Details of the Target

General Information of Target

Target ID LDTP10826
Target Name Protein cereblon (CRBN)
Gene Name CRBN
Gene ID 51185
Synonyms
Protein cereblon
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MASIMEGPLSKWTNVMKGWQYRWFVLDYNAGLLSYYTSKDKMMRGSRRGCVRLRGAVIGI
DDEDDSTFTITVDQKTFHFQARDADEREKWIHALEETILRHTLQLQGLDSGFVPSVQDFD
KKLTEADAYLQILIEQLKLFDDKLQNCKEDEQRKKIETLKETTNSMVESIKHCIVLLQIA
KDQSNAEKHADGMISTINPVDAIYQPSPLEPVISTMPSQTVLPPEPVQLCKSEQRPSSLP
VGPVLATLGHHQTPTPNSTGSGHSPPSSSLTSPSHVNLSPNTVPEFSYSSSEDEFYDADE
FHQSGSSPKRLIDSSGSASVLTHSSSGNSLKRPDTTESLNSSLSNGTSDADLFDSHDDRD
DDAEAGSVEEHKSVIMHLLSQVRLGMDLTKVVLPTFILERRSLLEMYADFFAHPDLFVSI
SDQKDPKDRMVQVVKWYLSAFHAGRKGSVAKKPYNPILGEIFQCHWTLPNDTEENTELVS
EGPVPWVSKNSVTFVAEQVSHHPPISAFYAECFNKKIQFNAHIWTKSKFLGMSIGVHNIG
QGCVSCLDYDEHYILTFPNGYGRSILTVPWVELGGECNINCSKTGYSANIIFHTKPFYGG
KKHRITAEIFSPNDKKSFCSIEGEWNGVMYAKYATGENTVFVDTKKLPIIKKKVRKLEDQ
NEYESRSLWKDVTFNLKIRDIDAATEAKHRLEERQRAEARERKEKEIQWETRLFHEDGEC
WVYDEPLLKRLGAAKH
Target Type
Clinical trial
Target Bioclass
Transporter and channel
Family
CRBN family
Subcellular location
Cytoplasm
Function
Substrate recognition component of a DCX (DDB1-CUL4-X-box) E3 protein ligase complex that mediates the ubiquitination and subsequent proteasomal degradation of target proteins, such as MEIS2 or ILF2. Normal degradation of key regulatory proteins is required for normal limb outgrowth and expression of the fibroblast growth factor FGF8. Maintains presynaptic glutamate release and consequently cognitive functions, such as memory and learning, by negatively regulating large-conductance calcium-activated potassium (BK) channels in excitatory neurons. Likely to function by regulating the assembly and neuronal surface expression of BK channels via its interaction with KCNT1. May also be involved in regulating anxiety-like behaviors via a BK channel-independent mechanism. Plays a negative role in TLR4 signaling by interacting with TRAF6 and ECSIT, leading to inhibition of ECSIT ubiquitination, an important step of the signaling.
TTD ID
T27861
Uniprot ID
Q96SW2
DrugMap ID
TTDKGTC
Ensemble ID
ENST00000231948.9
HGNC ID
HGNC:30185
ChEMBL ID
CHEMBL3763008

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
NALM6 SNV: p.K204E DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 15 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K211(10.00); K300(10.00)  LDD0277  [1]
m-APA
 Probe Info  		11.61  LDD0403  [2]
BTD
 Probe Info  		C366(0.63)  LDD2137  [3]
DBIA
 Probe Info  		C219(5.18)  LDD0209  [4]
CY-1
 Probe Info  		N.A.  LDD0246  [5]
4-Iodoacetamidophenylacetylene
 Probe Info  		C326(0.00); C287(0.00); C188(0.00); C205(0.00)  LDD0038  [6]
IA-alkyne
 Probe Info  		C310(0.00); C205(0.00); C234(0.00); C326(0.00)  LDD0036  [6]
Lodoacetamide azide
 Probe Info  		C310(0.00); C205(0.00); C234(0.00); C394(0.00)  LDD0037  [6]
IPM
 Probe Info  		N.A.  LDD0025  [7]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [7]
TFBX
 Probe Info  		N.A.  LDD0027  [7]
Compound 10
 Probe Info  		N.A.  LDD2216  [8]
Compound 11
 Probe Info  		N.A.  LDD2213  [8]
Acrolein
 Probe Info  		N.A.  LDD0217  [9]
NAIA_5
 Probe Info  		C441(0.00); C78(0.00); C188(0.00)  LDD2223  [10]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
pLen
 Probe Info  		8.01  LDD0254  [11]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HCT 116 C234(0.93)  LDD0531  [12]
 LDCM0215  AC10 HCT 116 C219(0.89); C234(0.95); C287(1.10)  LDD0532  [12]
 LDCM0216  AC100 HCT 116 C219(0.98); C234(0.84)  LDD0533  [12]
 LDCM0217  AC101 HCT 116 C219(1.16); C234(0.83)  LDD0534  [12]
 LDCM0218  AC102 HCT 116 C219(0.85); C234(0.82)  LDD0535  [12]
 LDCM0219  AC103 HCT 116 C219(0.96); C234(0.81)  LDD0536  [12]
 LDCM0220  AC104 HCT 116 C219(1.03); C234(0.83)  LDD0537  [12]
 LDCM0221  AC105 HCT 116 C219(1.08); C234(0.74)  LDD0538  [12]
 LDCM0222  AC106 HCT 116 C219(1.05); C234(0.72)  LDD0539  [12]
 LDCM0223  AC107 HCT 116 C219(1.55); C234(0.74)  LDD0540  [12]
 LDCM0224  AC108 HCT 116 C219(0.79); C234(0.80)  LDD0541  [12]
 LDCM0225  AC109 HCT 116 C219(0.86); C234(1.24)  LDD0542  [12]
 LDCM0226  AC11 HCT 116 C219(1.06); C234(0.74); C287(0.99)  LDD0543  [12]
 LDCM0227  AC110 HCT 116 C219(0.75); C234(0.92)  LDD0544  [12]
 LDCM0228  AC111 HCT 116 C219(0.83); C234(0.81)  LDD0545  [12]
 LDCM0229  AC112 HCT 116 C219(0.98); C234(0.75)  LDD0546  [12]
 LDCM0230  AC113 HCT 116 C219(0.96)  LDD0547  [12]
 LDCM0231  AC114 HCT 116 C219(0.85)  LDD0548  [12]
 LDCM0232  AC115 HCT 116 C219(0.81)  LDD0549  [12]
 LDCM0233  AC116 HCT 116 C219(1.21)  LDD0550  [12]
 LDCM0234  AC117 HCT 116 C219(0.96)  LDD0551  [12]
 LDCM0235  AC118 HCT 116 C219(0.91)  LDD0552  [12]
 LDCM0236  AC119 HCT 116 C219(1.10)  LDD0553  [12]
 LDCM0237  AC12 HCT 116 C219(0.88); C234(0.94); C287(0.94)  LDD0554  [12]
 LDCM0238  AC120 HCT 116 C219(0.94)  LDD0555  [12]
 LDCM0239  AC121 HCT 116 C219(0.75)  LDD0556  [12]
 LDCM0240  AC122 HCT 116 C219(0.92)  LDD0557  [12]
 LDCM0241  AC123 HCT 116 C219(0.69)  LDD0558  [12]
 LDCM0242  AC124 HCT 116 C219(0.82)  LDD0559  [12]
 LDCM0243  AC125 HCT 116 C219(0.95)  LDD0560  [12]
 LDCM0244  AC126 HCT 116 C219(0.89)  LDD0561  [12]
 LDCM0245  AC127 HCT 116 C219(0.84)  LDD0562  [12]
 LDCM0246  AC128 HEK-293T C234(0.91); C287(1.39)  LDD0844  [12]
 LDCM0247  AC129 HEK-293T C234(0.86); C287(1.26)  LDD0845  [12]
 LDCM0249  AC130 HEK-293T C234(0.78); C287(1.47)  LDD0847  [12]
 LDCM0250  AC131 HEK-293T C234(0.87); C287(1.06)  LDD0848  [12]
 LDCM0251  AC132 HEK-293T C234(0.77); C287(1.44)  LDD0849  [12]
 LDCM0252  AC133 HEK-293T C234(0.83); C287(0.96)  LDD0850  [12]
 LDCM0253  AC134 HEK-293T C234(0.89); C287(1.15)  LDD0851  [12]
 LDCM0254  AC135 HEK-293T C234(0.95); C287(1.13)  LDD0852  [12]
 LDCM0255  AC136 HEK-293T C234(0.76); C287(0.93)  LDD0853  [12]
 LDCM0256  AC137 HEK-293T C234(0.81); C287(1.24)  LDD0854  [12]
 LDCM0257  AC138 HEK-293T C234(0.88); C287(1.65)  LDD0855  [12]
 LDCM0258  AC139 HEK-293T C234(0.86); C287(1.47)  LDD0856  [12]
 LDCM0259  AC14 HCT 116 C219(0.83); C234(0.79); C287(1.10)  LDD0576  [12]
 LDCM0260  AC140 HEK-293T C234(0.89); C287(1.39)  LDD0858  [12]
 LDCM0261  AC141 HEK-293T C234(1.02); C287(1.08)  LDD0859  [12]
 LDCM0262  AC142 HEK-293T C234(0.75); C287(1.17)  LDD0860  [12]
 LDCM0263  AC143 HCT 116 C234(0.92)  LDD0580  [12]
 LDCM0264  AC144 HCT 116 C234(1.17)  LDD0581  [12]
 LDCM0265  AC145 HCT 116 C234(0.99)  LDD0582  [12]
 LDCM0266  AC146 HCT 116 C234(0.86)  LDD0583  [12]
 LDCM0267  AC147 HCT 116 C234(0.74)  LDD0584  [12]
 LDCM0268  AC148 HCT 116 C234(0.83)  LDD0585  [12]
 LDCM0269  AC149 HCT 116 C234(0.69)  LDD0586  [12]
 LDCM0270  AC15 HCT 116 C219(0.91); C234(0.97); C287(1.15)  LDD0587  [12]
 LDCM0271  AC150 HCT 116 C234(0.77)  LDD0588  [12]
 LDCM0272  AC151 HCT 116 C234(1.17)  LDD0589  [12]
 LDCM0273  AC152 HCT 116 C234(0.74)  LDD0590  [12]
 LDCM0274  AC153 HCT 116 C234(0.90)  LDD0591  [12]
 LDCM0621  AC154 HCT 116 C234(0.86)  LDD2158  [12]
 LDCM0622  AC155 HCT 116 C234(1.04)  LDD2159  [12]
 LDCM0623  AC156 HCT 116 C234(0.87)  LDD2160  [12]
 LDCM0624  AC157 HCT 116 C234(0.84)  LDD2161  [12]
 LDCM0276  AC17 HCT 116 C234(1.27)  LDD0593  [12]
 LDCM0277  AC18 HCT 116 C234(1.13)  LDD0594  [12]
 LDCM0278  AC19 HCT 116 C234(1.39)  LDD0595  [12]
 LDCM0279  AC2 HCT 116 C234(0.85)  LDD0596  [12]
 LDCM0280  AC20 HCT 116 C234(1.22)  LDD0597  [12]
 LDCM0281  AC21 HCT 116 C234(1.20)  LDD0598  [12]
 LDCM0282  AC22 HCT 116 C234(1.22)  LDD0599  [12]
 LDCM0283  AC23 HCT 116 C234(1.19)  LDD0600  [12]
 LDCM0284  AC24 HCT 116 C234(1.21)  LDD0601  [12]
 LDCM0285  AC25 HCT 116 C234(0.89)  LDD0602  [12]
 LDCM0286  AC26 HCT 116 C234(0.89)  LDD0603  [12]
 LDCM0287  AC27 HCT 116 C234(0.87)  LDD0604  [12]
 LDCM0288  AC28 HCT 116 C234(0.84)  LDD0605  [12]
 LDCM0289  AC29 HCT 116 C234(0.88)  LDD0606  [12]
 LDCM0290  AC3 HCT 116 C234(1.01)  LDD0607  [12]
 LDCM0291  AC30 HCT 116 C234(0.90)  LDD0608  [12]
 LDCM0292  AC31 HCT 116 C234(0.83)  LDD0609  [12]
 LDCM0293  AC32 HCT 116 C234(0.91)  LDD0610  [12]
 LDCM0294  AC33 HCT 116 C234(0.92)  LDD0611  [12]
 LDCM0295  AC34 HCT 116 C234(0.94)  LDD0612  [12]
 LDCM0296  AC35 HCT 116 C219(1.00); C234(1.07)  LDD0613  [12]
 LDCM0297  AC36 HCT 116 C234(1.01); C219(1.18)  LDD0614  [12]
 LDCM0298  AC37 HCT 116 C234(0.96); C219(1.11)  LDD0615  [12]
 LDCM0299  AC38 HCT 116 C234(1.12); C219(1.16)  LDD0616  [12]
 LDCM0300  AC39 HCT 116 C234(0.88); C219(1.05)  LDD0617  [12]
 LDCM0301  AC4 HCT 116 C234(1.04)  LDD0618  [12]
 LDCM0302  AC40 HCT 116 C234(0.88); C219(1.43)  LDD0619  [12]
 LDCM0303  AC41 HCT 116 C234(1.00); C219(1.38)  LDD0620  [12]
 LDCM0304  AC42 HCT 116 C234(0.97); C219(1.33)  LDD0621  [12]
 LDCM0305  AC43 HCT 116 C234(0.89); C219(1.26)  LDD0622  [12]
 LDCM0306  AC44 HCT 116 C234(0.90); C219(1.33)  LDD0623  [12]
 LDCM0307  AC45 HCT 116 C234(0.78); C219(1.39)  LDD0624  [12]
 LDCM0308  AC46 HCT 116 C234(1.06); C219(1.18)  LDD0625  [12]
 LDCM0309  AC47 HCT 116 C234(1.01); C219(1.06)  LDD0626  [12]
 LDCM0310  AC48 HCT 116 C234(0.79); C219(1.04)  LDD0627  [12]
 LDCM0311  AC49 HCT 116 C234(1.05); C219(1.24)  LDD0628  [12]
 LDCM0312  AC5 HCT 116 C234(1.01)  LDD0629  [12]
 LDCM0313  AC50 HCT 116 C234(0.93); C219(1.31)  LDD0630  [12]
 LDCM0314  AC51 HCT 116 C234(0.98); C219(1.17)  LDD0631  [12]
 LDCM0315  AC52 HCT 116 C219(1.13); C234(1.18)  LDD0632  [12]
 LDCM0316  AC53 HCT 116 C234(0.97); C219(1.20)  LDD0633  [12]
 LDCM0317  AC54 HCT 116 C234(0.90); C219(1.12)  LDD0634  [12]
 LDCM0318  AC55 HCT 116 C234(0.99); C219(1.34)  LDD0635  [12]
 LDCM0319  AC56 HCT 116 C234(0.87); C219(1.26)  LDD0636  [12]
 LDCM0320  AC57 HCT 116 C234(0.99); C219(1.50)  LDD0637  [12]
 LDCM0321  AC58 HCT 116 C234(1.02); C219(1.92)  LDD0638  [12]
 LDCM0322  AC59 HCT 116 C234(0.84); C219(1.31)  LDD0639  [12]
 LDCM0323  AC6 HCT 116 C234(1.00); C219(1.04); C287(1.12)  LDD0640  [12]
 LDCM0324  AC60 HCT 116 C234(0.87); C219(1.63)  LDD0641  [12]
 LDCM0325  AC61 HCT 116 C234(1.01); C219(1.64)  LDD0642  [12]
 LDCM0326  AC62 HCT 116 C234(0.91); C219(1.85)  LDD0643  [12]
 LDCM0327  AC63 HCT 116 C234(0.93); C219(1.99)  LDD0644  [12]
 LDCM0328  AC64 HCT 116 C234(0.85); C219(1.83)  LDD0645  [12]
 LDCM0329  AC65 HCT 116 C234(0.99); C219(2.65)  LDD0646  [12]
 LDCM0330  AC66 HCT 116 C234(1.10); C219(2.30)  LDD0647  [12]
 LDCM0331  AC67 HCT 116 C234(0.83); C219(3.19)  LDD0648  [12]
 LDCM0332  AC68 HCT 116 C219(0.80); C234(0.96)  LDD0649  [12]
 LDCM0333  AC69 HCT 116 C219(0.70); C234(0.87)  LDD0650  [12]
 LDCM0334  AC7 HCT 116 C234(0.89); C287(0.92); C219(0.98)  LDD0651  [12]
 LDCM0335  AC70 HCT 116 C234(0.89); C219(0.93)  LDD0652  [12]
 LDCM0336  AC71 HCT 116 C219(0.86); C234(1.00)  LDD0653  [12]
 LDCM0337  AC72 HCT 116 C234(0.95); C219(1.17)  LDD0654  [12]
 LDCM0338  AC73 HCT 116 C234(0.91); C219(1.12)  LDD0655  [12]
 LDCM0339  AC74 HCT 116 C234(0.85); C219(0.92)  LDD0656  [12]
 LDCM0340  AC75 HCT 116 C234(0.82); C219(1.15)  LDD0657  [12]
 LDCM0341  AC76 HCT 116 C219(0.62); C234(0.92)  LDD0658  [12]
 LDCM0342  AC77 HCT 116 C234(0.87); C219(0.88)  LDD0659  [12]
 LDCM0343  AC78 HCT 116 C234(0.80); C219(0.89)  LDD0660  [12]
 LDCM0344  AC79 HCT 116 C219(0.86); C234(0.98)  LDD0661  [12]
 LDCM0345  AC8 HCT 116 C234(0.90); C219(0.91); C287(1.02)  LDD0662  [12]
 LDCM0346  AC80 HCT 116 C219(0.69); C234(0.96)  LDD0663  [12]
 LDCM0347  AC81 HCT 116 C234(0.88); C219(0.92)  LDD0664  [12]
 LDCM0348  AC82 HCT 116 C234(0.78); C219(0.85)  LDD0665  [12]
 LDCM0349  AC83 HCT 116 C234(1.03); C219(1.19)  LDD0666  [12]
 LDCM0350  AC84 HCT 116 C234(0.99); C219(1.21)  LDD0667  [12]
 LDCM0351  AC85 HCT 116 C234(0.97); C219(1.20)  LDD0668  [12]
 LDCM0352  AC86 HCT 116 C234(1.08); C219(1.13)  LDD0669  [12]
 LDCM0353  AC87 HCT 116 C234(0.98); C219(1.12)  LDD0670  [12]
 LDCM0354  AC88 HCT 116 C234(1.01); C219(1.15)  LDD0671  [12]
 LDCM0355  AC89 HCT 116 C234(1.06); C219(1.28)  LDD0672  [12]
 LDCM0357  AC90 HCT 116 C219(1.16); C234(1.16)  LDD0674  [12]
 LDCM0358  AC91 HCT 116 C234(1.02); C219(1.30)  LDD0675  [12]
 LDCM0359  AC92 HCT 116 C234(0.95); C219(1.30)  LDD0676  [12]
 LDCM0360  AC93 HCT 116 C234(1.00); C219(1.41)  LDD0677  [12]
 LDCM0361  AC94 HCT 116 C234(1.15); C219(1.90)  LDD0678  [12]
 LDCM0362  AC95 HCT 116 C234(0.99); C219(1.53)  LDD0679  [12]
 LDCM0363  AC96 HCT 116 C234(1.04); C219(1.73)  LDD0680  [12]
 LDCM0364  AC97 HCT 116 C234(0.87); C219(1.88)  LDD0681  [12]
 LDCM0365  AC98 HCT 116 C234(0.63); C219(2.17)  LDD0682  [12]
 LDCM0366  AC99 HCT 116 C234(0.75); C219(0.93)  LDD0683  [12]
 LDCM0248  AKOS034007472 HCT 116 C219(0.92); C234(1.09); C287(1.01)  LDD0565  [12]
 LDCM0356  AKOS034007680 HCT 116 C287(0.85); C234(0.86); C219(1.13)  LDD0673  [12]
 LDCM0275  AKOS034007705 HCT 116 C219(0.93); C234(0.93); C287(1.40)  LDD0592  [12]
 LDCM0156  Aniline NCI-H1299 11.61  LDD0403  [2]
 LDCM0020  ARS-1620 HCC44 C205(1.07)  LDD2171  [12]
 LDCM0199  BPK-21 T cell C287(9.60)  LDD0530  [13]
 LDCM0632  CL-Sc Hep-G2 C219(1.49); C287(1.24); C188(0.81); C234(0.55)  LDD2227  [10]
 LDCM0367  CL1 HCT 116 C234(1.05); C287(1.10)  LDD0684  [12]
 LDCM0368  CL10 HCT 116 C234(1.01); C287(1.10)  LDD0685  [12]
 LDCM0369  CL100 HCT 116 C234(0.96)  LDD0686  [12]
 LDCM0370  CL101 HCT 116 C219(0.82); C234(0.84); C287(1.07)  LDD0687  [12]
 LDCM0371  CL102 HCT 116 C287(0.94); C219(0.97); C234(1.02)  LDD0688  [12]
 LDCM0372  CL103 HCT 116 C287(0.83); C219(0.85); C234(0.88)  LDD0689  [12]
 LDCM0373  CL104 HCT 116 C219(0.88); C287(0.89); C234(0.91)  LDD0690  [12]
 LDCM0374  CL105 HCT 116 C234(1.09)  LDD0691  [12]
 LDCM0375  CL106 HCT 116 C234(0.91)  LDD0692  [12]
 LDCM0376  CL107 HCT 116 C234(1.19)  LDD0693  [12]
 LDCM0377  CL108 HCT 116 C234(1.02)  LDD0694  [12]
 LDCM0378  CL109 HCT 116 C234(1.04)  LDD0695  [12]
 LDCM0379  CL11 HCT 116 C287(0.85); C234(1.06)  LDD0696  [12]
 LDCM0380  CL110 HCT 116 C234(1.02)  LDD0697  [12]
 LDCM0381  CL111 HCT 116 C234(1.16)  LDD0698  [12]
 LDCM0382  CL112 HCT 116 C234(0.99)  LDD0699  [12]
 LDCM0383  CL113 HCT 116 C234(0.96)  LDD0700  [12]
 LDCM0384  CL114 HCT 116 C234(1.05)  LDD0701  [12]
 LDCM0385  CL115 HCT 116 C234(0.98)  LDD0702  [12]
 LDCM0386  CL116 HCT 116 C234(1.08)  LDD0703  [12]
 LDCM0387  CL117 HCT 116 C234(0.90); C219(1.71)  LDD0704  [12]
 LDCM0388  CL118 HCT 116 C234(0.92); C219(1.20)  LDD0705  [12]
 LDCM0389  CL119 HCT 116 C234(1.00); C219(1.17)  LDD0706  [12]
 LDCM0390  CL12 HCT 116 C234(1.08); C287(1.24)  LDD0707  [12]
 LDCM0391  CL120 HCT 116 C234(0.80); C219(1.23)  LDD0708  [12]
 LDCM0392  CL121 HCT 116 C234(0.75); C219(1.16)  LDD0709  [12]
 LDCM0393  CL122 HCT 116 C234(0.97); C219(1.16)  LDD0710  [12]
 LDCM0394  CL123 HCT 116 C234(1.04); C219(1.46)  LDD0711  [12]
 LDCM0395  CL124 HCT 116 C234(1.01); C219(1.25)  LDD0712  [12]
 LDCM0396  CL125 HCT 116 C234(0.92); C219(1.33)  LDD0713  [12]
 LDCM0397  CL126 HCT 116 C234(1.04); C219(1.59)  LDD0714  [12]
 LDCM0398  CL127 HCT 116 C234(0.80); C219(1.34)  LDD0715  [12]
 LDCM0399  CL128 HCT 116 C234(1.00); C219(1.51)  LDD0716  [12]
 LDCM0400  CL13 HCT 116 C234(0.96); C287(1.20)  LDD0717  [12]
 LDCM0401  CL14 HCT 116 C234(1.15); C287(1.29)  LDD0718  [12]
 LDCM0402  CL15 HCT 116 C234(1.15); C287(1.51)  LDD0719  [12]
 LDCM0403  CL16 HCT 116 C234(0.87); C219(1.34)  LDD0720  [12]
 LDCM0404  CL17 HCT 116 C234(0.64); C219(1.14)  LDD0721  [12]
 LDCM0405  CL18 HCT 116 C234(0.61); C219(0.96)  LDD0722  [12]
 LDCM0406  CL19 HCT 116 C234(0.51); C219(1.07)  LDD0723  [12]
 LDCM0407  CL2 HCT 116 C234(0.82); C287(1.10)  LDD0724  [12]
 LDCM0408  CL20 HCT 116 C234(0.67); C219(1.20)  LDD0725  [12]
 LDCM0409  CL21 HCT 116 C234(0.73); C219(1.22)  LDD0726  [12]
 LDCM0410  CL22 HCT 116 C234(0.64); C219(0.89)  LDD0727  [12]
 LDCM0411  CL23 HCT 116 C234(0.58); C219(1.10)  LDD0728  [12]
 LDCM0412  CL24 HCT 116 C234(0.63); C219(0.90)  LDD0729  [12]
 LDCM0413  CL25 HCT 116 C219(0.96); C234(0.58)  LDD0730  [12]
 LDCM0414  CL26 HCT 116 C219(0.97); C234(0.65)  LDD0731  [12]
 LDCM0415  CL27 HCT 116 C219(1.05); C234(0.88)  LDD0732  [12]
 LDCM0416  CL28 HCT 116 C219(1.02); C234(0.88)  LDD0733  [12]
 LDCM0417  CL29 HCT 116 C219(1.01); C234(0.77)  LDD0734  [12]
 LDCM0418  CL3 HCT 116 C234(1.01); C287(1.04)  LDD0735  [12]
 LDCM0419  CL30 HCT 116 C219(0.92); C234(0.98)  LDD0736  [12]
 LDCM0420  CL31 HCT 116 C219(1.10); C287(0.99)  LDD0737  [12]
 LDCM0421  CL32 HCT 116 C219(1.45); C234(0.88); C287(1.03)  LDD0738  [12]
 LDCM0422  CL33 HCT 116 C219(2.33); C234(0.90); C287(1.14)  LDD0739  [12]
 LDCM0423  CL34 HCT 116 C219(1.37); C234(0.93); C287(1.15)  LDD0740  [12]
 LDCM0424  CL35 HCT 116 C219(1.36); C234(1.09); C287(1.08)  LDD0741  [12]
 LDCM0425  CL36 HCT 116 C219(1.33); C234(1.04); C287(1.04)  LDD0742  [12]
 LDCM0426  CL37 HCT 116 C219(1.62); C234(1.08); C287(0.97)  LDD0743  [12]
 LDCM0428  CL39 HCT 116 C219(2.31); C234(1.07); C287(1.02)  LDD0745  [12]
 LDCM0429  CL4 HCT 116 C234(0.96); C287(1.07)  LDD0746  [12]
 LDCM0430  CL40 HCT 116 C219(1.81); C234(0.91); C287(1.00)  LDD0747  [12]
 LDCM0431  CL41 HCT 116 C219(1.55); C234(0.94); C287(1.16)  LDD0748  [12]
 LDCM0432  CL42 HCT 116 C219(2.06); C234(0.98); C287(1.06)  LDD0749  [12]
 LDCM0433  CL43 HCT 116 C219(1.84); C234(0.95); C287(1.11)  LDD0750  [12]
 LDCM0434  CL44 HCT 116 C219(1.69); C234(1.04); C287(1.05)  LDD0751  [12]
 LDCM0435  CL45 HCT 116 C219(1.61); C234(1.03); C287(2.68)  LDD0752  [12]
 LDCM0436  CL46 HCT 116 C219(1.29)  LDD0753  [12]
 LDCM0437  CL47 HCT 116 C219(1.56)  LDD0754  [12]
 LDCM0438  CL48 HCT 116 C219(1.46)  LDD0755  [12]
 LDCM0439  CL49 HCT 116 C219(1.62)  LDD0756  [12]
 LDCM0440  CL5 HCT 116 C234(0.81); C287(1.12)  LDD0757  [12]
 LDCM0441  CL50 HCT 116 C219(1.90)  LDD0758  [12]
 LDCM0442  CL51 HCT 116 C219(1.84)  LDD0759  [12]
 LDCM0443  CL52 HCT 116 C219(1.40)  LDD0760  [12]
 LDCM0444  CL53 HCT 116 C219(1.42)  LDD0761  [12]
 LDCM0445  CL54 HCT 116 C219(1.54)  LDD0762  [12]
 LDCM0446  CL55 HCT 116 C219(1.29)  LDD0763  [12]
 LDCM0447  CL56 HCT 116 C219(1.68)  LDD0764  [12]
 LDCM0448  CL57 HCT 116 C219(2.08)  LDD0765  [12]
 LDCM0449  CL58 HCT 116 C219(0.98)  LDD0766  [12]
 LDCM0450  CL59 HCT 116 C219(1.49)  LDD0767  [12]
 LDCM0451  CL6 HCT 116 C234(1.00); C287(1.12)  LDD0768  [12]
 LDCM0452  CL60 HCT 116 C219(1.38)  LDD0769  [12]
 LDCM0453  CL61 HCT 116 C219(1.23); C234(1.02)  LDD0770  [12]
 LDCM0454  CL62 HCT 116 C219(1.20); C234(0.92)  LDD0771  [12]
 LDCM0455  CL63 HCT 116 C219(1.25); C234(0.84)  LDD0772  [12]
 LDCM0456  CL64 HCT 116 C219(1.11); C234(0.93)  LDD0773  [12]
 LDCM0457  CL65 HCT 116 C219(1.08); C234(1.06)  LDD0774  [12]
 LDCM0458  CL66 HCT 116 C219(1.12); C234(0.98)  LDD0775  [12]
 LDCM0459  CL67 HCT 116 C219(1.01); C234(1.04)  LDD0776  [12]
 LDCM0460  CL68 HCT 116 C219(1.11); C234(1.05)  LDD0777  [12]
 LDCM0461  CL69 HCT 116 C219(1.29); C234(0.81)  LDD0778  [12]
 LDCM0462  CL7 HCT 116 C234(1.16); C287(1.34)  LDD0779  [12]
 LDCM0463  CL70 HCT 116 C219(1.07); C234(0.97)  LDD0780  [12]
 LDCM0464  CL71 HCT 116 C219(1.32); C234(1.01)  LDD0781  [12]
 LDCM0465  CL72 HCT 116 C219(1.17); C234(0.89)  LDD0782  [12]
 LDCM0466  CL73 HCT 116 C219(1.33); C234(0.93)  LDD0783  [12]
 LDCM0467  CL74 HCT 116 C219(1.07); C234(1.05)  LDD0784  [12]
 LDCM0469  CL76 HCT 116 C219(1.02); C234(1.02); C287(1.01)  LDD0786  [12]
 LDCM0470  CL77 HCT 116 C219(1.16); C234(1.11); C287(1.37)  LDD0787  [12]
 LDCM0471  CL78 HCT 116 C219(0.96); C234(1.05); C287(1.10)  LDD0788  [12]
 LDCM0472  CL79 HCT 116 C219(1.09); C234(1.01); C287(0.97)  LDD0789  [12]
 LDCM0473  CL8 HCT 116 C234(0.84); C287(1.06)  LDD0790  [12]
 LDCM0474  CL80 HCT 116 C219(1.01); C234(1.10); C287(1.36)  LDD0791  [12]
 LDCM0475  CL81 HCT 116 C219(1.11); C234(1.09); C287(0.98)  LDD0792  [12]
 LDCM0476  CL82 HCT 116 C219(0.98); C234(0.93); C287(1.07)  LDD0793  [12]
 LDCM0477  CL83 HCT 116 C219(1.00); C234(0.87); C287(1.21)  LDD0794  [12]
 LDCM0478  CL84 HCT 116 C219(0.91); C234(1.01); C287(1.42)  LDD0795  [12]
 LDCM0479  CL85 HCT 116 C219(0.96); C234(0.97); C287(1.05)  LDD0796  [12]
 LDCM0480  CL86 HCT 116 C219(0.79); C234(0.93); C287(1.26)  LDD0797  [12]
 LDCM0481  CL87 HCT 116 C219(0.92); C234(0.91); C287(1.02)  LDD0798  [12]
 LDCM0482  CL88 HCT 116 C219(0.86); C234(1.07); C287(1.12)  LDD0799  [12]
 LDCM0483  CL89 HCT 116 C219(0.80); C234(1.03); C287(0.88)  LDD0800  [12]
 LDCM0484  CL9 HCT 116 C234(0.91); C287(1.16)  LDD0801  [12]
 LDCM0485  CL90 HCT 116 C219(1.52); C234(1.05); C287(1.24)  LDD0802  [12]
 LDCM0486  CL91 HCT 116 C234(0.83)  LDD0803  [12]
 LDCM0487  CL92 HCT 116 C234(0.99)  LDD0804  [12]
 LDCM0488  CL93 HCT 116 C234(1.18)  LDD0805  [12]
 LDCM0489  CL94 HCT 116 C234(1.00)  LDD0806  [12]
 LDCM0490  CL95 HCT 116 C234(1.00)  LDD0807  [12]
 LDCM0491  CL96 HCT 116 C234(0.95)  LDD0808  [12]
 LDCM0492  CL97 HCT 116 C234(0.86)  LDD0809  [12]
 LDCM0493  CL98 HCT 116 C234(0.91)  LDD0810  [12]
 LDCM0494  CL99 HCT 116 C234(0.85)  LDD0811  [12]
 LDCM0495  E2913 HEK-293T C326(1.20); C310(0.96); C287(0.87); C343(0.93)  LDD1698  [14]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C234(1.97); C366(1.26)  LDD1702  [3]
 LDCM0572  Fragment10 Ramos C287(0.78)  LDD2189  [15]
 LDCM0573  Fragment11 Ramos C287(0.05)  LDD2190  [15]
 LDCM0574  Fragment12 Ramos C287(0.83)  LDD2191  [15]
 LDCM0575  Fragment13 Ramos C287(0.93)  LDD2192  [15]
 LDCM0576  Fragment14 Ramos C287(1.09)  LDD2193  [15]
 LDCM0580  Fragment21 Ramos C287(0.89)  LDD2195  [15]
 LDCM0582  Fragment23 Ramos C287(2.08)  LDD2196  [15]
 LDCM0578  Fragment27 Ramos C287(0.84)  LDD2197  [15]
 LDCM0586  Fragment28 Ramos C287(0.73)  LDD2198  [15]
 LDCM0588  Fragment30 Ramos C287(0.80)  LDD2199  [15]
 LDCM0589  Fragment31 Ramos C287(1.00)  LDD2200  [15]
 LDCM0590  Fragment32 Ramos C287(0.51)  LDD2201  [15]
 LDCM0468  Fragment33 HCT 116 C219(1.17); C234(0.93)  LDD0785  [12]
 LDCM0596  Fragment38 Ramos C287(0.95)  LDD2203  [15]
 LDCM0427  Fragment51 HCT 116 C219(1.49); C234(1.05); C287(0.97)  LDD0744  [12]
 LDCM0610  Fragment52 Ramos C287(1.04)  LDD2204  [15]
 LDCM0614  Fragment56 Ramos C287(0.80)  LDD2205  [15]
 LDCM0569  Fragment7 Ramos C287(0.76)  LDD2186  [15]
 LDCM0571  Fragment9 Ramos C287(1.24)  LDD2188  [15]
 LDCM0107  IAA HeLa N.A.  LDD0221  [9]
 LDCM0022  KB02 HEK-293T C326(0.94); C234(0.93); C310(0.96); C287(0.88)  LDD1492  [14]
 LDCM0023  KB03 Jurkat C219(5.18)  LDD0209  [4]
 LDCM0024  KB05 HMCB C287(2.49)  LDD3312  [16]
 LDCM0114  Len MM1.S 8.01  LDD0254  [11]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C366(0.63)  LDD2137  [3]
 LDCM0021  THZ1 HCT 116 C205(1.07)  LDD2173  [12]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Casein kinase I isoform alpha (CSNK1A1) CK1 Ser/Thr protein kinase family P48729
Serine/threonine-protein kinase PAK 5 (PAK5) STE Ser/Thr protein kinase family Q9P286
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Krueppel-like factor 11 (KLF11) Sp1 C2H2-type zinc-finger protein family O14901
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
DNA damage-binding protein 1 (DDB1) DDB1 family Q16531
Mitotic interactor and substrate of PLK1 (MISP) MISP family Q8IVT2
RNA-binding protein with multiple splicing (RBPMS) . Q93062

The Drug(s) Related To This Target

Approved
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Lenalidomide Small molecular drug DB00480
Pomalidomide Small molecular drug DB08910
Thalidomide Small molecular drug DB01041
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cc-220 Small molecular drug D01XVX
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cc-122 Small molecular drug D03QZJ

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
2 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
3 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
4 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
5 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
6 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
7 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
8 Multiplexed CuAAC Suzuki-Miyaura Labeling for Tandem Activity-Based Chemoproteomic Profiling. Anal Chem. 2021 Feb 2;93(4):2610-2618. doi: 10.1021/acs.analchem.0c04726. Epub 2021 Jan 20.
Mass spectrometry data entry: PXD022279
9 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
10 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
11 Development of Photolenalidomide for Cellular Target Identification. J Am Chem Soc. 2022 Jan 12;144(1):606-614. doi: 10.1021/jacs.1c11920. Epub 2022 Jan 3.
12 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
13 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
14 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402
15 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578
16 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840