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Selectivity data for probe CCT369260 and control CCT393732


Jump to control PDSP data

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

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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