Details of the Target

General Information of Target

Target ID LDTP04948
Target Name WD repeat-containing protein 5 (WDR5)
Gene Name WDR5
Gene ID 11091
Synonyms
BIG3; WD repeat-containing protein 5; BMP2-induced 3-kb gene protein
3D Structure
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2D Sequence (FASTA)
Download
3D Structure (PDB)
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Sequence
MATEEKKPETEAARAQPTPSSSATQSKPTPVKPNYALKFTLAGHTKAVSSVKFSPNGEWL
ASSSADKLIKIWGAYDGKFEKTISGHKLGISDVAWSSDSNLLVSASDDKTLKIWDVSSGK
CLKTLKGHSNYVFCCNFNPQSNLIVSGSFDESVRIWDVKTGKCLKTLPAHSDPVSAVHFN
RDGSLIVSSSYDGLCRIWDTASGQCLKTLIDDDNPPVSFVKFSPNGKYILAATLDNTLKL
WDYSKGKCLKTYTGHKNEKYCIFANFSVTGGKWIVSGSEDNLVYIWNLQTKEIVQKLQGH
TDVVISTACHPTENIIASAALENDKTIKLWKSDC
Target Type
Literature-reported
Target Bioclass
Other
Family
WD repeat WDR5/wds family
Subcellular location
Nucleus
Function
Contributes to histone modification . May position the N-terminus of histone H3 for efficient trimethylation at 'Lys-4'. As part of the MLL1/MLL complex it is involved in methylation and dimethylation at 'Lys-4' of histone H3. H3 'Lys-4' methylation represents a specific tag for epigenetic transcriptional activation. As part of the NSL complex it may be involved in acetylation of nucleosomal histone H4 on several lysine residues. May regulate osteoblasts differentiation. In association with RBBP5 and ASH2L, stimulates the histone methyltransferase activities of KMT2A, KMT2B, KMT2C, KMT2D, SETD1A and SETD1B.
TTD ID
T77393
Uniprot ID
P61964
DrugMap ID
TT7OFWB
Ensemble ID
ENST00000358625.4
HGNC ID
HGNC:12757
ChEMBL ID
CHEMBL1075317

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 16 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
TH211
 Probe Info  		Y243(15.57); Y75(7.46)  LDD0257  [1]
TH216
 Probe Info  		Y191(8.19)  LDD0259  [1]
IPM
 Probe Info  		N.A.  LDD0241  [2]
m-APA
 Probe Info  		11.48  LDD0403  [3]
BTD
 Probe Info  		C205(0.49)  LDD2109  [4]
HHS-482
 Probe Info  		Y228(0.87)  LDD0285  [5]
HHS-475
 Probe Info  		Y228(0.98)  LDD0264  [6]
HHS-465
 Probe Info  		Y228(2.12)  LDD2237  [7]
DBIA
 Probe Info  		C205(1.09)  LDD0531  [8]
4-Iodoacetamidophenylacetylene
 Probe Info  		C195(0.00); C205(0.00); C261(0.00)  LDD0038  [9]
IA-alkyne
 Probe Info  		N.A.  LDD0032  [10]
Lodoacetamide azide
 Probe Info  		C195(0.00); C205(0.00); C309(0.00); C261(0.00)  LDD0037  [9]
PF-06672131
 Probe Info  		N.A.  LDD0152  [11]
SF
 Probe Info  		N.A.  LDD0028  [12]
Acrolein
 Probe Info  		N.A.  LDD0217  [13]
NAIA_5
 Probe Info  		C195(0.00); C205(0.00); C121(0.00); C309(0.00)  LDD2223  [14]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
VE-P
 Probe Info  		N.A.  LDD0396  [15]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C205(0.74)  LDD2117  [4]
 LDCM0214  AC1 HCT 116 C205(1.09)  LDD0531  [8]
 LDCM0215  AC10 HCT 116 C205(1.09)  LDD0532  [8]
 LDCM0216  AC100 HCT 116 C205(0.94)  LDD0533  [8]
 LDCM0217  AC101 HCT 116 C205(0.86)  LDD0534  [8]
 LDCM0218  AC102 HCT 116 C205(0.92)  LDD0535  [8]
 LDCM0219  AC103 HCT 116 C205(1.08)  LDD0536  [8]
 LDCM0220  AC104 HCT 116 C205(1.12)  LDD0537  [8]
 LDCM0221  AC105 HCT 116 C205(1.17)  LDD0538  [8]
 LDCM0222  AC106 HCT 116 C205(0.96)  LDD0539  [8]
 LDCM0223  AC107 HCT 116 C205(1.47)  LDD0540  [8]
 LDCM0224  AC108 HCT 116 C205(0.85)  LDD0541  [8]
 LDCM0225  AC109 HCT 116 C205(0.84)  LDD0542  [8]
 LDCM0226  AC11 HCT 116 C205(1.18)  LDD0543  [8]
 LDCM0227  AC110 HCT 116 C205(0.83)  LDD0544  [8]
 LDCM0228  AC111 HCT 116 C205(0.91)  LDD0545  [8]
 LDCM0229  AC112 HCT 116 C205(1.06)  LDD0546  [8]
 LDCM0230  AC113 HCT 116 C205(1.10)  LDD0547  [8]
 LDCM0231  AC114 HCT 116 C205(1.03)  LDD0548  [8]
 LDCM0232  AC115 HCT 116 C205(1.01)  LDD0549  [8]
 LDCM0233  AC116 HCT 116 C205(1.08)  LDD0550  [8]
 LDCM0234  AC117 HCT 116 C205(1.09)  LDD0551  [8]
 LDCM0235  AC118 HCT 116 C205(1.06)  LDD0552  [8]
 LDCM0236  AC119 HCT 116 C205(1.04)  LDD0553  [8]
 LDCM0237  AC12 HCT 116 C205(1.05)  LDD0554  [8]
 LDCM0238  AC120 HCT 116 C205(1.09)  LDD0555  [8]
 LDCM0239  AC121 HCT 116 C205(0.93)  LDD0556  [8]
 LDCM0240  AC122 HCT 116 C205(1.04)  LDD0557  [8]
 LDCM0241  AC123 HCT 116 C205(0.85)  LDD0558  [8]
 LDCM0242  AC124 HCT 116 C205(1.02)  LDD0559  [8]
 LDCM0243  AC125 HCT 116 C205(1.07)  LDD0560  [8]
 LDCM0244  AC126 HCT 116 C205(1.09)  LDD0561  [8]
 LDCM0245  AC127 HCT 116 C205(1.04)  LDD0562  [8]
 LDCM0259  AC14 HCT 116 C205(1.11)  LDD0576  [8]
 LDCM0263  AC143 HCT 116 C205(0.96)  LDD0580  [8]
 LDCM0264  AC144 HCT 116 C205(1.09)  LDD0581  [8]
 LDCM0265  AC145 HCT 116 C205(0.91)  LDD0582  [8]
 LDCM0266  AC146 HCT 116 C205(1.04)  LDD0583  [8]
 LDCM0267  AC147 HCT 116 C205(0.98)  LDD0584  [8]
 LDCM0268  AC148 HCT 116 C205(0.92)  LDD0585  [8]
 LDCM0269  AC149 HCT 116 C205(1.02)  LDD0586  [8]
 LDCM0270  AC15 HCT 116 C205(1.15)  LDD0587  [8]
 LDCM0271  AC150 HCT 116 C205(1.08)  LDD0588  [8]
 LDCM0272  AC151 HCT 116 C205(1.31)  LDD0589  [8]
 LDCM0273  AC152 HCT 116 C205(1.15)  LDD0590  [8]
 LDCM0274  AC153 HCT 116 C205(0.99)  LDD0591  [8]
 LDCM0621  AC154 HCT 116 C205(0.97)  LDD2158  [8]
 LDCM0622  AC155 HCT 116 C205(1.10)  LDD2159  [8]
 LDCM0623  AC156 HCT 116 C205(1.14)  LDD2160  [8]
 LDCM0624  AC157 HCT 116 C205(1.11)  LDD2161  [8]
 LDCM0276  AC17 HCT 116 C205(1.00)  LDD0593  [8]
 LDCM0277  AC18 HCT 116 C205(0.91)  LDD0594  [8]
 LDCM0278  AC19 HCT 116 C205(0.87)  LDD0595  [8]
 LDCM0279  AC2 HCT 116 C205(1.04)  LDD0596  [8]
 LDCM0280  AC20 HCT 116 C205(0.90)  LDD0597  [8]
 LDCM0281  AC21 HCT 116 C205(0.69)  LDD0598  [8]
 LDCM0282  AC22 HCT 116 C205(0.83)  LDD0599  [8]
 LDCM0283  AC23 HCT 116 C205(0.82)  LDD0600  [8]
 LDCM0284  AC24 HCT 116 C205(0.90)  LDD0601  [8]
 LDCM0285  AC25 HCT 116 C205(0.90)  LDD0602  [8]
 LDCM0286  AC26 HCT 116 C205(1.02)  LDD0603  [8]
 LDCM0287  AC27 HCT 116 C205(0.87)  LDD0604  [8]
 LDCM0288  AC28 HCT 116 C205(0.94)  LDD0605  [8]
 LDCM0289  AC29 HCT 116 C205(1.09)  LDD0606  [8]
 LDCM0290  AC3 HCT 116 C205(1.05)  LDD0607  [8]
 LDCM0291  AC30 HCT 116 C205(1.01)  LDD0608  [8]
 LDCM0292  AC31 HCT 116 C205(1.01)  LDD0609  [8]
 LDCM0293  AC32 HCT 116 C205(1.12)  LDD0610  [8]
 LDCM0294  AC33 HCT 116 C205(0.95)  LDD0611  [8]
 LDCM0295  AC34 HCT 116 C205(0.93)  LDD0612  [8]
 LDCM0296  AC35 HCT 116 C205(0.82)  LDD0613  [8]
 LDCM0297  AC36 HCT 116 C205(0.97)  LDD0614  [8]
 LDCM0298  AC37 HCT 116 C205(0.90)  LDD0615  [8]
 LDCM0299  AC38 HCT 116 C205(0.92)  LDD0616  [8]
 LDCM0300  AC39 HCT 116 C205(0.91)  LDD0617  [8]
 LDCM0301  AC4 HCT 116 C205(1.14)  LDD0618  [8]
 LDCM0302  AC40 HCT 116 C205(0.93)  LDD0619  [8]
 LDCM0303  AC41 HCT 116 C205(1.07)  LDD0620  [8]
 LDCM0304  AC42 HCT 116 C205(0.92)  LDD0621  [8]
 LDCM0305  AC43 HCT 116 C205(0.99)  LDD0622  [8]
 LDCM0306  AC44 HCT 116 C205(0.99)  LDD0623  [8]
 LDCM0307  AC45 HCT 116 C205(1.12)  LDD0624  [8]
 LDCM0308  AC46 HCT 116 C205(1.18)  LDD0625  [8]
 LDCM0309  AC47 HCT 116 C205(1.10)  LDD0626  [8]
 LDCM0310  AC48 HCT 116 C205(1.12)  LDD0627  [8]
 LDCM0311  AC49 HCT 116 C205(1.12)  LDD0628  [8]
 LDCM0312  AC5 HCT 116 C205(1.29)  LDD0629  [8]
 LDCM0313  AC50 HCT 116 C205(0.95)  LDD0630  [8]
 LDCM0314  AC51 HCT 116 C205(1.01)  LDD0631  [8]
 LDCM0315  AC52 HCT 116 C205(1.04)  LDD0632  [8]
 LDCM0316  AC53 HCT 116 C205(1.08)  LDD0633  [8]
 LDCM0317  AC54 HCT 116 C205(0.91)  LDD0634  [8]
 LDCM0318  AC55 HCT 116 C205(1.43)  LDD0635  [8]
 LDCM0319  AC56 HCT 116 C205(1.21)  LDD0636  [8]
 LDCM0320  AC57 HCT 116 C205(1.43)  LDD0637  [8]
 LDCM0321  AC58 HCT 116 C205(1.36)  LDD0638  [8]
 LDCM0322  AC59 HCT 116 C205(1.47)  LDD0639  [8]
 LDCM0323  AC6 HCT 116 C205(1.09)  LDD0640  [8]
 LDCM0324  AC60 HCT 116 C205(1.47)  LDD0641  [8]
 LDCM0325  AC61 HCT 116 C205(1.59)  LDD0642  [8]
 LDCM0326  AC62 HCT 116 C205(1.44)  LDD0643  [8]
 LDCM0327  AC63 HCT 116 C205(1.32)  LDD0644  [8]
 LDCM0328  AC64 HCT 116 C205(1.73)  LDD0645  [8]
 LDCM0329  AC65 HCT 116 C205(1.63)  LDD0646  [8]
 LDCM0330  AC66 HCT 116 C205(1.61)  LDD0647  [8]
 LDCM0331  AC67 HCT 116 C205(1.69)  LDD0648  [8]
 LDCM0332  AC68 HCT 116 C205(1.05)  LDD0649  [8]
 LDCM0333  AC69 HCT 116 C205(1.05)  LDD0650  [8]
 LDCM0334  AC7 HCT 116 C205(1.09)  LDD0651  [8]
 LDCM0335  AC70 HCT 116 C205(1.16)  LDD0652  [8]
 LDCM0336  AC71 HCT 116 C205(1.15)  LDD0653  [8]
 LDCM0337  AC72 HCT 116 C205(1.16)  LDD0654  [8]
 LDCM0338  AC73 HCT 116 C205(1.17)  LDD0655  [8]
 LDCM0339  AC74 HCT 116 C205(1.09)  LDD0656  [8]
 LDCM0340  AC75 HCT 116 C205(0.96)  LDD0657  [8]
 LDCM0341  AC76 HCT 116 C205(1.05)  LDD0658  [8]
 LDCM0342  AC77 HCT 116 C205(1.13)  LDD0659  [8]
 LDCM0343  AC78 HCT 116 C205(1.25)  LDD0660  [8]
 LDCM0344  AC79 HCT 116 C205(1.06)  LDD0661  [8]
 LDCM0345  AC8 HCT 116 C205(1.16)  LDD0662  [8]
 LDCM0346  AC80 HCT 116 C205(1.19)  LDD0663  [8]
 LDCM0347  AC81 HCT 116 C205(1.19)  LDD0664  [8]
 LDCM0348  AC82 HCT 116 C205(1.18)  LDD0665  [8]
 LDCM0349  AC83 HCT 116 C205(1.20)  LDD0666  [8]
 LDCM0350  AC84 HCT 116 C205(1.19)  LDD0667  [8]
 LDCM0351  AC85 HCT 116 C205(1.16)  LDD0668  [8]
 LDCM0352  AC86 HCT 116 C205(1.13)  LDD0669  [8]
 LDCM0353  AC87 HCT 116 C205(1.09)  LDD0670  [8]
 LDCM0354  AC88 HCT 116 C205(1.11)  LDD0671  [8]
 LDCM0355  AC89 HCT 116 C205(1.14)  LDD0672  [8]
 LDCM0357  AC90 HCT 116 C205(1.08)  LDD0674  [8]
 LDCM0358  AC91 HCT 116 C205(1.20)  LDD0675  [8]
 LDCM0359  AC92 HCT 116 C205(1.16)  LDD0676  [8]
 LDCM0360  AC93 HCT 116 C205(1.13)  LDD0677  [8]
 LDCM0361  AC94 HCT 116 C205(1.05)  LDD0678  [8]
 LDCM0362  AC95 HCT 116 C205(1.10)  LDD0679  [8]
 LDCM0363  AC96 HCT 116 C205(1.02)  LDD0680  [8]
 LDCM0364  AC97 HCT 116 C205(1.25)  LDD0681  [8]
 LDCM0365  AC98 HCT 116 C205(0.81)  LDD0682  [8]
 LDCM0366  AC99 HCT 116 C205(0.88)  LDD0683  [8]
 LDCM0248  AKOS034007472 HCT 116 C205(1.07)  LDD0565  [8]
 LDCM0356  AKOS034007680 HCT 116 C205(1.15)  LDD0673  [8]
 LDCM0275  AKOS034007705 HCT 116 C205(1.46)  LDD0592  [8]
 LDCM0156  Aniline NCI-H1299 11.48  LDD0403  [3]
 LDCM0020  ARS-1620 HCC44 C195(0.98); C205(0.79)  LDD2171  [8]
 LDCM0367  CL1 HEK-293T C205(1.01)  LDD1571  [16]
 LDCM0368  CL10 HEK-293T C205(0.70)  LDD1572  [16]
 LDCM0369  CL100 HCT 116 C205(1.05)  LDD0686  [8]
 LDCM0370  CL101 HCT 116 C205(1.09)  LDD0687  [8]
 LDCM0371  CL102 HCT 116 C205(1.01)  LDD0688  [8]
 LDCM0372  CL103 HCT 116 C205(0.91)  LDD0689  [8]
 LDCM0373  CL104 HCT 116 C205(0.98)  LDD0690  [8]
 LDCM0374  CL105 HCT 116 C205(0.89)  LDD0691  [8]
 LDCM0375  CL106 HCT 116 C205(0.77)  LDD0692  [8]
 LDCM0376  CL107 HCT 116 C205(0.91)  LDD0693  [8]
 LDCM0377  CL108 HCT 116 C205(1.06)  LDD0694  [8]
 LDCM0378  CL109 HCT 116 C205(0.85)  LDD0695  [8]
 LDCM0380  CL110 HCT 116 C205(1.07)  LDD0697  [8]
 LDCM0381  CL111 HCT 116 C205(1.00)  LDD0698  [8]
 LDCM0382  CL112 HCT 116 C205(0.82)  LDD0699  [8]
 LDCM0383  CL113 HCT 116 C205(0.97)  LDD0700  [8]
 LDCM0384  CL114 HCT 116 C205(0.95)  LDD0701  [8]
 LDCM0385  CL115 HCT 116 C205(0.90)  LDD0702  [8]
 LDCM0386  CL116 HCT 116 C205(0.92)  LDD0703  [8]
 LDCM0387  CL117 HCT 116 C205(0.91)  LDD0704  [8]
 LDCM0388  CL118 HCT 116 C205(0.93)  LDD0705  [8]
 LDCM0389  CL119 HCT 116 C205(0.97)  LDD0706  [8]
 LDCM0390  CL12 HEK-293T C205(0.77)  LDD1594  [16]
 LDCM0391  CL120 HCT 116 C205(1.04)  LDD0708  [8]
 LDCM0392  CL121 HCT 116 C205(1.10)  LDD0709  [8]
 LDCM0393  CL122 HCT 116 C205(1.05)  LDD0710  [8]
 LDCM0394  CL123 HCT 116 C205(0.82)  LDD0711  [8]
 LDCM0395  CL124 HCT 116 C205(1.24)  LDD0712  [8]
 LDCM0396  CL125 HCT 116 C205(1.15)  LDD0713  [8]
 LDCM0397  CL126 HCT 116 C205(1.01)  LDD0714  [8]
 LDCM0398  CL127 HCT 116 C205(1.07)  LDD0715  [8]
 LDCM0399  CL128 HCT 116 C205(1.52)  LDD0716  [8]
 LDCM0400  CL13 HEK-293T C205(0.97)  LDD1604  [16]
 LDCM0401  CL14 HEK-293T C205(0.91)  LDD1605  [16]
 LDCM0402  CL15 HEK-293T C205(0.88)  LDD1606  [16]
 LDCM0403  CL16 HEK-293T C205(0.99)  LDD1607  [16]
 LDCM0404  CL17 HEK-293T C205(0.85)  LDD1608  [16]
 LDCM0405  CL18 HEK-293T C205(1.15)  LDD1609  [16]
 LDCM0406  CL19 HEK-293T C205(1.07)  LDD1610  [16]
 LDCM0407  CL2 HEK-293T C205(0.93)  LDD1611  [16]
 LDCM0408  CL20 HEK-293T C205(0.99)  LDD1612  [16]
 LDCM0409  CL21 HEK-293T C205(0.84)  LDD1613  [16]
 LDCM0410  CL22 HEK-293T C205(0.75)  LDD1614  [16]
 LDCM0412  CL24 HEK-293T C205(0.70)  LDD1616  [16]
 LDCM0413  CL25 HEK-293T C205(0.95)  LDD1617  [16]
 LDCM0414  CL26 HEK-293T C205(1.15)  LDD1618  [16]
 LDCM0415  CL27 HEK-293T C205(1.06)  LDD1619  [16]
 LDCM0416  CL28 HEK-293T C205(1.01)  LDD1620  [16]
 LDCM0417  CL29 HEK-293T C205(0.97)  LDD1621  [16]
 LDCM0418  CL3 HEK-293T C205(0.99)  LDD1622  [16]
 LDCM0419  CL30 HEK-293T C205(1.11)  LDD1623  [16]
 LDCM0420  CL31 HCT 116 C205(0.86)  LDD0737  [8]
 LDCM0421  CL32 HCT 116 C205(0.94)  LDD0738  [8]
 LDCM0422  CL33 HCT 116 C205(1.12)  LDD0739  [8]
 LDCM0423  CL34 HCT 116 C205(1.24)  LDD0740  [8]
 LDCM0424  CL35 HCT 116 C205(0.95)  LDD0741  [8]
 LDCM0425  CL36 HCT 116 C205(0.93)  LDD0742  [8]
 LDCM0426  CL37 HCT 116 C205(0.86)  LDD0743  [8]
 LDCM0428  CL39 HCT 116 C205(0.92)  LDD0745  [8]
 LDCM0429  CL4 HEK-293T C205(0.84)  LDD1633  [16]
 LDCM0430  CL40 HCT 116 C205(0.80)  LDD0747  [8]
 LDCM0431  CL41 HCT 116 C205(0.86)  LDD0748  [8]
 LDCM0432  CL42 HCT 116 C205(0.75)  LDD0749  [8]
 LDCM0433  CL43 HCT 116 C205(0.98)  LDD0750  [8]
 LDCM0434  CL44 HCT 116 C205(0.98)  LDD0751  [8]
 LDCM0435  CL45 HCT 116 C205(1.00)  LDD0752  [8]
 LDCM0436  CL46 HEK-293T C205(0.72)  LDD1640  [16]
 LDCM0438  CL48 HEK-293T C205(0.71)  LDD1642  [16]
 LDCM0439  CL49 HEK-293T C205(1.04)  LDD1643  [16]
 LDCM0440  CL5 HEK-293T C205(1.04)  LDD1644  [16]
 LDCM0441  CL50 HEK-293T C205(1.03)  LDD1645  [16]
 LDCM0443  CL52 HEK-293T C205(1.15)  LDD1646  [16]
 LDCM0444  CL53 HEK-293T C205(0.86)  LDD1647  [16]
 LDCM0445  CL54 HEK-293T C205(0.98)  LDD1648  [16]
 LDCM0446  CL55 HEK-293T C205(0.95)  LDD1649  [16]
 LDCM0447  CL56 HEK-293T C205(0.94)  LDD1650  [16]
 LDCM0448  CL57 HEK-293T C205(0.90)  LDD1651  [16]
 LDCM0449  CL58 HEK-293T C205(0.82)  LDD1652  [16]
 LDCM0451  CL6 HEK-293T C205(1.14)  LDD1654  [16]
 LDCM0452  CL60 HEK-293T C205(0.73)  LDD1655  [16]
 LDCM0453  CL61 HCT 116 C205(1.05)  LDD0770  [8]
 LDCM0454  CL62 HCT 116 C205(1.02)  LDD0771  [8]
 LDCM0455  CL63 HCT 116 C205(0.84)  LDD0772  [8]
 LDCM0456  CL64 HCT 116 C205(1.04)  LDD0773  [8]
 LDCM0457  CL65 HCT 116 C205(0.96)  LDD0774  [8]
 LDCM0458  CL66 HCT 116 C205(1.12)  LDD0775  [8]
 LDCM0459  CL67 HCT 116 C205(0.92)  LDD0776  [8]
 LDCM0460  CL68 HCT 116 C205(0.98)  LDD0777  [8]
 LDCM0461  CL69 HCT 116 C205(1.02)  LDD0778  [8]
 LDCM0462  CL7 HEK-293T C205(1.05)  LDD1665  [16]
 LDCM0463  CL70 HCT 116 C205(1.04)  LDD0780  [8]
 LDCM0464  CL71 HCT 116 C205(0.84)  LDD0781  [8]
 LDCM0465  CL72 HCT 116 C205(1.16)  LDD0782  [8]
 LDCM0466  CL73 HCT 116 C205(0.93)  LDD0783  [8]
 LDCM0467  CL74 HCT 116 C205(0.87)  LDD0784  [8]
 LDCM0469  CL76 HCT 116 C205(0.88)  LDD0786  [8]
 LDCM0470  CL77 HCT 116 C205(0.87)  LDD0787  [8]
 LDCM0471  CL78 HCT 116 C205(0.90)  LDD0788  [8]
 LDCM0472  CL79 HCT 116 C205(0.93)  LDD0789  [8]
 LDCM0473  CL8 HEK-293T C205(0.76)  LDD1676  [16]
 LDCM0474  CL80 HCT 116 C205(1.00)  LDD0791  [8]
 LDCM0475  CL81 HCT 116 C205(0.86)  LDD0792  [8]
 LDCM0476  CL82 HCT 116 C205(0.96)  LDD0793  [8]
 LDCM0477  CL83 HCT 116 C205(0.83)  LDD0794  [8]
 LDCM0478  CL84 HCT 116 C205(0.96)  LDD0795  [8]
 LDCM0479  CL85 HCT 116 C205(1.03)  LDD0796  [8]
 LDCM0480  CL86 HCT 116 C205(0.99)  LDD0797  [8]
 LDCM0481  CL87 HCT 116 C205(0.85)  LDD0798  [8]
 LDCM0482  CL88 HCT 116 C205(0.82)  LDD0799  [8]
 LDCM0483  CL89 HCT 116 C205(0.88)  LDD0800  [8]
 LDCM0484  CL9 HEK-293T C205(1.01)  LDD1687  [16]
 LDCM0485  CL90 HCT 116 C205(0.75)  LDD0802  [8]
 LDCM0486  CL91 HCT 116 C205(1.07)  LDD0803  [8]
 LDCM0487  CL92 HCT 116 C205(0.93)  LDD0804  [8]
 LDCM0488  CL93 HCT 116 C205(0.99)  LDD0805  [8]
 LDCM0489  CL94 HCT 116 C205(0.85)  LDD0806  [8]
 LDCM0490  CL95 HCT 116 C205(0.96)  LDD0807  [8]
 LDCM0491  CL96 HCT 116 C205(1.14)  LDD0808  [8]
 LDCM0492  CL97 HCT 116 C205(1.27)  LDD0809  [8]
 LDCM0493  CL98 HCT 116 C205(1.03)  LDD0810  [8]
 LDCM0494  CL99 HCT 116 C205(1.16)  LDD0811  [8]
 LDCM0495  E2913 HEK-293T C205(0.96)  LDD1698  [16]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C205(0.83)  LDD1702  [4]
 LDCM0625  F8 Ramos C205(0.97)  LDD2187  [17]
 LDCM0572  Fragment10 Ramos C205(0.75)  LDD2189  [17]
 LDCM0573  Fragment11 Ramos C205(1.25)  LDD2190  [17]
 LDCM0574  Fragment12 Ramos C205(0.66)  LDD2191  [17]
 LDCM0575  Fragment13 Ramos C205(1.14)  LDD2192  [17]
 LDCM0576  Fragment14 Ramos C205(0.87)  LDD2193  [17]
 LDCM0579  Fragment20 Ramos C205(0.55)  LDD2194  [17]
 LDCM0580  Fragment21 Ramos C205(1.01)  LDD2195  [17]
 LDCM0582  Fragment23 Ramos C205(1.02)  LDD2196  [17]
 LDCM0578  Fragment27 Ramos C205(1.11)  LDD2197  [17]
 LDCM0586  Fragment28 Ramos C205(0.81)  LDD2198  [17]
 LDCM0588  Fragment30 Ramos C205(1.07)  LDD2199  [17]
 LDCM0589  Fragment31 Ramos C205(1.08)  LDD2200  [17]
 LDCM0590  Fragment32 Ramos C205(0.76)  LDD2201  [17]
 LDCM0468  Fragment33 HCT 116 C205(1.10)  LDD0785  [8]
 LDCM0596  Fragment38 Ramos C205(0.88)  LDD2203  [17]
 LDCM0566  Fragment4 Ramos C205(0.80)  LDD2184  [17]
 LDCM0427  Fragment51 HCT 116 C205(0.76)  LDD0744  [8]
 LDCM0610  Fragment52 Ramos C205(1.29)  LDD2204  [17]
 LDCM0614  Fragment56 Ramos C205(1.12)  LDD2205  [17]
 LDCM0569  Fragment7 Ramos C205(0.63)  LDD2186  [17]
 LDCM0571  Fragment9 Ramos C205(0.63)  LDD2188  [17]
 LDCM0116  HHS-0101 DM93 Y228(0.98)  LDD0264  [6]
 LDCM0117  HHS-0201 DM93 Y228(0.91)  LDD0265  [6]
 LDCM0118  HHS-0301 DM93 Y228(0.88)  LDD0266  [6]
 LDCM0119  HHS-0401 DM93 Y228(0.86)  LDD0267  [6]
 LDCM0120  HHS-0701 DM93 Y228(1.53)  LDD0268  [6]
 LDCM0123  JWB131 DM93 Y228(0.87)  LDD0285  [5]
 LDCM0124  JWB142 DM93 Y228(1.33)  LDD0286  [5]
 LDCM0126  JWB150 DM93 Y228(1.89)  LDD0288  [5]
 LDCM0129  JWB202 DM93 Y228(0.58)  LDD0291  [5]
 LDCM0130  JWB211 DM93 Y228(0.96)  LDD0292  [5]
 LDCM0022  KB02 HEK-293T C205(0.99)  LDD1492  [16]
 LDCM0023  KB03 HEK-293T C205(0.92)  LDD1497  [16]
 LDCM0024  KB05 UACC62 C195(1.46)  LDD3326  [18]
 LDCM0109  NEM HeLa N.A.  LDD0224  [13]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C205(0.49)  LDD2109  [4]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C205(0.79)  LDD2111  [4]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C205(1.00)  LDD2123  [4]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C205(0.63)  LDD2125  [4]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C205(1.11)  LDD2127  [4]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C205(0.93)  LDD2136  [4]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C205(0.77)  LDD2137  [4]
 LDCM0021  THZ1 HCT 116 C195(0.98); C205(0.79)  LDD2173  [8]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 11 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Histone-lysine N-methyltransferase 2A (KMT2A) Histone-lysine methyltransferase family Q03164
Histone-lysine N-methyltransferase 2B (KMT2B) Histone-lysine methyltransferase family Q9UMN6
Histone-lysine N-methyltransferase 2C (KMT2C) Histone-lysine methyltransferase family Q8NEZ4
Histone-lysine N-methyltransferase 2D (KMT2D) Histone-lysine methyltransferase family O14686
Histone acetyltransferase KAT6A (KAT6A) MYST (SAS/MOZ) family Q92794
Kallikrein-6 (KLK6) Peptidase S1 family Q92876
Chromodomain-helicase-DNA-binding protein 8 (CHD8) SNF2/RAD54 helicase family Q9HCK8
TNF receptor-associated factor 3 (TRAF3) TNF receptor-associated factor family Q13114
TNF receptor-associated factor 6 (TRAF6) TNF receptor-associated factor family Q9Y4K3
Lysine-specific demethylase 6A (KDM6A) UTX family O15550
NEDD4-like E3 ubiquitin-protein ligase WWP2 (WWP2) . O00308
Transcription factor
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Heat shock factor protein 2 (HSF2) HSF family Q03933
Telomere zinc finger-associated protein (ZBTB48) Krueppel C2H2-type zinc-finger protein family P10074
Photoreceptor-specific nuclear receptor (NR2E3) Nuclear hormone receptor family Q9Y5X4
Telomeric repeat-binding factor 2-interacting protein 1 (TERF2IP) RAP1 family Q9NYB0
Zinc finger protein ZXDC (ZXDC) ZXD family Q2QGD7
Other
Click To Hide/Show 21 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Afadin- and alpha-actinin-binding protein (SSX2IP) ADIP family Q9Y2D8
A-kinase anchor protein 8 (AKAP8) AKAP95 family O43823
Biorientation of chromosomes in cell division protein 1-like 1 (BOD1L1) BOD1 family Q8NFC6
Anaphase-promoting complex subunit 2 (ANAPC2) Cullin family Q9UJX6
Cytoplasmic dynein 1 heavy chain 1 (DYNC1H1) Dynein heavy chain family Q14204
Protein FAM199X (FAM199X) FAM199 family Q6PEV8
Histone H3.1 (H3C1; H3C2; H3C3; H3C4; H3C6; H3C7; H3C8; H3C10; H3C11; H3C12) Histone H3 family P68431
Protein Mdm4 (MDM4) MDM2/MDM4 family O15151
Serine/arginine repetitive matrix protein 4 (SRRM4) NSR100 family A7MD48
Atrophin-1 (ATN1) . P54259
Bcl-2-binding component 3, isoforms 3/4 (BBC3) . Q96PG8
Host cell factor 1 (HCFC1) . P51610
KAT8 regulatory NSL complex subunit 1 (KANSL1) . Q7Z3B3
KAT8 regulatory NSL complex subunit 2 (KANSL2) . Q9H9L4
MAP3K12-binding inhibitory protein 1 (MBIP) . Q9NS73
Meiosis regulator and mRNA stability factor 1 (MARF1) . Q9Y4F3
Menin (MEN1) . O00255
Nuclear receptor coactivator 6 (NCOA6) . Q14686
PAX-interacting protein 1 (PAXIP1) . Q6ZW49
Retinoblastoma-binding protein 5 (RBBP5) . Q15291
ZZ-type zinc finger-containing protein 3 (ZZZ3) . Q8IYH5

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Oicr-9429 Small molecular drug D0XI3W

References

1 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.
2 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.
3 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.
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 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.
6 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.
7 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.
8 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.
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 Site-Specific Activity-Based Protein Profiling Using Phosphonate Handles. Mol Cell Proteomics. 2023 Jan;22(1):100455. doi: 10.1016/j.mcpro.2022.100455. Epub 2022 Nov 24.
Mass spectrometry data entry: PXD036569
12 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
13 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.
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 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.
16 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
17 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
18 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