General Information of Target

Target ID LDTP11030
Target Name Serine/threonine-protein kinase VRK1 (VRK1)
Gene Name VRK1
Gene ID 7443
Synonyms
Serine/threonine-protein kinase VRK1; EC 2.7.11.1; Vaccinia-related kinase 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAFRTICVLVGVFICSICVKGSSQPQARVYLTFDELRETKTSEYFSLSHHPLDYRILLMD
EDQDRIYVGSKDHILSLNINNISQEALSVFWPASTIKVEECKMAGKDPTHGCGNFVRVIQ
TFNRTHLYVCGSGAFSPVCTYLNRGRRSEDQVFMIDSKCESGKGRCSFNPNVNTVSVMIN
EELFSGMYIDFMGTDAAIFRSLTKRNAVRTDQHNSKWLSEPMFVDAHVIPDGTDPNDAKV
YFFFKEKLTDNNRSTKQIHSMIARICPNDTGGLRSLVNKWTTFLKARLVCSVTDEDGPET
HFDELEDVFLLETDNPRTTLVYGIFTTSSSVFKGSAVCVYHLSDIQTVFNGPFAHKEGPN
HQLISYQGRIPYPRPGTCPGGAFTPNMRTTKEFPDDVVTFIRNHPLMYNSIYPIHKRPLI
VRIGTDYKYTKIAVDRVNAADGRYHVLFLGTDRGTVQKVVVLPTNNSVSGELILEELEVF
KNHAPITTMKISSKKQQLYVSSNEGVSQVSLHRCHIYGTACADCCLARDPYCAWDGHSCS
RFYPTGKRRSRRQDVRHGNPLTQCRGFNLKAYRNAAEIVQYGVKNNTTFLECAPKSPQAS
IKWLLQKDKDRRKEVKLNERIIATSQGLLIRSVQGSDQGLYHCIATENSFKQTIAKINFK
VLDSEMVAVVTDKWSPWTWASSVRALPFHPKDIMGAFSHSEMQMINQYCKDTRQQHQQGD
ESQKMRGDYGKLKALINSRKSRNRRNQLPES
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CK1 Ser/Thr protein kinase family, VRK subfamily
Subcellular location
Nucleus
Function
Serine/threonine kinase involved in cell cycle, nuclear condensation and transcription regulation. Involved in Golgi disassembly during the cell cycle: following phosphorylation by PLK3 during mitosis, required to induce Golgi fragmentation. Phosphorylates 'Thr-18' of p53/TP53 and may thereby prevent the interaction between p53/TP53 and MDM2. Phosphorylates KAT5 in response to DNA damage, promoting KAT5 association with chromatin and histone acetyltransferase activity. Phosphorylates BANF1: disrupts its ability to bind DNA, reduces its binding to LEM domain-containing proteins and causes its relocalization from the nucleus to the cytoplasm. Phosphorylates ATF2 which activates its transcriptional activity.
Uniprot ID
Q99986
Ensemble ID
ENST00000216639.8
HGNC ID
HGNC:12718
ChEMBL ID
CHEMBL1293199

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 
14.37  LDD0402  [1]
CY-1
 Probe Info 
100.00  LDD0243  [2]
N1
 Probe Info 
100.00  LDD0242  [2]
TH211
 Probe Info 
Y198(20.00); Y52(16.09); Y311(14.94); Y213(13.46)  LDD0257  [3]
TH214
 Probe Info 
Y204(9.78)  LDD0258  [3]
TH216
 Probe Info 
Y204(20.00); Y311(20.00); Y107(17.89); Y317(13.07)  LDD0259  [3]
STPyne
 Probe Info 
K147(4.41); K98(10.00)  LDD0277  [4]
BTD
 Probe Info 
C205(1.58)  LDD1700  [5]
AHL-Pu-1
 Probe Info 
C205(3.82)  LDD0170  [6]
DBIA
 Probe Info 
C50(2.22); C205(1.71)  LDD0080  [7]
1d-yne
 Probe Info 
N.A.  LDD0358  [8]
4-Iodoacetamidophenylacetylene
 Probe Info 
C220(0.00); C250(0.00); C205(0.00)  LDD0038  [9]
IA-alkyne
 Probe Info 
N.A.  LDD0032  [10]
IPIAA_L
 Probe Info 
C289(0.00); C220(0.00)  LDD0031  [11]
Lodoacetamide azide
 Probe Info 
C220(0.00); C289(0.00); C250(0.00); C50(0.00)  LDD0037  [9]
IPM
 Probe Info 
N.A.  LDD0025  [12]
NAIA_4
 Probe Info 
N.A.  LDD2226  [13]
Compound 10
 Probe Info 
N.A.  LDD2216  [14]
Compound 11
 Probe Info 
N.A.  LDD2213  [14]
NHS
 Probe Info 
K140(0.00); K329(0.00)  LDD0010  [15]
SF
 Probe Info 
N.A.  LDD0028  [16]
Ox-W18
 Probe Info 
N.A.  LDD2175  [17]
1c-yne
 Probe Info 
N.A.  LDD0228  [8]
Acrolein
 Probe Info 
N.A.  LDD0217  [18]
AOyne
 Probe Info 
11.90  LDD0443  [19]
NAIA_5
 Probe Info 
C220(0.00); C250(0.00); C205(0.00)  LDD2223  [13]
HHS-465
 Probe Info 
N.A.  LDD2240  [20]
HHS-482
 Probe Info 
Y113(0.50)  LDD2239  [21]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe3
 Probe Info 
6.03  LDD0465  [22]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0548  1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one MDA-MB-231 C205(1.41)  LDD2142  [5]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C205(0.70); C289(0.73)  LDD2117  [5]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C205(1.37); C289(1.19)  LDD2152  [5]
 LDCM0025  4SU-RNA DM93 C205(3.82)  LDD0170  [6]
 LDCM0214  AC1 HCT 116 C220(0.91); C50(0.67); C68(0.40)  LDD0531  [7]
 LDCM0215  AC10 HCT 116 C220(0.92); C50(1.03); C68(0.50)  LDD0532  [7]
 LDCM0216  AC100 HCT 116 C220(0.66); C50(0.43); C68(0.32)  LDD0533  [7]
 LDCM0217  AC101 HCT 116 C220(0.94); C50(0.56); C68(0.45)  LDD0534  [7]
 LDCM0218  AC102 HCT 116 C220(0.94); C50(0.41); C68(0.31)  LDD0535  [7]
 LDCM0219  AC103 HCT 116 C220(0.85); C50(0.31); C68(0.13)  LDD0536  [7]
 LDCM0220  AC104 HCT 116 C220(0.72); C50(0.38); C68(0.19)  LDD0537  [7]
 LDCM0221  AC105 HCT 116 C220(0.82); C50(0.33); C68(0.18)  LDD0538  [7]
 LDCM0222  AC106 HCT 116 C220(0.85); C50(0.29); C68(0.16)  LDD0539  [7]
 LDCM0223  AC107 HCT 116 C220(0.93); C50(0.32); C68(0.11)  LDD0540  [7]
 LDCM0224  AC108 HCT 116 C220(0.71); C50(0.58); C68(0.54)  LDD0541  [7]
 LDCM0225  AC109 HCT 116 C220(0.75); C50(0.56); C68(0.52)  LDD0542  [7]
 LDCM0226  AC11 HCT 116 C220(0.94); C50(1.02); C68(0.46)  LDD0543  [7]
 LDCM0227  AC110 HCT 116 C220(0.64); C50(0.54); C68(0.48)  LDD0544  [7]
 LDCM0228  AC111 HCT 116 C220(0.62); C50(0.47); C68(0.45)  LDD0545  [7]
 LDCM0229  AC112 HCT 116 C220(0.87); C50(0.38); C68(0.23)  LDD0546  [7]
 LDCM0230  AC113 HCT 116 C220(0.82); C50(1.14); C68(1.14)  LDD0547  [7]
 LDCM0231  AC114 HCT 116 C220(0.99); C50(0.61); C68(0.61)  LDD0548  [7]
 LDCM0232  AC115 HCT 116 C220(1.10); C50(0.31); C68(0.31)  LDD0549  [7]
 LDCM0233  AC116 HCT 116 C220(0.94); C50(0.33); C68(0.33)  LDD0550  [7]
 LDCM0234  AC117 HCT 116 C220(0.99); C50(0.74); C68(0.74)  LDD0551  [7]
 LDCM0235  AC118 HCT 116 C220(1.09); C50(0.76); C68(0.76)  LDD0552  [7]
 LDCM0236  AC119 HCT 116 C220(1.25); C50(0.69); C68(0.69)  LDD0553  [7]
 LDCM0237  AC12 HCT 116 C220(0.90); C50(0.88); C68(0.66)  LDD0554  [7]
 LDCM0238  AC120 HCT 116 C220(0.80); C50(0.60); C68(0.60)  LDD0555  [7]
 LDCM0239  AC121 HCT 116 C220(1.61); C50(0.77); C68(0.77)  LDD0556  [7]
 LDCM0240  AC122 HCT 116 C220(0.82); C50(0.58); C68(0.58)  LDD0557  [7]
 LDCM0241  AC123 HCT 116 C220(0.91); C50(0.70); C68(0.70)  LDD0558  [7]
 LDCM0242  AC124 HCT 116 C220(1.30); C50(0.79); C68(0.79)  LDD0559  [7]
 LDCM0243  AC125 HCT 116 C220(0.99); C50(0.86); C68(0.86)  LDD0560  [7]
 LDCM0244  AC126 HCT 116 C220(1.03); C50(0.35); C68(0.35)  LDD0561  [7]
 LDCM0245  AC127 HCT 116 C220(0.99); C50(0.46); C68(0.46)  LDD0562  [7]
 LDCM0246  AC128 HEK-293T C50(1.04); C68(1.09)  LDD0844  [7]
 LDCM0247  AC129 HEK-293T C50(1.25); C68(1.01)  LDD0845  [7]
 LDCM0249  AC130 HEK-293T C50(1.24); C68(1.10)  LDD0847  [7]
 LDCM0250  AC131 HEK-293T C50(1.00); C68(1.11)  LDD0848  [7]
 LDCM0251  AC132 HEK-293T C50(1.00); C68(1.08)  LDD0849  [7]
 LDCM0252  AC133 HEK-293T C50(1.21); C68(1.09)  LDD0850  [7]
 LDCM0253  AC134 HEK-293T C50(1.16); C68(1.07)  LDD0851  [7]
 LDCM0254  AC135 HEK-293T C50(1.36); C68(1.12)  LDD0852  [7]
 LDCM0255  AC136 HEK-293T C50(1.24); C68(1.21)  LDD0853  [7]
 LDCM0256  AC137 HEK-293T C50(1.56); C68(1.23)  LDD0854  [7]
 LDCM0257  AC138 HEK-293T C50(1.57); C68(1.29)  LDD0855  [7]
 LDCM0258  AC139 HEK-293T C50(1.55); C68(1.33)  LDD0856  [7]
 LDCM0259  AC14 HCT 116 C220(1.08); C50(0.73); C68(0.52)  LDD0576  [7]
 LDCM0260  AC140 HEK-293T C50(1.21); C68(1.14)  LDD0858  [7]
 LDCM0261  AC141 HEK-293T C50(1.49); C68(1.23)  LDD0859  [7]
 LDCM0262  AC142 HEK-293T C50(1.37); C68(1.19)  LDD0860  [7]
 LDCM0263  AC143 HCT 116 C68(0.45); C50(0.55)  LDD0580  [7]
 LDCM0264  AC144 HCT 116 C68(0.12); C50(0.39)  LDD0581  [7]
 LDCM0265  AC145 HCT 116 C68(0.29); C50(0.47)  LDD0582  [7]
 LDCM0266  AC146 HCT 116 C68(0.17); C50(0.39)  LDD0583  [7]
 LDCM0267  AC147 HCT 116 C68(0.10); C50(0.35)  LDD0584  [7]
 LDCM0268  AC148 HCT 116 C68(0.09); C50(0.42)  LDD0585  [7]
 LDCM0269  AC149 HCT 116 C68(0.10); C50(0.36)  LDD0586  [7]
 LDCM0270  AC15 HCT 116 C68(0.47); C50(0.80); C220(0.97)  LDD0587  [7]
 LDCM0271  AC150 HCT 116 C68(0.32); C50(0.48)  LDD0588  [7]
 LDCM0272  AC151 HCT 116 C68(0.43); C50(0.62)  LDD0589  [7]
 LDCM0273  AC152 HCT 116 C68(0.10); C50(0.39)  LDD0590  [7]
 LDCM0274  AC153 HCT 116 C68(0.09); C50(0.46)  LDD0591  [7]
 LDCM0621  AC154 HCT 116 C50(0.39); C68(0.15)  LDD2158  [7]
 LDCM0622  AC155 HCT 116 C50(0.32); C68(0.15)  LDD2159  [7]
 LDCM0623  AC156 HCT 116 C50(0.55); C68(0.52)  LDD2160  [7]
 LDCM0624  AC157 HCT 116 C50(0.85); C68(0.78)  LDD2161  [7]
 LDCM0276  AC17 HCT 116 C50(0.84); C68(0.84)  LDD0593  [7]
 LDCM0277  AC18 HCT 116 C50(0.37); C68(0.37)  LDD0594  [7]
 LDCM0278  AC19 HCT 116 C50(0.66); C68(0.66)  LDD0595  [7]
 LDCM0279  AC2 HCT 116 C68(0.66); C220(0.94); C50(1.13)  LDD0596  [7]
 LDCM0280  AC20 HCT 116 C50(0.85); C68(0.85)  LDD0597  [7]
 LDCM0281  AC21 HCT 116 C50(0.82); C68(0.82)  LDD0598  [7]
 LDCM0282  AC22 HCT 116 C50(1.00); C68(1.00)  LDD0599  [7]
 LDCM0283  AC23 HCT 116 C50(0.83); C68(0.83)  LDD0600  [7]
 LDCM0284  AC24 HCT 116 C50(0.93); C68(0.93)  LDD0601  [7]
 LDCM0285  AC25 HCT 116 C50(0.99); C220(1.03)  LDD0602  [7]
 LDCM0286  AC26 HCT 116 C220(1.08); C50(1.10)  LDD0603  [7]
 LDCM0287  AC27 HCT 116 C50(0.95); C220(1.32)  LDD0604  [7]
 LDCM0288  AC28 HCT 116 C220(1.15); C50(1.21)  LDD0605  [7]
 LDCM0289  AC29 HCT 116 C220(1.07); C50(1.10)  LDD0606  [7]
 LDCM0290  AC3 HCT 116 C68(0.60); C50(0.80); C220(1.03)  LDD0607  [7]
 LDCM0291  AC30 HCT 116 C50(1.03); C220(1.17)  LDD0608  [7]
 LDCM0292  AC31 HCT 116 C50(1.04); C220(1.21)  LDD0609  [7]
 LDCM0293  AC32 HCT 116 C50(1.11); C220(1.33)  LDD0610  [7]
 LDCM0294  AC33 HCT 116 C50(1.09); C220(1.22)  LDD0611  [7]
 LDCM0295  AC34 HCT 116 C220(1.08); C50(1.22)  LDD0612  [7]
 LDCM0296  AC35 HCT 116 C220(0.90); C50(0.91); C68(1.08)  LDD0613  [7]
 LDCM0297  AC36 HCT 116 C68(0.77); C50(0.93); C220(0.97)  LDD0614  [7]
 LDCM0298  AC37 HCT 116 C50(1.35); C220(1.40); C68(1.90)  LDD0615  [7]
 LDCM0299  AC38 HCT 116 C68(0.53); C50(0.81); C220(1.45)  LDD0616  [7]
 LDCM0300  AC39 HCT 116 C68(0.65); C50(0.87); C220(1.11)  LDD0617  [7]
 LDCM0301  AC4 HCT 116 C68(0.39); C50(0.63); C220(0.90)  LDD0618  [7]
 LDCM0302  AC40 HCT 116 C50(0.96); C68(1.18); C220(1.27)  LDD0619  [7]
 LDCM0303  AC41 HCT 116 C68(0.69); C50(0.82); C220(1.17)  LDD0620  [7]
 LDCM0304  AC42 HCT 116 C68(0.56); C50(0.74); C220(1.35)  LDD0621  [7]
 LDCM0305  AC43 HCT 116 C68(0.67); C50(1.10); C220(1.32)  LDD0622  [7]
 LDCM0306  AC44 HCT 116 C50(1.16); C220(1.26); C68(1.61)  LDD0623  [7]
 LDCM0307  AC45 HCT 116 C50(1.08); C220(1.21); C68(1.39)  LDD0624  [7]
 LDCM0308  AC46 HCT 116 C50(1.00); C68(1.00); C220(1.14)  LDD0625  [7]
 LDCM0309  AC47 HCT 116 C50(0.78); C68(0.78); C220(1.01)  LDD0626  [7]
 LDCM0310  AC48 HCT 116 C50(0.72); C68(0.72); C220(1.18)  LDD0627  [7]
 LDCM0311  AC49 HCT 116 C50(0.48); C68(0.48); C220(1.24)  LDD0628  [7]
 LDCM0312  AC5 HCT 116 C68(0.42); C50(0.76); C220(0.91)  LDD0629  [7]
 LDCM0313  AC50 HCT 116 C50(0.42); C68(0.42); C220(0.97)  LDD0630  [7]
 LDCM0314  AC51 HCT 116 C220(0.98); C50(1.33); C68(1.33)  LDD0631  [7]
 LDCM0315  AC52 HCT 116 C50(0.72); C68(0.72); C220(1.10)  LDD0632  [7]
 LDCM0316  AC53 HCT 116 C50(0.55); C68(0.55); C220(0.84)  LDD0633  [7]
 LDCM0317  AC54 HCT 116 C50(0.55); C68(0.55); C220(0.94)  LDD0634  [7]
 LDCM0318  AC55 HCT 116 C50(0.52); C68(0.52); C220(0.92)  LDD0635  [7]
 LDCM0319  AC56 HCT 116 C50(0.59); C68(0.59); C220(0.61)  LDD0636  [7]
 LDCM0320  AC57 HCT 116 C50(0.22); C68(0.22)  LDD0637  [7]
 LDCM0321  AC58 HCT 116 C50(0.22); C68(0.22)  LDD0638  [7]
 LDCM0322  AC59 HCT 116 C50(0.14); C68(0.14)  LDD0639  [7]
 LDCM0323  AC6 HCT 116 C68(0.50); C50(0.72); C220(0.99)  LDD0640  [7]
 LDCM0324  AC60 HCT 116 C50(0.20); C68(0.20)  LDD0641  [7]
 LDCM0325  AC61 HCT 116 C50(0.22); C68(0.22)  LDD0642  [7]
 LDCM0326  AC62 HCT 116 C50(0.13); C68(0.13)  LDD0643  [7]
 LDCM0327  AC63 HCT 116 C50(0.17); C68(0.17)  LDD0644  [7]
 LDCM0328  AC64 HCT 116 C50(0.15); C68(0.15)  LDD0645  [7]
 LDCM0329  AC65 HCT 116 C50(0.17); C68(0.17)  LDD0646  [7]
 LDCM0330  AC66 HCT 116 C50(0.22); C68(0.22)  LDD0647  [7]
 LDCM0331  AC67 HCT 116 C50(0.14); C68(0.14)  LDD0648  [7]
 LDCM0332  AC68 HCT 116 C50(0.41); C68(0.41)  LDD0649  [7]
 LDCM0333  AC69 HCT 116 C50(0.37); C68(0.37)  LDD0650  [7]
 LDCM0334  AC7 HCT 116 C68(0.65); C50(0.90); C220(1.19)  LDD0651  [7]
 LDCM0335  AC70 HCT 116 C50(0.24); C68(0.24)  LDD0652  [7]
 LDCM0336  AC71 HCT 116 C50(0.66); C68(0.66)  LDD0653  [7]
 LDCM0337  AC72 HCT 116 C50(0.33); C68(0.33)  LDD0654  [7]
 LDCM0338  AC73 HCT 116 C50(0.35); C68(0.35)  LDD0655  [7]
 LDCM0339  AC74 HCT 116 C50(0.29); C68(0.29)  LDD0656  [7]
 LDCM0340  AC75 HCT 116 C50(0.33); C68(0.33)  LDD0657  [7]
 LDCM0341  AC76 HCT 116 C50(0.29); C68(0.29)  LDD0658  [7]
 LDCM0342  AC77 HCT 116 C50(0.23); C68(0.23)  LDD0659  [7]
 LDCM0343  AC78 HCT 116 C50(0.59); C68(0.59)  LDD0660  [7]
 LDCM0344  AC79 HCT 116 C50(0.63); C68(0.63)  LDD0661  [7]
 LDCM0345  AC8 HCT 116 C68(0.63); C220(1.04); C50(1.08)  LDD0662  [7]
 LDCM0346  AC80 HCT 116 C50(0.35); C68(0.35)  LDD0663  [7]
 LDCM0347  AC81 HCT 116 C50(1.01); C68(1.01)  LDD0664  [7]
 LDCM0348  AC82 HCT 116 C50(0.35); C68(0.35)  LDD0665  [7]
 LDCM0349  AC83 HCT 116 C68(0.24); C50(0.49)  LDD0666  [7]
 LDCM0350  AC84 HCT 116 C68(0.28); C50(0.53)  LDD0667  [7]
 LDCM0351  AC85 HCT 116 C68(0.61); C50(0.74)  LDD0668  [7]
 LDCM0352  AC86 HCT 116 C68(0.73); C50(0.82)  LDD0669  [7]
 LDCM0353  AC87 HCT 116 C50(0.74); C68(0.75)  LDD0670  [7]
 LDCM0354  AC88 HCT 116 C50(0.72); C68(0.79)  LDD0671  [7]
 LDCM0355  AC89 HCT 116 C68(0.37); C50(0.43)  LDD0672  [7]
 LDCM0357  AC90 HCT 116 C50(2.10); C68(3.92)  LDD0674  [7]
 LDCM0358  AC91 HCT 116 C68(0.23); C50(0.51)  LDD0675  [7]
 LDCM0359  AC92 HCT 116 C68(0.23); C50(0.40)  LDD0676  [7]
 LDCM0360  AC93 HCT 116 C50(0.53); C68(0.62)  LDD0677  [7]
 LDCM0361  AC94 HCT 116 C68(0.74); C50(0.82)  LDD0678  [7]
 LDCM0362  AC95 HCT 116 C68(0.43); C50(0.56)  LDD0679  [7]
 LDCM0363  AC96 HCT 116 C68(0.47); C50(0.49)  LDD0680  [7]
 LDCM0364  AC97 HCT 116 C68(0.35); C50(0.67)  LDD0681  [7]
 LDCM0365  AC98 HCT 116 C68(0.11); C50(0.38); C220(0.67)  LDD0682  [7]
 LDCM0366  AC99 HCT 116 C68(0.57); C50(0.60); C220(0.62)  LDD0683  [7]
 LDCM0520  AKOS000195272 MDA-MB-231 C205(0.92)  LDD2113  [5]
 LDCM0248  AKOS034007472 HCT 116 C220(0.91); C50(0.92); C68(0.87)  LDD0565  [7]
 LDCM0356  AKOS034007680 HCT 116 C68(0.60); C50(0.95); C220(1.14)  LDD0673  [7]
 LDCM0275  AKOS034007705 HCT 116 C68(0.15); C50(0.65); C220(1.29)  LDD0592  [7]
 LDCM0156  Aniline NCI-H1299 12.03  LDD0403  [1]
 LDCM0020  ARS-1620 HCC44 C205(1.01)  LDD2171  [7]
 LDCM0498  BS-3668 MDA-MB-231 C205(0.53)  LDD2091  [5]
 LDCM0630  CCW28-3 231MFP C50(0.54)  LDD2214  [23]
 LDCM0632  CL-Sc Hep-G2 C220(0.79)  LDD2227  [13]
 LDCM0367  CL1 HCT 116 C50(1.24); C68(1.87)  LDD0684  [7]
 LDCM0368  CL10 HCT 116 C68(0.39); C50(0.78)  LDD0685  [7]
 LDCM0369  CL100 HCT 116 C68(0.46); C220(0.88); C50(0.92)  LDD0686  [7]
 LDCM0370  CL101 HCT 116 C68(0.44); C50(0.91); C220(1.20)  LDD0687  [7]
 LDCM0371  CL102 HCT 116 C68(0.70); C50(0.93); C220(1.01)  LDD0688  [7]
 LDCM0372  CL103 HCT 116 C220(1.00); C68(1.14); C50(1.32)  LDD0689  [7]
 LDCM0373  CL104 HCT 116 C68(0.70); C50(1.03); C220(1.07)  LDD0690  [7]
 LDCM0374  CL105 HCT 116 C50(0.47); C68(0.47)  LDD0691  [7]
 LDCM0375  CL106 HCT 116 C50(0.28); C68(0.28)  LDD0692  [7]
 LDCM0376  CL107 HCT 116 C50(0.26); C68(0.26)  LDD0693  [7]
 LDCM0377  CL108 HCT 116 C50(0.23); C68(0.23)  LDD0694  [7]
 LDCM0378  CL109 HCT 116 C50(0.55); C68(0.55)  LDD0695  [7]
 LDCM0379  CL11 HCT 116 C68(0.28); C50(0.93)  LDD0696  [7]
 LDCM0380  CL110 HCT 116 C50(0.49); C68(0.49)  LDD0697  [7]
 LDCM0381  CL111 HCT 116 C50(0.61); C68(0.61)  LDD0698  [7]
 LDCM0382  CL112 HCT 116 C220(1.12); C50(1.19)  LDD0699  [7]
 LDCM0383  CL113 HCT 116 C220(1.12); C50(1.36)  LDD0700  [7]
 LDCM0384  CL114 HCT 116 C50(0.83); C220(1.23)  LDD0701  [7]
 LDCM0385  CL115 HCT 116 C220(1.12); C50(1.56)  LDD0702  [7]
 LDCM0386  CL116 HCT 116 C220(1.19); C50(1.24)  LDD0703  [7]
 LDCM0387  CL117 HCT 116 C68(0.87); C50(0.99); C220(1.00)  LDD0704  [7]
 LDCM0388  CL118 HCT 116 C68(0.66); C50(1.01); C220(1.02)  LDD0705  [7]
 LDCM0389  CL119 HCT 116 C68(0.78); C50(0.81); C220(1.04)  LDD0706  [7]
 LDCM0390  CL12 HCT 116 C68(0.24); C50(1.21)  LDD0707  [7]
 LDCM0391  CL120 HCT 116 C68(0.78); C50(0.93); C220(0.99)  LDD0708  [7]
 LDCM0392  CL121 HCT 116 C220(1.00); C50(1.99); C68(1.99)  LDD0709  [7]
 LDCM0393  CL122 HCT 116 C50(0.80); C68(0.80); C220(1.06)  LDD0710  [7]
 LDCM0394  CL123 HCT 116 C50(0.56); C68(0.56); C220(0.95)  LDD0711  [7]
 LDCM0395  CL124 HCT 116 C50(0.51); C68(0.51); C220(0.98)  LDD0712  [7]
 LDCM0396  CL125 HCT 116 C50(1.01); C68(1.01)  LDD0713  [7]
 LDCM0397  CL126 HCT 116 C50(0.46); C68(0.46)  LDD0714  [7]
 LDCM0398  CL127 HCT 116 C50(0.41); C68(0.41)  LDD0715  [7]
 LDCM0399  CL128 HCT 116 C50(0.18); C68(0.18)  LDD0716  [7]
 LDCM0400  CL13 HCT 116 C68(0.44); C50(0.78)  LDD0717  [7]
 LDCM0401  CL14 HCT 116 C50(0.63); C68(0.66)  LDD0718  [7]
 LDCM0402  CL15 HCT 116 C68(0.43); C50(0.69)  LDD0719  [7]
 LDCM0403  CL16 HCT 116 C68(0.70); C50(1.02)  LDD0720  [7]
 LDCM0404  CL17 HCT 116 C68(0.50); C50(0.81)  LDD0721  [7]
 LDCM0405  CL18 HCT 116 C68(0.26); C50(1.02)  LDD0722  [7]
 LDCM0406  CL19 HCT 116 C68(0.47); C50(1.17)  LDD0723  [7]
 LDCM0407  CL2 HCT 116 C50(0.76); C68(0.93)  LDD0724  [7]
 LDCM0408  CL20 HCT 116 C68(0.28); C50(1.15)  LDD0725  [7]
 LDCM0409  CL21 HCT 116 C68(0.25); C50(1.02)  LDD0726  [7]
 LDCM0410  CL22 HCT 116 C68(0.30); C50(1.64)  LDD0727  [7]
 LDCM0411  CL23 HCT 116 C68(0.39); C50(1.04)  LDD0728  [7]
 LDCM0412  CL24 HCT 116 C50(1.37); C68(0.22)  LDD0729  [7]
 LDCM0413  CL25 HCT 116 C50(0.93); C68(0.25)  LDD0730  [7]
 LDCM0414  CL26 HCT 116 C50(0.95); C68(0.40)  LDD0731  [7]
 LDCM0415  CL27 HCT 116 C50(0.89); C68(0.42)  LDD0732  [7]
 LDCM0416  CL28 HCT 116 C50(1.05); C68(0.37)  LDD0733  [7]
 LDCM0417  CL29 HCT 116 C50(0.94); C68(0.31)  LDD0734  [7]
 LDCM0418  CL3 HCT 116 C50(0.91); C68(0.92)  LDD0735  [7]
 LDCM0419  CL30 HCT 116 C50(0.97); C68(0.63)  LDD0736  [7]
 LDCM0420  CL31 HCT 116 C50(0.48); C68(0.48)  LDD0737  [7]
 LDCM0421  CL32 HCT 116 C50(0.22); C68(0.22)  LDD0738  [7]
 LDCM0422  CL33 HCT 116 C50(0.36); C68(0.36)  LDD0739  [7]
 LDCM0423  CL34 HCT 116 C50(0.32); C68(0.32)  LDD0740  [7]
 LDCM0424  CL35 HCT 116 C50(0.23); C68(0.23)  LDD0741  [7]
 LDCM0425  CL36 HCT 116 C50(0.21); C68(0.21)  LDD0742  [7]
 LDCM0426  CL37 HCT 116 C50(0.21); C68(0.21)  LDD0743  [7]
 LDCM0428  CL39 HCT 116 C50(0.21); C68(0.21)  LDD0745  [7]
 LDCM0429  CL4 HCT 116 C50(0.87); C68(0.76)  LDD0746  [7]
 LDCM0430  CL40 HCT 116 C50(0.26); C68(0.26)  LDD0747  [7]
 LDCM0431  CL41 HCT 116 C50(0.44); C68(0.44)  LDD0748  [7]
 LDCM0432  CL42 HCT 116 C50(0.29); C68(0.29)  LDD0749  [7]
 LDCM0433  CL43 HCT 116 C50(0.27); C68(0.27)  LDD0750  [7]
 LDCM0434  CL44 HCT 116 C50(0.26); C68(0.26)  LDD0751  [7]
 LDCM0435  CL45 HCT 116 C50(0.23); C68(0.23)  LDD0752  [7]
 LDCM0436  CL46 HCT 116 C220(0.86); C50(1.27); C68(2.18)  LDD0753  [7]
 LDCM0437  CL47 HCT 116 C220(0.95); C50(1.30); C68(1.82)  LDD0754  [7]
 LDCM0438  CL48 HCT 116 C220(0.93); C50(1.48); C68(2.16)  LDD0755  [7]
 LDCM0439  CL49 HCT 116 C220(0.81); C50(0.89); C68(1.10)  LDD0756  [7]
 LDCM0440  CL5 HCT 116 C50(0.73); C68(0.58)  LDD0757  [7]
 LDCM0441  CL50 HCT 116 C220(1.01); C50(0.98); C68(1.49)  LDD0758  [7]
 LDCM0442  CL51 HCT 116 C220(0.76); C50(1.21); C68(1.71)  LDD0759  [7]
 LDCM0443  CL52 HCT 116 C220(1.02); C50(1.18); C68(1.72)  LDD0760  [7]
 LDCM0444  CL53 HCT 116 C220(1.09); C50(1.18); C68(1.64)  LDD0761  [7]
 LDCM0445  CL54 HCT 116 C220(0.85); C50(1.21); C68(2.00)  LDD0762  [7]
 LDCM0446  CL55 HCT 116 C220(0.84); C50(1.20); C68(1.75)  LDD0763  [7]
 LDCM0447  CL56 HCT 116 C220(0.88); C50(1.06); C68(1.19)  LDD0764  [7]
 LDCM0448  CL57 HCT 116 C220(1.05); C50(1.14); C68(1.64)  LDD0765  [7]
 LDCM0449  CL58 HCT 116 C220(0.87); C50(1.47); C68(2.02)  LDD0766  [7]
 LDCM0450  CL59 HCT 116 C220(1.09); C50(0.92); C68(1.27)  LDD0767  [7]
 LDCM0451  CL6 HCT 116 C50(0.62); C68(0.47)  LDD0768  [7]
 LDCM0452  CL60 HCT 116 C220(0.96); C50(1.45); C68(1.43)  LDD0769  [7]
 LDCM0453  CL61 HCT 116 C220(2.34); C50(0.70); C68(0.72)  LDD0770  [7]
 LDCM0454  CL62 HCT 116 C220(1.37); C50(0.66); C68(0.80)  LDD0771  [7]
 LDCM0455  CL63 HCT 116 C220(1.21); C50(0.54); C68(0.57)  LDD0772  [7]
 LDCM0456  CL64 HCT 116 C220(1.19); C50(0.47); C68(0.41)  LDD0773  [7]
 LDCM0457  CL65 HCT 116 C220(1.79); C50(0.68); C68(0.63)  LDD0774  [7]
 LDCM0458  CL66 HCT 116 C220(1.51); C50(0.38); C68(0.24)  LDD0775  [7]
 LDCM0459  CL67 HCT 116 C220(1.23); C50(0.55); C68(0.34)  LDD0776  [7]
 LDCM0460  CL68 HCT 116 C220(1.32); C50(0.58); C68(0.40)  LDD0777  [7]
 LDCM0461  CL69 HCT 116 C220(1.13); C50(0.44); C68(0.37)  LDD0778  [7]
 LDCM0462  CL7 HCT 116 C50(0.68); C68(0.29)  LDD0779  [7]
 LDCM0463  CL70 HCT 116 C220(1.29); C50(0.49); C68(0.42)  LDD0780  [7]
 LDCM0464  CL71 HCT 116 C220(1.03); C50(0.58); C68(0.54)  LDD0781  [7]
 LDCM0465  CL72 HCT 116 C220(1.34); C50(0.82); C68(0.90)  LDD0782  [7]
 LDCM0466  CL73 HCT 116 C220(1.37); C50(0.74); C68(0.74)  LDD0783  [7]
 LDCM0467  CL74 HCT 116 C220(1.75); C50(0.59); C68(0.49)  LDD0784  [7]
 LDCM0469  CL76 HCT 116 C220(1.37); C50(0.98); C68(0.55)  LDD0786  [7]
 LDCM0470  CL77 HCT 116 C220(1.30); C50(1.15); C68(1.15)  LDD0787  [7]
 LDCM0471  CL78 HCT 116 C220(0.89); C50(0.91); C68(0.72)  LDD0788  [7]
 LDCM0472  CL79 HCT 116 C220(1.04); C50(1.08); C68(0.35)  LDD0789  [7]
 LDCM0473  CL8 HCT 116 C50(1.03); C68(0.24)  LDD0790  [7]
 LDCM0474  CL80 HCT 116 C220(0.98); C50(0.90); C68(0.44)  LDD0791  [7]
 LDCM0475  CL81 HCT 116 C220(0.89); C50(1.00); C68(0.54)  LDD0792  [7]
 LDCM0476  CL82 HCT 116 C220(0.85); C50(1.22); C68(0.24)  LDD0793  [7]
 LDCM0477  CL83 HCT 116 C220(1.01); C50(0.97); C68(0.26)  LDD0794  [7]
 LDCM0478  CL84 HCT 116 C220(1.04); C50(1.22); C68(0.33)  LDD0795  [7]
 LDCM0479  CL85 HCT 116 C220(0.96); C50(0.86); C68(0.45)  LDD0796  [7]
 LDCM0480  CL86 HCT 116 C220(1.11); C50(1.29); C68(0.62)  LDD0797  [7]
 LDCM0481  CL87 HCT 116 C220(0.97); C50(0.88); C68(0.42)  LDD0798  [7]
 LDCM0482  CL88 HCT 116 C220(1.01); C50(0.93); C68(0.32)  LDD0799  [7]
 LDCM0483  CL89 HCT 116 C220(1.05); C50(1.45); C68(0.38)  LDD0800  [7]
 LDCM0484  CL9 HCT 116 C50(0.59); C68(0.38)  LDD0801  [7]
 LDCM0485  CL90 HCT 116 C220(0.79); C50(1.36); C68(0.84)  LDD0802  [7]
 LDCM0486  CL91 HCT 116 C220(0.85); C50(0.80); C68(0.64)  LDD0803  [7]
 LDCM0487  CL92 HCT 116 C220(0.75); C50(0.74); C68(0.59)  LDD0804  [7]
 LDCM0488  CL93 HCT 116 C220(0.80); C50(0.86); C68(0.70)  LDD0805  [7]
 LDCM0489  CL94 HCT 116 C220(0.75); C50(0.93); C68(0.41)  LDD0806  [7]
 LDCM0490  CL95 HCT 116 C220(0.80); C50(0.57); C68(0.50)  LDD0807  [7]
 LDCM0491  CL96 HCT 116 C220(0.95); C50(0.85); C68(0.67)  LDD0808  [7]
 LDCM0492  CL97 HCT 116 C220(0.88); C50(0.66); C68(0.56)  LDD0809  [7]
 LDCM0493  CL98 HCT 116 C220(0.90); C50(0.81); C68(0.42)  LDD0810  [7]
 LDCM0494  CL99 HCT 116 C220(0.78); C50(0.60); C68(0.50)  LDD0811  [7]
 LDCM0495  E2913 HEK-293T C205(1.08); C220(0.99); C50(1.01)  LDD1698  [24]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C205(1.17); C220(1.11)  LDD1702  [5]
 LDCM0202  EV-93 T cell C50, C68(4.95)  LDD0527  [25]
 LDCM0625  F8 Ramos C220(1.62)  LDD2187  [26]
 LDCM0572  Fragment10 Ramos C50(0.67)  LDD1466  [27]
 LDCM0573  Fragment11 MDA-MB-231 C50(3.34)  LDD1391  [27]
 LDCM0575  Fragment13 MDA-MB-231 C50(1.06)  LDD1395  [27]
 LDCM0576  Fragment14 MDA-MB-231 C50(1.49)  LDD1397  [27]
 LDCM0579  Fragment20 Ramos C50(20.00)  LDD1403  [27]
 LDCM0580  Fragment21 MDA-MB-231 C50(2.10)  LDD1404  [27]
 LDCM0578  Fragment27 MDA-MB-231 C50(1.67)  LDD1401  [27]
 LDCM0586  Fragment28 Ramos C220(0.87)  LDD2198  [26]
 LDCM0588  Fragment30 Ramos C220(1.08)  LDD2199  [26]
 LDCM0590  Fragment32 Ramos C220(1.03)  LDD2201  [26]
 LDCM0468  Fragment33 HCT 116 C220(1.29); C50(0.79); C68(0.55)  LDD0785  [7]
 LDCM0566  Fragment4 Ramos C50(1.30)  LDD1379  [27]
 LDCM0601  Fragment43 Ramos C50(2.03)  LDD1442  [27]
 LDCM0603  Fragment45 MDA-MB-231 C50(4.13)  LDD1482  [27]
 LDCM0607  Fragment49 MDA-MB-231 C50(3.71)  LDD1448  [27]
 LDCM0427  Fragment51 HCT 116 C50(0.29); C68(0.29)  LDD0744  [7]
 LDCM0610  Fragment52 MDA-MB-231 C50(2.72)  LDD1452  [27]
 LDCM0614  Fragment56 Ramos C220(0.59)  LDD2205  [26]
 LDCM0568  Fragment6 MDA-MB-231 C50(1.45)  LDD1382  [27]
 LDCM0569  Fragment7 MDA-MB-231 C50(0.97)  LDD1383  [27]
 LDCM0570  Fragment8 MDA-MB-231 C50(2.02)  LDD1385  [27]
 LDCM0571  Fragment9 Ramos C50(20.00)  LDD1388  [27]
 LDCM0022  KB02 HCT 116 C50(2.22); C205(1.71)  LDD0080  [7]
 LDCM0023  KB03 HCT 116 C50(1.34); C205(2.27)  LDD0081  [7]
 LDCM0024  KB05 HCT 116 C50(20.00); C205(1.20)  LDD0082  [7]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C205(0.48)  LDD2121  [5]
 LDCM0109  NEM HeLa N.A.  LDD0223  [18]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C205(0.46)  LDD2089  [5]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C205(0.84)  LDD2093  [5]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C205(0.89)  LDD2096  [5]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C205(1.73)  LDD2097  [5]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C205(1.19)  LDD2099  [5]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C205(1.11)  LDD2101  [5]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C205(1.14)  LDD2105  [5]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C205(1.03); C289(1.38)  LDD2107  [5]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C205(1.66)  LDD2108  [5]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C205(0.64)  LDD2109  [5]
 LDCM0517  Nucleophilic fragment 21b MDA-MB-231 C205(1.01)  LDD2110  [5]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C205(0.74)  LDD2111  [5]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C205(1.08)  LDD2115  [5]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C205(1.86)  LDD2119  [5]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C205(0.99)  LDD2120  [5]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C205(1.36)  LDD2122  [5]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C289(1.17)  LDD2123  [5]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C205(0.75); C289(1.47)  LDD2125  [5]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C205(0.88)  LDD2127  [5]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C205(0.84)  LDD2128  [5]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C205(1.03)  LDD2129  [5]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C205(0.91)  LDD2133  [5]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C205(0.86)  LDD2134  [5]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C205(1.15)  LDD2135  [5]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C289(1.05)  LDD2137  [5]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C205(1.58)  LDD1700  [5]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C205(0.77)  LDD2140  [5]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C205(2.27)  LDD2144  [5]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C205(0.87)  LDD2146  [5]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C205(0.91)  LDD2148  [5]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C205(0.36)  LDD2150  [5]
 LDCM0557  Nucleophilic fragment 8b MDA-MB-231 C205(1.13)  LDD2151  [5]
 LDCM0131  RA190 MM1.R C50(1.27)  LDD0304  [28]
 LDCM0021  THZ1 HCT 116 C205(1.01)  LDD2173  [7]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Histone acetyltransferase KAT5 (KAT5) MYST (SAS/MOZ) family Q92993
Aurora kinase B (AURKB) Ser/Thr protein kinase family Q96GD4
Serine/threonine-protein kinase PLK3 (PLK3) Ser/Thr protein kinase family Q9H4B4
E3 ubiquitin-protein ligase RNF8 (RNF8) RNF8 family O76064
GTP-binding nuclear protein Ran (RAN) Ran family P62826
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cellular tumor antigen p53 (TP53) P53 family P04637
Transcription factor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Transcription factor Jun (JUN) BZIP family P05412
Transcription factor SOX-2 (SOX2) . P48431
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cyclic AMP-dependent transcription factor ATF-2 (ATF2) BZIP family P15336
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Coilin (COIL) Coilin family P38432
Histone H2AX (H2AX) Histone H2A family P16104
Nibrin (NBN) . O60934
TP53-binding protein 1 (TP53BP1) . Q12888

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 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.
3 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.
4 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
5 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
6 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
7 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.
8 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.
9 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
10 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
11 SP3-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
12 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
13 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
14 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
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 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.
19 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.
20 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
21 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.
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 Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications. ACS Chem Biol. 2019 Nov 15;14(11):2430-2440. doi: 10.1021/acschembio.8b01083. Epub 2019 May 13.
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 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.
26 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
27 Proteome-wide covalent ligand discovery in native biological systems. Nature. 2016 Jun 23;534(7608):570-4. doi: 10.1038/nature18002. Epub 2016 Jun 15.
28 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.