Details of the Target

General Information of Target

Target ID LDTP02164
Target Name Nucleophosmin (NPM1)
Gene Name NPM1
Gene ID 4869
Synonyms
NPM; Nucleophosmin; NPM; Nucleolar phosphoprotein B23; Nucleolar protein NO38; Numatrin
3D Structure
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2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MEDSMDMDMSPLRPQNYLFGCELKADKDYHFKVDNDENEHQLSLRTVSLGAGAKDELHIV
EAEAMNYEGSPIKVTLATLKMSVQPTVSLGGFEITPPVVLRLKCGSGPVHISGQHLVAVE
EDAESEDEEEEDVKLLSISGKRSAPGGGSKVPQKKVKLAADEDDDDDDEEDDDEDDDDDD
FDDEEAEEKAPVKKSIRDTPAKNAQKSNQNGKDSKPSSTPRSKGQESFKKQEKTPKTPKG
PSSVEDIKAKMQASIEKGGSLPKVEAKFINYVKNCFRMTDQEAIQDLWQWRKSL
Target Type
Clinical trial
Target Bioclass
Other
Family
Nucleoplasmin family
Subcellular location
Nucleus, nucleolus
Function
Involved in diverse cellular processes such as ribosome biogenesis, centrosome duplication, protein chaperoning, histone assembly, cell proliferation, and regulation of tumor suppressors p53/TP53 and ARF. Binds ribosome presumably to drive ribosome nuclear export. Associated with nucleolar ribonucleoprotein structures and bind single-stranded nucleic acids. Acts as a chaperonin for the core histones H3, H2B and H4. Stimulates APEX1 endonuclease activity on apurinic/apyrimidinic (AP) double-stranded DNA but inhibits APEX1 endonuclease activity on AP single-stranded RNA. May exert a control of APEX1 endonuclease activity within nucleoli devoted to repair AP on rDNA and the removal of oxidized rRNA molecules. In concert with BRCA2, regulates centrosome duplication. Regulates centriole duplication: phosphorylation by PLK2 is able to trigger centriole replication. Negatively regulates the activation of EIF2AK2/PKR and suppresses apoptosis through inhibition of EIF2AK2/PKR autophosphorylation. Antagonizes the inhibitory effect of ATF5 on cell proliferation and relieves ATF5-induced G2/M blockade. In complex with MYC enhances the transcription of MYC target genes. May act as chaperonin or cotransporter in the nucleolar localization of transcription termination factor TTF1.
TTD ID
T45591
Uniprot ID
P06748
DrugMap ID
TTHBS98
Ensemble ID
ENST00000296930.10
HGNC ID
HGNC:7910
ChEMBL ID
CHEMBL5178

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
Ishikawa (Heraklio) 02 ER SNV: p.K141R .
TYKNU SNV: p.A186V .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 49 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [2]
P1
 Probe Info  		1.50  LDD0452  [3]
P2
 Probe Info  		1.53  LDD0449  [3]
P8
 Probe Info  		1.95  LDD0451  [3]
A-EBA
 Probe Info  		3.84  LDD0215  [4]
CY-1
 Probe Info  		21.80  LDD0243  [5]
CY4
 Probe Info  		3.50  LDD0244  [5]
N1
 Probe Info  		3.27  LDD0242  [5]
C-Sul
 Probe Info  		2.45  LDD0066  [6]
TH211
 Probe Info  		Y29(20.00); Y271(6.45)  LDD0257  [7]
TH214
 Probe Info  		Y29(11.70)  LDD0258  [7]
TH216
 Probe Info  		Y29(18.66); Y271(10.22)  LDD0259  [7]
YN-4
 Probe Info  		100.00  LDD0445  [8]
AZ-9
 Probe Info  		E256(0.93); E245(1.46)  LDD2208  [9]
ONAyne
 Probe Info  		K236(0.00); K202(0.00); K215(0.00); K150(0.00)  LDD0273  [10]
Probe 1
 Probe Info  		Y67(19.55)  LDD3495  [11]
Alkylaryl probe 3
 Probe Info  		3.36  LDD0384  [12]
BTD
 Probe Info  		C21(2.04)  LDD2092  [13]
EA-probe
 Probe Info  		N.A.  LDD0440  [14]
HHS-482
 Probe Info  		Y271(0.90); Y29(1.04); Y67(0.60)  LDD0285  [15]
HHS-475
 Probe Info  		Y271(0.95); Y67(1.01); Y29(1.41)  LDD0264  [16]
HHS-465
 Probe Info  		Y29(9.75); Y67(2.48)  LDD2237  [17]
DBIA
 Probe Info  		C275(0.98)  LDD0532  [18]
5E-2FA
 Probe Info  		H30(0.00); H40(0.00)  LDD2235  [19]
AMP probe
 Probe Info  		K267(0.00); K223(0.00); K239(0.00); K250(0.00)  LDD0200  [20]
ATP probe
 Probe Info  		K267(0.00); K223(0.00); K239(0.00); K250(0.00)  LDD0199  [20]
IA-alkyne
 Probe Info  		N.A.  LDD0032  [21]
ATP probe
 Probe Info  		K32(0.00); K27(0.00); K212(0.00); K250(0.00)  LDD0035  [22]
IPM
 Probe Info  		N.A.  LDD0025  [23]
JW-RF-010
 Probe Info  		C275(0.00); C104(0.00)  LDD0026  [23]
NAIA_4
 Probe Info  		N.A.  LDD2226  [24]
1d-yne
 Probe Info  		K80(0.00); K54(0.00); K32(0.00); K73(0.00)  LDD0356  [25]
Compound 10
 Probe Info  		N.A.  LDD2216  [26]
NHS
 Probe Info  		K32(0.00); K212(0.00); K239(0.00); K54(0.00)  LDD0010  [27]
OSF
 Probe Info  		N.A.  LDD0029  [28]
SF
 Probe Info  		K257(0.00); K248(0.00); K212(0.00); K233(0.00)  LDD0028  [28]
STPyne
 Probe Info  		K257(0.00); K32(0.00); K212(0.00); K150(0.00)  LDD0009  [27]
TFBX
 Probe Info  		C275(0.00); C104(0.00)  LDD0148  [23]
VSF
 Probe Info  		N.A.  LDD0007  [27]
Phosphinate-6
 Probe Info  		C21(0.00); C275(0.00); C104(0.00)  LDD0018  [29]
Ox-W18
 Probe Info  		W288(0.00); W290(0.00)  LDD2175  [30]
1c-yne
 Probe Info  		K212(0.00); K215(0.00); K27(0.00); K32(0.00)  LDD0228  [25]
Acrolein
 Probe Info  		H58(0.00); C104(0.00); H40(0.00); H30(0.00)  LDD0217  [31]
Crotonaldehyde
 Probe Info  		H40(0.00); H30(0.00); C21(0.00)  LDD0219  [31]
Methacrolein
 Probe Info  		H40(0.00); H30(0.00); C21(0.00)  LDD0218  [31]
W1
 Probe Info  		N.A.  LDD0236  [32]
AOyne
 Probe Info  		14.80  LDD0443  [33]
MPP-AC
 Probe Info  		N.A.  LDD0428  [34]
NAIA_5
 Probe Info  		C104(0.00); C21(0.00); C275(0.00)  LDD2223  [24]
PAL-AfBPP Probe
Click To Hide/Show 13 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C187
 Probe Info  		20.25  LDD1865  [35]
C191
 Probe Info  		12.30  LDD1868  [35]
C193
 Probe Info  		7.06  LDD1869  [35]
FFF probe13
 Probe Info  		7.02  LDD0475  [36]
STS-1
 Probe Info  		N.A.  LDD0136  [37]
STS-2
 Probe Info  		N.A.  LDD0138  [37]
VE-P
 Probe Info  		N.A.  LDD0396  [38]
Diazir
 Probe Info  		E93(0.00); E37(0.00); E39(0.00)  LDD0011  [27]
BD-F
 Probe Info  		V99(0.00); S88(0.00); T95(0.00); E93(0.00)  LDD0024  [39]
Photocelecoxib
 Probe Info  		G90(0.00); E93(0.00)  LDD0019  [40]
Photoindomethacin
 Probe Info  		N.A.  LDD0154  [40]
Photonaproxen
 Probe Info  		V33(0.00); D34(0.00); E39(0.00); E93(0.00)  LDD0156  [40]
DA-2
 Probe Info  		N.A.  LDD0071  [41]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C21(0.60)  LDD2112  [13]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C21(0.99)  LDD2117  [13]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C21(0.44)  LDD2132  [13]
 LDCM0215  AC10 HCT 116 C275(0.98)  LDD0532  [18]
 LDCM0216  AC100 HEK-293T C275(1.54)  LDD0814  [18]
 LDCM0217  AC101 HEK-293T C275(0.84)  LDD0815  [18]
 LDCM0218  AC102 HEK-293T C275(0.50)  LDD0816  [18]
 LDCM0219  AC103 HEK-293T C275(0.61)  LDD0817  [18]
 LDCM0220  AC104 HEK-293T C275(0.87)  LDD0818  [18]
 LDCM0221  AC105 HEK-293T C275(1.07)  LDD0819  [18]
 LDCM0222  AC106 HEK-293T C275(0.76)  LDD0820  [18]
 LDCM0223  AC107 HEK-293T C275(0.46)  LDD0821  [18]
 LDCM0224  AC108 HEK-293T C275(0.70)  LDD0822  [18]
 LDCM0225  AC109 HEK-293T C275(0.37)  LDD0823  [18]
 LDCM0226  AC11 HCT 116 C275(0.74)  LDD0543  [18]
 LDCM0227  AC110 HEK-293T C275(1.17)  LDD0825  [18]
 LDCM0228  AC111 HEK-293T C275(0.73)  LDD0826  [18]
 LDCM0229  AC112 HEK-293T C275(0.83)  LDD0827  [18]
 LDCM0237  AC12 HCT 116 C275(0.47)  LDD0554  [18]
 LDCM0246  AC128 PaTu 8988t C275(0.97)  LDD1125  [18]
 LDCM0247  AC129 PaTu 8988t C275(0.85)  LDD1126  [18]
 LDCM0249  AC130 PaTu 8988t C275(0.74)  LDD1128  [18]
 LDCM0250  AC131 PaTu 8988t C275(0.95)  LDD1129  [18]
 LDCM0251  AC132 PaTu 8988t C275(0.72)  LDD1130  [18]
 LDCM0252  AC133 PaTu 8988t C275(1.39)  LDD1131  [18]
 LDCM0253  AC134 PaTu 8988t C275(1.43)  LDD1132  [18]
 LDCM0254  AC135 PaTu 8988t C275(0.95)  LDD1133  [18]
 LDCM0255  AC136 PaTu 8988t C275(1.15)  LDD1134  [18]
 LDCM0256  AC137 PaTu 8988t C275(1.71)  LDD1135  [18]
 LDCM0257  AC138 PaTu 8988t C275(0.98)  LDD1136  [18]
 LDCM0258  AC139 PaTu 8988t C275(0.78)  LDD1137  [18]
 LDCM0259  AC14 HCT 116 C275(0.96)  LDD0576  [18]
 LDCM0260  AC140 PaTu 8988t C275(0.32)  LDD1139  [18]
 LDCM0261  AC141 PaTu 8988t C275(0.91)  LDD1140  [18]
 LDCM0262  AC142 PaTu 8988t C275(0.88)  LDD1141  [18]
 LDCM0263  AC143 HEK-293T C275(0.48)  LDD0861  [18]
 LDCM0264  AC144 HEK-293T C275(0.97)  LDD0862  [18]
 LDCM0265  AC145 HEK-293T C275(0.95)  LDD0863  [18]
 LDCM0266  AC146 HEK-293T C275(1.25)  LDD0864  [18]
 LDCM0267  AC147 HEK-293T C275(0.61)  LDD0865  [18]
 LDCM0268  AC148 HEK-293T C275(1.19)  LDD0866  [18]
 LDCM0269  AC149 HEK-293T C275(1.49)  LDD0867  [18]
 LDCM0270  AC15 HCT 116 C275(1.23)  LDD0587  [18]
 LDCM0271  AC150 HEK-293T C275(1.66)  LDD0869  [18]
 LDCM0272  AC151 HEK-293T C275(1.87)  LDD0870  [18]
 LDCM0273  AC152 HEK-293T C275(1.59)  LDD0871  [18]
 LDCM0274  AC153 HEK-293T C275(1.28)  LDD0872  [18]
 LDCM0621  AC154 HEK-293T C275(0.45)  LDD2162  [18]
 LDCM0622  AC155 HEK-293T C275(0.62)  LDD2163  [18]
 LDCM0623  AC156 HEK-293T C275(1.13)  LDD2164  [18]
 LDCM0624  AC157 HEK-293T C275(1.78)  LDD2165  [18]
 LDCM0276  AC17 HCT 116 C275(1.00)  LDD0593  [18]
 LDCM0277  AC18 HCT 116 C275(0.88)  LDD0594  [18]
 LDCM0278  AC19 HCT 116 C275(0.88)  LDD0595  [18]
 LDCM0280  AC20 HCT 116 C275(0.20)  LDD0597  [18]
 LDCM0281  AC21 HCT 116 C275(0.66)  LDD0598  [18]
 LDCM0282  AC22 HCT 116 C275(0.47)  LDD0599  [18]
 LDCM0283  AC23 HCT 116 C275(0.36)  LDD0600  [18]
 LDCM0284  AC24 HCT 116 C275(0.92)  LDD0601  [18]
 LDCM0285  AC25 HEK-293T C275(0.98)  LDD0883  [18]
 LDCM0286  AC26 HEK-293T C275(1.12)  LDD0884  [18]
 LDCM0287  AC27 HEK-293T C275(1.17)  LDD0885  [18]
 LDCM0288  AC28 HEK-293T C275(0.78)  LDD0886  [18]
 LDCM0289  AC29 HEK-293T C275(1.08)  LDD0887  [18]
 LDCM0291  AC30 HEK-293T C275(1.06)  LDD0889  [18]
 LDCM0292  AC31 HEK-293T C275(0.90)  LDD0890  [18]
 LDCM0293  AC32 HEK-293T C275(0.98)  LDD0891  [18]
 LDCM0294  AC33 HEK-293T C275(1.01)  LDD0892  [18]
 LDCM0295  AC34 HEK-293T C275(0.96)  LDD0893  [18]
 LDCM0296  AC35 HEK-293T C275(1.38)  LDD0894  [18]
 LDCM0297  AC36 HEK-293T C275(0.82)  LDD0895  [18]
 LDCM0298  AC37 HEK-293T C275(1.08)  LDD0896  [18]
 LDCM0299  AC38 HEK-293T C275(1.52)  LDD0897  [18]
 LDCM0300  AC39 HEK-293T C275(1.14)  LDD0898  [18]
 LDCM0302  AC40 HEK-293T C275(0.95)  LDD0900  [18]
 LDCM0303  AC41 HEK-293T C275(0.94)  LDD0901  [18]
 LDCM0304  AC42 HEK-293T C275(1.77)  LDD0902  [18]
 LDCM0305  AC43 HEK-293T C275(1.29)  LDD0903  [18]
 LDCM0306  AC44 HEK-293T C275(1.44)  LDD0904  [18]
 LDCM0307  AC45 HEK-293T C275(1.06)  LDD0905  [18]
 LDCM0308  AC46 HEK-293T C275(1.00)  LDD0906  [18]
 LDCM0309  AC47 HEK-293T C275(1.17)  LDD0907  [18]
 LDCM0310  AC48 HEK-293T C275(1.10)  LDD0908  [18]
 LDCM0311  AC49 HEK-293T C275(1.10)  LDD0909  [18]
 LDCM0313  AC50 HEK-293T C275(1.36)  LDD0911  [18]
 LDCM0314  AC51 HEK-293T C275(1.35)  LDD0912  [18]
 LDCM0315  AC52 HEK-293T C275(1.49)  LDD0913  [18]
 LDCM0316  AC53 HEK-293T C275(1.08)  LDD0914  [18]
 LDCM0317  AC54 HEK-293T C275(1.73)  LDD0915  [18]
 LDCM0318  AC55 HEK-293T C275(1.32)  LDD0916  [18]
 LDCM0319  AC56 HEK-293T C275(1.27)  LDD0917  [18]
 LDCM0320  AC57 HCT 116 C275(1.86)  LDD0637  [18]
 LDCM0321  AC58 HCT 116 C275(1.08)  LDD0638  [18]
 LDCM0322  AC59 HCT 116 C275(1.10)  LDD0639  [18]
 LDCM0323  AC6 HCT 116 C275(1.41)  LDD0640  [18]
 LDCM0324  AC60 HCT 116 C275(4.35)  LDD0641  [18]
 LDCM0325  AC61 HCT 116 C275(0.73)  LDD0642  [18]
 LDCM0326  AC62 HCT 116 C275(1.38)  LDD0643  [18]
 LDCM0327  AC63 HCT 116 C275(1.79)  LDD0644  [18]
 LDCM0328  AC64 HCT 116 C275(1.44)  LDD0645  [18]
 LDCM0329  AC65 HCT 116 C275(2.48)  LDD0646  [18]
 LDCM0330  AC66 HCT 116 C275(2.15)  LDD0647  [18]
 LDCM0331  AC67 HCT 116 C275(1.22)  LDD0648  [18]
 LDCM0332  AC68 HCT 116 C275(0.62)  LDD0649  [18]
 LDCM0333  AC69 HCT 116 C275(0.73)  LDD0650  [18]
 LDCM0334  AC7 HCT 116 C275(0.93)  LDD0651  [18]
 LDCM0335  AC70 HCT 116 C275(0.79)  LDD0652  [18]
 LDCM0336  AC71 HCT 116 C275(0.75)  LDD0653  [18]
 LDCM0337  AC72 HCT 116 C275(1.14)  LDD0654  [18]
 LDCM0338  AC73 HCT 116 C275(0.82)  LDD0655  [18]
 LDCM0339  AC74 HCT 116 C275(0.87)  LDD0656  [18]
 LDCM0340  AC75 HCT 116 C275(1.11)  LDD0657  [18]
 LDCM0341  AC76 HCT 116 C275(0.92)  LDD0658  [18]
 LDCM0342  AC77 HCT 116 C275(0.71)  LDD0659  [18]
 LDCM0343  AC78 HCT 116 C275(0.93)  LDD0660  [18]
 LDCM0344  AC79 HCT 116 C275(1.08)  LDD0661  [18]
 LDCM0345  AC8 HCT 116 C275(1.23)  LDD0662  [18]
 LDCM0346  AC80 HCT 116 C275(0.92)  LDD0663  [18]
 LDCM0347  AC81 HCT 116 C275(0.79)  LDD0664  [18]
 LDCM0348  AC82 HCT 116 C275(0.74)  LDD0665  [18]
 LDCM0349  AC83 HEK-293T C275(1.07)  LDD0947  [18]
 LDCM0350  AC84 HEK-293T C275(1.60)  LDD0948  [18]
 LDCM0351  AC85 HEK-293T C275(0.84)  LDD0949  [18]
 LDCM0352  AC86 HEK-293T C275(1.36)  LDD0950  [18]
 LDCM0353  AC87 HEK-293T C275(1.35)  LDD0951  [18]
 LDCM0354  AC88 HEK-293T C275(1.16)  LDD0952  [18]
 LDCM0355  AC89 HEK-293T C275(1.33)  LDD0953  [18]
 LDCM0357  AC90 HEK-293T C275(1.23)  LDD0955  [18]
 LDCM0358  AC91 HEK-293T C275(1.14)  LDD0956  [18]
 LDCM0359  AC92 HEK-293T C275(1.28)  LDD0957  [18]
 LDCM0360  AC93 HEK-293T C275(0.91)  LDD0958  [18]
 LDCM0361  AC94 HEK-293T C275(0.82)  LDD0959  [18]
 LDCM0362  AC95 HEK-293T C275(1.05)  LDD0960  [18]
 LDCM0363  AC96 HEK-293T C275(1.06)  LDD0961  [18]
 LDCM0364  AC97 HEK-293T C275(1.90)  LDD0962  [18]
 LDCM0365  AC98 HEK-293T C275(1.35)  LDD0963  [18]
 LDCM0366  AC99 HEK-293T C275(0.76)  LDD0964  [18]
 LDCM0520  AKOS000195272 MDA-MB-231 C21(1.07)  LDD2113  [13]
 LDCM0248  AKOS034007472 HCT 116 C275(0.90)  LDD0565  [18]
 LDCM0356  AKOS034007680 HCT 116 C275(0.90)  LDD0673  [18]
 LDCM0275  AKOS034007705 HCT 116 C275(1.37)  LDD0592  [18]
 LDCM0156  Aniline NCI-H1299 12.44  LDD0403  [2]
 LDCM0108  Chloroacetamide HeLa H58(0.00); C104(0.00); H30(0.00); H40(0.00)  LDD0222  [31]
 LDCM0367  CL1 PaTu 8988t C275(1.46)  LDD1246  [18]
 LDCM0368  CL10 PaTu 8988t C275(0.90)  LDD1247  [18]
 LDCM0370  CL101 HCT 116 C275(1.25)  LDD0687  [18]
 LDCM0371  CL102 HCT 116 C275(0.84)  LDD0688  [18]
 LDCM0372  CL103 HCT 116 C275(0.73)  LDD0689  [18]
 LDCM0373  CL104 HCT 116 C275(1.22)  LDD0690  [18]
 LDCM0374  CL105 HCT 116 C275(0.95)  LDD0691  [18]
 LDCM0375  CL106 HCT 116 C275(1.26)  LDD0692  [18]
 LDCM0376  CL107 HCT 116 C275(0.84)  LDD0693  [18]
 LDCM0377  CL108 HCT 116 C275(1.37)  LDD0694  [18]
 LDCM0378  CL109 HCT 116 C275(0.38)  LDD0695  [18]
 LDCM0379  CL11 PaTu 8988t C275(0.89)  LDD1258  [18]
 LDCM0380  CL110 HCT 116 C275(0.48)  LDD0697  [18]
 LDCM0381  CL111 HCT 116 C275(0.86)  LDD0698  [18]
 LDCM0382  CL112 HEK-293T C275(0.95)  LDD0980  [18]
 LDCM0383  CL113 HEK-293T C275(0.96)  LDD0981  [18]
 LDCM0384  CL114 HEK-293T C275(1.10)  LDD0982  [18]
 LDCM0385  CL115 HEK-293T C275(0.86)  LDD0983  [18]
 LDCM0386  CL116 HEK-293T C275(1.21)  LDD0984  [18]
 LDCM0387  CL117 HEK-293T C275(0.90)  LDD0985  [18]
 LDCM0388  CL118 HEK-293T C275(1.24)  LDD0986  [18]
 LDCM0389  CL119 HEK-293T C275(1.09)  LDD0987  [18]
 LDCM0390  CL12 PaTu 8988t C275(0.84)  LDD1269  [18]
 LDCM0391  CL120 HEK-293T C275(1.08)  LDD0989  [18]
 LDCM0392  CL121 HEK-293T C275(1.11)  LDD0990  [18]
 LDCM0393  CL122 HEK-293T C275(1.15)  LDD0991  [18]
 LDCM0394  CL123 HEK-293T C275(0.79)  LDD0992  [18]
 LDCM0395  CL124 HEK-293T C275(0.91)  LDD0993  [18]
 LDCM0396  CL125 HCT 116 C275(2.15)  LDD0713  [18]
 LDCM0397  CL126 HCT 116 C275(2.02)  LDD0714  [18]
 LDCM0398  CL127 HCT 116 C275(1.90)  LDD0715  [18]
 LDCM0399  CL128 HCT 116 C275(2.32)  LDD0716  [18]
 LDCM0400  CL13 PaTu 8988t C275(2.68)  LDD1279  [18]
 LDCM0401  CL14 PaTu 8988t C275(1.72)  LDD1280  [18]
 LDCM0402  CL15 PaTu 8988t C275(1.71)  LDD1281  [18]
 LDCM0403  CL16 HCT 116 C275(2.85)  LDD0720  [18]
 LDCM0404  CL17 HCT 116 C275(0.65)  LDD0721  [18]
 LDCM0405  CL18 HCT 116 C275(1.97)  LDD0722  [18]
 LDCM0406  CL19 HCT 116 C275(2.61)  LDD0723  [18]
 LDCM0407  CL2 PaTu 8988t C275(1.56)  LDD1286  [18]
 LDCM0408  CL20 HCT 116 C275(2.20)  LDD0725  [18]
 LDCM0409  CL21 HCT 116 C275(2.28)  LDD0726  [18]
 LDCM0410  CL22 HCT 116 C275(2.95)  LDD0727  [18]
 LDCM0411  CL23 HCT 116 C275(0.76)  LDD0728  [18]
 LDCM0412  CL24 HCT 116 C275(2.99)  LDD0729  [18]
 LDCM0413  CL25 HCT 116 C275(2.12)  LDD0730  [18]
 LDCM0414  CL26 HCT 116 C275(2.74)  LDD0731  [18]
 LDCM0415  CL27 HCT 116 C275(2.78)  LDD0732  [18]
 LDCM0416  CL28 HCT 116 C275(2.20)  LDD0733  [18]
 LDCM0417  CL29 HCT 116 C275(1.98)  LDD0734  [18]
 LDCM0418  CL3 PaTu 8988t C275(1.45)  LDD1297  [18]
 LDCM0419  CL30 HCT 116 C275(1.82)  LDD0736  [18]
 LDCM0420  CL31 HCT 116 C275(0.97)  LDD0737  [18]
 LDCM0421  CL32 HCT 116 C275(0.87)  LDD0738  [18]
 LDCM0422  CL33 HCT 116 C275(0.12)  LDD0739  [18]
 LDCM0423  CL34 HCT 116 C275(1.82)  LDD0740  [18]
 LDCM0424  CL35 HCT 116 C275(2.31)  LDD0741  [18]
 LDCM0425  CL36 HCT 116 C275(1.51)  LDD0742  [18]
 LDCM0426  CL37 HCT 116 C275(1.18)  LDD0743  [18]
 LDCM0428  CL39 HCT 116 C275(0.23)  LDD0745  [18]
 LDCM0429  CL4 PaTu 8988t C275(0.81)  LDD1308  [18]
 LDCM0430  CL40 HCT 116 C275(1.59)  LDD0747  [18]
 LDCM0431  CL41 HCT 116 C275(2.05)  LDD0748  [18]
 LDCM0432  CL42 HCT 116 C275(0.22)  LDD0749  [18]
 LDCM0433  CL43 HCT 116 C275(2.13)  LDD0750  [18]
 LDCM0434  CL44 HCT 116 C275(2.31)  LDD0751  [18]
 LDCM0435  CL45 HCT 116 C275(1.79)  LDD0752  [18]
 LDCM0436  CL46 HCT 116 C275(1.93)  LDD0753  [18]
 LDCM0437  CL47 HCT 116 C275(1.44)  LDD0754  [18]
 LDCM0438  CL48 HCT 116 C275(1.60)  LDD0755  [18]
 LDCM0439  CL49 HCT 116 C275(1.61)  LDD0756  [18]
 LDCM0440  CL5 PaTu 8988t C275(2.45)  LDD1319  [18]
 LDCM0441  CL50 HCT 116 C275(1.32)  LDD0758  [18]
 LDCM0442  CL51 HCT 116 C275(1.01)  LDD0759  [18]
 LDCM0443  CL52 HCT 116 C275(1.74)  LDD0760  [18]
 LDCM0444  CL53 HCT 116 C275(1.08)  LDD0761  [18]
 LDCM0445  CL54 HCT 116 C275(3.00)  LDD0762  [18]
 LDCM0446  CL55 HCT 116 C275(2.50)  LDD0763  [18]
 LDCM0447  CL56 HCT 116 C275(2.52)  LDD0764  [18]
 LDCM0448  CL57 HCT 116 C275(1.19)  LDD0765  [18]
 LDCM0449  CL58 HCT 116 C275(2.75)  LDD0766  [18]
 LDCM0450  CL59 HCT 116 C275(2.62)  LDD0767  [18]
 LDCM0451  CL6 PaTu 8988t C275(1.75)  LDD1330  [18]
 LDCM0452  CL60 HCT 116 C275(1.31)  LDD0769  [18]
 LDCM0453  CL61 HCT 116 C275(1.45)  LDD0770  [18]
 LDCM0454  CL62 HCT 116 C275(1.43)  LDD0771  [18]
 LDCM0455  CL63 HCT 116 C275(1.38)  LDD0772  [18]
 LDCM0456  CL64 HCT 116 C275(1.64)  LDD0773  [18]
 LDCM0457  CL65 HCT 116 C275(1.28)  LDD0774  [18]
 LDCM0458  CL66 HCT 116 C275(1.18)  LDD0775  [18]
 LDCM0459  CL67 HCT 116 C275(0.66)  LDD0776  [18]
 LDCM0460  CL68 HCT 116 C275(1.09)  LDD0777  [18]
 LDCM0461  CL69 HCT 116 C275(2.14)  LDD0778  [18]
 LDCM0462  CL7 PaTu 8988t C275(2.46)  LDD1341  [18]
 LDCM0463  CL70 HCT 116 C275(2.11)  LDD0780  [18]
 LDCM0464  CL71 HCT 116 C275(1.49)  LDD0781  [18]
 LDCM0465  CL72 HCT 116 C275(1.67)  LDD0782  [18]
 LDCM0466  CL73 HCT 116 C275(1.72)  LDD0783  [18]
 LDCM0467  CL74 HCT 116 C275(1.22)  LDD0784  [18]
 LDCM0469  CL76 HEK-293T C275(1.02)  LDD1067  [18]
 LDCM0470  CL77 HEK-293T C275(0.94)  LDD1068  [18]
 LDCM0471  CL78 HEK-293T C275(0.80)  LDD1069  [18]
 LDCM0472  CL79 HEK-293T C275(0.99)  LDD1070  [18]
 LDCM0473  CL8 PaTu 8988t C275(1.69)  LDD1352  [18]
 LDCM0474  CL80 HEK-293T C275(0.88)  LDD1072  [18]
 LDCM0475  CL81 HEK-293T C275(1.03)  LDD1073  [18]
 LDCM0476  CL82 HEK-293T C275(1.04)  LDD1074  [18]
 LDCM0477  CL83 HEK-293T C275(1.18)  LDD1075  [18]
 LDCM0478  CL84 HEK-293T C275(0.94)  LDD1076  [18]
 LDCM0479  CL85 HEK-293T C275(1.12)  LDD1077  [18]
 LDCM0480  CL86 HEK-293T C275(1.23)  LDD1078  [18]
 LDCM0481  CL87 HEK-293T C275(0.98)  LDD1079  [18]
 LDCM0482  CL88 HEK-293T C275(1.25)  LDD1080  [18]
 LDCM0483  CL89 HEK-293T C275(0.99)  LDD1081  [18]
 LDCM0484  CL9 PaTu 8988t C275(0.97)  LDD1363  [18]
 LDCM0485  CL90 HEK-293T C275(1.12)  LDD1083  [18]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C21(0.99)  LDD1702  [13]
 LDCM0175  Ethacrynic acid HeLa N.A.  LDD0440  [14]
 LDCM0625  F8 Ramos C275(1.01); C104(6.20)  LDD2187  [42]
 LDCM0572  Fragment10 Ramos C275(0.31); C104(1.47)  LDD2189  [42]
 LDCM0573  Fragment11 Ramos C275(0.87)  LDD2190  [42]
 LDCM0574  Fragment12 Ramos C275(0.39)  LDD2191  [42]
 LDCM0575  Fragment13 Ramos C275(0.90)  LDD2192  [42]
 LDCM0576  Fragment14 Ramos C275(0.34); C104(0.76)  LDD2193  [42]
 LDCM0579  Fragment20 Ramos C275(0.25); C104(0.95)  LDD2194  [42]
 LDCM0580  Fragment21 Ramos C275(0.63)  LDD2195  [42]
 LDCM0582  Fragment23 Ramos C275(1.26)  LDD2196  [42]
 LDCM0578  Fragment27 Ramos C275(1.10)  LDD2197  [42]
 LDCM0586  Fragment28 Ramos C275(0.99)  LDD2198  [42]
 LDCM0588  Fragment30 Ramos C275(0.95); C104(0.73)  LDD2199  [42]
 LDCM0589  Fragment31 Ramos C275(0.74)  LDD2200  [42]
 LDCM0590  Fragment32 Ramos C275(0.39); C104(0.30)  LDD2201  [42]
 LDCM0468  Fragment33 HCT 116 C275(1.56)  LDD0785  [18]
 LDCM0596  Fragment38 Ramos C275(0.92)  LDD2203  [42]
 LDCM0566  Fragment4 Ramos C275(1.01)  LDD2184  [42]
 LDCM0427  Fragment51 HCT 116 C275(1.98)  LDD0744  [18]
 LDCM0610  Fragment52 Ramos C275(0.93)  LDD2204  [42]
 LDCM0614  Fragment56 Ramos C275(0.90)  LDD2205  [42]
 LDCM0569  Fragment7 Ramos C275(0.39)  LDD2186  [42]
 LDCM0571  Fragment9 Ramos C275(0.24)  LDD2188  [42]
 LDCM0149  GA MCF-7 C275(2.06)  LDD0379  [43]
 LDCM0116  HHS-0101 DM93 Y271(0.95); Y67(1.01); Y29(1.41)  LDD0264  [16]
 LDCM0117  HHS-0201 DM93 Y29(0.84); Y271(0.91); Y67(1.81)  LDD0265  [16]
 LDCM0118  HHS-0301 DM93 Y271(0.91); Y29(0.93); Y67(2.07)  LDD0266  [16]
 LDCM0119  HHS-0401 DM93 Y29(0.78); Y271(0.94); Y67(1.74)  LDD0267  [16]
 LDCM0120  HHS-0701 DM93 Y29(0.80); Y271(0.80); Y67(0.96)  LDD0268  [16]
 LDCM0107  IAA HeLa H58(0.00); H40(0.00); H30(0.00); C21(0.00)  LDD0221  [31]
 LDCM0123  JWB131 DM93 Y271(0.90); Y29(1.04); Y67(0.60)  LDD0285  [15]
 LDCM0124  JWB142 DM93 Y271(0.84); Y29(0.93); Y67(0.51)  LDD0286  [15]
 LDCM0125  JWB146 DM93 Y271(0.95); Y29(1.15); Y67(0.73)  LDD0287  [15]
 LDCM0126  JWB150 DM93 Y271(2.83); Y29(3.18); Y67(2.50)  LDD0288  [15]
 LDCM0127  JWB152 DM93 Y271(2.11); Y29(2.07); Y67(0.42)  LDD0289  [15]
 LDCM0128  JWB198 DM93 Y271(1.05); Y29(1.36)  LDD0290  [15]
 LDCM0129  JWB202 DM93 Y271(0.72); Y29(0.69); Y67(0.59)  LDD0291  [15]
 LDCM0130  JWB211 DM93 Y271(0.95); Y29(1.26); Y67(0.37)  LDD0292  [15]
 LDCM0022  KB02 Ramos C275(0.28); C104(1.38)  LDD2182  [42]
 LDCM0023  KB03 MDA-MB-231 C21(3.11)  LDD1701  [13]
 LDCM0024  KB05 MV4-11 C104(1.98)  LDD3338  [44]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C21(1.04)  LDD2102  [13]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C21(1.40)  LDD2121  [13]
 LDCM0109  NEM HeLa H58(0.00); H30(0.00); H40(0.00); H115(0.00)  LDD0223  [31]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C21(2.04)  LDD2092  [13]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C21(1.17)  LDD2094  [13]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C21(1.05)  LDD2097  [13]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C21(0.92)  LDD2098  [13]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C21(1.71)  LDD2099  [13]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C21(0.44)  LDD2100  [13]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C21(0.96)  LDD2101  [13]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C21(0.30)  LDD2106  [13]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C21(1.19)  LDD2107  [13]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C21(0.46)  LDD2108  [13]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C21(1.15)  LDD2109  [13]
 LDCM0517  Nucleophilic fragment 21b MDA-MB-231 C21(0.31)  LDD2110  [13]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C21(1.42)  LDD2111  [13]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C21(0.45)  LDD2114  [13]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C21(1.35)  LDD2118  [13]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C21(1.79)  LDD2119  [13]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C21(0.59)  LDD2120  [13]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C21(0.97)  LDD2123  [13]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C21(1.10)  LDD2125  [13]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C21(0.89)  LDD2126  [13]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C21(1.02)  LDD2127  [13]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C21(0.69)  LDD2128  [13]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C21(1.55)  LDD2129  [13]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C21(0.47)  LDD2133  [13]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C21(0.60)  LDD2134  [13]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C21(1.88)  LDD2135  [13]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C21(1.18)  LDD2136  [13]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C21(1.07)  LDD2137  [13]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C21(1.15)  LDD2140  [13]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C21(1.25)  LDD2141  [13]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C21(0.70)  LDD2143  [13]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C21(2.41)  LDD2144  [13]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C21(0.08)  LDD2145  [13]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C21(1.30)  LDD2146  [13]
 LDCM0553  Nucleophilic fragment 6b MDA-MB-231 C21(0.99)  LDD2147  [13]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C21(0.58)  LDD2148  [13]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C21(2.37)  LDD2153  [13]
 LDCM0628  OTUB2-COV-1 HEK-293T C104(0.20)  LDD2207  [45]
 LDCM0099  Phenelzine MDA-MB-231 3.36  LDD0384  [12]
 LDCM0111  W14 Hep-G2 K273(2.32)  LDD0238  [32]
 LDCM0112  W16 Hep-G2 N274(0.65)  LDD0239  [32]
 LDCM0113  W17 Hep-G2 K273(1.10); N274(1.10)  LDD0240  [32]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 10 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Histone deacetylase 1 (HDAC1) Histone deacetylase family Q13547
Histone deacetylase 2 (HDAC2) Histone deacetylase family Q92769
E3 ubiquitin-protein ligase Mdm2 (MDM2) MDM2/MDM4 family Q00987
Sentrin-specific protease 3 (SENP3) Peptidase C48 family Q9H4L4
Kallikrein-6 (KLK6) Peptidase S1 family Q92876
Aurora kinase A (AURKA) Ser/Thr protein kinase family O14965
Aurora kinase B (AURKB) Ser/Thr protein kinase family Q96GD4
Interferon-induced, double-stranded RNA-activated protein kinase (EIF2AK2) Ser/Thr protein kinase family P19525
Telomerase reverse transcriptase (TERT) Reverse transcriptase family O14746
E3 ubiquitin-protein ligase TRIP12 (TRIP12) UPL family Q14669
Transporter and channel
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein zeta/delta (YWHAZ) 14-3-3 family P63104
Cytochrome c oxidase subunit 8A, mitochondrial (COX8A) Cytochrome c oxidase VIII family P10176
Cellular tumor antigen p53 (TP53) P53 family P04637
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Transcription factor AP-2-alpha (TFAP2A) AP-2 family P05549
Other
Click To Hide/Show 10 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cleavage and polyadenylation specificity factor subunit 1 (CPSF1) CPSF1 family Q10570
Small ribosomal subunit protein eS6 (RPS6) Eukaryotic ribosomal protein eS6 family P62753
Protein Niban 1 (NIBAN1) Niban family Q9BZQ8
Nucleoplasmin-2 (NPM2) Nucleoplasmin family Q86SE8
PIN2/TERF1-interacting telomerase inhibitor 1 (PINX1) PINX1 family Q96BK5
Proline-, glutamic acid- and leucine-rich protein 1 (PELP1) RIX1/PELP1 family Q8IZL8
Small ubiquitin-related modifier 1 (SUMO1) Ubiquitin family P63165
Hemogen (HEMGN) . Q9BXL5
La-related protein 4 (LARP4) . Q71RC2
Tumor suppressor ARF (CDKN2A) . Q8N726

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
Artenimol . DB11638
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ipp-204106 . D0Z1OR

References

1 Labeling Preferences of Diazirines with Protein Biomolecules. J Am Chem Soc. 2021 May 5;143(17):6691-6700. doi: 10.1021/jacs.1c02509. Epub 2021 Apr 20.
Mass spectrometry data entry: PXD025140
2 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
3 Comparison of Different Competitive Proteome Profiling Approaches in Target Identification of Covalent Inhibitors. Chembiochem. 2022 Dec 16;23(24):e202200389. doi: 10.1002/cbic.202200389. Epub 2022 Nov 22.
4 2-Ethynylbenzaldehyde-Based, Lysine-Targeting Irreversible Covalent Inhibitors for Protein Kinases and Nonkinases. J Am Chem Soc. 2023 Feb 12. doi: 10.1021/jacs.2c11595. Online ahead of print.
Mass spectrometry data entry: PXD037665
5 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
6 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.
7 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.
8 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.
9 2H-Azirine-Based Reagents for Chemoselective Bioconjugation at Carboxyl Residues Inside Live Cells. J Am Chem Soc. 2020 Apr 1;142(13):6051-6059. doi: 10.1021/jacs.9b12116. Epub 2020 Mar 23.
10 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
11 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
12 Hydrazines as versatile chemical biology probes and drug-discovery tools for cofactor-dependent enzymes. bioRxiv, 2020-06.
13 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
14 Chemoproteomic Profiling Reveals Ethacrynic Acid Targets Adenine Nucleotide Translocases to Impair Mitochondrial Function. Mol Pharm. 2018 Jun 4;15(6):2413-2422. doi: 10.1021/acs.molpharmaceut.8b00250. Epub 2018 May 15.
15 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.
16 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
17 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.
18 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.
19 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
20 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.
21 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
22 Comparison of Quantitative Mass Spectrometry Platforms for Monitoring Kinase ATP Probe Uptake in Lung Cancer. J Proteome Res. 2018 Jan 5;17(1):63-75. doi: 10.1021/acs.jproteome.7b00329. Epub 2017 Nov 22.
Mass spectrometry data entry: PXD006095 , PXD006096
23 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
24 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
25 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.
26 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
27 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
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Mass spectrometry data entry: PXD039931
29 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
30 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
31 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.
32 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.
33 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.
34 Differently Tagged Probes for Protein Profiling of Mitochondria. Chembiochem. 2019 May 2;20(9):1155-1160. doi: 10.1002/cbic.201800735. Epub 2019 Mar 26.
35 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
36 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.
37 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.
38 Pharmacological Targeting of Vacuolar H(+)-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Nov 19;27(11):1359-1370.e8. doi: 10.1016/j.chembiol.2020.06.011. Epub 2020 Jul 9.
39 Evaluation of fully-functionalized diazirine tags for chemical proteomic applications. Chem Sci. 2021 May 7;12(22):7839-7847. doi: 10.1039/d1sc01360b.
Mass spectrometry data entry: PXD025652
40 Small Molecule Interactome Mapping by Photoaffinity Labeling Reveals Binding Site Hotspots for the NSAIDs. J Am Chem Soc. 2018 Mar 28;140(12):4259-4268. doi: 10.1021/jacs.7b11639. Epub 2018 Mar 15.
Mass spectrometry data entry: PXD007094
41 Cell-based proteome profiling of potential dasatinib targets by use of affinity-based probes. J Am Chem Soc. 2012 Feb 15;134(6):3001-14. doi: 10.1021/ja208518u. Epub 2012 Feb 1.
42 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
43 Combined Omics Approach Identifies Gambogic Acid and Related Xanthones as Covalent Inhibitors of the Serine Palmitoyltransferase Complex. Cell Chem Biol. 2020 May 21;27(5):586-597.e12. doi: 10.1016/j.chembiol.2020.03.008. Epub 2020 Apr 23.
44 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
45 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.