Details of the Target

General Information of Target

Target ID LDTP06502
Target Name Histone-lysine N-methyltransferase EZH2 (EZH2)
Gene Name EZH2
Gene ID 2146
Synonyms
KMT6; Histone-lysine N-methyltransferase EZH2; EC 2.1.1.356; ENX-1; Enhancer of zeste homolog 2; Lysine N-methyltransferase 6
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFH
ATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPN
NSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKM
KPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPA
PAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQ
NFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVS
CKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDK
YMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGE
ELFFDYRYSQADALKYVGIEREMEIP
Target Type
Successful
Target Bioclass
Enzyme
Family
Class V-like SAM-binding methyltransferase superfamily, Histone-lysine methyltransferase family, EZ subfamily
Subcellular location
Nucleus
Function
Polycomb group (PcG) protein. Catalytic subunit of the PRC2/EED-EZH2 complex, which methylates 'Lys-9' (H3K9me) and 'Lys-27' (H3K27me) of histone H3, leading to transcriptional repression of the affected target gene. Able to mono-, di- and trimethylate 'Lys-27' of histone H3 to form H3K27me1, H3K27me2 and H3K27me3, respectively. Displays a preference for substrates with less methylation, loses activity when progressively more methyl groups are incorporated into H3K27, H3K27me0 > H3K27me1 > H3K27me2. Compared to EZH1-containing complexes, it is more abundant in embryonic stem cells and plays a major role in forming H3K27me3, which is required for embryonic stem cell identity and proper differentiation. The PRC2/EED-EZH2 complex may also serve as a recruiting platform for DNA methyltransferases, thereby linking two epigenetic repression systems. Genes repressed by the PRC2/EED-EZH2 complex include HOXC8, HOXA9, MYT1, CDKN2A and retinoic acid target genes. EZH2 can also methylate non-histone proteins such as the transcription factor GATA4 and the nuclear receptor RORA. Regulates the circadian clock via histone methylation at the promoter of the circadian genes. Essential for the CRY1/2-mediated repression of the transcriptional activation of PER1/2 by the CLOCK-BMAL1 heterodimer; involved in the di and trimethylation of 'Lys-27' of histone H3 on PER1/2 promoters which is necessary for the CRY1/2 proteins to inhibit transcription.
TTD ID
T25265
Uniprot ID
Q15910
DrugMap ID
TTJW2UQ
Ensemble ID
ENST00000320356.7
HGNC ID
HGNC:3527
ChEMBL ID
CHEMBL2189110

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 21 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
STPyne
 Probe Info  		K713(7.39)  LDD0277  [2]
BTD
 Probe Info  		C604(1.44)  LDD2099  [3]
AHL-Pu-1
 Probe Info  		C503(2.18)  LDD0171  [4]
DBIA
 Probe Info  		C663(6.73)  LDD0204  [5]
5E-2FA
 Probe Info  		H69(0.00); H327(0.00)  LDD2235  [6]
4-Iodoacetamidophenylacetylene
 Probe Info  		C523(0.00); C83(0.00); C695(0.00); C503(0.00)  LDD0038  [7]
IA-alkyne
 Probe Info  		C83(0.00); C286(0.00); C695(0.00); C503(0.00)  LDD0036  [7]
IPIAA_L
 Probe Info  		N.A.  LDD0031  [8]
Lodoacetamide azide
 Probe Info  		C523(0.00); C286(0.00); C695(0.00); C503(0.00)  LDD0037  [7]
NAIA_4
 Probe Info  		N.A.  LDD2226  [9]
WYneN
 Probe Info  		N.A.  LDD0021  [10]
Compound 10
 Probe Info  		C14(0.00); C503(0.00)  LDD2216  [11]
ENE
 Probe Info  		N.A.  LDD0006  [10]
IPM
 Probe Info  		C414(0.00); C14(0.00)  LDD0005  [10]
Phosphinate-6
 Probe Info  		C503(0.00); C14(0.00)  LDD0018  [12]
Acrolein
 Probe Info  		C695(0.00); C642(0.00)  LDD0217  [13]
Crotonaldehyde
 Probe Info  		N.A.  LDD0219  [13]
Methacrolein
 Probe Info  		N.A.  LDD0218  [13]
AOyne
 Probe Info  		15.00  LDD0443  [14]
NAIA_5
 Probe Info  		N.A.  LDD2223  [9]

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 C14(2.54)  LDD2117  [3]
 LDCM0025  4SU-RNA HEK-293T C163(2.15)  LDD0371  [4]
 LDCM0026  4SU-RNA+native RNA DM93 C503(2.18)  LDD0171  [4]
 LDCM0214  AC1 HEK-293T C695(1.10); C663(1.01); C642(0.55); C260(0.96)  LDD1507  [15]
 LDCM0215  AC10 HEK-293T C695(1.13); C663(0.96); C260(1.11); C503(1.24)  LDD1508  [15]
 LDCM0226  AC11 HEK-293T C260(1.01); C83(1.06); C503(0.88)  LDD1509  [15]
 LDCM0237  AC12 HEK-293T C695(0.99); C294(0.68); C663(0.95); C260(1.14)  LDD1510  [15]
 LDCM0259  AC14 HEK-293T C695(1.01); C663(0.90); C642(0.97); C260(1.04)  LDD1512  [15]
 LDCM0270  AC15 HEK-293T C695(0.88); C663(0.91); C260(1.17); C83(1.05)  LDD1513  [15]
 LDCM0276  AC17 HEK-293T C695(0.88); C663(1.04); C642(0.85); C260(0.96)  LDD1515  [15]
 LDCM0277  AC18 HEK-293T C695(1.10); C663(0.89); C260(1.16); C503(1.30)  LDD1516  [15]
 LDCM0278  AC19 HEK-293T C260(1.02); C83(0.82); C503(1.37)  LDD1517  [15]
 LDCM0279  AC2 HEK-293T C695(0.99); C663(0.97); C260(1.37); C503(1.33)  LDD1518  [15]
 LDCM0280  AC20 HEK-293T C695(0.99); C294(0.96); C663(1.07); C260(1.09)  LDD1519  [15]
 LDCM0281  AC21 HEK-293T C663(1.23); C83(1.26); C503(0.91)  LDD1520  [15]
 LDCM0282  AC22 HEK-293T C695(1.06); C663(0.94); C642(0.96); C260(0.99)  LDD1521  [15]
 LDCM0283  AC23 HEK-293T C695(0.93); C663(0.95); C260(1.15); C83(1.16)  LDD1522  [15]
 LDCM0284  AC24 HEK-293T C695(0.96); C663(0.87); C503(1.03)  LDD1523  [15]
 LDCM0285  AC25 HEK-293T C695(0.87); C663(0.99); C642(0.53); C260(1.14)  LDD1524  [15]
 LDCM0286  AC26 HEK-293T C695(0.98); C663(1.07); C260(1.12); C503(1.06)  LDD1525  [15]
 LDCM0287  AC27 HEK-293T C260(0.94); C83(0.91); C503(1.15)  LDD1526  [15]
 LDCM0288  AC28 HEK-293T C695(1.04); C294(1.11); C663(1.03); C260(0.97)  LDD1527  [15]
 LDCM0289  AC29 HEK-293T C663(1.26); C83(1.02); C503(1.02)  LDD1528  [15]
 LDCM0290  AC3 HEK-293T C260(1.04); C83(0.97); C503(1.27)  LDD1529  [15]
 LDCM0291  AC30 HEK-293T C695(1.01); C663(0.76); C642(1.03); C260(1.09)  LDD1530  [15]
 LDCM0292  AC31 HEK-293T C695(1.02); C663(1.05); C260(1.12); C83(1.07)  LDD1531  [15]
 LDCM0293  AC32 HEK-293T C695(1.00); C663(1.22); C503(1.10)  LDD1532  [15]
 LDCM0294  AC33 HEK-293T C695(0.97); C663(1.28); C642(0.91); C260(0.68)  LDD1533  [15]
 LDCM0295  AC34 HEK-293T C695(1.03); C663(0.91); C260(1.14); C503(1.09)  LDD1534  [15]
 LDCM0296  AC35 HEK-293T C260(1.00); C83(0.94); C503(1.05)  LDD1535  [15]
 LDCM0297  AC36 HEK-293T C695(1.08); C294(0.82); C663(1.10); C260(1.15)  LDD1536  [15]
 LDCM0298  AC37 HEK-293T C663(0.99); C83(1.12); C503(0.98)  LDD1537  [15]
 LDCM0299  AC38 HEK-293T C695(1.03); C663(0.75); C642(1.06); C260(1.13)  LDD1538  [15]
 LDCM0300  AC39 HEK-293T C695(0.95); C663(1.31); C260(1.05); C83(1.10)  LDD1539  [15]
 LDCM0301  AC4 HEK-293T C695(1.14); C294(1.02); C663(1.06); C260(1.13)  LDD1540  [15]
 LDCM0302  AC40 HEK-293T C695(0.98); C663(0.87); C503(1.01)  LDD1541  [15]
 LDCM0303  AC41 HEK-293T C695(0.99); C663(1.11); C642(0.96); C260(1.08)  LDD1542  [15]
 LDCM0304  AC42 HEK-293T C695(1.09); C663(0.91); C260(1.24); C503(1.25)  LDD1543  [15]
 LDCM0305  AC43 HEK-293T C260(1.10); C83(1.00); C503(1.12)  LDD1544  [15]
 LDCM0306  AC44 HEK-293T C695(1.00); C294(0.77); C663(1.10); C260(1.18)  LDD1545  [15]
 LDCM0307  AC45 HEK-293T C663(0.96); C83(1.17); C503(1.01)  LDD1546  [15]
 LDCM0308  AC46 HEK-293T C695(1.12); C663(0.93); C642(1.21); C260(0.98)  LDD1547  [15]
 LDCM0309  AC47 HEK-293T C695(1.02); C663(1.15); C260(1.33); C83(1.18)  LDD1548  [15]
 LDCM0310  AC48 HEK-293T C695(1.02); C663(1.07); C503(1.16)  LDD1549  [15]
 LDCM0311  AC49 HEK-293T C695(1.00); C663(1.03); C642(0.94); C260(1.18)  LDD1550  [15]
 LDCM0312  AC5 HEK-293T C663(0.81); C83(0.94); C503(1.10)  LDD1551  [15]
 LDCM0313  AC50 HEK-293T C695(1.09); C663(1.06); C260(1.03); C503(1.22)  LDD1552  [15]
 LDCM0314  AC51 HEK-293T C260(1.03); C83(1.02); C503(1.24)  LDD1553  [15]
 LDCM0315  AC52 HEK-293T C695(1.02); C294(0.73); C663(1.22); C260(1.01)  LDD1554  [15]
 LDCM0316  AC53 HEK-293T C663(1.01); C83(1.08); C503(1.00)  LDD1555  [15]
 LDCM0317  AC54 HEK-293T C695(1.09); C663(0.81); C642(1.18); C260(1.13)  LDD1556  [15]
 LDCM0318  AC55 HEK-293T C695(0.95); C663(1.06); C260(1.09); C83(1.22)  LDD1557  [15]
 LDCM0319  AC56 HEK-293T C695(1.01); C663(1.04); C503(1.22)  LDD1558  [15]
 LDCM0320  AC57 HEK-293T C695(0.95); C663(1.27); C642(1.35); C260(1.17)  LDD1559  [15]
 LDCM0321  AC58 HEK-293T C695(1.08); C663(1.05); C260(1.15); C503(1.15)  LDD1560  [15]
 LDCM0322  AC59 HEK-293T C260(1.05); C83(1.14); C503(1.20)  LDD1561  [15]
 LDCM0323  AC6 HEK-293T C695(1.11); C663(0.92); C642(1.02); C260(1.11)  LDD1562  [15]
 LDCM0324  AC60 HEK-293T C695(1.08); C294(0.83); C663(1.10); C260(1.14)  LDD1563  [15]
 LDCM0325  AC61 HEK-293T C663(0.99); C83(1.30); C503(1.08)  LDD1564  [15]
 LDCM0326  AC62 HEK-293T C695(1.08); C663(1.03); C642(1.12); C260(1.06)  LDD1565  [15]
 LDCM0327  AC63 HEK-293T C695(1.09); C663(1.14); C260(1.06); C83(1.09)  LDD1566  [15]
 LDCM0328  AC64 HEK-293T C695(1.04); C663(1.02); C503(1.21)  LDD1567  [15]
 LDCM0334  AC7 HEK-293T C695(1.05); C663(1.36); C260(1.11); C83(1.13)  LDD1568  [15]
 LDCM0345  AC8 HEK-293T C695(1.08); C663(1.15); C503(1.14)  LDD1569  [15]
 LDCM0248  AKOS034007472 HEK-293T C663(0.99); C83(0.93); C503(0.96)  LDD1511  [15]
 LDCM0356  AKOS034007680 HEK-293T C695(0.91); C663(1.21); C642(1.01); C260(1.15)  LDD1570  [15]
 LDCM0275  AKOS034007705 HEK-293T C695(0.98); C663(0.97); C503(1.20)  LDD1514  [15]
 LDCM0156  Aniline NCI-H1299 11.99  LDD0403  [1]
 LDCM0102  BDHI 8 Jurkat C663(6.73)  LDD0204  [5]
 LDCM0108  Chloroacetamide HeLa C695(0.00); C642(0.00)  LDD0222  [13]
 LDCM0367  CL1 HEK-293T C695(1.07); C294(1.22); C663(1.01); C642(0.88)  LDD1571  [15]
 LDCM0368  CL10 HEK-293T C695(0.74); C663(1.06); C642(1.05); C260(0.87)  LDD1572  [15]
 LDCM0369  CL100 HEK-293T C695(1.15); C663(1.11); C260(1.03); C83(0.84)  LDD1573  [15]
 LDCM0370  CL101 HEK-293T C695(0.95); C294(1.01); C663(1.26); C642(0.92)  LDD1574  [15]
 LDCM0371  CL102 HEK-293T C260(0.89); C83(0.86); C503(1.11)  LDD1575  [15]
 LDCM0372  CL103 HEK-293T C695(0.94); C663(1.08); C260(0.92); C83(0.93)  LDD1576  [15]
 LDCM0373  CL104 HEK-293T C695(1.12); C663(1.07); C260(1.08); C83(0.88)  LDD1577  [15]
 LDCM0374  CL105 HEK-293T C695(0.90); C294(1.28); C663(1.20); C642(0.84)  LDD1578  [15]
 LDCM0375  CL106 HEK-293T C260(0.98); C83(1.04); C503(1.06)  LDD1579  [15]
 LDCM0376  CL107 HEK-293T C695(1.06); C663(1.03); C260(1.00); C83(1.06)  LDD1580  [15]
 LDCM0377  CL108 HEK-293T C695(1.22); C663(1.02); C260(0.99); C83(0.72)  LDD1581  [15]
 LDCM0378  CL109 HEK-293T C695(0.95); C294(1.18); C663(1.09); C642(1.00)  LDD1582  [15]
 LDCM0379  CL11 HEK-293T C695(0.79); C663(0.65); C260(1.06); C83(0.92)  LDD1583  [15]
 LDCM0380  CL110 HEK-293T C260(0.87); C83(0.96); C503(1.06)  LDD1584  [15]
 LDCM0381  CL111 HEK-293T C695(1.06); C663(0.89); C260(0.86); C83(0.92)  LDD1585  [15]
 LDCM0382  CL112 HEK-293T C695(1.21); C663(1.11); C260(0.96); C83(1.00)  LDD1586  [15]
 LDCM0383  CL113 HEK-293T C695(1.06); C294(1.48); C663(1.16); C642(0.98)  LDD1587  [15]
 LDCM0384  CL114 HEK-293T C260(0.81); C83(1.03); C503(1.21)  LDD1588  [15]
 LDCM0385  CL115 HEK-293T C695(1.03); C663(1.20); C260(0.99); C83(1.01)  LDD1589  [15]
 LDCM0386  CL116 HEK-293T C695(1.07); C663(1.01); C260(1.01); C83(1.11)  LDD1590  [15]
 LDCM0387  CL117 HEK-293T C695(1.04); C294(1.30); C663(1.17); C642(0.81)  LDD1591  [15]
 LDCM0388  CL118 HEK-293T C260(1.04); C83(1.19); C503(1.09)  LDD1592  [15]
 LDCM0389  CL119 HEK-293T C695(1.24); C663(0.95); C260(1.10); C83(1.13)  LDD1593  [15]
 LDCM0390  CL12 HEK-293T C695(0.80); C663(1.12); C503(0.29)  LDD1594  [15]
 LDCM0391  CL120 HEK-293T C695(1.25); C663(1.12); C260(0.97); C83(0.91)  LDD1595  [15]
 LDCM0392  CL121 HEK-293T C695(0.97); C294(1.30); C663(1.18); C642(1.05)  LDD1596  [15]
 LDCM0393  CL122 HEK-293T C260(1.04); C83(0.92); C503(1.17)  LDD1597  [15]
 LDCM0394  CL123 HEK-293T C695(1.06); C663(1.00); C260(0.89); C83(0.90)  LDD1598  [15]
 LDCM0395  CL124 HEK-293T C695(1.16); C663(0.96); C260(1.02); C83(0.90)  LDD1599  [15]
 LDCM0396  CL125 HEK-293T C695(0.94); C294(0.68); C663(1.10); C642(0.87)  LDD1600  [15]
 LDCM0397  CL126 HEK-293T C260(1.03); C83(1.24); C503(1.22)  LDD1601  [15]
 LDCM0398  CL127 HEK-293T C695(0.99); C663(1.24); C260(1.01); C83(1.10)  LDD1602  [15]
 LDCM0399  CL128 HEK-293T C695(0.99); C663(1.10); C260(0.99); C83(0.84)  LDD1603  [15]
 LDCM0400  CL13 HEK-293T C695(0.98); C294(1.00); C663(1.12); C642(0.91)  LDD1604  [15]
 LDCM0401  CL14 HEK-293T C260(1.01); C83(1.06); C503(0.86)  LDD1605  [15]
 LDCM0402  CL15 HEK-293T C695(0.79); C663(0.80); C260(0.87); C83(0.92)  LDD1606  [15]
 LDCM0403  CL16 HEK-293T C695(0.97); C663(0.96); C260(1.25); C83(0.80)  LDD1607  [15]
 LDCM0404  CL17 HEK-293T C695(0.77); C663(0.97); C642(0.58); C260(1.10)  LDD1608  [15]
 LDCM0405  CL18 HEK-293T C695(0.93); C663(1.12); C260(1.18); C503(0.50)  LDD1609  [15]
 LDCM0406  CL19 HEK-293T C260(1.05); C83(1.04); C503(0.41)  LDD1610  [15]
 LDCM0407  CL2 HEK-293T C260(1.09); C83(1.00); C503(0.81)  LDD1611  [15]
 LDCM0408  CL20 HEK-293T C695(0.97); C294(0.62); C663(0.97); C260(1.14)  LDD1612  [15]
 LDCM0409  CL21 HEK-293T C663(1.06); C83(1.04); C503(0.37)  LDD1613  [15]
 LDCM0410  CL22 HEK-293T C695(0.84); C663(0.62); C642(1.16); C260(1.01)  LDD1614  [15]
 LDCM0411  CL23 HEK-293T C695(0.77); C663(0.76); C260(1.21); C83(0.94)  LDD1615  [15]
 LDCM0412  CL24 HEK-293T C695(0.86); C663(1.18); C503(0.28)  LDD1616  [15]
 LDCM0413  CL25 HEK-293T C695(0.96); C294(0.98); C663(0.92); C642(0.97)  LDD1617  [15]
 LDCM0414  CL26 HEK-293T C260(1.12); C83(1.00); C503(0.95)  LDD1618  [15]
 LDCM0415  CL27 HEK-293T C695(1.13); C663(0.84); C260(0.89); C83(1.16)  LDD1619  [15]
 LDCM0416  CL28 HEK-293T C695(0.96); C663(0.82); C260(1.03); C83(0.83)  LDD1620  [15]
 LDCM0417  CL29 HEK-293T C695(0.85); C663(1.05); C642(1.14); C260(1.09)  LDD1621  [15]
 LDCM0418  CL3 HEK-293T C695(1.01); C663(0.96); C260(1.16); C83(0.99)  LDD1622  [15]
 LDCM0419  CL30 HEK-293T C695(0.91); C663(0.88); C260(1.04); C503(0.53)  LDD1623  [15]
 LDCM0420  CL31 HEK-293T C260(1.04); C83(0.97); C503(0.42)  LDD1624  [15]
 LDCM0421  CL32 HEK-293T C695(0.86); C294(0.56); C663(1.05); C260(0.98)  LDD1625  [15]
 LDCM0422  CL33 HEK-293T C663(0.81); C83(0.98); C503(0.44)  LDD1626  [15]
 LDCM0423  CL34 HEK-293T C695(0.98); C663(0.50); C642(0.95); C260(0.95)  LDD1627  [15]
 LDCM0424  CL35 HEK-293T C695(0.74); C663(0.69); C260(1.09); C83(1.09)  LDD1628  [15]
 LDCM0425  CL36 HEK-293T C695(0.86); C663(1.06); C503(0.25)  LDD1629  [15]
 LDCM0426  CL37 HEK-293T C695(0.94); C294(0.90); C663(1.18); C642(0.91)  LDD1630  [15]
 LDCM0428  CL39 HEK-293T C695(1.03); C663(1.08); C260(0.94); C83(1.07)  LDD1632  [15]
 LDCM0429  CL4 HEK-293T C695(1.03); C663(0.95); C260(0.98); C83(1.01)  LDD1633  [15]
 LDCM0430  CL40 HEK-293T C695(1.11); C663(1.07); C260(1.07); C83(0.79)  LDD1634  [15]
 LDCM0431  CL41 HEK-293T C695(0.99); C663(0.88); C642(1.00); C260(0.80)  LDD1635  [15]
 LDCM0432  CL42 HEK-293T C695(1.01); C663(1.01); C260(1.10); C503(0.64)  LDD1636  [15]
 LDCM0433  CL43 HEK-293T C260(1.03); C83(1.06); C503(0.41)  LDD1637  [15]
 LDCM0434  CL44 HEK-293T C695(0.79); C294(0.50); C663(0.87); C260(1.07)  LDD1638  [15]
 LDCM0435  CL45 HEK-293T C663(0.86); C83(1.07); C503(0.43)  LDD1639  [15]
 LDCM0436  CL46 HEK-293T C695(0.87); C663(0.72); C642(1.07); C260(1.03)  LDD1640  [15]
 LDCM0437  CL47 HEK-293T C695(0.78); C663(0.73); C260(1.05); C83(1.15)  LDD1641  [15]
 LDCM0438  CL48 HEK-293T C695(0.86); C663(0.81); C503(0.34)  LDD1642  [15]
 LDCM0439  CL49 HEK-293T C695(0.92); C294(1.04); C663(1.25); C642(0.92)  LDD1643  [15]
 LDCM0440  CL5 HEK-293T C695(0.84); C663(1.23); C642(0.49); C260(1.01)  LDD1644  [15]
 LDCM0441  CL50 HEK-293T C260(0.99); C83(1.05); C503(0.91)  LDD1645  [15]
 LDCM0443  CL52 HEK-293T C695(1.09); C663(1.00); C260(1.09); C83(1.03)  LDD1646  [15]
 LDCM0444  CL53 HEK-293T C695(0.95); C663(0.98); C642(0.93); C260(0.97)  LDD1647  [15]
 LDCM0445  CL54 HEK-293T C695(0.95); C663(0.88); C260(0.98); C503(0.53)  LDD1648  [15]
 LDCM0446  CL55 HEK-293T C260(1.03); C83(1.10); C503(0.40)  LDD1649  [15]
 LDCM0447  CL56 HEK-293T C695(0.88); C294(0.69); C663(1.06); C260(1.12)  LDD1650  [15]
 LDCM0448  CL57 HEK-293T C663(1.05); C83(0.98); C503(0.44)  LDD1651  [15]
 LDCM0449  CL58 HEK-293T C695(0.89); C663(0.58); C642(1.07); C260(1.13)  LDD1652  [15]
 LDCM0450  CL59 HEK-293T C695(0.78); C663(0.86); C260(1.15); C83(1.01)  LDD1653  [15]
 LDCM0451  CL6 HEK-293T C695(0.90); C663(1.14); C260(1.12); C503(0.52)  LDD1654  [15]
 LDCM0452  CL60 HEK-293T C695(0.82); C663(0.76); C503(0.28)  LDD1655  [15]
 LDCM0453  CL61 HEK-293T C695(1.16); C294(1.51); C663(1.03); C642(0.95)  LDD1656  [15]
 LDCM0454  CL62 HEK-293T C260(1.07); C83(1.09); C503(1.05)  LDD1657  [15]
 LDCM0455  CL63 HEK-293T C695(1.08); C663(1.02); C260(0.96); C83(0.94)  LDD1658  [15]
 LDCM0456  CL64 HEK-293T C695(1.05); C663(1.09); C260(1.00); C83(0.84)  LDD1659  [15]
 LDCM0457  CL65 HEK-293T C695(0.77); C663(1.24); C642(0.94); C260(0.85)  LDD1660  [15]
 LDCM0458  CL66 HEK-293T C695(0.94); C663(1.04); C260(1.22); C503(0.68)  LDD1661  [15]
 LDCM0459  CL67 HEK-293T C260(1.05); C83(0.97); C503(0.52)  LDD1662  [15]
 LDCM0460  CL68 HEK-293T C695(0.97); C294(0.53); C663(0.82); C260(1.04)  LDD1663  [15]
 LDCM0461  CL69 HEK-293T C663(1.09); C83(1.18); C503(0.43)  LDD1664  [15]
 LDCM0462  CL7 HEK-293T C260(1.21); C83(0.97); C503(0.42)  LDD1665  [15]
 LDCM0463  CL70 HEK-293T C695(0.86); C663(0.62); C642(0.98); C260(1.04)  LDD1666  [15]
 LDCM0464  CL71 HEK-293T C695(0.78); C663(0.74); C260(1.15); C83(0.85)  LDD1667  [15]
 LDCM0465  CL72 HEK-293T C695(0.81); C663(1.05); C503(0.36)  LDD1668  [15]
 LDCM0466  CL73 HEK-293T C695(1.10); C294(1.12); C663(1.01); C642(1.00)  LDD1669  [15]
 LDCM0467  CL74 HEK-293T C260(1.09); C83(1.11); C503(1.06)  LDD1670  [15]
 LDCM0469  CL76 HEK-293T C695(1.24); C663(1.18); C260(1.20); C83(0.98)  LDD1672  [15]
 LDCM0470  CL77 HEK-293T C695(0.93); C663(1.00); C642(1.13); C260(1.19)  LDD1673  [15]
 LDCM0471  CL78 HEK-293T C695(0.98); C663(1.18); C260(1.15); C503(0.66)  LDD1674  [15]
 LDCM0472  CL79 HEK-293T C260(1.04); C83(1.07); C503(0.54)  LDD1675  [15]
 LDCM0473  CL8 HEK-293T C695(0.75); C294(0.51); C663(0.83); C260(0.81)  LDD1676  [15]
 LDCM0474  CL80 HEK-293T C695(0.95); C294(0.67); C663(0.98); C260(0.99)  LDD1677  [15]
 LDCM0475  CL81 HEK-293T C663(0.95); C83(1.25); C503(0.45)  LDD1678  [15]
 LDCM0476  CL82 HEK-293T C695(0.97); C663(0.71); C642(1.04); C260(1.23)  LDD1679  [15]
 LDCM0477  CL83 HEK-293T C695(0.85); C663(0.73); C260(1.06); C83(0.97)  LDD1680  [15]
 LDCM0478  CL84 HEK-293T C695(0.81); C663(0.93); C503(0.35)  LDD1681  [15]
 LDCM0479  CL85 HEK-293T C695(1.12); C294(0.80); C663(1.22); C642(0.86)  LDD1682  [15]
 LDCM0480  CL86 HEK-293T C260(1.05); C83(1.15); C503(1.16)  LDD1683  [15]
 LDCM0481  CL87 HEK-293T C695(0.95); C663(1.13); C260(1.04); C83(1.20)  LDD1684  [15]
 LDCM0482  CL88 HEK-293T C695(1.29); C663(1.04); C260(1.24); C83(0.92)  LDD1685  [15]
 LDCM0483  CL89 HEK-293T C695(0.90); C663(1.01); C642(0.81); C260(1.06)  LDD1686  [15]
 LDCM0484  CL9 HEK-293T C663(0.91); C83(0.89); C503(0.42)  LDD1687  [15]
 LDCM0485  CL90 HEK-293T C695(0.78); C663(0.83); C260(0.96); C503(0.81)  LDD1688  [15]
 LDCM0486  CL91 HEK-293T C260(1.11); C83(1.31); C503(0.61)  LDD1689  [15]
 LDCM0487  CL92 HEK-293T C695(0.89); C294(0.58); C663(1.05); C260(1.34)  LDD1690  [15]
 LDCM0488  CL93 HEK-293T C663(0.84); C83(0.84); C503(0.48)  LDD1691  [15]
 LDCM0489  CL94 HEK-293T C695(0.90); C663(1.01); C642(1.36); C260(1.25)  LDD1692  [15]
 LDCM0490  CL95 HEK-293T C695(0.78); C663(0.97); C260(1.12); C83(0.91)  LDD1693  [15]
 LDCM0491  CL96 HEK-293T C695(0.94); C663(0.92); C503(0.54)  LDD1694  [15]
 LDCM0492  CL97 HEK-293T C695(0.97); C294(1.25); C663(1.11); C642(0.92)  LDD1695  [15]
 LDCM0493  CL98 HEK-293T C260(0.95); C83(1.05); C503(1.01)  LDD1696  [15]
 LDCM0494  CL99 HEK-293T C695(1.01); C663(1.01); C260(0.94); C83(0.95)  LDD1697  [15]
 LDCM0495  E2913 HEK-293T C695(1.04); C663(1.27); C260(0.98); C83(1.07)  LDD1698  [15]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C14(3.01); C604(0.48)  LDD1702  [3]
 LDCM0625  F8 Ramos C695(1.40); C14(4.19)  LDD2187  [16]
 LDCM0572  Fragment10 Ramos C695(0.58)  LDD2189  [16]
 LDCM0573  Fragment11 Ramos C695(1.40); C14(0.71)  LDD2190  [16]
 LDCM0574  Fragment12 Ramos C695(0.76)  LDD2191  [16]
 LDCM0575  Fragment13 Ramos C695(0.53)  LDD2192  [16]
 LDCM0576  Fragment14 Ramos C695(0.88); C14(0.79)  LDD2193  [16]
 LDCM0579  Fragment20 Ramos C695(0.68)  LDD2194  [16]
 LDCM0580  Fragment21 Ramos C695(0.71)  LDD2195  [16]
 LDCM0582  Fragment23 Ramos C695(0.90)  LDD2196  [16]
 LDCM0578  Fragment27 Ramos C695(1.20)  LDD2197  [16]
 LDCM0586  Fragment28 Ramos C695(0.78); C14(0.90)  LDD2198  [16]
 LDCM0588  Fragment30 Ramos C695(0.70)  LDD2199  [16]
 LDCM0589  Fragment31 Ramos C695(1.05)  LDD2200  [16]
 LDCM0590  Fragment32 Ramos C695(1.19)  LDD2201  [16]
 LDCM0468  Fragment33 HEK-293T C695(1.11); C663(1.10); C260(0.90); C83(1.04)  LDD1671  [15]
 LDCM0596  Fragment38 Ramos C695(0.74)  LDD2203  [16]
 LDCM0566  Fragment4 Ramos C695(0.96); C14(1.16)  LDD2184  [16]
 LDCM0427  Fragment51 HEK-293T C260(1.09); C83(1.16); C503(1.01)  LDD1631  [15]
 LDCM0610  Fragment52 Ramos C695(0.81)  LDD2204  [16]
 LDCM0614  Fragment56 Ramos C695(1.44)  LDD2205  [16]
 LDCM0569  Fragment7 Ramos C695(0.72); C14(0.83)  LDD2186  [16]
 LDCM0571  Fragment9 Ramos C695(0.42)  LDD2188  [16]
 LDCM0022  KB02 HEK-293T C523(0.92); C503(1.19); C695(1.08); C260(0.94)  LDD1492  [15]
 LDCM0023  KB03 Jurkat C642(4.95); C503(4.02); C14(3,203.03)  LDD0209  [5]
 LDCM0024  KB05 COLO792 C528(0.89); C702(2.93)  LDD3310  [17]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C604(1.44)  LDD2099  [3]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C604(0.86)  LDD2109  [3]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C604(1.04)  LDD2119  [3]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C14(2.51); C604(0.93)  LDD2125  [3]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C14(2.34)  LDD2129  [3]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C14(3.32)  LDD2137  [3]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C14(1.07)  LDD2146  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
DNA (cytosine-5)-methyltransferase 1 (DNMT1) C5-methyltransferase family P26358
DNA (cytosine-5)-methyltransferase 3A (DNMT3A) C5-methyltransferase family Q9Y6K1
DNA (cytosine-5)-methyltransferase 3B (DNMT3B) C5-methyltransferase family Q9UBC3
Histone-lysine N-methyltransferase SUV39H1 (SUV39H1) Histone-lysine methyltransferase family O43463
Fibroblast growth factor receptor 3 (FGFR3) Tyr protein kinase family P22607
Transcriptional regulator ATRX (ATRX) SNF2/RAD54 helicase family P46100
Transcription factor
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Retinoic acid receptor alpha (RARA) Nuclear hormone receptor family P10276
PHD finger protein 1 (PHF1) Polycomblike family O43189
Signal transducer and activator of transcription 3 (STAT3) Transcription factor STAT family P40763
GPCR
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Beta-2 adrenergic receptor (ADRB2) G-protein coupled receptor 1 family P07550
Other
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Polycomb group protein ASXL1 (ASXL1) Asx family Q8IXJ9
Centrosomal protein of 63 kDa (CEP63) CEP63 family Q96MT8
Keratin-associated protein 10-9 (KRTAP10-9) KRTAP type 10 family P60411
Polycomb protein SUZ12 (SUZ12) VEFS (VRN2-EMF2-FIS2-SU(Z)12) family Q15022
Polycomb protein EED (EED) WD repeat ESC family O75530
Sprouty-related, EVH1 domain-containing protein 1 (SPRED1) . Q7Z699

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
Tazemetostat Small molecular drug D00EQL
Phase 2
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cpi-0209 Small molecular drug DXL38G
Ds-3201b Small molecular drug DNM79H
Shr2554 Small molecular drug DM5X0L
Cpi-1205 . D0E6AG
Phase 1
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gsk2816126 Small molecular drug D05FIJ
Hh2853 Small molecular drug D6EU7R
Pf-06821497 Small molecular drug DI1L7M
Ds-3201 . D0LG8T
Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ei1 Small molecular drug D02CIT
Epz005687 Small molecular drug D02BBA
Gsk343 Small molecular drug D02TVQ
Ms1943 Small molecular drug D65IMT
Unc1999 Small molecular drug D02YXP
Patented
Click To Hide/Show 50 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid26882240-compound-1 Small molecular drug D0L1TA
Pmid28394193-compound-12 Small molecular drug D0H8VN
Pmid28394193-compound-13 Small molecular drug D0TA4N
Pmid28394193-compound-14 Small molecular drug D0GT7A
Pmid28394193-compound-15 Small molecular drug D0KR2T
Pmid28394193-compound-16 Small molecular drug D0T8QL
Pmid28394193-compound-17 Small molecular drug D0Z0QS
Pmid28394193-compound-18 Small molecular drug D0SY6P
Pmid28394193-compound-19 Small molecular drug D0VF0M
Pmid28394193-compound-20 Small molecular drug D0UG5O
Pmid28394193-compound-21 Small molecular drug D0BL8W
Pmid28394193-compound-22 Small molecular drug D0SQ1R
Pmid28394193-compound-23 Small molecular drug D0M9BY
Pmid28394193-compound-24 Small molecular drug D08MXO
Pmid28394193-compound-25 Small molecular drug D09PQQ
Pmid28394193-compound-26 Small molecular drug D0Z0NC
Pmid28394193-compound-27 Small molecular drug D09GFF
Pmid28394193-compound-28 Small molecular drug D0S4OP
Pmid28394193-compound-29 Small molecular drug D0MH8G
Pmid28394193-compound-30 Small molecular drug D0MO2X
Pmid28394193-compound-31 Small molecular drug D0FI3A
Pmid28394193-compound-32 Small molecular drug D0M1TG
Pmid28394193-compound-33 Small molecular drug D03MYI
Pmid28394193-compound-34 Small molecular drug D0Z7GN
Pmid28394193-compound-35 Small molecular drug D05MAR
Pmid28394193-compound-36 Small molecular drug D0RD5P
Pmid28394193-compound-37 Small molecular drug D0W2KL
Pmid28394193-compound-38 Small molecular drug D0DQ6N
Pmid28394193-compound-39 Small molecular drug D0MZ8D
Pmid28394193-compound-40 Small molecular drug D0QH1J
Pmid28394193-compound-41 Small molecular drug D0BT6Y
Pmid28394193-compound-42 Small molecular drug D0H4HR
Pmid28394193-compound-43 Small molecular drug D0PI5O
Pmid28394193-compound-44 Small molecular drug D0U9OH
Pmid28394193-compound-45 Small molecular drug D0M8AA
Pmid28394193-compound-46 Small molecular drug D0D4UH
Pmid28394193-compound-47 Small molecular drug D0B4TX
Pmid28394193-compound-49 Small molecular drug D0PB6T
Pmid28394193-compound-50 Small molecular drug D0A0VH
Pmid28394193-compound-51 Small molecular drug D0FC9J
Pmid28394193-compound-52 Small molecular drug D0LR5O
Pmid28394193-compound-53 Small molecular drug D0CH4O
Pmid28394193-compound-54 Small molecular drug D07CZI
Pmid28394193-compound-55 Small molecular drug D0M4LK
Pmid28394193-compound-56 Small molecular drug D01PZZ
Pmid28394193-compound-57 Small molecular drug D0G1JR
Pmid28394193-compound-figure3bi Small molecular drug D04PCW
Pmid28394193-compound-figure3bii Small molecular drug D0W4MW
Pmid28394193-compound-figure3biii Small molecular drug D0R2TQ
Pmid28394193-compound-figure5aviii Small molecular drug D0D1QD

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 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
3 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
4 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
5 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
6 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
7 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
8 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
9 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
10 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
11 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
12 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
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 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.
15 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
16 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
17 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