Details of the Target

General Information of Target

Target ID LDTP03011
Target Name Casein kinase II subunit alpha' (CSNK2A2)
Gene Name CSNK2A2
Gene ID 1459
Synonyms
CK2A2; Casein kinase II subunit alpha'; CK II alpha'; EC 2.7.11.1
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MPGPAAGSRARVYAEVNSLRSREYWDYEAHVPSWGNQDDYQLVRKLGRGKYSEVFEAINI
TNNERVVVKILKPVKKKKIKREVKILENLRGGTNIIKLIDTVKDPVSKTPALVFEYINNT
DFKQLYQILTDFDIRFYMYELLKALDYCHSKGIMHRDVKPHNVMIDHQQKKLRLIDWGLA
EFYHPAQEYNVRVASRYFKGPELLVDYQMYDYSLDMWSLGCMLASMIFRREPFFHGQDNY
DQLVRIAKVLGTEELYGYLKKYHIDLDPHFNDILGQHSRKRWENFIHSENRHLVSPEALD
LLDKLLRYDHQQRLTAKEAMEHPYFYPVVKEQSQPCADNAVLSSGLTAAR
Target Type
Patented-recorded
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Ser/Thr protein kinase family, CK2 subfamily
Subcellular location
Nucleus
Function
Catalytic subunit of a constitutively active serine/threonine-protein kinase complex that phosphorylates a large number of substrates containing acidic residues C-terminal to the phosphorylated serine or threonine. Regulates numerous cellular processes, such as cell cycle progression, apoptosis and transcription, as well as viral infection. May act as a regulatory node which integrates and coordinates numerous signals leading to an appropriate cellular response. During mitosis, functions as a component of the p53/TP53-dependent spindle assembly checkpoint (SAC) that maintains cyclin-B-CDK1 activity and G2 arrest in response to spindle damage. Also required for p53/TP53-mediated apoptosis, phosphorylating 'Ser-392' of p53/TP53 following UV irradiation. Phosphorylates a number of DNA repair proteins in response to DNA damage, such as MDC1, RAD9A, RAD51 and HTATSF1, promoting their recruitment to DNA damage sites . Can also negatively regulate apoptosis. Phosphorylates the caspases CASP9 and CASP2 and the apoptotic regulator NOL3. Phosphorylation protects CASP9 from cleavage and activation by CASP8, and inhibits the dimerization of CASP2 and activation of CASP8. Regulates transcription by direct phosphorylation of RNA polymerases I, II, III and IV. Also phosphorylates and regulates numerous transcription factors including NF-kappa-B, STAT1, CREB1, IRF1, IRF2, ATF1, SRF, MAX, JUN, FOS, MYC and MYB. Phosphorylates Hsp90 and its co-chaperones FKBP4 and CDC37, which is essential for chaperone function. Regulates Wnt signaling by phosphorylating CTNNB1 and the transcription factor LEF1. Acts as an ectokinase that phosphorylates several extracellular proteins. During viral infection, phosphorylates various proteins involved in the viral life cycles of EBV, HSV, HBV, HCV, HIV, CMV and HPV.
TTD ID
T80526
Uniprot ID
P19784
DrugMap ID
TTR93NU
Ensemble ID
ENST00000262506.8
HGNC ID
HGNC:2459
ChEMBL ID
CHEMBL4070

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 28 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
TH211
 Probe Info  		Y308(20.00)  LDD0260  [2]
C-Sul
 Probe Info  		8.38  LDD0066  [3]
YN-1
 Probe Info  		100.00  LDD0444  [4]
ONAyne
 Probe Info  		K103(10.00)  LDD0275  [5]
BTD
 Probe Info  		C148(3.25)  LDD1700  [6]
D5yne
 Probe Info  		1.65  LDD0055  [7]
DA-P3
 Probe Info  		6.89  LDD0183  [8]
AHL-Pu-1
 Probe Info  		C336(2.26)  LDD0168  [9]
Acrolein
 Probe Info  		H263(0.00); C221(0.00)  LDD0222  [10]
DBIA
 Probe Info  		C336(0.95)  LDD0078  [11]
ATP probe
 Probe Info  		K248(0.00); K103(0.00); K260(0.00); K261(0.00)  LDD0199  [12]
4-Iodoacetamidophenylacetylene
 Probe Info  		C148(0.00); C336(0.00)  LDD0038  [13]
IA-alkyne
 Probe Info  		C148(0.00); C336(0.00)  LDD0036  [13]
Lodoacetamide azide
 Probe Info  		C148(0.00); C336(0.00)  LDD0037  [13]
IPM
 Probe Info  		N.A.  LDD0025  [14]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [14]
TFBX
 Probe Info  		N.A.  LDD0027  [14]
NHS
 Probe Info  		K103(0.00); K260(0.00)  LDD0010  [15]
PPMS
 Probe Info  		N.A.  LDD0008  [15]
SF
 Probe Info  		N.A.  LDD0028  [16]
STPyne
 Probe Info  		N.A.  LDD0009  [15]
Ox-W18
 Probe Info  		N.A.  LDD2175  [17]
1c-yne
 Probe Info  		N.A.  LDD0228  [18]
Methacrolein
 Probe Info  		N.A.  LDD0218  [10]
W1
 Probe Info  		C336(0.00); K103(0.00); S107(0.00)  LDD0236  [19]
NAIA_5
 Probe Info  		N.A.  LDD2223  [20]
HHS-465
 Probe Info  		N.A.  LDD2240  [21]
PAL-AfBPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe12
 Probe Info  		7.62  LDD0473  [22]
FFF probe13
 Probe Info  		15.61  LDD0475  [22]
FFF probe3
 Probe Info  		20.00  LDD0464  [22]
STS-1
 Probe Info  		N.A.  LDD0137  [23]
STS-2
 Probe Info  		N.A.  LDD0138  [23]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C148(1.15)  LDD2117  [6]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C148(1.49)  LDD2152  [6]
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C148(1.00)  LDD2103  [6]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C148(0.82)  LDD2132  [6]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C148(1.15)  LDD2131  [6]
 LDCM0025  4SU-RNA HEK-293T C336(2.26)  LDD0168  [9]
 LDCM0026  4SU-RNA+native RNA HEK-293T C336(2.04)  LDD0169  [9]
 LDCM0214  AC1 HCT 116 C336(1.17)  LDD0531  [11]
 LDCM0215  AC10 HCT 116 C336(1.17)  LDD0532  [11]
 LDCM0216  AC100 HCT 116 C336(1.04)  LDD0533  [11]
 LDCM0217  AC101 HCT 116 C336(1.00)  LDD0534  [11]
 LDCM0218  AC102 HCT 116 C336(1.04)  LDD0535  [11]
 LDCM0219  AC103 HCT 116 C336(1.22)  LDD0536  [11]
 LDCM0220  AC104 HCT 116 C336(1.06)  LDD0537  [11]
 LDCM0221  AC105 HCT 116 C336(1.10)  LDD0538  [11]
 LDCM0222  AC106 HCT 116 C336(1.14)  LDD0539  [11]
 LDCM0223  AC107 HCT 116 C336(0.91)  LDD0540  [11]
 LDCM0224  AC108 HCT 116 C336(0.91)  LDD0541  [11]
 LDCM0225  AC109 HCT 116 C336(0.80)  LDD0542  [11]
 LDCM0226  AC11 HCT 116 C336(1.17)  LDD0543  [11]
 LDCM0227  AC110 HCT 116 C336(0.93)  LDD0544  [11]
 LDCM0228  AC111 HCT 116 C336(0.96)  LDD0545  [11]
 LDCM0229  AC112 HCT 116 C336(0.93)  LDD0546  [11]
 LDCM0230  AC113 HCT 116 C336(1.07)  LDD0547  [11]
 LDCM0231  AC114 HCT 116 C336(1.07)  LDD0548  [11]
 LDCM0232  AC115 HCT 116 C336(1.35)  LDD0549  [11]
 LDCM0233  AC116 HCT 116 C336(1.33)  LDD0550  [11]
 LDCM0234  AC117 HCT 116 C336(1.25)  LDD0551  [11]
 LDCM0235  AC118 HCT 116 C336(1.12)  LDD0552  [11]
 LDCM0236  AC119 HCT 116 C336(1.21)  LDD0553  [11]
 LDCM0237  AC12 HCT 116 C336(0.95)  LDD0554  [11]
 LDCM0238  AC120 HCT 116 C336(1.25)  LDD0555  [11]
 LDCM0239  AC121 HCT 116 C336(1.16)  LDD0556  [11]
 LDCM0240  AC122 HCT 116 C336(1.20)  LDD0557  [11]
 LDCM0241  AC123 HCT 116 C336(1.15)  LDD0558  [11]
 LDCM0242  AC124 HCT 116 C336(1.10)  LDD0559  [11]
 LDCM0243  AC125 HCT 116 C336(1.00)  LDD0560  [11]
 LDCM0244  AC126 HCT 116 C336(1.28)  LDD0561  [11]
 LDCM0245  AC127 HCT 116 C336(1.29)  LDD0562  [11]
 LDCM0246  AC128 HCT 116 C336(1.01)  LDD0563  [11]
 LDCM0247  AC129 HCT 116 C336(0.97)  LDD0564  [11]
 LDCM0249  AC130 HCT 116 C336(1.30)  LDD0566  [11]
 LDCM0250  AC131 HCT 116 C336(0.92)  LDD0567  [11]
 LDCM0251  AC132 HCT 116 C336(1.10)  LDD0568  [11]
 LDCM0252  AC133 HCT 116 C336(1.08)  LDD0569  [11]
 LDCM0253  AC134 HCT 116 C336(1.26)  LDD0570  [11]
 LDCM0254  AC135 HCT 116 C336(1.24)  LDD0571  [11]
 LDCM0255  AC136 HCT 116 C336(1.36)  LDD0572  [11]
 LDCM0256  AC137 HCT 116 C336(1.36)  LDD0573  [11]
 LDCM0257  AC138 HCT 116 C336(1.49)  LDD0574  [11]
 LDCM0258  AC139 HCT 116 C336(1.38)  LDD0575  [11]
 LDCM0259  AC14 HCT 116 C336(1.08)  LDD0576  [11]
 LDCM0260  AC140 HCT 116 C336(1.78)  LDD0577  [11]
 LDCM0261  AC141 HCT 116 C336(1.36)  LDD0578  [11]
 LDCM0262  AC142 HCT 116 C336(1.12)  LDD0579  [11]
 LDCM0263  AC143 HCT 116 C336(1.16)  LDD0580  [11]
 LDCM0264  AC144 HCT 116 C336(1.20)  LDD0581  [11]
 LDCM0265  AC145 HCT 116 C336(1.23)  LDD0582  [11]
 LDCM0266  AC146 HCT 116 C336(1.36)  LDD0583  [11]
 LDCM0267  AC147 HCT 116 C336(1.33)  LDD0584  [11]
 LDCM0268  AC148 HCT 116 C336(1.54)  LDD0585  [11]
 LDCM0269  AC149 HCT 116 C336(1.49)  LDD0586  [11]
 LDCM0270  AC15 HCT 116 C336(1.13)  LDD0587  [11]
 LDCM0271  AC150 HCT 116 C336(1.12)  LDD0588  [11]
 LDCM0272  AC151 HCT 116 C336(1.19)  LDD0589  [11]
 LDCM0273  AC152 HCT 116 C336(1.40)  LDD0590  [11]
 LDCM0274  AC153 HCT 116 C336(1.67)  LDD0591  [11]
 LDCM0621  AC154 HCT 116 C336(1.21)  LDD2158  [11]
 LDCM0622  AC155 HCT 116 C336(1.31)  LDD2159  [11]
 LDCM0623  AC156 HCT 116 C336(1.04)  LDD2160  [11]
 LDCM0624  AC157 HCT 116 C336(1.01)  LDD2161  [11]
 LDCM0276  AC17 HCT 116 C336(1.10)  LDD0593  [11]
 LDCM0277  AC18 HCT 116 C336(1.49)  LDD0594  [11]
 LDCM0278  AC19 HCT 116 C336(1.14)  LDD0595  [11]
 LDCM0279  AC2 HCT 116 C336(1.06)  LDD0596  [11]
 LDCM0280  AC20 HCT 116 C336(1.13)  LDD0597  [11]
 LDCM0281  AC21 HCT 116 C336(1.14)  LDD0598  [11]
 LDCM0282  AC22 HCT 116 C336(1.05)  LDD0599  [11]
 LDCM0283  AC23 HCT 116 C336(1.04)  LDD0600  [11]
 LDCM0284  AC24 HCT 116 C336(1.07)  LDD0601  [11]
 LDCM0285  AC25 HCT 116 C336(1.04)  LDD0602  [11]
 LDCM0286  AC26 HCT 116 C336(1.13)  LDD0603  [11]
 LDCM0287  AC27 HCT 116 C336(1.17)  LDD0604  [11]
 LDCM0288  AC28 HCT 116 C336(1.30)  LDD0605  [11]
 LDCM0289  AC29 HCT 116 C336(1.27)  LDD0606  [11]
 LDCM0290  AC3 HCT 116 C336(0.99)  LDD0607  [11]
 LDCM0291  AC30 HCT 116 C336(1.35)  LDD0608  [11]
 LDCM0292  AC31 HCT 116 C336(1.16)  LDD0609  [11]
 LDCM0293  AC32 HCT 116 C336(1.52)  LDD0610  [11]
 LDCM0294  AC33 HCT 116 C336(1.25)  LDD0611  [11]
 LDCM0295  AC34 HCT 116 C336(1.39)  LDD0612  [11]
 LDCM0296  AC35 HCT 116 C336(0.88)  LDD0613  [11]
 LDCM0297  AC36 HCT 116 C336(0.96)  LDD0614  [11]
 LDCM0298  AC37 HCT 116 C336(0.89)  LDD0615  [11]
 LDCM0299  AC38 HCT 116 C336(0.98)  LDD0616  [11]
 LDCM0300  AC39 HCT 116 C336(1.11)  LDD0617  [11]
 LDCM0301  AC4 HCT 116 C336(1.12)  LDD0618  [11]
 LDCM0302  AC40 HCT 116 C336(1.07)  LDD0619  [11]
 LDCM0303  AC41 HCT 116 C336(1.02)  LDD0620  [11]
 LDCM0304  AC42 HCT 116 C336(1.05)  LDD0621  [11]
 LDCM0305  AC43 HCT 116 C336(1.13)  LDD0622  [11]
 LDCM0306  AC44 HCT 116 C336(1.12)  LDD0623  [11]
 LDCM0307  AC45 HCT 116 C336(1.15)  LDD0624  [11]
 LDCM0308  AC46 HCT 116 C336(1.13)  LDD0625  [11]
 LDCM0309  AC47 HCT 116 C336(1.09)  LDD0626  [11]
 LDCM0310  AC48 HCT 116 C336(1.17)  LDD0627  [11]
 LDCM0311  AC49 HCT 116 C336(1.46)  LDD0628  [11]
 LDCM0312  AC5 HCT 116 C336(1.07)  LDD0629  [11]
 LDCM0313  AC50 HCT 116 C336(1.51)  LDD0630  [11]
 LDCM0314  AC51 HCT 116 C336(0.99)  LDD0631  [11]
 LDCM0315  AC52 HCT 116 C336(1.04)  LDD0632  [11]
 LDCM0316  AC53 HCT 116 C336(1.19)  LDD0633  [11]
 LDCM0317  AC54 HCT 116 C336(1.17)  LDD0634  [11]
 LDCM0318  AC55 HCT 116 C336(1.41)  LDD0635  [11]
 LDCM0319  AC56 HCT 116 C336(1.74)  LDD0636  [11]
 LDCM0320  AC57 HCT 116 C336(1.36)  LDD0637  [11]
 LDCM0321  AC58 HCT 116 C336(1.39)  LDD0638  [11]
 LDCM0322  AC59 HCT 116 C336(1.58)  LDD0639  [11]
 LDCM0323  AC6 HCT 116 C336(1.18)  LDD0640  [11]
 LDCM0324  AC60 HCT 116 C336(1.41)  LDD0641  [11]
 LDCM0325  AC61 HCT 116 C336(1.24)  LDD0642  [11]
 LDCM0326  AC62 HCT 116 C336(1.43)  LDD0643  [11]
 LDCM0327  AC63 HCT 116 C336(1.28)  LDD0644  [11]
 LDCM0328  AC64 HCT 116 C336(1.47)  LDD0645  [11]
 LDCM0329  AC65 HCT 116 C336(1.53)  LDD0646  [11]
 LDCM0330  AC66 HCT 116 C336(1.43)  LDD0647  [11]
 LDCM0331  AC67 HCT 116 C336(1.61)  LDD0648  [11]
 LDCM0332  AC68 HCT 116 C336(1.11)  LDD0649  [11]
 LDCM0333  AC69 HCT 116 C336(1.08)  LDD0650  [11]
 LDCM0334  AC7 HCT 116 C336(1.01)  LDD0651  [11]
 LDCM0335  AC70 HCT 116 C336(1.13)  LDD0652  [11]
 LDCM0336  AC71 HCT 116 C336(0.94)  LDD0653  [11]
 LDCM0337  AC72 HCT 116 C336(1.12)  LDD0654  [11]
 LDCM0338  AC73 HCT 116 C336(1.48)  LDD0655  [11]
 LDCM0339  AC74 HCT 116 C336(1.35)  LDD0656  [11]
 LDCM0340  AC75 HCT 116 C336(1.43)  LDD0657  [11]
 LDCM0341  AC76 HCT 116 C336(1.15)  LDD0658  [11]
 LDCM0342  AC77 HCT 116 C336(1.15)  LDD0659  [11]
 LDCM0343  AC78 HCT 116 C336(1.05)  LDD0660  [11]
 LDCM0344  AC79 HCT 116 C336(1.08)  LDD0661  [11]
 LDCM0345  AC8 HCT 116 C336(1.21)  LDD0662  [11]
 LDCM0346  AC80 HCT 116 C336(1.05)  LDD0663  [11]
 LDCM0347  AC81 HCT 116 C336(1.04)  LDD0664  [11]
 LDCM0348  AC82 HCT 116 C336(1.47)  LDD0665  [11]
 LDCM0349  AC83 HCT 116 C336(1.55)  LDD0666  [11]
 LDCM0350  AC84 HCT 116 C336(1.65)  LDD0667  [11]
 LDCM0351  AC85 HCT 116 C336(1.15)  LDD0668  [11]
 LDCM0352  AC86 HCT 116 C336(1.15)  LDD0669  [11]
 LDCM0353  AC87 HCT 116 C336(1.03)  LDD0670  [11]
 LDCM0354  AC88 HCT 116 C336(1.06)  LDD0671  [11]
 LDCM0355  AC89 HCT 116 C336(1.09)  LDD0672  [11]
 LDCM0357  AC90 HCT 116 C336(1.01)  LDD0674  [11]
 LDCM0358  AC91 HCT 116 C336(1.68)  LDD0675  [11]
 LDCM0359  AC92 HCT 116 C336(1.38)  LDD0676  [11]
 LDCM0360  AC93 HCT 116 C336(1.09)  LDD0677  [11]
 LDCM0361  AC94 HCT 116 C336(1.13)  LDD0678  [11]
 LDCM0362  AC95 HCT 116 C336(1.10)  LDD0679  [11]
 LDCM0363  AC96 HCT 116 C336(1.19)  LDD0680  [11]
 LDCM0364  AC97 HCT 116 C336(1.29)  LDD0681  [11]
 LDCM0365  AC98 HCT 116 C336(1.41)  LDD0682  [11]
 LDCM0366  AC99 HCT 116 C336(0.98)  LDD0683  [11]
 LDCM0545  Acetamide MDA-MB-231 C148(0.56)  LDD2138  [6]
 LDCM0520  AKOS000195272 MDA-MB-231 C148(0.98)  LDD2113  [6]
 LDCM0248  AKOS034007472 HCT 116 C336(0.94)  LDD0565  [11]
 LDCM0356  AKOS034007680 HCT 116 C336(1.06)  LDD0673  [11]
 LDCM0275  AKOS034007705 HCT 116 C336(1.65)  LDD0592  [11]
 LDCM0156  Aniline NCI-H1299 15.00  LDD0403  [1]
 LDCM0020  ARS-1620 HCC44 C336(0.95)  LDD0078  [11]
 LDCM0498  BS-3668 MDA-MB-231 C148(0.57)  LDD2091  [6]
 LDCM0108  Chloroacetamide HeLa H263(0.00); C221(0.00)  LDD0222  [10]
 LDCM0367  CL1 HCT 116 C336(0.87)  LDD0684  [11]
 LDCM0368  CL10 HCT 116 C336(0.87)  LDD0685  [11]
 LDCM0369  CL100 HCT 116 C336(1.12)  LDD0686  [11]
 LDCM0370  CL101 HCT 116 C336(1.13)  LDD0687  [11]
 LDCM0371  CL102 HCT 116 C336(0.95)  LDD0688  [11]
 LDCM0372  CL103 HCT 116 C336(0.99)  LDD0689  [11]
 LDCM0373  CL104 HCT 116 C336(0.97)  LDD0690  [11]
 LDCM0374  CL105 HCT 116 C336(1.23)  LDD0691  [11]
 LDCM0375  CL106 HCT 116 C336(1.44)  LDD0692  [11]
 LDCM0376  CL107 HCT 116 C336(1.27)  LDD0693  [11]
 LDCM0377  CL108 HCT 116 C336(1.39)  LDD0694  [11]
 LDCM0378  CL109 HCT 116 C336(1.12)  LDD0695  [11]
 LDCM0379  CL11 HCT 116 C336(1.26)  LDD0696  [11]
 LDCM0380  CL110 HCT 116 C336(1.14)  LDD0697  [11]
 LDCM0381  CL111 HCT 116 C336(1.22)  LDD0698  [11]
 LDCM0382  CL112 HCT 116 C336(1.03)  LDD0699  [11]
 LDCM0383  CL113 HCT 116 C336(1.31)  LDD0700  [11]
 LDCM0384  CL114 HCT 116 C336(1.15)  LDD0701  [11]
 LDCM0385  CL115 HCT 116 C336(1.27)  LDD0702  [11]
 LDCM0386  CL116 HCT 116 C336(1.21)  LDD0703  [11]
 LDCM0387  CL117 HCT 116 C336(1.38)  LDD0704  [11]
 LDCM0388  CL118 HCT 116 C336(1.05)  LDD0705  [11]
 LDCM0389  CL119 HCT 116 C336(1.12)  LDD0706  [11]
 LDCM0390  CL12 HCT 116 C336(1.30)  LDD0707  [11]
 LDCM0391  CL120 HCT 116 C336(1.02)  LDD0708  [11]
 LDCM0392  CL121 HCT 116 C336(1.01)  LDD0709  [11]
 LDCM0393  CL122 HCT 116 C336(1.19)  LDD0710  [11]
 LDCM0394  CL123 HCT 116 C336(1.28)  LDD0711  [11]
 LDCM0395  CL124 HCT 116 C336(1.29)  LDD0712  [11]
 LDCM0396  CL125 HCT 116 C336(1.06)  LDD0713  [11]
 LDCM0397  CL126 HCT 116 C336(1.06)  LDD0714  [11]
 LDCM0398  CL127 HCT 116 C336(1.13)  LDD0715  [11]
 LDCM0399  CL128 HCT 116 C336(1.29)  LDD0716  [11]
 LDCM0400  CL13 HCT 116 C336(1.36)  LDD0717  [11]
 LDCM0401  CL14 HCT 116 C336(0.84)  LDD0718  [11]
 LDCM0402  CL15 HCT 116 C336(0.95)  LDD0719  [11]
 LDCM0403  CL16 HCT 116 C336(1.06)  LDD0720  [11]
 LDCM0404  CL17 HCT 116 C336(1.01)  LDD0721  [11]
 LDCM0405  CL18 HCT 116 C336(1.25)  LDD0722  [11]
 LDCM0406  CL19 HCT 116 C336(1.17)  LDD0723  [11]
 LDCM0407  CL2 HCT 116 C336(0.79)  LDD0724  [11]
 LDCM0408  CL20 HCT 116 C336(1.19)  LDD0725  [11]
 LDCM0409  CL21 HCT 116 C336(1.28)  LDD0726  [11]
 LDCM0410  CL22 HCT 116 C336(1.76)  LDD0727  [11]
 LDCM0411  CL23 HCT 116 C336(1.16)  LDD0728  [11]
 LDCM0412  CL24 HCT 116 C336(1.41)  LDD0729  [11]
 LDCM0413  CL25 HCT 116 C336(1.19)  LDD0730  [11]
 LDCM0414  CL26 HCT 116 C336(1.24)  LDD0731  [11]
 LDCM0415  CL27 HCT 116 C336(1.07)  LDD0732  [11]
 LDCM0416  CL28 HCT 116 C336(1.20)  LDD0733  [11]
 LDCM0417  CL29 HCT 116 C336(1.21)  LDD0734  [11]
 LDCM0418  CL3 HCT 116 C336(0.96)  LDD0735  [11]
 LDCM0419  CL30 HCT 116 C336(1.01)  LDD0736  [11]
 LDCM0420  CL31 HCT 116 C336(0.98)  LDD0737  [11]
 LDCM0421  CL32 HCT 116 C336(1.13)  LDD0738  [11]
 LDCM0422  CL33 HCT 116 C336(0.95)  LDD0739  [11]
 LDCM0423  CL34 HCT 116 C336(1.23)  LDD0740  [11]
 LDCM0424  CL35 HCT 116 C336(1.19)  LDD0741  [11]
 LDCM0425  CL36 HCT 116 C336(1.04)  LDD0742  [11]
 LDCM0426  CL37 HCT 116 C336(1.12)  LDD0743  [11]
 LDCM0428  CL39 HCT 116 C336(1.29)  LDD0745  [11]
 LDCM0429  CL4 HCT 116 C336(0.99)  LDD0746  [11]
 LDCM0430  CL40 HCT 116 C336(1.10)  LDD0747  [11]
 LDCM0431  CL41 HCT 116 C336(1.16)  LDD0748  [11]
 LDCM0432  CL42 HCT 116 C336(1.45)  LDD0749  [11]
 LDCM0433  CL43 HCT 116 C336(1.16)  LDD0750  [11]
 LDCM0434  CL44 HCT 116 C336(1.11)  LDD0751  [11]
 LDCM0435  CL45 HCT 116 C336(1.23)  LDD0752  [11]
 LDCM0436  CL46 HCT 116 C336(0.88)  LDD0753  [11]
 LDCM0437  CL47 HCT 116 C336(0.91)  LDD0754  [11]
 LDCM0438  CL48 HCT 116 C336(0.84)  LDD0755  [11]
 LDCM0439  CL49 HCT 116 C336(0.88)  LDD0756  [11]
 LDCM0440  CL5 HCT 116 C336(0.96)  LDD0757  [11]
 LDCM0441  CL50 HCT 116 C336(0.87)  LDD0758  [11]
 LDCM0442  CL51 HCT 116 C336(0.84)  LDD0759  [11]
 LDCM0443  CL52 HCT 116 C336(0.95)  LDD0760  [11]
 LDCM0444  CL53 HCT 116 C336(1.00)  LDD0761  [11]
 LDCM0445  CL54 HCT 116 C336(0.89)  LDD0762  [11]
 LDCM0446  CL55 HCT 116 C336(0.83)  LDD0763  [11]
 LDCM0447  CL56 HCT 116 C336(0.94)  LDD0764  [11]
 LDCM0448  CL57 HCT 116 C336(0.84)  LDD0765  [11]
 LDCM0449  CL58 HCT 116 C336(0.83)  LDD0766  [11]
 LDCM0450  CL59 HCT 116 C336(0.84)  LDD0767  [11]
 LDCM0451  CL6 HCT 116 C336(1.00)  LDD0768  [11]
 LDCM0452  CL60 HCT 116 C336(0.88)  LDD0769  [11]
 LDCM0453  CL61 HCT 116 C336(0.96)  LDD0770  [11]
 LDCM0454  CL62 HCT 116 C336(0.98)  LDD0771  [11]
 LDCM0455  CL63 HCT 116 C336(1.06)  LDD0772  [11]
 LDCM0456  CL64 HCT 116 C336(1.13)  LDD0773  [11]
 LDCM0457  CL65 HCT 116 C336(0.95)  LDD0774  [11]
 LDCM0458  CL66 HCT 116 C336(1.36)  LDD0775  [11]
 LDCM0459  CL67 HCT 116 C336(1.05)  LDD0776  [11]
 LDCM0460  CL68 HCT 116 C336(1.02)  LDD0777  [11]
 LDCM0461  CL69 HCT 116 C336(1.06)  LDD0778  [11]
 LDCM0462  CL7 HCT 116 C336(1.23)  LDD0779  [11]
 LDCM0463  CL70 HCT 116 C336(1.12)  LDD0780  [11]
 LDCM0464  CL71 HCT 116 C336(1.07)  LDD0781  [11]
 LDCM0465  CL72 HCT 116 C336(1.08)  LDD0782  [11]
 LDCM0466  CL73 HCT 116 C336(1.14)  LDD0783  [11]
 LDCM0467  CL74 HCT 116 C336(1.03)  LDD0784  [11]
 LDCM0469  CL76 HCT 116 C336(1.11)  LDD0786  [11]
 LDCM0470  CL77 HCT 116 C336(1.02)  LDD0787  [11]
 LDCM0471  CL78 HCT 116 C336(1.17)  LDD0788  [11]
 LDCM0472  CL79 HCT 116 C336(1.32)  LDD0789  [11]
 LDCM0473  CL8 HCT 116 C336(1.29)  LDD0790  [11]
 LDCM0474  CL80 HCT 116 C336(1.13)  LDD0791  [11]
 LDCM0475  CL81 HCT 116 C336(1.09)  LDD0792  [11]
 LDCM0476  CL82 HCT 116 C336(1.63)  LDD0793  [11]
 LDCM0477  CL83 HCT 116 C336(1.56)  LDD0794  [11]
 LDCM0478  CL84 HCT 116 C336(1.87)  LDD0795  [11]
 LDCM0479  CL85 HCT 116 C336(1.21)  LDD0796  [11]
 LDCM0480  CL86 HCT 116 C336(1.07)  LDD0797  [11]
 LDCM0481  CL87 HCT 116 C336(1.21)  LDD0798  [11]
 LDCM0482  CL88 HCT 116 C336(1.48)  LDD0799  [11]
 LDCM0483  CL89 HCT 116 C336(2.11)  LDD0800  [11]
 LDCM0484  CL9 HCT 116 C336(0.99)  LDD0801  [11]
 LDCM0485  CL90 HCT 116 C336(0.96)  LDD0802  [11]
 LDCM0486  CL91 HCT 116 C336(1.17)  LDD0803  [11]
 LDCM0487  CL92 HCT 116 C336(1.09)  LDD0804  [11]
 LDCM0488  CL93 HCT 116 C336(1.00)  LDD0805  [11]
 LDCM0489  CL94 HCT 116 C336(1.12)  LDD0806  [11]
 LDCM0490  CL95 HCT 116 C336(1.12)  LDD0807  [11]
 LDCM0491  CL96 HCT 116 C336(1.10)  LDD0808  [11]
 LDCM0492  CL97 HCT 116 C336(1.14)  LDD0809  [11]
 LDCM0493  CL98 HCT 116 C336(1.21)  LDD0810  [11]
 LDCM0494  CL99 HCT 116 C336(1.14)  LDD0811  [11]
 LDCM0634  CY-0357 Hep-G2 C336(50.00)  LDD2228  [20]
 LDCM0095  DC-LC3IN-D5 HeLa 1.65  LDD0055  [7]
 LDCM0495  E2913 HEK-293T C336(0.96); C148(0.89)  LDD1698  [24]
 LDCM0031  Epigallocatechin gallate HEK-293T 6.89  LDD0183  [8]
 LDCM0625  F8 Ramos C336(1.15)  LDD2187  [25]
 LDCM0572  Fragment10 Ramos C336(1.07)  LDD2189  [25]
 LDCM0574  Fragment12 Ramos C336(0.74)  LDD2191  [25]
 LDCM0575  Fragment13 Ramos C336(0.90)  LDD2192  [25]
 LDCM0576  Fragment14 Ramos C336(0.53)  LDD2193  [25]
 LDCM0579  Fragment20 Ramos C336(0.62)  LDD2194  [25]
 LDCM0580  Fragment21 Ramos C336(0.83)  LDD2195  [25]
 LDCM0582  Fragment23 Ramos C336(1.00)  LDD2196  [25]
 LDCM0578  Fragment27 Ramos C336(0.90)  LDD2197  [25]
 LDCM0586  Fragment28 Ramos C336(0.98)  LDD2198  [25]
 LDCM0588  Fragment30 Ramos C336(1.02)  LDD2199  [25]
 LDCM0589  Fragment31 Ramos C336(0.80)  LDD2200  [25]
 LDCM0590  Fragment32 Ramos C336(1.03)  LDD2201  [25]
 LDCM0468  Fragment33 HCT 116 C336(0.95)  LDD0785  [11]
 LDCM0596  Fragment38 Ramos C336(0.69)  LDD2203  [25]
 LDCM0566  Fragment4 Ramos C336(0.82)  LDD2184  [25]
 LDCM0427  Fragment51 HCT 116 C336(1.81)  LDD0744  [11]
 LDCM0610  Fragment52 Ramos C336(1.15)  LDD2204  [25]
 LDCM0614  Fragment56 Ramos C336(1.09)  LDD2205  [25]
 LDCM0569  Fragment7 Ramos C336(0.70)  LDD2186  [25]
 LDCM0571  Fragment9 Ramos C336(0.78)  LDD2188  [25]
 LDCM0022  KB02 HCT 116 C336(1.58)  LDD0080  [11]
 LDCM0023  KB03 HCT 116 C336(0.99)  LDD0081  [11]
 LDCM0024  KB05 HCT 116 C336(1.09)  LDD0082  [11]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C148(0.69)  LDD2121  [6]
 LDCM0109  NEM HeLa H263(0.00); H292(0.00)  LDD0223  [10]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C148(1.24)  LDD2093  [6]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C148(0.50)  LDD2096  [6]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C148(0.88); C336(0.87)  LDD2098  [6]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C148(1.89)  LDD2099  [6]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C148(0.98)  LDD2101  [6]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C148(1.17)  LDD2107  [6]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C148(0.68)  LDD2109  [6]
 LDCM0517  Nucleophilic fragment 21b MDA-MB-231 C148(0.74)  LDD2110  [6]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C148(1.42)  LDD2111  [6]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C148(0.47)  LDD2115  [6]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C148(0.75)  LDD2120  [6]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C148(0.96)  LDD2123  [6]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C148(0.93)  LDD2125  [6]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C148(1.13)  LDD2127  [6]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C148(0.90)  LDD2128  [6]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C148(1.19)  LDD2129  [6]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C148(0.72)  LDD2134  [6]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C148(1.82)  LDD2135  [6]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C148(1.44)  LDD2136  [6]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C148(1.02)  LDD2137  [6]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C148(3.25)  LDD1700  [6]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C148(1.23)  LDD2140  [6]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C148(0.93)  LDD2143  [6]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C148(2.03)  LDD2144  [6]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C148(1.20)  LDD2146  [6]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C148(0.69)  LDD2150  [6]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C336(1.24)  LDD2153  [6]
 LDCM0627  NUDT7-COV-1 HEK-293T C336(1.06)  LDD2206  [26]
 LDCM0628  OTUB2-COV-1 HEK-293T C336(0.83)  LDD2207  [26]
 LDCM0131  RA190 MM1.R C336(1.06)  LDD0304  [27]
 LDCM0021  THZ1 HCT 116 C336(1.22); C148(0.93)  LDD2173  [11]
 LDCM0111  W14 Hep-G2 R107(0.52)  LDD0238  [19]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Casein kinase II subunit beta (CSNK2B) Casein kinase 2 subunit beta family P67870
Casein kinase II subunit alpha (CSNK2A1) Ser/Thr protein kinase family P68400
Kinesin heavy chain isoform 5C (KIF5C) Kinesin family O60282
E3 ubiquitin-protein ligase TRIM41 (TRIM41) TRIM/RBCC family Q8WV44
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Zinc finger protein 670 (ZNF670) Krueppel C2H2-type zinc-finger protein family Q9BS34
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
PRKCA-binding protein (PICK1) . Q9NRD5

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010
Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid22115617c2c Small molecular drug D0K6BI
[1-(6-{6-[(1-methylethyl)Amino]-1h-indazol-1-yl}Pyrazin-2-yl)-1h-pyrrol-3-yl]Acetic Acid . DB07546
Patented
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Us8791257, 17 Small molecular drug D0NM6I
Us8791257, 38 Small molecular drug D0E7ZS
Us8791257, 4 Small molecular drug D0H6DS
Us8940736, 23 Small molecular drug D0D2CR
Us8940736, 6 Small molecular drug D01QPX
Us8940736, 7 Small molecular drug D0XY1Z

References

1 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.
2 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
3 Low-Toxicity Sulfonium-Based Probes for Cysteine-Specific Profiling in Live Cells. Anal Chem. 2022 Mar 15;94(10):4366-4372. doi: 10.1021/acs.analchem.1c05129. Epub 2022 Mar 4.
4 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
5 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
6 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
7 Inhibition of Autophagy by a Small Molecule through Covalent Modification of the LC3 Protein. Angew Chem Int Ed Engl. 2021 Dec 6;60(50):26105-26114. doi: 10.1002/anie.202109464. Epub 2021 Nov 5.
Mass spectrometry data entry: PXD026874
8 A chemical probe unravels the reactive proteome of health-associated catechols. Chem Sci. 2023 Jul 22;14(32):8635-8643. doi: 10.1039/d3sc00888f. eCollection 2023 Aug 16.
Mass spectrometry data entry: PXD043348
9 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
10 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.
11 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.
12 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
13 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
14 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
15 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
16 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
17 Oxidative cyclization reagents reveal tryptophan cation- interactions. Nature. 2024 Mar;627(8004):680-687. doi: 10.1038/s41586-024-07140-6. Epub 2024 Mar 6.
Mass spectrometry data entry: PXD001377 , PXD005252
18 Tunable Amine-Reactive Electrophiles for Selective Profiling of Lysine. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202112107. doi: 10.1002/anie.202112107. Epub 2021 Dec 16.
19 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
20 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
21 Global profiling identifies a stress-responsive tyrosine site on EDC3 regulating biomolecular condensate formation. Cell Chem Biol. 2022 Dec 15;29(12):1709-1720.e7. doi: 10.1016/j.chembiol.2022.11.008. Epub 2022 Dec 6.
Mass spectrometry data entry: PXD038010
22 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
23 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.
24 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
25 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
26 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.
27 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.