Details of the Target

General Information of Target

Target ID LDTP01195
Target Name Core histone macro-H2A.1 (MACROH2A1)
Gene Name MACROH2A1
Gene ID 9555
Synonyms
H2AFY; Core histone macro-H2A.1; Histone macroH2A1; mH2A1; Histone H2A.y; H2A/y; Medulloblastoma antigen MU-MB-50.205
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSSRGGKKKSTKTSRSAKAGVIFPVGRMLRYIKKGHPKYRIGVGAPVYMAAVLEYLTAEI
LELAGNAARDNKKGRVTPRHILLAVANDEELNQLLKGVTIASGGVLPNIHPELLAKKRGS
KGKLEAIITPPPAKKAKSPSQKKPVSKKAGGKKGARKSKKKQGEVSKAASADSTTEGTPA
DGFTVLSTKSLFLGQKLQVVQADIASIDSDAVVHPTNTDFYIGGEVGNTLEKKGGKEFVE
AVLELRKKNGPLEVAGAAVSAGHGLPAKFVIHCNSPVWGADKCEELLEKTVKNCLALADD
KKLKSIAFPSIGSGRNGFPKQTAAQLILKAISSYFVSTMSSSIKTVYFVLFDSESIGIYV
QEMAKLDAN
Target Bioclass
Other
Family
Histone H2A family
Subcellular location
Nucleus
Function
Variant histone H2A which replaces conventional H2A in a subset of nucleosomes where it represses transcription. Nucleosomes wrap and compact DNA into chromatin, limiting DNA accessibility to the cellular machineries which require DNA as a template. Histones thereby play a central role in transcription regulation, DNA repair, DNA replication and chromosomal stability. DNA accessibility is regulated via a complex set of post-translational modifications of histones, also called histone code, and nucleosome remodeling. Involved in stable X chromosome inactivation. Inhibits the binding of transcription factors, including NF-kappa-B, and interferes with the activity of remodeling SWI/SNF complexes. Inhibits histone acetylation by EP300 and recruits class I HDACs, which induces a hypoacetylated state of chromatin.; [Isoform 1]: Isoform that specifically binds poly-ADP-ribose and O-acetyl-ADP-ribose and plays a key role in NAD(+) metabolism. Able to bind to the ends of poly-ADP-ribose chains created by PARP1 and cap them. This prevents PARP1 from further addition of ADP-ribose and thus limits the consumption of nuclear NAD(+), allowing the cell to maintain proper NAD(+) levels in both the nucleus and the mitochondria to promote proper mitochondrial respiration. Increases the expression of genes involved in redox metabolism, including SOD3.; [Isoform 2]: In contrast to isoform 1, does not bind poly-ADP-ribose. Represses SOD3 gene expression.
Uniprot ID
O75367
Ensemble ID
ENST00000304332.8
HGNC ID
HGNC:4740

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.R75Q DBIA    Probe Info 
HT SNV: p.K148I .
HT1376 SNV: p.E291V DBIA    Probe Info 
IPC298 SNV: p.S140F DBIA    Probe Info 
JURKAT SNV: p.A67T Compound 10    Probe Info 
MCC13 SNV: p.A333V DBIA    Probe Info 
SNU1 SNV: p.R69S; p.T175A DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 27 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
CY-1
 Probe Info  		100.00  LDD0243  [1]
YN-1
 Probe Info  		100.00  LDD0444  [2]
STPyne
 Probe Info  		K116(5.16); K12(2.22); K123(5.63); K137(6.91)  LDD0277  [3]
BTD
 Probe Info  		C297(0.95)  LDD1699  [4]
OPA-S-S-alkyne
 Probe Info  		K18(3.07); K307(3.13)  LDD3494  [5]
m-APA
 Probe Info  		11.18  LDD0403  [6]
Johansson_61
 Probe Info  		_(10.27)  LDD1489  [7]
AHL-Pu-1
 Probe Info  		C286(2.04)  LDD0171  [8]
DBIA
 Probe Info  		C276(0.84); C297(0.83)  LDD0531  [9]
4-Iodoacetamidophenylacetylene
 Probe Info  		C294(0.00); C283(0.00); C273(0.00)  LDD0038  [10]
IA-alkyne
 Probe Info  		C273(0.00); C294(0.00)  LDD0032  [11]
IPIAA_L
 Probe Info  		C273(0.00); C294(0.00)  LDD0031  [12]
Lodoacetamide azide
 Probe Info  		C294(0.00); C283(0.00); C273(0.00)  LDD0037  [10]
IPM
 Probe Info  		N.A.  LDD0025  [13]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [13]
NAIA_4
 Probe Info  		N.A.  LDD2226  [14]
TFBX
 Probe Info  		N.A.  LDD0027  [13]
Compound 10
 Probe Info  		C286(0.00); C297(0.00)  LDD2216  [15]
NHS
 Probe Info  		K18(0.00); K167(0.00)  LDD0010  [16]
1c-yne
 Probe Info  		N.A.  LDD0228  [17]
1d-yne
 Probe Info  		N.A.  LDD0357  [17]
Acrolein
 Probe Info  		C276(0.00); C297(0.00); H110(0.00); C286(0.00)  LDD0217  [18]
Cinnamaldehyde
 Probe Info  		N.A.  LDD0220  [18]
Crotonaldehyde
 Probe Info  		N.A.  LDD0219  [18]
Methacrolein
 Probe Info  		C297(0.00); C276(0.00)  LDD0218  [18]
NAIA_5
 Probe Info  		C283(0.00); C273(0.00); C294(0.00)  LDD2223  [14]
TPP-AC
 Probe Info  		N.A.  LDD0427  [19]
PAL-AfBPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe13
 Probe Info  		7.07  LDD0475  [20]
FFF probe3
 Probe Info  		5.06  LDD0464  [20]
JN0003
 Probe Info  		7.88  LDD0469  [20]
STS-2
 Probe Info  		N.A.  LDD0138  [21]
VE-P
 Probe Info  		N.A.  LDD0396  [22]
CA
 Probe Info  		2.12  LDD0419  [23]
DA-2
 Probe Info  		N.A.  LDD0072  [24]

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 C297(0.40)  LDD2142  [4]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C297(0.92)  LDD2112  [4]
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C297(0.47)  LDD2095  [4]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C297(0.67)  LDD2130  [4]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C297(1.61); C276(1.13)  LDD2117  [4]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C297(2.44)  LDD2152  [4]
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C297(0.69)  LDD2103  [4]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C297(0.43)  LDD2132  [4]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C297(0.49)  LDD2131  [4]
 LDCM0025  4SU-RNA HEK-293T C297(3.54)  LDD0172  [8]
 LDCM0026  4SU-RNA+native RNA DM93 C286(2.04)  LDD0171  [8]
 LDCM0214  AC1 HCT 116 C276(0.84); C297(0.83)  LDD0531  [9]
 LDCM0215  AC10 HCT 116 C276(0.84); C286(1.22)  LDD0532  [9]
 LDCM0216  AC100 HCT 116 C276(1.13); C286(0.63); C297(0.78)  LDD0533  [9]
 LDCM0217  AC101 HCT 116 C276(0.82); C286(0.64); C297(0.84)  LDD0534  [9]
 LDCM0218  AC102 HCT 116 C276(0.96); C286(0.68); C297(0.75)  LDD0535  [9]
 LDCM0219  AC103 HCT 116 C276(0.75); C286(0.57); C297(0.71)  LDD0536  [9]
 LDCM0220  AC104 HCT 116 C276(1.09); C286(0.75); C297(0.87)  LDD0537  [9]
 LDCM0221  AC105 HCT 116 C276(0.85); C286(0.56); C297(0.81)  LDD0538  [9]
 LDCM0222  AC106 HCT 116 C276(0.85); C286(0.52); C297(0.78)  LDD0539  [9]
 LDCM0223  AC107 HCT 116 C276(1.12); C286(0.65); C297(0.74)  LDD0540  [9]
 LDCM0224  AC108 HCT 116 C276(0.93); C286(0.56); C297(0.66)  LDD0541  [9]
 LDCM0225  AC109 HCT 116 C276(0.92); C286(0.78); C297(0.79)  LDD0542  [9]
 LDCM0226  AC11 HCT 116 C276(0.75); C286(1.39)  LDD0543  [9]
 LDCM0227  AC110 HCT 116 C276(0.90); C286(0.60); C297(0.77)  LDD0544  [9]
 LDCM0228  AC111 HCT 116 C276(0.73); C286(0.60); C297(0.70)  LDD0545  [9]
 LDCM0229  AC112 HCT 116 C276(0.71); C286(0.57); C297(0.77)  LDD0546  [9]
 LDCM0230  AC113 HCT 116 C276(1.00); C286(1.27); C297(1.08)  LDD0547  [9]
 LDCM0231  AC114 HCT 116 C276(0.91); C286(1.02); C297(1.18)  LDD0548  [9]
 LDCM0232  AC115 HCT 116 C276(0.84); C286(1.17); C297(0.84)  LDD0549  [9]
 LDCM0233  AC116 HCT 116 C276(0.88); C286(0.95); C297(1.05)  LDD0550  [9]
 LDCM0234  AC117 HCT 116 C276(0.86); C286(1.12); C297(0.85)  LDD0551  [9]
 LDCM0235  AC118 HCT 116 C276(1.02); C286(0.99); C297(0.94)  LDD0552  [9]
 LDCM0236  AC119 HCT 116 C276(0.91); C286(1.04); C297(1.00)  LDD0553  [9]
 LDCM0237  AC12 HCT 116 C276(0.92); C286(1.40)  LDD0554  [9]
 LDCM0238  AC120 HCT 116 C276(0.92); C286(1.05); C297(1.04)  LDD0555  [9]
 LDCM0239  AC121 HCT 116 C276(1.08); C286(1.22); C297(1.24)  LDD0556  [9]
 LDCM0240  AC122 HCT 116 C276(0.80); C286(1.17); C297(1.29)  LDD0557  [9]
 LDCM0241  AC123 HCT 116 C276(1.02); C286(1.29); C297(0.93)  LDD0558  [9]
 LDCM0242  AC124 HCT 116 C276(1.15); C286(1.24); C297(1.10)  LDD0559  [9]
 LDCM0243  AC125 HCT 116 C276(0.93); C286(1.13); C297(1.30)  LDD0560  [9]
 LDCM0244  AC126 HCT 116 C276(0.93); C286(0.89); C297(1.16)  LDD0561  [9]
 LDCM0245  AC127 HCT 116 C276(0.92); C286(1.06); C297(1.04)  LDD0562  [9]
 LDCM0246  AC128 HCT 116 C276(1.21); C286(1.52)  LDD0563  [9]
 LDCM0247  AC129 HCT 116 C276(1.07); C286(1.53)  LDD0564  [9]
 LDCM0249  AC130 HCT 116 C276(0.87); C286(1.38)  LDD0566  [9]
 LDCM0250  AC131 HCT 116 C276(1.04); C286(1.32)  LDD0567  [9]
 LDCM0251  AC132 HCT 116 C276(0.93); C286(1.12)  LDD0568  [9]
 LDCM0252  AC133 HCT 116 C276(0.92); C286(1.15)  LDD0569  [9]
 LDCM0253  AC134 HCT 116 C276(0.79); C286(0.97)  LDD0570  [9]
 LDCM0254  AC135 HCT 116 C276(0.96); C286(1.33)  LDD0571  [9]
 LDCM0255  AC136 HCT 116 C276(0.90); C286(1.06)  LDD0572  [9]
 LDCM0256  AC137 HCT 116 C276(1.07); C286(1.24)  LDD0573  [9]
 LDCM0257  AC138 HCT 116 C276(0.94); C286(1.06)  LDD0574  [9]
 LDCM0258  AC139 HCT 116 C276(0.85); C286(1.01)  LDD0575  [9]
 LDCM0259  AC14 HCT 116 C276(0.94); C286(1.30)  LDD0576  [9]
 LDCM0260  AC140 HCT 116 C276(0.85); C286(0.90)  LDD0577  [9]
 LDCM0261  AC141 HCT 116 C276(0.84); C286(0.94)  LDD0578  [9]
 LDCM0262  AC142 HCT 116 C276(0.96); C286(1.22)  LDD0579  [9]
 LDCM0263  AC143 HCT 116 C276(0.92); C286(1.15); C297(1.98)  LDD0580  [9]
 LDCM0264  AC144 HCT 116 C276(0.75); C286(0.91); C297(1.37)  LDD0581  [9]
 LDCM0265  AC145 HCT 116 C276(1.01); C286(1.43); C297(2.32)  LDD0582  [9]
 LDCM0266  AC146 HCT 116 C276(0.78); C286(1.13); C297(1.90)  LDD0583  [9]
 LDCM0267  AC147 HCT 116 C276(0.90); C286(1.32); C297(1.59)  LDD0584  [9]
 LDCM0268  AC148 HCT 116 C276(0.97); C286(1.54); C297(1.72)  LDD0585  [9]
 LDCM0269  AC149 HCT 116 C276(0.81); C286(1.29); C297(2.21)  LDD0586  [9]
 LDCM0270  AC15 HCT 116 C276(0.91); C286(1.03)  LDD0587  [9]
 LDCM0271  AC150 HCT 116 C297(1.02); C276(1.11); C286(1.95)  LDD0588  [9]
 LDCM0272  AC151 HCT 116 C276(0.80); C286(0.86); C297(1.33)  LDD0589  [9]
 LDCM0273  AC152 HCT 116 C276(0.97); C297(1.06); C286(1.85)  LDD0590  [9]
 LDCM0274  AC153 HCT 116 C276(0.76); C286(1.26); C297(1.75)  LDD0591  [9]
 LDCM0621  AC154 HCT 116 C276(0.91); C286(1.43); C297(1.98)  LDD2158  [9]
 LDCM0622  AC155 HCT 116 C276(0.77); C286(0.95); C297(1.21)  LDD2159  [9]
 LDCM0623  AC156 HCT 116 C276(0.99); C286(1.48); C297(2.35)  LDD2160  [9]
 LDCM0624  AC157 HCT 116 C276(1.02); C286(1.98); C297(1.22)  LDD2161  [9]
 LDCM0276  AC17 HCT 116 C276(0.95); C286(1.11); C297(1.13)  LDD0593  [9]
 LDCM0277  AC18 HCT 116 C276(0.79); C297(0.97); C286(1.82)  LDD0594  [9]
 LDCM0278  AC19 HCT 116 C276(0.86); C297(0.92); C286(1.32)  LDD0595  [9]
 LDCM0279  AC2 HCT 116 C297(0.87); C276(0.97)  LDD0596  [9]
 LDCM0280  AC20 HCT 116 C297(0.91); C276(1.00); C286(1.16)  LDD0597  [9]
 LDCM0281  AC21 HCT 116 C276(0.93); C297(1.02); C286(1.47)  LDD0598  [9]
 LDCM0282  AC22 HCT 116 C297(0.93); C276(1.08); C286(1.21)  LDD0599  [9]
 LDCM0283  AC23 HCT 116 C276(0.91); C297(0.93); C286(1.40)  LDD0600  [9]
 LDCM0284  AC24 HCT 116 C276(1.01); C297(1.09); C286(1.09)  LDD0601  [9]
 LDCM0285  AC25 HCT 116 C286(0.99); C297(1.01); C276(1.10)  LDD0602  [9]
 LDCM0286  AC26 HCT 116 C276(0.88); C286(0.91); C297(0.92)  LDD0603  [9]
 LDCM0287  AC27 HCT 116 C276(0.82); C286(0.84); C297(1.31)  LDD0604  [9]
 LDCM0288  AC28 HCT 116 C286(0.82); C276(0.85); C297(0.87)  LDD0605  [9]
 LDCM0289  AC29 HCT 116 C297(0.70); C276(0.79); C286(0.82)  LDD0606  [9]
 LDCM0290  AC3 HCT 116 C276(0.99); C297(1.02)  LDD0607  [9]
 LDCM0291  AC30 HCT 116 C286(0.71); C276(0.76); C297(0.79)  LDD0608  [9]
 LDCM0292  AC31 HCT 116 C276(0.76); C286(0.77); C297(1.07)  LDD0609  [9]
 LDCM0293  AC32 HCT 116 C286(0.73); C276(0.74); C297(1.10)  LDD0610  [9]
 LDCM0294  AC33 HCT 116 C286(0.83); C276(0.85); C297(1.24)  LDD0611  [9]
 LDCM0295  AC34 HCT 116 C286(0.71); C297(0.82); C276(0.89)  LDD0612  [9]
 LDCM0296  AC35 HCT 116 C286(1.00); C297(1.08); C276(1.53)  LDD0613  [9]
 LDCM0297  AC36 HCT 116 C286(0.76); C276(1.32); C297(1.39)  LDD0614  [9]
 LDCM0298  AC37 HCT 116 C276(1.02); C297(1.32); C286(1.33)  LDD0615  [9]
 LDCM0299  AC38 HCT 116 C286(0.85); C297(1.11); C276(1.34)  LDD0616  [9]
 LDCM0300  AC39 HCT 116 C286(0.79); C297(0.99); C276(1.22)  LDD0617  [9]
 LDCM0301  AC4 HCT 116 C276(1.00); C297(1.01)  LDD0618  [9]
 LDCM0302  AC40 HCT 116 C297(1.08); C286(1.10); C276(1.11)  LDD0619  [9]
 LDCM0303  AC41 HCT 116 C297(0.91); C286(1.02); C276(1.04)  LDD0620  [9]
 LDCM0304  AC42 HCT 116 C297(0.99); C286(1.08); C276(1.13)  LDD0621  [9]
 LDCM0305  AC43 HCT 116 C297(0.95); C276(0.96); C286(1.11)  LDD0622  [9]
 LDCM0306  AC44 HCT 116 C276(1.06); C297(1.13); C286(1.47)  LDD0623  [9]
 LDCM0307  AC45 HCT 116 C276(0.96); C297(1.15); C286(1.49)  LDD0624  [9]
 LDCM0308  AC46 HCT 116 C276(0.58); C286(0.84); C297(0.86)  LDD0625  [9]
 LDCM0309  AC47 HCT 116 C276(0.76); C297(0.96); C286(0.97)  LDD0626  [9]
 LDCM0310  AC48 HCT 116 C276(0.65); C286(0.84); C297(0.91)  LDD0627  [9]
 LDCM0311  AC49 HCT 116 C276(0.55); C286(0.72); C297(0.79)  LDD0628  [9]
 LDCM0312  AC5 HCT 116 C297(0.91); C276(1.09)  LDD0629  [9]
 LDCM0313  AC50 HCT 116 C276(0.54); C286(0.80); C297(0.85)  LDD0630  [9]
 LDCM0314  AC51 HCT 116 C276(0.61); C297(0.90); C286(0.99)  LDD0631  [9]
 LDCM0315  AC52 HCT 116 C276(0.64); C297(0.90); C286(0.95)  LDD0632  [9]
 LDCM0316  AC53 HCT 116 C276(0.67); C286(0.87); C297(1.02)  LDD0633  [9]
 LDCM0317  AC54 HCT 116 C276(0.63); C286(0.78); C297(1.01)  LDD0634  [9]
 LDCM0318  AC55 HCT 116 C286(1.00); C297(1.01); C276(1.05)  LDD0635  [9]
 LDCM0319  AC56 HCT 116 C276(0.66); C286(0.76); C297(0.92)  LDD0636  [9]
 LDCM0320  AC57 HCT 116 C276(0.82); C297(1.14)  LDD0637  [9]
 LDCM0321  AC58 HCT 116 C276(0.75); C297(1.17)  LDD0638  [9]
 LDCM0322  AC59 HCT 116 C276(0.90); C297(1.24)  LDD0639  [9]
 LDCM0323  AC6 HCT 116 C276(0.86); C286(0.94)  LDD0640  [9]
 LDCM0324  AC60 HCT 116 C276(0.87); C297(1.07)  LDD0641  [9]
 LDCM0325  AC61 HCT 116 C276(0.72); C297(1.22)  LDD0642  [9]
 LDCM0326  AC62 HCT 116 C276(0.82); C297(1.12)  LDD0643  [9]
 LDCM0327  AC63 HCT 116 C276(0.92); C297(0.96)  LDD0644  [9]
 LDCM0328  AC64 HCT 116 C276(1.06); C297(1.09)  LDD0645  [9]
 LDCM0329  AC65 HCT 116 C276(0.75); C297(1.19)  LDD0646  [9]
 LDCM0330  AC66 HCT 116 C276(0.70); C297(1.16)  LDD0647  [9]
 LDCM0331  AC67 HCT 116 C276(0.75); C297(1.24)  LDD0648  [9]
 LDCM0332  AC68 HCT 116 C276(0.83); C286(0.98); C297(1.16)  LDD0649  [9]
 LDCM0333  AC69 HCT 116 C276(0.89); C286(0.93); C297(1.15)  LDD0650  [9]
 LDCM0334  AC7 HCT 116 C276(0.97); C286(1.05)  LDD0651  [9]
 LDCM0335  AC70 HCT 116 C276(0.76); C286(0.89); C297(1.01)  LDD0652  [9]
 LDCM0336  AC71 HCT 116 C276(1.04); C286(1.07); C297(1.19)  LDD0653  [9]
 LDCM0337  AC72 HCT 116 C276(0.89); C286(1.01); C297(1.10)  LDD0654  [9]
 LDCM0338  AC73 HCT 116 C276(0.69); C286(0.86); C297(0.97)  LDD0655  [9]
 LDCM0339  AC74 HCT 116 C276(0.84); C286(0.88); C297(1.04)  LDD0656  [9]
 LDCM0340  AC75 HCT 116 C276(0.71); C286(0.84); C297(0.90)  LDD0657  [9]
 LDCM0341  AC76 HCT 116 C276(0.92); C286(1.20); C297(1.26)  LDD0658  [9]
 LDCM0342  AC77 HCT 116 C276(0.81); C286(1.07); C297(1.10)  LDD0659  [9]
 LDCM0343  AC78 HCT 116 C276(0.78); C286(0.91); C297(1.01)  LDD0660  [9]
 LDCM0344  AC79 HCT 116 C276(0.97); C286(1.08); C297(1.16)  LDD0661  [9]
 LDCM0345  AC8 HCT 116 C286(0.89); C276(0.92)  LDD0662  [9]
 LDCM0346  AC80 HCT 116 C276(0.98); C297(1.05); C286(1.14)  LDD0663  [9]
 LDCM0347  AC81 HCT 116 C286(0.99); C276(1.02); C297(1.22)  LDD0664  [9]
 LDCM0348  AC82 HCT 116 C276(0.68); C286(0.78); C297(0.82)  LDD0665  [9]
 LDCM0349  AC83 HCT 116 C276(0.82)  LDD0666  [9]
 LDCM0350  AC84 HCT 116 C276(0.81)  LDD0667  [9]
 LDCM0351  AC85 HCT 116 C276(0.78)  LDD0668  [9]
 LDCM0352  AC86 HCT 116 C276(0.86)  LDD0669  [9]
 LDCM0353  AC87 HCT 116 C276(0.89)  LDD0670  [9]
 LDCM0354  AC88 HCT 116 C276(0.92)  LDD0671  [9]
 LDCM0355  AC89 HCT 116 C276(0.85)  LDD0672  [9]
 LDCM0357  AC90 HCT 116 C276(1.11)  LDD0674  [9]
 LDCM0358  AC91 HCT 116 C276(0.86)  LDD0675  [9]
 LDCM0359  AC92 HCT 116 C276(0.93)  LDD0676  [9]
 LDCM0360  AC93 HCT 116 C276(0.93)  LDD0677  [9]
 LDCM0361  AC94 HCT 116 C276(0.89)  LDD0678  [9]
 LDCM0362  AC95 HCT 116 C276(0.88)  LDD0679  [9]
 LDCM0363  AC96 HCT 116 C276(0.98)  LDD0680  [9]
 LDCM0364  AC97 HCT 116 C276(0.81)  LDD0681  [9]
 LDCM0365  AC98 HCT 116 C297(0.61); C286(0.61); C276(0.74)  LDD0682  [9]
 LDCM0366  AC99 HCT 116 C286(0.63); C297(0.73); C276(1.10)  LDD0683  [9]
 LDCM0545  Acetamide MDA-MB-231 C297(0.61)  LDD2138  [4]
 LDCM0520  AKOS000195272 MDA-MB-231 C297(0.95)  LDD2113  [4]
 LDCM0248  AKOS034007472 HCT 116 C276(0.95); C286(1.27)  LDD0565  [9]
 LDCM0356  AKOS034007680 HCT 116 C276(0.81); C286(1.13)  LDD0673  [9]
 LDCM0275  AKOS034007705 HCT 116 C276(0.78); C286(0.91)  LDD0592  [9]
 LDCM0156  Aniline NCI-H1299 11.18  LDD0403  [6]
 LDCM0498  BS-3668 MDA-MB-231 C297(0.81)  LDD2091  [4]
 LDCM0164  Camptothecin MCF-7 2.12  LDD0419  [23]
 LDCM0108  Chloroacetamide HeLa C297(0.00); H110(0.00); C276(0.00); C286(0.00)  LDD0222  [18]
 LDCM0367  CL1 HCT 116 C286(0.71); C297(0.81); C276(1.04)  LDD0684  [9]
 LDCM0368  CL10 HCT 116 C276(0.67); C297(0.86); C286(1.05)  LDD0685  [9]
 LDCM0369  CL100 HCT 116 C297(0.86); C276(0.89)  LDD0686  [9]
 LDCM0370  CL101 HCT 116 C276(0.82); C286(0.89)  LDD0687  [9]
 LDCM0371  CL102 HCT 116 C276(0.93); C286(1.24)  LDD0688  [9]
 LDCM0372  CL103 HCT 116 C276(0.90); C286(1.14)  LDD0689  [9]
 LDCM0373  CL104 HCT 116 C276(0.78); C286(1.02)  LDD0690  [9]
 LDCM0374  CL105 HCT 116 C276(0.83); C297(0.91); C286(1.34)  LDD0691  [9]
 LDCM0375  CL106 HCT 116 C276(0.61); C297(0.96); C286(2.10)  LDD0692  [9]
 LDCM0376  CL107 HCT 116 C276(0.78); C297(0.98); C286(1.58)  LDD0693  [9]
 LDCM0377  CL108 HCT 116 C276(0.81); C297(0.99); C286(1.32)  LDD0694  [9]
 LDCM0378  CL109 HCT 116 C276(0.78); C297(1.05); C286(1.43)  LDD0695  [9]
 LDCM0379  CL11 HCT 116 C276(0.72); C297(0.84); C286(1.10)  LDD0696  [9]
 LDCM0380  CL110 HCT 116 C276(0.77); C297(1.11); C286(1.30)  LDD0697  [9]
 LDCM0381  CL111 HCT 116 C276(0.86); C297(0.89); C286(1.24)  LDD0698  [9]
 LDCM0382  CL112 HCT 116 C286(0.85); C297(0.93); C276(1.00)  LDD0699  [9]
 LDCM0383  CL113 HCT 116 C286(0.72); C276(0.73); C297(0.95)  LDD0700  [9]
 LDCM0384  CL114 HCT 116 C286(0.81); C297(0.81); C276(0.82)  LDD0701  [9]
 LDCM0385  CL115 HCT 116 C286(0.74); C276(0.89); C297(0.97)  LDD0702  [9]
 LDCM0386  CL116 HCT 116 C286(0.85); C276(0.94); C297(1.01)  LDD0703  [9]
 LDCM0387  CL117 HCT 116 C286(0.87); C297(0.90); C276(1.53)  LDD0704  [9]
 LDCM0388  CL118 HCT 116 C286(0.98); C276(1.04); C297(1.07)  LDD0705  [9]
 LDCM0389  CL119 HCT 116 C297(0.93); C286(0.99); C276(1.16)  LDD0706  [9]
 LDCM0390  CL12 HCT 116 C276(0.77); C297(0.80); C286(0.99)  LDD0707  [9]
 LDCM0391  CL120 HCT 116 C297(0.99); C286(1.01); C276(1.07)  LDD0708  [9]
 LDCM0392  CL121 HCT 116 C276(0.72); C286(0.87); C297(0.98)  LDD0709  [9]
 LDCM0393  CL122 HCT 116 C276(0.65); C286(0.83); C297(0.84)  LDD0710  [9]
 LDCM0394  CL123 HCT 116 C276(0.65); C286(0.76); C297(0.94)  LDD0711  [9]
 LDCM0395  CL124 HCT 116 C276(0.56); C286(0.79); C297(0.87)  LDD0712  [9]
 LDCM0396  CL125 HCT 116 C276(0.94); C297(1.23)  LDD0713  [9]
 LDCM0397  CL126 HCT 116 C276(0.86); C297(1.27)  LDD0714  [9]
 LDCM0398  CL127 HCT 116 C276(0.88); C297(1.18)  LDD0715  [9]
 LDCM0399  CL128 HCT 116 C276(0.88); C297(1.12)  LDD0716  [9]
 LDCM0400  CL13 HCT 116 C276(0.70); C297(0.82); C286(1.02)  LDD0717  [9]
 LDCM0401  CL14 HCT 116 C276(0.80); C297(0.90); C286(1.08)  LDD0718  [9]
 LDCM0402  CL15 HCT 116 C276(0.73); C297(0.98); C286(1.19)  LDD0719  [9]
 LDCM0403  CL16 HCT 116 C276(0.75); C297(0.79)  LDD0720  [9]
 LDCM0404  CL17 HCT 116 C297(0.71); C276(0.78)  LDD0721  [9]
 LDCM0405  CL18 HCT 116 C276(0.64); C297(0.80)  LDD0722  [9]
 LDCM0406  CL19 HCT 116 C276(0.74); C297(0.87)  LDD0723  [9]
 LDCM0407  CL2 HCT 116 C286(0.80); C297(0.84); C276(1.18)  LDD0724  [9]
 LDCM0408  CL20 HCT 116 C276(0.68); C297(0.97)  LDD0725  [9]
 LDCM0409  CL21 HCT 116 C276(0.75); C297(0.94)  LDD0726  [9]
 LDCM0410  CL22 HCT 116 C276(0.65); C297(0.82)  LDD0727  [9]
 LDCM0411  CL23 HCT 116 C276(0.73); C297(0.84)  LDD0728  [9]
 LDCM0412  CL24 HCT 116 C276(0.73); C297(0.87)  LDD0729  [9]
 LDCM0413  CL25 HCT 116 C276(0.71); C297(0.80)  LDD0730  [9]
 LDCM0414  CL26 HCT 116 C276(0.77); C297(0.84)  LDD0731  [9]
 LDCM0415  CL27 HCT 116 C276(0.75); C297(0.90)  LDD0732  [9]
 LDCM0416  CL28 HCT 116 C276(0.63); C297(0.77)  LDD0733  [9]
 LDCM0417  CL29 HCT 116 C276(0.67); C297(0.90)  LDD0734  [9]
 LDCM0418  CL3 HCT 116 C276(0.92); C286(1.16); C297(0.97)  LDD0735  [9]
 LDCM0419  CL30 HCT 116 C276(0.81); C297(0.82)  LDD0736  [9]
 LDCM0420  CL31 HCT 116 C276(1.08); C286(1.04)  LDD0737  [9]
 LDCM0421  CL32 HCT 116 C276(1.26); C286(1.07); C297(0.88)  LDD0738  [9]
 LDCM0422  CL33 HCT 116 C276(0.88); C286(0.86); C297(1.05)  LDD0739  [9]
 LDCM0423  CL34 HCT 116 C276(0.85); C286(0.94); C297(1.11)  LDD0740  [9]
 LDCM0424  CL35 HCT 116 C276(0.91); C286(0.87); C297(1.22)  LDD0741  [9]
 LDCM0425  CL36 HCT 116 C276(0.91); C286(0.93); C297(1.05)  LDD0742  [9]
 LDCM0426  CL37 HCT 116 C276(1.13); C286(0.93); C297(1.08)  LDD0743  [9]
 LDCM0428  CL39 HCT 116 C276(1.52); C286(1.27); C297(0.99)  LDD0745  [9]
 LDCM0429  CL4 HCT 116 C276(1.00); C286(0.85); C297(0.80)  LDD0746  [9]
 LDCM0430  CL40 HCT 116 C276(1.22); C286(1.11); C297(0.90)  LDD0747  [9]
 LDCM0431  CL41 HCT 116 C276(1.10); C286(0.99); C297(0.97)  LDD0748  [9]
 LDCM0432  CL42 HCT 116 C276(1.23); C286(1.11); C297(0.92)  LDD0749  [9]
 LDCM0433  CL43 HCT 116 C276(1.23); C286(1.18); C297(1.17)  LDD0750  [9]
 LDCM0434  CL44 HCT 116 C276(1.10); C286(1.08); C297(1.18)  LDD0751  [9]
 LDCM0435  CL45 HCT 116 C276(1.05); C286(1.08); C297(1.07)  LDD0752  [9]
 LDCM0436  CL46 HCT 116 C276(1.02); C286(0.78); C297(1.09)  LDD0753  [9]
 LDCM0437  CL47 HCT 116 C276(1.01); C286(0.68); C297(1.08)  LDD0754  [9]
 LDCM0438  CL48 HCT 116 C276(1.08); C286(0.82); C297(1.02)  LDD0755  [9]
 LDCM0439  CL49 HCT 116 C276(0.93); C286(1.09); C297(1.12)  LDD0756  [9]
 LDCM0440  CL5 HCT 116 C276(1.04); C286(1.03); C297(0.78)  LDD0757  [9]
 LDCM0441  CL50 HCT 116 C276(1.02); C286(0.96); C297(1.01)  LDD0758  [9]
 LDCM0442  CL51 HCT 116 C276(0.94); C286(0.80); C297(1.49)  LDD0759  [9]
 LDCM0443  CL52 HCT 116 C276(0.91); C286(0.77); C297(0.99)  LDD0760  [9]
 LDCM0444  CL53 HCT 116 C276(1.01); C286(0.65); C297(1.07)  LDD0761  [9]
 LDCM0445  CL54 HCT 116 C276(0.95); C286(0.79); C297(1.12)  LDD0762  [9]
 LDCM0446  CL55 HCT 116 C276(1.02); C286(0.87); C297(1.24)  LDD0763  [9]
 LDCM0447  CL56 HCT 116 C276(1.03); C286(0.88); C297(0.99)  LDD0764  [9]
 LDCM0448  CL57 HCT 116 C276(0.97); C286(0.77); C297(1.03)  LDD0765  [9]
 LDCM0449  CL58 HCT 116 C276(1.05); C286(0.87); C297(1.12)  LDD0766  [9]
 LDCM0450  CL59 HCT 116 C276(0.99); C286(0.89); C297(1.07)  LDD0767  [9]
 LDCM0451  CL6 HCT 116 C276(0.72); C286(0.91); C297(0.81)  LDD0768  [9]
 LDCM0452  CL60 HCT 116 C276(0.90); C286(0.81); C297(0.88)  LDD0769  [9]
 LDCM0453  CL61 HCT 116 C276(0.94); C297(0.83)  LDD0770  [9]
 LDCM0454  CL62 HCT 116 C276(0.92); C297(0.81)  LDD0771  [9]
 LDCM0455  CL63 HCT 116 C276(0.80); C297(0.78)  LDD0772  [9]
 LDCM0456  CL64 HCT 116 C276(0.87); C297(0.77)  LDD0773  [9]
 LDCM0457  CL65 HCT 116 C276(0.96); C297(0.88)  LDD0774  [9]
 LDCM0458  CL66 HCT 116 C276(0.76); C297(0.73)  LDD0775  [9]
 LDCM0459  CL67 HCT 116 C276(0.83); C297(0.70)  LDD0776  [9]
 LDCM0460  CL68 HCT 116 C276(0.75); C297(0.66)  LDD0777  [9]
 LDCM0461  CL69 HCT 116 C276(0.86); C297(0.65)  LDD0778  [9]
 LDCM0462  CL7 HCT 116 C276(0.80); C286(0.99); C297(0.80)  LDD0779  [9]
 LDCM0463  CL70 HCT 116 C276(0.76); C297(0.64)  LDD0780  [9]
 LDCM0464  CL71 HCT 116 C276(0.86); C297(0.63)  LDD0781  [9]
 LDCM0465  CL72 HCT 116 C276(0.96); C297(0.78)  LDD0782  [9]
 LDCM0466  CL73 HCT 116 C276(0.96); C297(0.69)  LDD0783  [9]
 LDCM0467  CL74 HCT 116 C276(0.81); C297(0.72)  LDD0784  [9]
 LDCM0469  CL76 HCT 116 C276(0.69); C297(0.95)  LDD0786  [9]
 LDCM0470  CL77 HCT 116 C276(0.78); C297(0.84)  LDD0787  [9]
 LDCM0471  CL78 HCT 116 C276(0.76); C297(1.26)  LDD0788  [9]
 LDCM0472  CL79 HCT 116 C276(0.73); C297(0.81)  LDD0789  [9]
 LDCM0473  CL8 HCT 116 C276(0.74); C286(0.95); C297(0.84)  LDD0790  [9]
 LDCM0474  CL80 HCT 116 C276(0.63); C297(1.08)  LDD0791  [9]
 LDCM0475  CL81 HCT 116 C276(0.73); C297(0.94)  LDD0792  [9]
 LDCM0476  CL82 HCT 116 C276(0.60); C297(1.01)  LDD0793  [9]
 LDCM0477  CL83 HCT 116 C276(0.59); C297(0.89)  LDD0794  [9]
 LDCM0478  CL84 HCT 116 C276(0.56); C297(1.04)  LDD0795  [9]
 LDCM0479  CL85 HCT 116 C276(0.75); C297(1.13)  LDD0796  [9]
 LDCM0480  CL86 HCT 116 C276(0.94); C297(1.24)  LDD0797  [9]
 LDCM0481  CL87 HCT 116 C276(0.80); C297(0.92)  LDD0798  [9]
 LDCM0482  CL88 HCT 116 C276(0.62); C297(1.13)  LDD0799  [9]
 LDCM0483  CL89 HCT 116 C276(0.50); C297(1.09)  LDD0800  [9]
 LDCM0484  CL9 HCT 116 C276(0.84); C286(0.78); C297(0.81)  LDD0801  [9]
 LDCM0485  CL90 HCT 116 C276(1.06); C297(1.15)  LDD0802  [9]
 LDCM0486  CL91 HCT 116 C276(0.81); C297(0.99)  LDD0803  [9]
 LDCM0487  CL92 HCT 116 C276(0.99); C297(0.93)  LDD0804  [9]
 LDCM0488  CL93 HCT 116 C276(0.89); C297(1.00)  LDD0805  [9]
 LDCM0489  CL94 HCT 116 C276(0.97); C297(0.79)  LDD0806  [9]
 LDCM0490  CL95 HCT 116 C276(0.80); C297(0.85)  LDD0807  [9]
 LDCM0491  CL96 HCT 116 C276(0.83); C297(0.93)  LDD0808  [9]
 LDCM0492  CL97 HCT 116 C276(0.83); C297(0.83)  LDD0809  [9]
 LDCM0493  CL98 HCT 116 C276(0.81); C297(0.86)  LDD0810  [9]
 LDCM0494  CL99 HCT 116 C276(0.82); C297(0.83)  LDD0811  [9]
 LDCM0495  E2913 HEK-293T C297(1.04); C276(1.22); C286(1.03)  LDD1698  [25]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C297(1.77)  LDD1702  [4]
 LDCM0468  Fragment33 HCT 116 C276(0.79); C297(0.80)  LDD0785  [9]
 LDCM0427  Fragment51 HCT 116 C276(0.96); C286(0.75); C297(1.17)  LDD0744  [9]
 LDCM0616  Fragment61 Jurkat _(10.27)  LDD1489  [7]
 LDCM0107  IAA HeLa C276(0.00); H275(0.00); H110(0.00); H266(0.00)  LDD0221  [18]
 LDCM0022  KB02 HEK-293T C297(0.92); C286(0.91); C276(1.03)  LDD1492  [25]
 LDCM0023  KB03 HEK-293T C297(1.05); C286(1.00); C276(0.99)  LDD1497  [25]
 LDCM0024  KB05 COLO792 C276(3.49)  LDD3310  [26]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C297(1.09)  LDD2102  [4]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C297(1.15)  LDD2121  [4]
 LDCM0109  NEM HeLa H110(0.00); H266(0.00)  LDD0223  [18]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C297(1.02)  LDD2089  [4]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C297(0.93)  LDD2092  [4]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C297(1.19)  LDD2093  [4]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C297(1.82)  LDD2094  [4]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C297(0.33)  LDD2096  [4]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C297(1.03)  LDD2097  [4]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C297(2.32); C276(1.36)  LDD2099  [4]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C297(0.40)  LDD2100  [4]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C297(0.82)  LDD2101  [4]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C297(0.49)  LDD2104  [4]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C297(1.00)  LDD2105  [4]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C297(0.23)  LDD2106  [4]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C297(1.42)  LDD2107  [4]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C297(0.65)  LDD2108  [4]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C297(0.65); C276(1.02)  LDD2109  [4]
 LDCM0517  Nucleophilic fragment 21b MDA-MB-231 C297(0.42)  LDD2110  [4]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C297(1.44)  LDD2111  [4]
 LDCM0523  Nucleophilic fragment 24b MDA-MB-231 C297(0.88)  LDD2116  [4]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C297(0.91)  LDD2118  [4]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C297(1.07); C276(1.21)  LDD2119  [4]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C297(0.59)  LDD2120  [4]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C297(1.26); C276(1.41)  LDD2123  [4]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C297(0.59)  LDD2124  [4]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C297(1.02)  LDD2125  [4]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C297(0.51)  LDD2126  [4]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C297(1.22); C276(0.99)  LDD2127  [4]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C297(0.59)  LDD2128  [4]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C297(2.33)  LDD2129  [4]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C297(0.47)  LDD2133  [4]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C297(0.63)  LDD2134  [4]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C297(2.38)  LDD2135  [4]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C297(1.69); C276(1.16)  LDD2136  [4]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C297(1.14); C276(1.06)  LDD2137  [4]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C297(6.75)  LDD1700  [4]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C297(1.12)  LDD2140  [4]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C297(0.76)  LDD2141  [4]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C297(0.55)  LDD2143  [4]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C297(1.82); C276(1.23)  LDD2144  [4]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C297(0.44)  LDD2145  [4]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C297(1.34); C276(1.62)  LDD2146  [4]
 LDCM0553  Nucleophilic fragment 6b MDA-MB-231 C297(0.91)  LDD2147  [4]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C297(0.38)  LDD2148  [4]
 LDCM0555  Nucleophilic fragment 7b MDA-MB-231 C297(0.69)  LDD2149  [4]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C297(0.58)  LDD2150  [4]
 LDCM0557  Nucleophilic fragment 8b MDA-MB-231 C297(0.52)  LDD2151  [4]
 LDCM0131  RA190 MM1.R C297(1.35)  LDD0304  [27]

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
Poly [ADP-ribose] polymerase tankyrase-1 (TNKS) ARTD/PARP family O95271
Receptor tyrosine-protein kinase erbB-2 (ERBB2) Tyr protein kinase family P04626
Transcriptional regulator ATRX (ATRX) SNF2/RAD54 helicase family P46100
TNF receptor-associated factor 2 (TRAF2) TNF receptor-associated factor family Q12933
Tripartite motif-containing protein 26 (TRIM26) TRIM/RBCC family Q12899
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein max (MAX) MAX family P61244
Other
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cysteine-rich tail protein 1 (CYSRT1) CYSRT1 family A8MQ03
Protein FAM133A (FAM133A) FAM133 family Q8N9E0
Keratin-associated protein 10-8 (KRTAP10-8) KRTAP type 10 family P60410
Cytoplasmic 60S subunit biogenesis factor ZNF622 (ZNF622) REI1 family Q969S3
Glutamate-rich protein 2 (ERICH2) . A1L162
Protein SREK1IP1 (SREK1IP1) . Q8N9Q2
Uncharacterized protein NKAPD1 (NKAPD1) . Q6ZUT1

References

1 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.
2 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.
3 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
4 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
5 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
6 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.
7 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.
8 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
9 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.
10 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
11 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
12 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
13 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
14 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
15 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
16 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
17 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.
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 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.
20 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.
21 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.
22 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.
23 Expanding the "minimalist" small molecule tagging approach to different bioactive compounds. Org Biomol Chem. 2019 Mar 13;17(11):3010-3017. doi: 10.1039/c8ob03175d.
24 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.
25 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
26 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
27 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.