Details of the Target

General Information of Target

Target ID LDTP01754
Target Name Serine/threonine-protein kinase Chk2 (CHEK2)
Gene Name CHEK2
Gene ID 11200
Synonyms
CDS1; CHK2; RAD53; Serine/threonine-protein kinase Chk2; EC 2.7.11.1; CHK2 checkpoint homolog; Cds1 homolog; Hucds1; hCds1; Checkpoint kinase 2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSRESDVEAQQSHGSSACSQPHGSVTQSQGSSSQSQGISSSSTSTMPNSSQSSHSSSGTL
SSLETVSTQELYSIPEDQEPEDQEPEEPTPAPWARLWALQDGFANLECVNDNYWFGRDKS
CEYCFDEPLLKRTDKYRTYSKKHFRIFREVGPKNSYIAYIEDHSGNGTFVNTELVGKGKR
RPLNNNSEIALSLSRNKVFVFFDLTVDDQSVYPKALRDEYIMSKTLGSGACGEVKLAFER
KTCKKVAIKIISKRKFAIGSAREADPALNVETEIEILKKLNHPCIIKIKNFFDAEDYYIV
LELMEGGELFDKVVGNKRLKEATCKLYFYQMLLAVQYLHENGIIHRDLKPENVLLSSQEE
DCLIKITDFGHSKILGETSLMRTLCGTPTYLAPEVLVSVGTAGYNRAVDCWSLGVILFIC
LSGYPPFSEHRTQVSLKDQITSGKYNFIPEVWAEVSEKALDLVKKLLVVDPKARFTTEEA
LRHPWLQDEDMKRKFQDLLSEENESTALPQVLAQPSTSRKRPREGEAEGAETTKRPAVCA
AVL
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CAMK Ser/Thr protein kinase family, CHK2 subfamily
Subcellular location
Nucleus; Nucleus, PML body
Function
Serine/threonine-protein kinase which is required for checkpoint-mediated cell cycle arrest, activation of DNA repair and apoptosis in response to the presence of DNA double-strand breaks. May also negatively regulate cell cycle progression during unperturbed cell cycles. Following activation, phosphorylates numerous effectors preferentially at the consensus sequence [L-X-R-X-X-S/T]. Regulates cell cycle checkpoint arrest through phosphorylation of CDC25A, CDC25B and CDC25C, inhibiting their activity. Inhibition of CDC25 phosphatase activity leads to increased inhibitory tyrosine phosphorylation of CDK-cyclin complexes and blocks cell cycle progression. May also phosphorylate NEK6 which is involved in G2/M cell cycle arrest. Regulates DNA repair through phosphorylation of BRCA2, enhancing the association of RAD51 with chromatin which promotes DNA repair by homologous recombination. Also stimulates the transcription of genes involved in DNA repair (including BRCA2) through the phosphorylation and activation of the transcription factor FOXM1. Regulates apoptosis through the phosphorylation of p53/TP53, MDM4 and PML. Phosphorylation of p53/TP53 at 'Ser-20' by CHEK2 may alleviate inhibition by MDM2, leading to accumulation of active p53/TP53. Phosphorylation of MDM4 may also reduce degradation of p53/TP53. Also controls the transcription of pro-apoptotic genes through phosphorylation of the transcription factor E2F1. Tumor suppressor, it may also have a DNA damage-independent function in mitotic spindle assembly by phosphorylating BRCA1. Its absence may be a cause of the chromosomal instability observed in some cancer cells. Promotes the CCAR2-SIRT1 association and is required for CCAR2-mediated SIRT1 inhibition.; (Microbial infection) Phosphorylates herpes simplex virus 1/HHV-1 protein ICP0 and thus activates its SUMO-targeted ubiquitin ligase activity.
TTD ID
T28713
Uniprot ID
O96017
DrugMap ID
TT9ABMF
Ensemble ID
ENST00000348295.7
HGNC ID
HGNC:16627
ChEMBL ID
CHEMBL2527

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
C32 Deletion: p.S422VfsTer15 .
CCK81 Deletion: p.R132EfsTer29
SNV: p.S164N		 .
HCT116 SNV: p.L355P .
HCT15 SNV: p.A247D DBIA    Probe Info 
HT115 SNV: p.N290T DBIA    Probe Info 
JEKO1 SNV: p.V175A .
LNCaP clone FGC SNV: p.T387N .

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
m-APA
 Probe Info  		15.00  LDD0402  [1]
TH216
 Probe Info  		Y404(19.19)  LDD0259  [2]
BTD
 Probe Info  		C539(1.20)  LDD2103  [3]
DBIA
 Probe Info  		C362(4.99); C231(22.30); C539(10.14); C121(26.41)  LDD0209  [4]
ATP probe
 Probe Info  		K349(0.00); K373(0.00); K131(0.00)  LDD0199  [5]
4-Iodoacetamidophenylacetylene
 Probe Info  		C362(0.00); C108(0.00); C385(0.00); C231(0.00)  LDD0038  [6]
IA-alkyne
 Probe Info  		C362(0.00); C284(0.00); C108(0.00); C231(0.00)  LDD0036  [6]
Lodoacetamide azide
 Probe Info  		C362(0.00); C284(0.00); C108(0.00); C539(0.00)  LDD0037  [6]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [7]
TFBX
 Probe Info  		N.A.  LDD0027  [7]
IPM
 Probe Info  		N.A.  LDD0005  [8]
Phosphinate-6
 Probe Info  		C539(0.00); C231(0.00)  LDD0018  [9]
1c-yne
 Probe Info  		N.A.  LDD0228  [10]
AOyne
 Probe Info  		15.00  LDD0443  [11]
NAIA_5
 Probe Info  		C539(0.00); C108(0.00); C385(0.00)  LDD2223  [12]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C539(1.20)  LDD2103  [3]
 LDCM0214  AC1 HEK-293T C284(0.82)  LDD0812  [13]
 LDCM0215  AC10 PaTu 8988t C231(2.00)  LDD1094  [13]
 LDCM0216  AC100 HEK-293T C124(0.70); C284(0.65)  LDD0814  [13]
 LDCM0217  AC101 HEK-293T C124(0.87); C284(0.81)  LDD0815  [13]
 LDCM0218  AC102 HEK-293T C124(0.71); C284(0.66)  LDD0816  [13]
 LDCM0219  AC103 HEK-293T C124(0.59); C284(0.53)  LDD0817  [13]
 LDCM0220  AC104 HEK-293T C124(0.57); C284(0.62)  LDD0818  [13]
 LDCM0221  AC105 HEK-293T C124(3.21); C284(1.15)  LDD0819  [13]
 LDCM0222  AC106 HEK-293T C124(3.67); C284(1.40)  LDD0820  [13]
 LDCM0223  AC107 HEK-293T C124(0.59); C284(0.65)  LDD0821  [13]
 LDCM0224  AC108 HEK-293T C124(1.71); C284(1.44)  LDD0822  [13]
 LDCM0225  AC109 HEK-293T C124(1.05); C284(1.05)  LDD0823  [13]
 LDCM0226  AC11 PaTu 8988t C231(1.74)  LDD1105  [13]
 LDCM0227  AC110 HEK-293T C124(0.68); C284(0.41)  LDD0825  [13]
 LDCM0228  AC111 HEK-293T C124(1.06); C284(0.55)  LDD0826  [13]
 LDCM0229  AC112 HEK-293T C124(0.82); C284(0.44)  LDD0827  [13]
 LDCM0230  AC113 HEK-293T C108(1.18); C284(1.04)  LDD0828  [13]
 LDCM0231  AC114 HEK-293T C108(1.00); C284(0.91)  LDD0829  [13]
 LDCM0232  AC115 HEK-293T C108(0.98); C284(0.98)  LDD0830  [13]
 LDCM0233  AC116 HEK-293T C108(0.99); C284(0.94)  LDD0831  [13]
 LDCM0234  AC117 HEK-293T C108(1.01); C284(0.64)  LDD0832  [13]
 LDCM0235  AC118 HEK-293T C108(0.98); C284(0.56)  LDD0833  [13]
 LDCM0236  AC119 HEK-293T C108(1.02); C284(0.52)  LDD0834  [13]
 LDCM0237  AC12 PaTu 8988t C231(1.60)  LDD1116  [13]
 LDCM0238  AC120 HEK-293T C108(1.14); C284(0.69)  LDD0836  [13]
 LDCM0239  AC121 HEK-293T C108(1.04); C284(0.50)  LDD0837  [13]
 LDCM0240  AC122 HEK-293T C108(1.16); C284(0.42)  LDD0838  [13]
 LDCM0241  AC123 HEK-293T C108(1.17); C284(0.40)  LDD0839  [13]
 LDCM0242  AC124 HEK-293T C108(1.02); C284(0.49)  LDD0840  [13]
 LDCM0243  AC125 HEK-293T C108(1.27); C284(0.42)  LDD0841  [13]
 LDCM0244  AC126 HEK-293T C108(1.43); C284(0.45)  LDD0842  [13]
 LDCM0245  AC127 HEK-293T C108(1.51); C284(0.49)  LDD0843  [13]
 LDCM0246  AC128 HEK-293T C121(0.55); C284(1.32)  LDD0844  [13]
 LDCM0247  AC129 HEK-293T C121(1.35); C284(0.66)  LDD0845  [13]
 LDCM0249  AC130 HEK-293T C121(0.66); C284(0.71)  LDD0847  [13]
 LDCM0250  AC131 HEK-293T C121(0.88); C284(1.43)  LDD0848  [13]
 LDCM0251  AC132 HEK-293T C121(0.83); C284(1.10)  LDD0849  [13]
 LDCM0252  AC133 HEK-293T C121(0.62); C284(0.48)  LDD0850  [13]
 LDCM0253  AC134 HEK-293T C121(0.71); C284(0.62)  LDD0851  [13]
 LDCM0254  AC135 HEK-293T C121(0.62); C284(0.81)  LDD0852  [13]
 LDCM0255  AC136 HEK-293T C121(0.86); C284(0.68)  LDD0853  [13]
 LDCM0256  AC137 HEK-293T C121(0.49); C284(0.38)  LDD0854  [13]
 LDCM0257  AC138 HEK-293T C121(0.58); C284(0.39)  LDD0855  [13]
 LDCM0258  AC139 HEK-293T C121(0.63); C284(0.41)  LDD0856  [13]
 LDCM0259  AC14 PaTu 8988t C231(1.59)  LDD1138  [13]
 LDCM0260  AC140 HEK-293T C121(0.43); C284(0.54)  LDD0858  [13]
 LDCM0261  AC141 HEK-293T C121(0.51); C284(0.38)  LDD0859  [13]
 LDCM0262  AC142 HEK-293T C121(0.73); C284(0.51)  LDD0860  [13]
 LDCM0263  AC143 HEK-293T C108(1.14); C284(1.25)  LDD0861  [13]
 LDCM0264  AC144 HEK-293T C108(1.25); C284(0.32)  LDD0862  [13]
 LDCM0265  AC145 HEK-293T C108(1.11); C284(0.34)  LDD0863  [13]
 LDCM0266  AC146 HEK-293T C108(1.32); C284(0.32)  LDD0864  [13]
 LDCM0267  AC147 HEK-293T C108(1.31); C284(0.36)  LDD0865  [13]
 LDCM0268  AC148 HEK-293T C108(1.30); C284(0.46)  LDD0866  [13]
 LDCM0269  AC149 HEK-293T C108(0.96); C284(0.94)  LDD0867  [13]
 LDCM0270  AC15 PaTu 8988t C231(1.78)  LDD1149  [13]
 LDCM0271  AC150 HEK-293T C108(1.28); C284(0.47)  LDD0869  [13]
 LDCM0272  AC151 HEK-293T C108(1.15); C284(0.38)  LDD0870  [13]
 LDCM0273  AC152 HEK-293T C108(1.31); C284(0.71)  LDD0871  [13]
 LDCM0274  AC153 HEK-293T C108(1.11); C284(0.41)  LDD0872  [13]
 LDCM0621  AC154 HEK-293T C108(0.94); C284(0.66)  LDD2162  [13]
 LDCM0622  AC155 HEK-293T C108(1.12); C284(0.71)  LDD2163  [13]
 LDCM0623  AC156 HEK-293T C108(1.43); C284(0.35)  LDD2164  [13]
 LDCM0624  AC157 HEK-293T C108(2.02); C284(0.39)  LDD2165  [13]
 LDCM0276  AC17 HEK-293T C284(0.36)  LDD0874  [13]
 LDCM0277  AC18 HEK-293T C284(0.80)  LDD0875  [13]
 LDCM0278  AC19 HEK-293T C284(0.89)  LDD0876  [13]
 LDCM0279  AC2 HEK-293T C284(0.80)  LDD0877  [13]
 LDCM0280  AC20 HEK-293T C284(0.59)  LDD0878  [13]
 LDCM0281  AC21 HEK-293T C284(0.80)  LDD0879  [13]
 LDCM0282  AC22 HEK-293T C284(0.63)  LDD0880  [13]
 LDCM0283  AC23 HEK-293T C284(0.39)  LDD0881  [13]
 LDCM0284  AC24 HEK-293T C284(0.76)  LDD0882  [13]
 LDCM0285  AC25 HEK-293T C284(0.82)  LDD0883  [13]
 LDCM0286  AC26 HEK-293T C284(0.76)  LDD0884  [13]
 LDCM0287  AC27 HEK-293T C284(0.74)  LDD0885  [13]
 LDCM0288  AC28 HEK-293T C284(0.72)  LDD0886  [13]
 LDCM0289  AC29 HEK-293T C284(0.91)  LDD0887  [13]
 LDCM0290  AC3 HEK-293T C284(1.34)  LDD0888  [13]
 LDCM0291  AC30 HEK-293T C284(0.97)  LDD0889  [13]
 LDCM0292  AC31 HEK-293T C284(0.81)  LDD0890  [13]
 LDCM0293  AC32 HEK-293T C284(0.97)  LDD0891  [13]
 LDCM0294  AC33 HEK-293T C284(0.87)  LDD0892  [13]
 LDCM0295  AC34 HEK-293T C284(0.84)  LDD0893  [13]
 LDCM0296  AC35 PaTu 8988t C231(1.20)  LDD1175  [13]
 LDCM0297  AC36 PaTu 8988t C231(1.31)  LDD1176  [13]
 LDCM0298  AC37 PaTu 8988t C231(1.75)  LDD1177  [13]
 LDCM0299  AC38 PaTu 8988t C231(1.59)  LDD1178  [13]
 LDCM0300  AC39 PaTu 8988t C231(1.53)  LDD1179  [13]
 LDCM0301  AC4 HEK-293T C284(1.16)  LDD0899  [13]
 LDCM0302  AC40 PaTu 8988t C231(2.11)  LDD1181  [13]
 LDCM0303  AC41 PaTu 8988t C231(1.43)  LDD1182  [13]
 LDCM0304  AC42 PaTu 8988t C231(1.65)  LDD1183  [13]
 LDCM0305  AC43 PaTu 8988t C231(1.38)  LDD1184  [13]
 LDCM0306  AC44 PaTu 8988t C231(2.80)  LDD1185  [13]
 LDCM0307  AC45 PaTu 8988t C231(2.14)  LDD1186  [13]
 LDCM0308  AC46 HEK-293T C108(0.94); C284(1.18)  LDD0906  [13]
 LDCM0309  AC47 HEK-293T C108(1.14); C284(0.92)  LDD0907  [13]
 LDCM0310  AC48 HEK-293T C108(0.94); C284(0.88)  LDD0908  [13]
 LDCM0311  AC49 HEK-293T C108(1.15); C284(0.82)  LDD0909  [13]
 LDCM0312  AC5 HEK-293T C284(0.89)  LDD0910  [13]
 LDCM0313  AC50 HEK-293T C108(0.97); C284(0.90)  LDD0911  [13]
 LDCM0314  AC51 HEK-293T C108(0.94); C284(0.75)  LDD0912  [13]
 LDCM0315  AC52 HEK-293T C108(1.03); C284(0.79)  LDD0913  [13]
 LDCM0316  AC53 HEK-293T C108(0.98); C284(1.08)  LDD0914  [13]
 LDCM0317  AC54 HEK-293T C108(1.05); C284(0.89)  LDD0915  [13]
 LDCM0318  AC55 HEK-293T C108(1.15); C284(1.02)  LDD0916  [13]
 LDCM0319  AC56 HEK-293T C108(1.11); C284(1.00)  LDD0917  [13]
 LDCM0320  AC57 HEK-293T C121(1.14); C284(1.21)  LDD0918  [13]
 LDCM0321  AC58 HEK-293T C121(1.63); C284(1.04)  LDD0919  [13]
 LDCM0322  AC59 HEK-293T C121(0.99); C284(1.01)  LDD0920  [13]
 LDCM0323  AC6 PaTu 8988t C231(1.21)  LDD1202  [13]
 LDCM0324  AC60 HEK-293T C121(0.61); C284(0.75)  LDD0922  [13]
 LDCM0325  AC61 HEK-293T C121(0.40); C284(0.81)  LDD0923  [13]
 LDCM0326  AC62 HEK-293T C121(0.96); C284(0.98)  LDD0924  [13]
 LDCM0327  AC63 HEK-293T C121(0.43); C284(0.91)  LDD0925  [13]
 LDCM0328  AC64 HEK-293T C121(0.75); C284(1.05)  LDD0926  [13]
 LDCM0329  AC65 HEK-293T C121(0.32); C284(0.83)  LDD0927  [13]
 LDCM0330  AC66 HEK-293T C121(0.90); C284(0.97)  LDD0928  [13]
 LDCM0331  AC67 HEK-293T C121(0.53); C284(0.74)  LDD0929  [13]
 LDCM0332  AC68 PaTu 8988t C385(0.68); C231(0.70)  LDD1211  [13]
 LDCM0333  AC69 PaTu 8988t C385(1.00); C231(1.24)  LDD1212  [13]
 LDCM0334  AC7 PaTu 8988t C231(0.83)  LDD1213  [13]
 LDCM0335  AC70 PaTu 8988t C385(0.47); C231(0.75)  LDD1214  [13]
 LDCM0336  AC71 PaTu 8988t C385(0.49); C231(0.87)  LDD1215  [13]
 LDCM0337  AC72 PaTu 8988t C385(0.62); C231(0.70)  LDD1216  [13]
 LDCM0338  AC73 PaTu 8988t C385(0.74); C231(0.59)  LDD1217  [13]
 LDCM0339  AC74 PaTu 8988t C385(0.69); C231(0.65)  LDD1218  [13]
 LDCM0340  AC75 PaTu 8988t C385(1.05); C231(0.92)  LDD1219  [13]
 LDCM0341  AC76 PaTu 8988t C385(0.66); C231(0.56)  LDD1220  [13]
 LDCM0342  AC77 PaTu 8988t C385(0.60); C231(0.64)  LDD1221  [13]
 LDCM0343  AC78 PaTu 8988t C385(0.51); C231(0.60)  LDD1222  [13]
 LDCM0344  AC79 PaTu 8988t C385(0.80); C231(0.78)  LDD1223  [13]
 LDCM0345  AC8 PaTu 8988t C231(1.08)  LDD1224  [13]
 LDCM0346  AC80 PaTu 8988t C385(0.50); C231(0.64)  LDD1225  [13]
 LDCM0347  AC81 PaTu 8988t C385(0.78); C231(0.58)  LDD1226  [13]
 LDCM0348  AC82 PaTu 8988t C385(0.97); C231(0.58)  LDD1227  [13]
 LDCM0349  AC83 HEK-293T C284(0.88)  LDD0947  [13]
 LDCM0350  AC84 HEK-293T C284(0.49)  LDD0948  [13]
 LDCM0351  AC85 HEK-293T C284(0.72)  LDD0949  [13]
 LDCM0352  AC86 HEK-293T C284(0.77)  LDD0950  [13]
 LDCM0353  AC87 HEK-293T C284(0.76)  LDD0951  [13]
 LDCM0354  AC88 HEK-293T C284(0.43)  LDD0952  [13]
 LDCM0355  AC89 HEK-293T C284(0.35)  LDD0953  [13]
 LDCM0357  AC90 HEK-293T C284(0.41)  LDD0955  [13]
 LDCM0358  AC91 HEK-293T C284(0.48)  LDD0956  [13]
 LDCM0359  AC92 HEK-293T C284(0.59)  LDD0957  [13]
 LDCM0360  AC93 HEK-293T C284(0.46)  LDD0958  [13]
 LDCM0361  AC94 HEK-293T C284(0.32)  LDD0959  [13]
 LDCM0362  AC95 HEK-293T C284(0.43)  LDD0960  [13]
 LDCM0363  AC96 HEK-293T C284(0.73)  LDD0961  [13]
 LDCM0364  AC97 HEK-293T C284(0.23)  LDD0962  [13]
 LDCM0365  AC98 HEK-293T C124(1.12); C284(1.08)  LDD0963  [13]
 LDCM0366  AC99 HEK-293T C124(2.02); C284(1.23)  LDD0964  [13]
 LDCM0248  AKOS034007472 PaTu 8988t C231(2.00)  LDD1127  [13]
 LDCM0356  AKOS034007680 PaTu 8988t C231(1.41)  LDD1235  [13]
 LDCM0275  AKOS034007705 PaTu 8988t C231(1.45)  LDD1154  [13]
 LDCM0156  Aniline NCI-H1299 15.00  LDD0403  [1]
 LDCM0632  CL-Sc Hep-G2 C539(0.24)  LDD2227  [12]
 LDCM0367  CL1 HEK-293T C121(0.96); C124(0.92); C284(0.88)  LDD0965  [13]
 LDCM0368  CL10 HEK-293T C121(0.20); C124(0.25); C284(0.22)  LDD0966  [13]
 LDCM0369  CL100 HEK-293T C284(0.71)  LDD0967  [13]
 LDCM0370  CL101 PaTu 8988t C231(1.09)  LDD1249  [13]
 LDCM0371  CL102 PaTu 8988t C231(1.15)  LDD1250  [13]
 LDCM0372  CL103 PaTu 8988t C231(2.33)  LDD1251  [13]
 LDCM0373  CL104 PaTu 8988t C231(1.38)  LDD1252  [13]
 LDCM0374  CL105 HEK-293T C284(0.70)  LDD0972  [13]
 LDCM0375  CL106 HEK-293T C284(0.61)  LDD0973  [13]
 LDCM0376  CL107 HEK-293T C284(0.98)  LDD0974  [13]
 LDCM0377  CL108 HEK-293T C284(0.74)  LDD0975  [13]
 LDCM0378  CL109 HEK-293T C284(0.86)  LDD0976  [13]
 LDCM0379  CL11 HEK-293T C121(0.17); C124(0.24); C284(0.24)  LDD0977  [13]
 LDCM0380  CL110 HEK-293T C284(0.80)  LDD0978  [13]
 LDCM0381  CL111 HEK-293T C284(0.67)  LDD0979  [13]
 LDCM0382  CL112 HEK-293T C284(0.73)  LDD0980  [13]
 LDCM0383  CL113 HEK-293T C284(1.02)  LDD0981  [13]
 LDCM0384  CL114 HEK-293T C284(0.33)  LDD0982  [13]
 LDCM0385  CL115 HEK-293T C284(0.81)  LDD0983  [13]
 LDCM0386  CL116 HEK-293T C284(0.72)  LDD0984  [13]
 LDCM0387  CL117 PaTu 8988t C231(1.38)  LDD1266  [13]
 LDCM0388  CL118 PaTu 8988t C231(1.56)  LDD1267  [13]
 LDCM0389  CL119 PaTu 8988t C231(1.56)  LDD1268  [13]
 LDCM0390  CL12 HEK-293T C121(0.70); C124(0.93); C284(1.53)  LDD0988  [13]
 LDCM0391  CL120 PaTu 8988t C231(1.34)  LDD1270  [13]
 LDCM0392  CL121 HEK-293T C108(1.21); C284(1.00)  LDD0990  [13]
 LDCM0393  CL122 HEK-293T C108(1.23); C284(0.92)  LDD0991  [13]
 LDCM0394  CL123 HEK-293T C108(0.99); C284(0.89)  LDD0992  [13]
 LDCM0395  CL124 HEK-293T C108(1.03); C284(0.93)  LDD0993  [13]
 LDCM0396  CL125 HEK-293T C121(0.78); C284(1.00)  LDD0994  [13]
 LDCM0397  CL126 HEK-293T C121(1.22); C284(0.96)  LDD0995  [13]
 LDCM0398  CL127 HEK-293T C121(0.95); C284(1.05)  LDD0996  [13]
 LDCM0399  CL128 HEK-293T C121(1.27); C284(0.93)  LDD0997  [13]
 LDCM0400  CL13 HEK-293T C121(0.78); C124(0.77); C284(1.28)  LDD0998  [13]
 LDCM0401  CL14 HEK-293T C121(0.57); C124(0.74); C284(0.78)  LDD0999  [13]
 LDCM0402  CL15 HEK-293T C121(0.30); C124(0.35); C284(0.56)  LDD1000  [13]
 LDCM0403  CL16 HEK-293T C124(1.20); C284(1.22)  LDD1001  [13]
 LDCM0404  CL17 HEK-293T C124(1.03); C284(1.00)  LDD1002  [13]
 LDCM0405  CL18 HEK-293T C124(0.45); C284(0.73)  LDD1003  [13]
 LDCM0406  CL19 HEK-293T C124(0.56); C284(0.80)  LDD1004  [13]
 LDCM0407  CL2 HEK-293T C121(1.05); C124(0.86); C284(1.00)  LDD1005  [13]
 LDCM0408  CL20 HEK-293T C124(0.87); C284(1.07)  LDD1006  [13]
 LDCM0409  CL21 HEK-293T C124(0.39); C284(0.59)  LDD1007  [13]
 LDCM0410  CL22 HEK-293T C124(0.31); C284(0.59)  LDD1008  [13]
 LDCM0411  CL23 HEK-293T C124(0.97); C284(1.13)  LDD1009  [13]
 LDCM0412  CL24 HEK-293T C124(0.88); C284(1.19)  LDD1010  [13]
 LDCM0413  CL25 HEK-293T C124(0.67); C284(0.96)  LDD1011  [13]
 LDCM0414  CL26 HEK-293T C124(1.43); C284(1.56)  LDD1012  [13]
 LDCM0415  CL27 HEK-293T C124(0.75); C284(1.12)  LDD1013  [13]
 LDCM0416  CL28 HEK-293T C124(1.18); C284(1.09)  LDD1014  [13]
 LDCM0417  CL29 HEK-293T C124(0.99); C284(1.17)  LDD1015  [13]
 LDCM0418  CL3 HEK-293T C121(0.84); C124(0.77); C284(0.95)  LDD1016  [13]
 LDCM0419  CL30 HEK-293T C124(0.32); C284(0.42)  LDD1017  [13]
 LDCM0420  CL31 PaTu 8988t C385(1.57); C231(1.28)  LDD1299  [13]
 LDCM0421  CL32 PaTu 8988t C385(1.57); C231(1.77)  LDD1300  [13]
 LDCM0422  CL33 PaTu 8988t C385(1.49); C231(1.77)  LDD1301  [13]
 LDCM0423  CL34 PaTu 8988t C385(1.84); C231(1.90)  LDD1302  [13]
 LDCM0424  CL35 PaTu 8988t C231(1.90); C385(1.70)  LDD1303  [13]
 LDCM0425  CL36 PaTu 8988t C385(1.86); C231(2.02)  LDD1304  [13]
 LDCM0426  CL37 PaTu 8988t C385(1.76); C231(2.61)  LDD1305  [13]
 LDCM0428  CL39 PaTu 8988t C385(1.44); C231(1.76)  LDD1307  [13]
 LDCM0429  CL4 HEK-293T C121(0.66); C124(0.62); C284(1.00)  LDD1027  [13]
 LDCM0430  CL40 PaTu 8988t C385(1.31); C231(1.41)  LDD1309  [13]
 LDCM0431  CL41 PaTu 8988t C385(1.61); C231(1.90)  LDD1310  [13]
 LDCM0432  CL42 PaTu 8988t C385(2.15); C231(2.53)  LDD1311  [13]
 LDCM0433  CL43 PaTu 8988t C385(3.04); C231(3.45)  LDD1312  [13]
 LDCM0434  CL44 PaTu 8988t C385(1.85); C231(2.19)  LDD1313  [13]
 LDCM0435  CL45 PaTu 8988t C385(1.49); C231(1.62)  LDD1314  [13]
 LDCM0436  CL46 HEK-293T C124(0.34)  LDD1034  [13]
 LDCM0437  CL47 HEK-293T C124(0.70)  LDD1035  [13]
 LDCM0438  CL48 HEK-293T C124(0.86)  LDD1036  [13]
 LDCM0439  CL49 HEK-293T C124(0.55)  LDD1037  [13]
 LDCM0440  CL5 HEK-293T C121(0.45); C124(0.48); C284(0.88)  LDD1038  [13]
 LDCM0441  CL50 HEK-293T C124(0.25)  LDD1039  [13]
 LDCM0442  CL51 HEK-293T C124(0.44)  LDD1040  [13]
 LDCM0443  CL52 HEK-293T C124(2.22)  LDD1041  [13]
 LDCM0444  CL53 HEK-293T C124(1.52)  LDD1042  [13]
 LDCM0445  CL54 HEK-293T C124(0.65)  LDD1043  [13]
 LDCM0446  CL55 HEK-293T C124(0.40)  LDD1044  [13]
 LDCM0447  CL56 HEK-293T C124(1.06)  LDD1045  [13]
 LDCM0448  CL57 HEK-293T C124(0.73)  LDD1046  [13]
 LDCM0449  CL58 HEK-293T C124(0.71)  LDD1047  [13]
 LDCM0450  CL59 HEK-293T C124(0.26)  LDD1048  [13]
 LDCM0451  CL6 HEK-293T C121(0.64); C124(0.66); C284(0.92)  LDD1049  [13]
 LDCM0452  CL60 HEK-293T C124(0.24)  LDD1050  [13]
 LDCM0453  CL61 HEK-293T C121(1.11)  LDD1051  [13]
 LDCM0454  CL62 HEK-293T C121(1.02)  LDD1052  [13]
 LDCM0455  CL63 HEK-293T C121(0.57)  LDD1053  [13]
 LDCM0456  CL64 HEK-293T C121(1.22)  LDD1054  [13]
 LDCM0457  CL65 HEK-293T C121(0.81)  LDD1055  [13]
 LDCM0458  CL66 HEK-293T C121(1.01)  LDD1056  [13]
 LDCM0459  CL67 HEK-293T C121(0.93)  LDD1057  [13]
 LDCM0460  CL68 HEK-293T C121(0.80)  LDD1058  [13]
 LDCM0461  CL69 HEK-293T C121(1.05)  LDD1059  [13]
 LDCM0462  CL7 HEK-293T C121(0.24); C124(0.26); C284(0.56)  LDD1060  [13]
 LDCM0463  CL70 HEK-293T C121(0.93)  LDD1061  [13]
 LDCM0464  CL71 HEK-293T C121(0.60)  LDD1062  [13]
 LDCM0465  CL72 HEK-293T C121(0.80)  LDD1063  [13]
 LDCM0466  CL73 HEK-293T C121(0.52)  LDD1064  [13]
 LDCM0467  CL74 HEK-293T C121(0.20)  LDD1065  [13]
 LDCM0469  CL76 HEK-293T C108(1.07); C284(0.84)  LDD1067  [13]
 LDCM0470  CL77 HEK-293T C108(0.99); C284(0.67)  LDD1068  [13]
 LDCM0471  CL78 HEK-293T C108(1.16); C284(0.67)  LDD1069  [13]
 LDCM0472  CL79 HEK-293T C108(1.03); C284(0.53)  LDD1070  [13]
 LDCM0473  CL8 HEK-293T C121(0.19); C124(0.84); C284(1.91)  LDD1071  [13]
 LDCM0474  CL80 HEK-293T C108(1.16); C284(0.78)  LDD1072  [13]
 LDCM0475  CL81 HEK-293T C108(1.09); C284(0.61)  LDD1073  [13]
 LDCM0476  CL82 HEK-293T C108(0.98); C284(1.15)  LDD1074  [13]
 LDCM0477  CL83 HEK-293T C108(0.89); C284(1.21)  LDD1075  [13]
 LDCM0478  CL84 HEK-293T C108(1.08); C284(0.65)  LDD1076  [13]
 LDCM0479  CL85 HEK-293T C108(1.12); C284(0.73)  LDD1077  [13]
 LDCM0480  CL86 HEK-293T C108(1.09); C284(0.61)  LDD1078  [13]
 LDCM0481  CL87 HEK-293T C108(0.96); C284(0.73)  LDD1079  [13]
 LDCM0482  CL88 HEK-293T C108(0.95); C284(0.98)  LDD1080  [13]
 LDCM0483  CL89 HEK-293T C108(0.99); C284(0.80)  LDD1081  [13]
 LDCM0484  CL9 HEK-293T C121(0.44); C124(0.90); C284(1.29)  LDD1082  [13]
 LDCM0485  CL90 HEK-293T C108(0.89); C284(0.80)  LDD1083  [13]
 LDCM0486  CL91 HEK-293T C284(1.27)  LDD1084  [13]
 LDCM0487  CL92 HEK-293T C284(0.97)  LDD1085  [13]
 LDCM0488  CL93 HEK-293T C284(1.03)  LDD1086  [13]
 LDCM0489  CL94 HEK-293T C284(0.64)  LDD1087  [13]
 LDCM0490  CL95 HEK-293T C284(0.52)  LDD1088  [13]
 LDCM0491  CL96 HEK-293T C284(0.82)  LDD1089  [13]
 LDCM0492  CL97 HEK-293T C284(1.01)  LDD1090  [13]
 LDCM0493  CL98 HEK-293T C284(1.04)  LDD1091  [13]
 LDCM0494  CL99 HEK-293T C284(0.98)  LDD1092  [13]
 LDCM0634  CY-0357 Hep-G2 C231(1.02)  LDD2228  [12]
 LDCM0495  E2913 HEK-293T C231(0.85); C284(1.04); C385(0.92); C539(1.16)  LDD1698  [14]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C539(1.33)  LDD1702  [3]
 LDCM0625  F8 Ramos C324(0.92); C539(1.52); C231(1.50); C362(0.62)  LDD2187  [15]
 LDCM0572  Fragment10 Ramos C324(0.64); C539(1.02); C231(1.47); C362(0.70)  LDD2189  [15]
 LDCM0573  Fragment11 Ramos C324(1.84); C539(5.68); C231(1.38); C362(2.75)  LDD2190  [15]
 LDCM0574  Fragment12 Ramos C324(0.72); C539(0.75); C231(1.90); C362(0.80)  LDD2191  [15]
 LDCM0575  Fragment13 Ramos C324(1.05); C539(0.91); C231(0.97); C362(0.72)  LDD2192  [15]
 LDCM0576  Fragment14 Ramos C324(0.70); C539(0.55); C231(9.38); C362(2.19)  LDD2193  [15]
 LDCM0579  Fragment20 Ramos C324(0.59); C539(0.66); C362(0.56)  LDD2194  [15]
 LDCM0580  Fragment21 Ramos C324(0.74); C539(0.96); C231(0.73); C362(0.86)  LDD2195  [15]
 LDCM0582  Fragment23 Ramos C324(0.76); C539(0.86); C362(0.95)  LDD2196  [15]
 LDCM0578  Fragment27 Ramos C324(0.90); C539(0.92); C231(0.61); C362(1.24)  LDD2197  [15]
 LDCM0586  Fragment28 Ramos C324(0.56); C539(0.76); C231(0.66); C362(1.37)  LDD2198  [15]
 LDCM0588  Fragment30 Ramos C324(1.30); C539(1.08); C231(0.61); C362(0.63)  LDD2199  [15]
 LDCM0589  Fragment31 Ramos C324(0.82); C539(1.01); C231(0.70); C362(0.83)  LDD2200  [15]
 LDCM0590  Fragment32 Ramos C324(0.88); C539(1.21); C362(0.77)  LDD2201  [15]
 LDCM0468  Fragment33 HEK-293T C121(0.65)  LDD1066  [13]
 LDCM0596  Fragment38 Ramos C324(0.90); C539(0.81); C231(0.74); C362(0.74)  LDD2203  [15]
 LDCM0566  Fragment4 Ramos C324(0.61); C539(0.95); C231(1.46); C362(0.49)  LDD2184  [15]
 LDCM0427  Fragment51 PaTu 8988t C385(1.67); C231(2.43)  LDD1306  [13]
 LDCM0610  Fragment52 Ramos C324(1.27); C539(1.00)  LDD2204  [15]
 LDCM0614  Fragment56 Ramos C324(1.22); C539(1.24); C231(0.71); C362(0.53)  LDD2205  [15]
 LDCM0569  Fragment7 Ramos C324(0.52); C539(0.90); C231(1.83); C362(1.11)  LDD2186  [15]
 LDCM0571  Fragment9 Ramos C324(0.63); C539(0.96); C231(2.33); C362(0.45)  LDD2188  [15]
 LDCM0022  KB02 HEK-293T C284(1.00); C362(1.02); C385(1.05); C539(1.06)  LDD1492  [14]
 LDCM0023  KB03 Jurkat C362(4.99); C231(22.30); C539(10.14); C121(26.41)  LDD0209  [4]
 LDCM0024  KB05 COLO792 C10(1.44)  LDD3310  [16]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C539(1.04)  LDD2105  [3]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C539(0.87)  LDD2153  [3]
 LDCM0628  OTUB2-COV-1 HEK-293T C231(1.15)  LDD2207  [17]
 LDCM0131  RA190 MM1.R C385(1.92)  LDD0304  [18]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Transitional endoplasmic reticulum ATPase (VCP) AAA ATPase family P55072
E3 ubiquitin-protein ligase BRE1A (RNF20) BRE1 family Q5VTR2
Serine/threonine-protein phosphatase 2A 56 kDa regulatory subunit alpha isoform (PPP2R5A) Phosphatase 2A regulatory subunit B56 family Q15172
Serine/threonine-protein phosphatase 2A 56 kDa regulatory subunit beta isoform (PPP2R5B) Phosphatase 2A regulatory subunit B56 family Q15173
Serine/threonine-protein phosphatase 2A 56 kDa regulatory subunit epsilon isoform (PPP2R5E) Phosphatase 2A regulatory subunit B56 family Q16537
Protein phosphatase 1G (PPM1G) PP2C family O15355
Serine/threonine-protein kinase Chk2 (CHEK2) CAMK Ser/Thr protein kinase family O96017
Serine/threonine-protein kinase PLK1 (PLK1) Ser/Thr protein kinase family P53350
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Interleukin-24 (IL24) IL-10 family Q13007
Other
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein AATF (AATF) AATF family Q9NY61
DNA replication complex GINS protein PSF2 (GINS2) GINS2/PSF2 family Q9Y248
Protein LRATD2 (LRATD2) LRATD family Q96KN1
Retinoblastoma-associated protein (RB1) Retinoblastoma protein (RB) family P06400
DNA repair protein XRCC1 (XRCC1) . P18887
Period circadian protein homolog 3 (PER3) . P56645

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
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
E7850 Small molecular drug D00EPT
Investigative
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
2-(4-phenoxy-phenyl)-1h-benzoimidazol-5-ylamine Small molecular drug D00MLE
5-nitro-2-(4-phenoxy-phenyl)-1h-benzoimidazole Small molecular drug D0D3AS
Cct-241533 Small molecular drug D0DH1H
Chk2 Inhibitor Ii Small molecular drug D0EM1C
Debromohymenialdisine Small molecular drug D01WAI
Enzastaurin Small molecular drug DB06486
Pmid22564207c25b Small molecular drug D09AID
Pv-1019 . D02HWR
Patented
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid27410995-compound-figure3j Small molecular drug D0O6TG
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Xl844 Small molecular drug D05UGJ

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 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 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.
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 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
9 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
10 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.
11 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
12 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
13 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.
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
17 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.
18 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.