 µM | 90.0 | Old_Cerep_39 |
| D1/H | DRD1 | Homo sapiens | 10 µM | 97.0 | Cerep_44 |
| D2SH_AGON | DRD2 | Homo sapiens | 10 µM | 106.0 | Cerep_1322 |
| DATRANS/HUM | SLC6A3 | Homo sapiens | 10 µM | 107.0 | Old_Cerep_52 |
| DELTA2/H | OPRD1 | Homo sapiens | 10 µM | 99.0 | Cerep_114 |
| ETA/H | EDNRA | Homo sapiens | 10 µM | 113.0 | Cerep_54 |
| GCORTICOID/H | NR3C1 | Homo sapiens | 10 µM | 101.0 | Old_Cerep_469 |
| H1/PYRIL/HS | HRH1 | Homo sapiens | 10 µM | 109.0 | Cerep_870 |
| H2/APT/HS | HRH2 | Homo sapiens | 10 µM | 115.0 | Cerep_1208 |
| HERG_DOFETILIDE | KCNH2 | Homo sapiens | 10 µM | 103.0 | Cerep_4094 |
| K+/VOLT/RA | Rattus norvegicus | 10 µM | 106.0 | Cerep_166 | |
| LCK_CE | LCK | Homo sapiens | 10 µM | 103.0 | Old_Cerep_2906 |
| M1/H | CHRM1 | Homo sapiens | 10 µM | 108.0 | Cerep_91 |
| M2/H | CHRM2 | Homo sapiens | 10 µM | 104.0 | Cerep_93 |
| M3/H | CHRM3 | Homo sapiens | 10 µM | 100.0 | Cerep_95 |
| MAO-A_ANTAG | MAOA | Rattus norvegicus | 10 µM | 79.0 | Cerep_443 |
| MU/H | OPRM1 | Homo sapiens | 10 µM | 94.0 | Cerep_118 |
| NA+/SITE2/R | Rattus norvegicus | 10 µM | 96.0 | Old_Cerep_169 | |
| NEUP/H | SLC6A2 | Homo sapiens | 10 µM | 101.0 | Cerep_355 |
| NMDA/R | Rattus norvegicus | 10 µM | 106.0 | Cerep_66 | |
| N_NEURO_A4B2 |
CHRNA4 CHRNB2 |
Homo sapiens | 10 µM | 104.0 | Cerep_3029 |
| PDE3A | PDE3A | Homo sapiens | 10 µM | 74.0 | Cerep_4072 |
| PDE4D2 | PDE4D | Homo sapiens | 10 µM | 66.0 | Cerep_4077 |
| SLC6A4/H | SCL6A4 | Homo sapiens | 10 µM | 96.0 | Cerep_439 |
| V1A/HUM | AVPR1A | Homo sapiens | 10 µM | 93.0 | Cerep_159 |