Selectivity data for probe T3-CLK and control T3-CLK-N
Jump to control PDSP data
T3-CLK
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| Beta1 | ADRB1 | -7.22 | ||
| Beta3 | ADRB3 | -11.51 | ||
| H1 | HRH1 | 54.89 | 2154.79 average (n=2) | 5.67 |
| H2 | HRH2 | 19.41 | ||
| 5-HT1A | HTR1A | -11.70 | ||
| 5-HT1B | HTR1B | 7.83 | ||
| 5-HT1D | HTR1D | 5.95 | ||
| Sigma 1 | SIGMAR1 | 16.86 | ||
| Sigma 2 | TMEM97 | 13.44 | ||
| 5-HT1E | HTR1E | -1.52 | ||
| 5-HT2A | HTR2A | -2.63 | ||
| 5-HT2B | HTR2B | -7.63 | ||
| 5-HT2C | HTR2C | 12.44 | ||
| 5-HT3 | HTR3A | 1.81 | ||
| 5-HT5A | HTR5A | 4.00 | ||
| 5-HT6 | HTR6 | -15.74 | ||
| 5-HT7A | HTR7 | -5.21 | ||
| GABAA/BZP | 7.47 | |||
| D1 | DRD1 | 4.41 | ||
| D2 | DRD2 | 10.85 | ||
| D3 | DRD3 | 12.75 | ||
| D4 | DRD4 | 9.12 | ||
| DAT | SLC6A3 | 8.33 | ||
| DOR | OPRD1 | 4.05 | ||
| KOR | OPRK1 | -6.32 | ||
| MOR | OPRM1 | 5.33 | ||
| Alpha1A | ADRA1A | -5.18 | ||
| Alpha1B | ADRA1B | 4.68 | ||
| Alpha1D | ADRA1D | -12.43 | ||
| Alpha2A | ADRA2A | 2.61 | ||
| Alpha2B | ADRA2B | 19.27 | ||
| Alpha2C | ADRA2C | 17.17 | ||
| D5 | DRD5 | -7.30 | ||
| M1 | CHRM1 | -10.83 | ||
| M3 | CHRM3 | 21.12 | ||
| M4 | CHRM4 | 25.17 | ||
| M5 | CHRM5 | 9.31 | ||
| NET | SLC6A2 | 5.30 | ||
| GABA/PBR | -18.71 | |||
| H3 | HRH3 | 16.64 | ||
| M2 | CHRM2 | 3.82 | ||
| SERT | SLC6A4 | -3.55 | ||
| Beta2 | ADRB2 | 16.61 | ||
| H4 | HRH4 | 0.74 | ||
| GABAA | -5.11 |
T3-CLK-N
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| Sigma 2 | TMEM97 | 97.92 | 411.90 average (n=2) | 6.39 |
| 5-HT1E | HTR1E | 60.45 | 3555.25 average (n=2) | 5.46 |
| 5-HT2C | HTR2C | 82.98 | 1066.46 average (n=2) | 5.98 |
| 5-HT3 | HTR3A | 6.47 | ||
| 5-HT5A | HTR5A | 83.24 | 2494.89 average (n=2) | 5.65 |
| 5-HT6 | HTR6 | 30.77 | ||
| 5-HT7A | HTR7 | 45.25 | ||
| Alpha2A | ADRA2A | 83.67 | 2658.89 | 5.58 |
| Alpha2B | ADRA2B | 77.56 | 1646.19 average (n=2) | 5.79 |
| Alpha2C | ADRA2C | 88.54 | > 10000.00 average (n=3) | < 5.00 |
| Beta3 | ADRB3 | 78.09 | > 10000.00 average (n=2) | < 5.00 |
| GABAA/BZP | 13.48 | |||
| D2 | DRD2 | 57.48 | 2752.36 average (n=2) | 5.63 |
| D4 | DRD4 | 34.78 | ||
| DAT | SLC6A3 | -0.51 | ||
| DOR | OPRD1 | 46.16 | ||
| KOR | OPRK1 | 54.39 | 990.27 average (n=2) | 6.01 |
| MOR | OPRM1 | 55.67 | 4021.59 average (n=2) | 5.40 |
| SERT | SLC6A4 | 26.33 | ||
| Sigma 1 | SIGMAR1 | 90.03 | 798.34 average (n=2) | 6.13 |
| 5-HT2A | HTR2A | 92.34 | 1526.37 average (n=3) | 5.88 |
| 5-HT2B | HTR2B | 44.06 | ||
| Alpha1A | ADRA1A | 66.42 | 1394.62 average (n=2) | 5.87 |
| Alpha1D | ADRA1D | 57.00 | 1453.09 average (n=2) | 5.84 |
| Beta1 | ADRB1 | 27.98 | ||
| Beta2 | ADRB2 | 17.20 | ||
| D1 | DRD1 | 58.21 | 1496.83 average (n=2) | 5.89 |
| D3 | DRD3 | 78.87 | 2249.15 average (n=2) | 5.72 |
| D5 | DRD5 | 29.67 | ||
| GABAA | 4.08 | |||
| H1 | HRH1 | 83.01 | 1901.20 average (n=3) | 5.88 |
| H2 | HRH2 | 86.75 | 1725.74 average (n=2) | 5.79 |
| H3 | HRH3 | 43.77 | ||
| H4 | HRH4 | 31.89 | ||
| M1 | CHRM1 | 68.31 | 2092.27 average (n=2) | 5.71 |
| M3 | CHRM3 | 40.35 | ||
| M4 | CHRM4 | 0.99 | ||
| M5 | CHRM5 | 30.78 | ||
| NET | SLC6A2 | 40.84 | ||
| GABA/PBR | -6.10 | |||
| 5-HT1A | HTR1A | 51.29 | 2557.41 average (n=2) | 5.60 |
| M2 | CHRM2 | 6.55 | ||
| 5-HT1B | HTR1B | 66.90 | 2168.63 average (n=2) | 5.70 |
| 5-HT1D | HTR1D | 50.55 | 3073.30 average (n=2) | 5.55 |
| Alpha1B | ADRA1B | 50.45 | 5525.80 average (n=2) | 5.27 |
T3-CLK
Results are expressed as percent inhibition of control specific binding (mean values; n=2). Shown are supplementary data from PMID: 28232751 .
Conclusion: No additional kinases beyond the CMGC group of kinases were inhibited in this panel.
| Target protein | HGNC name | Species | % inhibition at 1 µM | % inhibition at 1.11 µM | % inhibition at 0.1 µM | % inhibition at 0.123 µM |
|---|---|---|---|---|---|---|
| CLK1 | CLK1 | 99.13 | 91.21 | |||
| CLK2 | CLK2 | 100.48 | 92.10 | |||
| CLK3 | CLK3 | 88.72 | 38.33 | |||
| DYRK1A | DYRK1A | 97.46 | 74.17 | |||
| DYRK1B | DYRK1B | 94.08 | 62.70 | |||
| DYRK3 | DYRK3 | 3.70 | -1.82 | |||
| DYRK4 | DYRK4 | -2.87 | -8.38 | |||
| SRPK1 | SRPK1 | -2.58 | -3.09 | |||
| SRPK2 | SRPK2 | 5.16 | 1.82 | |||
| ABL1 | ABL1 | 55.7 | 10.14 | |||
| AKT1 (PKB alpha) | AKT1 | -11.8 | -8.24 | |||
| AMPK A1/B1/G1 |
PRKAA1 PRKAB1 PRKAG1 |
0.5 | -2.00 | |||
| AURKA (Aurora A) | AURKA | 8.6 | 4.51 | |||
| AURKB (Aurora B) | AURKB | 16.1 | 6.77 | |||
| AXL | AXL | -13.7 | -10.19 | |||
| BRAF | BRAF | 17.2 | 8.71 | |||
| CDK1/cyclin B | CDK1 | 7.1 | 7.95 | |||
| CDK2/cyclin A |
CDK2 CCNA2 |
3.3 | 0.33 | |||
| CDK5/p25 |
CDK5 CDK5R1 |
0.8 | 1.84 | |||
| CDK5/p35 |
CDK5 CDK5R1 |
-1.1 | 1.85 | |||
| CHEK1 (CHK1) | CHEK1 | 18.4 | 9.74 | |||
| CHEK2 (CHK2) | CHEK2 | 24.2 | 21.89 | |||
| CSNK1A1 (CK1 alpha 1) | CSNK1A1 | -2.7 | -3.75 | |||
| CSNK1D (CK1 delta) | CSNK1D | 4.3 | -2.92 | |||
| EGFR (ErbB1) | EGFR | -16.6 | -19.66 | |||
| EPHA1 | EPHA1 | -0.6 | -1.64 | |||
| EPHA2 | EPHA2 | -6.3 | -4.09 | |||
| EPHA5 | EPHA5 | -5.0 | -5.80 | |||
| EPHB1 | EPHB1 | 4.1 | 4.83 | |||
| ERBB2 (HER2) | ERBB2 | -28.0 | -21.31 | |||
| FGFR1 | FGFR1 | 9.2 | 4.26 | |||
| FLT1 (VEGFR1) | FLT1 | -11.2 | -15.17 | |||
| FRAP1 (mTOR) | MTOR | -8.5 | -5.58 | |||
| GSK3B (GSK3 beta) | GSK3B | -3.1 | -3.21 | |||
| HIPK1 (Myak) | HIPK1 | 2.7 | -0.71 | |||
| HIPK2 | HIPK2 | -1.8 | -3.60 | |||
| IKBKB (IKK beta) | IKBKB | -4.7 | -6.11 | |||
| IRAK4 | IRAK4 | 42.4 | 25.34 | |||
| JAK1 | JAK1 | -27.0 | 10.93 | |||
| JAK2 | JAK2 | -6.3 | -7.35 | |||
| KIT | KIT | 37.5 | 10.97 | |||
| MAP2K1 (MEK1) | MAP2K1 | 10.9 | 12.37 | |||
| MAP2K2 (MEK2) | MAP2K2 | 13.8 | 16.95 | |||
| MAPK1 (ERK2) | MAPK1 | 4.0 | 2.74 | |||
| MAPK11 (p38 beta) | MAPK11 | 0.9 | 0.67 | |||
| MAPK14 (p38 alpha) | MAPK14 | 6.4 | 4.88 | |||
| MAPK3 (ERK1) | MAPK3 | 6.1 | 5.63 | |||
| MAPK8 (JNK1) | MAPK8 | 2.6 | 5.45 | |||
| MAPK9 (JNK2) | MAPK9 | -1.5 | 3.18 | |||
| MAPKAPK2 | MAPKAPK2 | 2.1 | 3.68 | |||
| MET (cMet) | MET | -7.4 | -16.16 | |||
| NEK1 | NEK1 | 25.1 | 3.86 | |||
| NEK2 | NEK2 | 24.3 | 11.86 | |||
| PDK1 Direct | PDK1 | 1.9 | -0.83 | |||
| PIM1 | PIM1 | 11.3 | 15.55 | |||
| PLK1 | PLK1 | 2.5 | 7.85 | |||
| PRKACA (PKA) | PRKACA | 3.6 | -1.57 | |||
| PRKCA (PKC alpha) | PRKCA | 3.7 | 4.38 | |||
| PRKCQ (PKC theta) | PRKCQ | 4.2 | 5.46 | |||
| PTK2 (FAK) | PTK2 | -7.4 | -9.12 | |||
| RET | RET | -2.4 | -1.05 | |||
| ROCK1 | ROCK1 | 9.4 | 5.17 | |||
| ROS1 | ROS1 | -0.4 | -3.68 | |||
| RPS6KB1 (p70S6K) | RPS6KB1 | 0.7 | 2.21 | |||
| SRC | SRC | 46.7 | 13.15 | |||
| TEK (Tie2) | TEK | -0.3 | 0.11 | |||
| CAMK1 (CaMK1) | CAMK1 | 5.3 | 7.14 | |||
| CDK7/cyclin H/MNAT1 | CDK7 | -3.4 | 0.55 | |||
| CDK9/cyclin T1 | CDK9 | -17.0 | -13.96 | |||
| DAPK1 | DAPK1 | -6.4 | -4.42 | |||
| PIK3CA/PIK3R1 (p110 alpha/p85 alpha) |
PIK3CA PIK3R1 |
3.6 | 3.58 |