Selectivity data for probe CCT369260 and control CCT393732
CCT369260
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| 5-HT1A | HTR1A | 5.99 | ||
| 5-HT1B | HTR1B | 3.38 | ||
| 5-HT1D | HTR1D | 56.54 | 6174.88 average (n=2) | 5.21 |
| 5-HT1E | HTR1E | -24.02 | ||
| 5-HT2A | HTR2A | 23.55 | ||
| 5-HT2B | HTR2B | 34.59 | ||
| 5-HT2C | HTR2C | 16.11 | ||
| 5-HT3 | HTR3A | -5.81 | ||
| 5-HT5A | HTR5A | 13.19 | ||
| 5-HT6 | HTR6 | 3.94 | ||
| 5-HT7A | HTR7 | -11.89 | ||
| A1 | ADORA1 | 93.08 | 1630.55 average (n=3) | 5.96 |
| A2A | ADORA2A | -3.49 | ||
| Alpha1A | ADRA1A | 7.70 | ||
| Alpha1B | ADRA1B | 12.40 | ||
| Alpha1D | ADRA1D | 16.02 | ||
| Alpha2A | ADRA2A | 14.03 | ||
| Alpha2B | ADRA2B | 7.28 | ||
| Alpha2C | ADRA2C | 15.12 | ||
| Beta1 | ADRB1 | -2.67 | ||
| Beta2 | ADRB2 | -42.26 | ||
| Beta3 | ADRB3 | 65.27 | 3994.88 average (n=2) | 5.41 |
| GABAA/BZP | 7.06 | |||
| D1 | DRD1 | 27.29 | ||
| D2 | DRD2 | 20.83 | ||
| D3 | DRD3 | -14.23 | ||
| D4 | DRD4 | 15.21 | ||
| D5 | DRD5 | 26.22 | ||
| DAT | SLC6A3 | 50.76 | 5087.69 average (n=2) | 5.31 |
| DOR | OPRD1 | 18.11 | ||
| GABAA | -40.99 | |||
| H1 | HRH1 | 10.28 | ||
| H2 | HRH2 | 43.67 | ||
| H3 | HRH3 | 60.67 | 2333.56 average (n=2) | 5.69 |
| H4 | HRH4 | -0.79 | ||
| KOR | OPRK1 | -22.62 | ||
| M1 | CHRM1 | 3.30 | ||
| M2 | CHRM2 | 0.77 | ||
| M3 | CHRM3 | 11.98 | ||
| M4 | CHRM4 | -2.86 | ||
| M5 | CHRM5 | 20.58 | ||
| MOR | OPRM1 | 86.60 | 872.47 average (n=3) | 6.07 |
| NET | SLC6A2 | 18.13 | ||
| GABA/PBR | 59.57 | 1113.88 average (n=2) | 6.01 | |
| SERT | SLC6A4 | -20.69 | ||
| Sigma 1 | SIGMAR1 | 47.38 | ||
| Sigma 2 | TMEM97 | 85.65 | 2503.46 average (n=2) | 5.60 |
| V1A | AVPR1A | 78.62 |
CCT369260
SUDHL4 or OCI-Ly1 cells were treated with 1 µM CCT369260 for 1h or 6 h and the protein abundance analysed by MS. LogFC is equal the binary logarithm of the normalized abundances for the compound divided by the normalized abundances for DMSO.
Conclusion: Clean panel. Only the target BCL6 is degraded.
| Target protein | HGNC name | Species | Normalized abundances for DMSO | Normalized abundances for compound | LogFC |
|---|---|---|---|---|---|
| BCL6 | BCL6 | Homo sapiens | 12088.8 | 5265.00 | -1.20 |
| MYNN | MYNN | Homo sapiens | 121.9 | 111.00 | -0.14 |
| ZBTB11 | ZBTB11 | Homo sapiens | 2812.5 | 2715.90 | -0.05 |
| BACH2 | BACH2 | Homo sapiens | 2131.1 | 2078.90 | -0.04 |
| ZBTB9 | ZBTB9 | Homo sapiens | 964.2 | 949.50 | -0.02 |
| ZBTB48 | ZBTB48 | Homo sapiens | 1048.1 | 1037.10 | -0.02 |
| ZBTB44 | ZBTB44 | Homo sapiens | 566.5 | 563.20 | -0.01 |
| ZBTB21 (ZNF295) | ZBTB21 | Homo sapiens | 433.0 | 436.10 | 0.01 |
| ZBTB43 | ZBTB43 | Homo sapiens | 634.8 | 643.40 | 0.02 |
| ZBTB1 | ZBTB1 | Homo sapiens | 3559.4 | 3617.80 | 0.02 |
| ZBTB24 | ZBTB24 | Homo sapiens | 287.8 | 293.00 | 0.03 |
| ZBTB10 | ZBTB10 | Homo sapiens | 3595.0 | 3666.30 | 0.03 |
| ZBTB2 | ZBTB2 | Homo sapiens | 685.6 | 699.50 | 0.03 |
| ZBTB17 | ZBTB17 | Homo sapiens | 257.4 | 262.70 | 0.03 |
| ZBTB7A | ZBTB7A | Homo sapiens | 915.2 | 936.80 | 0.03 |
| ZBTB33 | ZBTB33 | Homo sapiens | 2149.7 | 2263.40 | 0.07 |
| ZBTB14 (ZFP161) | ZBTB14 | Homo sapiens | 351.0 | 371.70 | 0.08 |
| ZBTB40 | ZBTB40 | Homo sapiens | 1218.7 | 1292.20 | 0.08 |
| ZBTB8OS | ZBTB8OS | Homo sapiens | 1431.5 | 1538.90 | 0.10 |
| ZNF131 | ZNF131 | Homo sapiens | 1720.7 | 1858.30 | 0.11 |
CCT369260
SUDHL4 or OCI-Ly1 cells were treated with 1 µM CCT369260 for 1h or 6 h and the protein abundance analysed by MS. LogFC is equal the binary logarithm of the normalized abundances for the compound divided by the normalized abundances for DMSO.
Conclusion: Clean panel. Only the target BCL6 is degraded.
| Target protein | HGNC name | Species | Normalized abundances for DMSO | Normalized abundances for compound | LogFC |
|---|---|---|---|---|---|
| BCL6 | BCL6 | Homo sapiens | 12162.7 | 5545.20 | -1.13 |
| MYNN | MYNN | Homo sapiens | 124.8 | 109.50 | -0.19 |
| ZBTB11 | ZBTB11 | Homo sapiens | 2736.5 | 2802.00 | 0.03 |
| BACH2 | BACH2 | Homo sapiens | 2165.7 | 2035.40 | -0.09 |
| ZBTB9 | ZBTB9 | Homo sapiens | 942.4 | 1001.20 | 0.09 |
| ZBTB48 | ZBTB48 | Homo sapiens | 1057.5 | 1081.50 | 0.03 |
| ZBTB44 | ZBTB44 | Homo sapiens | 565.4 | 480.30 | -0.24 |
| ZBTB21 (ZNF295) | ZBTB21 | Homo sapiens | 401.9 | 407.20 | 0.02 |
| ZBTB43 | ZBTB43 | Homo sapiens | 643.1 | 660.70 | 0.04 |
| ZBTB1 | ZBTB1 | Homo sapiens | 3560.1 | 3497.70 | -0.03 |
| ZBTB24 | ZBTB24 | Homo sapiens | 290.9 | 291.20 | 0.00 |
| ZBTB10 | ZBTB10 | Homo sapiens | 3644.2 | 3963.10 | 0.12 |
| ZBTB2 | ZBTB2 | Homo sapiens | 675.5 | 751.10 | 0.15 |
| ZBTB17 | ZBTB17 | Homo sapiens | 273.3 | 264.50 | -0.05 |
| ZBTB7A | ZBTB7A | Homo sapiens | 911.2 | 869.40 | -0.07 |
| ZBTB33 | ZBTB33 | Homo sapiens | 2177.8 | 2144.90 | -0.02 |
| ZBTB14 (ZFP161) | ZBTB14 | Homo sapiens | 354.5 | 362.10 | 0.03 |
| ZBTB40 | ZBTB40 | Homo sapiens | 1291.1 | 1290.00 | 0.00 |
| ZBTB8OS | ZBTB8OS | Homo sapiens | 1469.0 | 1496.10 | 0.03 |
| ZNF131 | ZNF131 | Homo sapiens | 1849.8 | 1794.20 | -0.04 |
CCT369260
SUDHL4 or OCI-Ly1 cells were treated with 1 µM CCT369260 for 1h or 6 h and the protein abundance analysed by MS. LogFC is equal the binary logarithm of the normalized abundances for the compound divided by the normalized abundances for DMSO.
Conclusion: Clean panel. Only the target BCL6 is degraded.
| Target protein | HGNC name | Species | Normalized abundances for DMSO | Normalized abundances for compound | LogFC |
|---|---|---|---|---|---|
| BCL6 | BCL6 | Homo sapiens | 1066.0 | 154.00 | -2.79 |
| ZBTB11 | ZBTB11 | Homo sapiens | 366.0 | 364.30 | -0.01 |
| BACH2 | BACH2 | Homo sapiens | 520.6 | 520.10 | 0.00 |
| ZBTB9 | ZBTB9 | Homo sapiens | 40.5 | 39.80 | -0.03 |
| ZBTB48 | ZBTB48 | Homo sapiens | 555.6 | 564.50 | 0.02 |
| ZBTB44 | ZBTB44 | Homo sapiens | 9.4 | 12.60 | 0.42 |
| ZBTB1 | ZBTB1 | Homo sapiens | 115.5 | 110.70 | -0.06 |
| ZBTB24 | ZBTB24 | Homo sapiens | 39.1 | 36.20 | -0.11 |
| ZBTB10 | ZBTB10 | Homo sapiens | 345.7 | 371.20 | 0.10 |
| ZBTB2 | ZBTB2 | Homo sapiens | 15.0 | 17.70 | 0.24 |
| ZBTB33 | ZBTB33 | Homo sapiens | 142.3 | 133.10 | -0.10 |
| ZBTB40 | ZBTB40 | Homo sapiens | 94.7 | 82.80 | -0.19 |
| ZNF131 | ZNF131 | Homo sapiens | 34.9 | 21.30 | -0.71 |
CCT369260
For the DSF screen 20 µM compound and 2 µM target protein was used.
Conclusion: Clean panel
| Target protein | HGNC name | Species | Tm [°C] | Tm shift [°C] | Comment |
|---|---|---|---|---|---|
| AAK1 | AAK1 | Homo sapiens | 47.0 | 0.00 | Cpd not binding |
| ABL1 | ABL1 | Homo sapiens | 46.0 | 0.00 | Cpd not binding |
| AKT3 | AKT3 | Homo sapiens | 49.0 | 0.00 | Cpd not binding |
| AURKB | AURKB | Homo sapiens | 46.0 | -1.00 | Cpd not binding |
| BMP2K | BMP2K | Homo sapiens | 43.0 | 0.00 | Cpd not binding |
| BMPR2 | BMPR2 | Homo sapiens | 51.0 | 0.00 | Cpd not binding |
| BMX | BMX | Homo sapiens | 48.0 | -5.00 | Cpd not binding |
| BRAF | BRAF | Homo sapiens | 39.0 | 0.00 | |
| BRD4 | BRD4 | Homo sapiens | 44.0 | -1.00 | Cpd not binding |
| BRPF1 | BRPF1 | Homo sapiens | 44.0 | 0.00 | Cpd not binding |
| CAMK1D | CAMK1D | Homo sapiens | 49.0 | -4.00 | Cpd not binding |
| CAMK1G | CAMK1G | Homo sapiens | 44.0 | -1.00 | Cpd not binding |
| CAMK2B | CAMK2B | Homo sapiens | 47.0 | 0.00 | Cpd not binding |
| CAMK2D | CAMK2D | Homo sapiens | 47.0 | -2.00 | Cpd not binding |
| CAMK4 | CAMK4 | Homo sapiens | 48.0 | 0.00 | Cpd not binding |
| CAMKK2 | CAMKK2 | Homo sapiens | 38.0 | 0.00 | |
| CASK | CASK | Homo sapiens | 68.0 | 0.00 | Cpd not binding |
| CDC42BPA | CDC42 | Homo sapiens | 43.0 | -1.00 | Cpd not binding |
| CDK2 | CDK2 | Homo sapiens | 46.0 | -1.00 | Cpd not binding |
| CDKL1 | CDKL1 | Homo sapiens | 45.0 | -5.00 | Cpd not binding |
| CHEK2 | CHEK2 | Homo sapiens | 44.0 | 0.00 | Cpd not binding |
| CLK1 | CLK1 | Homo sapiens | 36.0 | 0.00 | |
| CLK3 | CLK3 | Homo sapiens | 34.0 | 0.00 | |
| CSNK1D | CSNK1D | Homo sapiens | 52.0 | 0.00 | Cpd not binding |
| CSNK2A1 | CSNK2A1 | Homo sapiens | 44.0 | 0.00 | Cpd not binding |
| CSNK2A2 | CSNK2A2 | Homo sapiens | 43.0 | 0.00 | Cpd not binding |
| DAPK1 | DAPK1 | Homo sapiens | 53.0 | 0.00 | Cpd not binding |
| DAPK3 | DAPK3 | Homo sapiens | 39.0 | 0.00 | Cpd not binding |
| DCAMKL1 | DCLK1 | Homo sapiens | 42.0 | 0.00 | Cpd not binding |
| DMPK1 | DMPK | Homo sapiens | 50.0 | 0.00 | |
| DYRK1A | DYRK1A | Homo sapiens | 45.0 | -1.00 | Cpd not binding |
| DYRK2 | DYRK2 | Homo sapiens | 46.0 | 0.00 | Cpd not binding |
| EPHA2 | EPHA2 | Homo sapiens | 46.0 | -1.00 | Cpd not binding |
| EPHA4 | EPHA4 | Homo sapiens | 54.0 | 0.00 | Cpd not binding |
| EPHA5 | EPHA5 | Homo sapiens | 44.0 | -1.00 | Cpd not binding |
| EPHA7 | EPHA7 | Homo sapiens | 48.0 | -1.00 | Cpd not binding |
| EPHB1 | EPHB1 | Homo sapiens | 57.0 | -1.00 | Cpd not binding |
| EPHB3 | EPHB3 | Homo sapiens | 52.0 | -1.00 | Cpd not binding |
| FES | FES | Homo sapiens | 44.0 | 0.00 | Cpd not binding |
| FGFR1 | FGFR1 | Homo sapiens | 50.0 | 0.00 | Cpd not binding |
| FGFR2 | FGFR2 | Homo sapiens | 50.0 | -1.00 | Cpd not binding |
| FGFR3 | FGFR3 | Homo sapiens | 42.0 | 0.00 | Cpd not binding |
| FLT1 | FLT1 | Homo sapiens | 45.0 | 0.00 | |
| GAK | GAK | Homo sapiens | 52.0 | 0.00 | Cpd not binding |
| GPRK5 | GRK5 | Homo sapiens | 40.0 | 0.00 | |
| GSG2 | HASPIN | Homo sapiens | 45.0 | -1.00 | Cpd not binding |
| GSK3B | GSK3B | Homo sapiens | 45.0 | 0.00 | Cpd not binding |
| HIPK2 | HIPK2 | Homo sapiens | 43.0 | 0.00 | Cpd not binding |
| MAP2K1 | MAP2K1 | Homo sapiens | 45.0 | 0.00 | Cpd not binding |
| MAP2K4 | MAP2K4 | Homo sapiens | 41.0 | 0.00 | Cpd not binding |
| MAP2K6 | MAP2K6 | Homo sapiens | 45.0 | 0.00 | Cpd not binding |
| MAP2K7 | MAP2K7 | Homo sapiens | 44.0 | -1.00 | Cpd not binding |
| MAP3K5 | MAP3K5 | Homo sapiens | 40.0 | 0.00 | |
| MAPK10 | MAPK10 | Homo sapiens | 48.0 | -1.00 | Cpd not binding |
| MAPK13 | MAPK13 | Homo sapiens | 49.0 | 0.00 | Cpd not binding |
| MAPK14 | MAPK14 | Homo sapiens | 45.0 | -1.00 | Cpd not binding |
| MAPK15 | MAPK15 | Homo sapiens | 50.0 | 0.00 | Cpd not binding |
| MAPK1 | MAPK1 | Homo sapiens | 56.0 | 0.00 | Cpd not binding |
| MAPK8 | MAPK8 | Homo sapiens | 43.0 | 0.00 | Cpd not binding |
| MAPK9 | MAPK9 | Homo sapiens | 54.0 | 0.00 | Cpd not binding |
| MAPKAPK2 | MAPKAPK2 | Homo sapiens | 46.0 | 0.00 | Cpd not binding |
| MARK3 | MARK3 | Homo sapiens | 35.0 | 0.00 | Cpd not binding |
| MARK4 | MARK4 | Homo sapiens | 36.0 | 0.00 | |
| MELK | MELK | Homo sapiens | 41.0 | 0.00 | |
| MERTK | MERTK | Homo sapiens | 47.0 | -2.00 | Cpd not binding |
| MST4 | STK26 | Homo sapiens | 44.0 | 0.00 | |
| NEK1 | NEK1 | Homo sapiens | 47.0 | 0.00 | Cpd not binding |
| NEK2 | NEK2 | Homo sapiens | 40.0 | 0.00 | Cpd not binding |
| NEK7 | NEK7 | Homo sapiens | 42.0 | 0.00 | Cpd not binding |
| OSR1 | OXSR1 | Homo sapiens | 39.0 | 0.00 | Cpd not binding |
| PAK1 | PAK1 | Homo sapiens | 46.0 | 0.00 | Cpd not binding |
| PAK4 | PAK4 | Homo sapiens | 46.0 | 0.00 | Cpd not binding |
| PCTK1 | CDK16 | Homo sapiens | 52.0 | 0.00 | Cpd not binding |
| PHKG2 | PHKG2 | Homo sapiens | 46.0 | -1.00 | Cpd not binding |
| PIM1 | PIM1 | Homo sapiens | 41.0 | -1.00 | Cpd not binding |
| PIM3 | PIM3 | Homo sapiens | 40.0 | 0.00 | |
| PKMYT1 | PKMYT1 | Homo sapiens | 49.0 | 0.00 | Cpd not binding |
| PLK4 | PLK4 | Homo sapiens | 0.0 | 0.00 | Curve omited |
| RIOK1 | RIOK1 | Homo sapiens | 40.0 | -1.00 | Cpd not binding |
| RPS6KA1 | RPS6KA1 | Homo sapiens | 50.0 | 0.00 | |
| RPS6KA5 | RPS6KA5 | Homo sapiens | 37.0 | -1.00 | Cpd not binding |
| SLK | SLK | Homo sapiens | 42.0 | 0.00 | Cpd not binding |
| SRC | SRC | Homo sapiens | 53.0 | 0.00 | Cpd not binding |
| SRPK1 | SRPK1 | Homo sapiens | 45.0 | -1.00 | Cpd not binding |
| STK10 | STK10 | Homo sapiens | 42.0 | -1.00 | Cpd not binding |
| STK17A | STK17A | Homo sapiens | 42.0 | 0.00 | Cpd not binding |
| STK17B | STK17B | Homo sapiens | 43.0 | -4.00 | Cpd not binding |
| STK24 | STK24 | Homo sapiens | 36.0 | 0.00 | |
| STK38L | STK38L | Homo sapiens | 47.0 | 0.00 | Cpd not binding |
| STK39 | STK39 | Homo sapiens | 37.0 | 0.00 | |
| STK3 | STK3 | Homo sapiens | 47.0 | -1.00 | Cpd not binding |
| STK4 | STK4 | Homo sapiens | 46.0 | -1.00 | Cpd not binding |
| STK6 | AURKA | Homo sapiens | 45.0 | 0.00 | Cpd not binding |
| TAF1 | TAF1 | Homo sapiens | 56.0 | 0.00 | Cpd not binding |
| TIF1 | TRIM24 | Homo sapiens | 36.0 | 0.00 | |
| TLK1 | TLK1 | Homo sapiens | 49.0 | 0.00 | Cpd not binding |
| TOPK | PBK | Homo sapiens | 43.0 | -1.00 | Cpd not binding |
| TTK | TTK | Homo sapiens | 46.0 | -3.00 | Cpd not binding |
| ULK1 | ULK1 | Homo sapiens | 41.0 | 0.00 | |
| ULK3 | ULK3 | Homo sapiens | 44.0 | -1.00 | Cpd not binding |
| VRK1 | VRK1 | Homo sapiens | 46.0 | 0.00 | Cpd not binding |
| WNK1 | WNK1 | Homo sapiens | 51.0 | 0.00 | Cpd not binding |