Details of the Target

General Information of Target

Target ID LDTP10845
Target Name E3 ubiquitin-protein ligase UHRF1 (UHRF1)
Gene Name UHRF1
Gene ID 29128
Synonyms
ICBP90; NP95; RNF106; E3 ubiquitin-protein ligase UHRF1; EC 2.3.2.27; Inverted CCAAT box-binding protein of 90 kDa; Nuclear protein 95; Nuclear zinc finger protein Np95; HuNp95; hNp95; RING finger protein 106; RING-type E3 ubiquitin transferase UHRF1; Transcription factor ICBP90; Ubiquitin-like PHD and RING finger domain-containing protein 1; hUHRF1; Ubiquitin-like-containing PHD and RING finger domains protein 1
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MEPGDAARPGSGRATGAPPPRLLLLPLLLGWGLRVAAAASASSSGAAAEDSSAMEELATE
KEAEESHRQDSVSLLTFILLLTLTILTIWLFKHRRVRFLHETGLAMIYGLIVGVILRYGT
PATSGRDKSLSCTQEDRAFSTLLVNVSGKFFEYTLKGEISPGKINSVEQNDMLRKVTFDP
EVFFNILLPPIIFHAGYSLKKRHFFRNLGSILAYAFLGTAVSCFIIGNLMYGVVKLMKIM
GQLSDKFYYTDCLFFGAIISATDPVTVLAIFNELHADVDLYALLFGESVLNDAVAIVLSS
SIVAYQPAGLNTHAFDAAAFFKSVGIFLGIFSGSFTMGAVTGVNANVTKFTKLHCFPLLE
TALFFLMSWSTFLLAEACGFTGVVAVLFCGITQAHYTYNNLSVESRSRTKQLFEVLHFLA
ENFIFSYMGLALFTFQKHVFSPIFIIGAFVAIFLGRAAHIYPLSFFLNLGRRHKIGWNFQ
HMMMFSGLRGAMAFALAIRDTASYARQMMFTTTLLIVFFTVWIIGGGTTPMLSWLNIRVG
VEEPSEEDQNEHHWQYFRVGVDPDQDPPPNNDSFQVLQGDGPDSARGNRTKQESAWIFRL
WYSFDHNYLKPILTHSGPPLTTTLPAWCGLLARCLTSPQVYDNQEPLREEDSDFILTEGD
LTLTYGDSTVTANGSSSSHTASTSLEGSRRTKSSSEEVLERDLGMGDQKVSSRGTRLVFP
LEDNA
Target Bioclass
Enzyme
Subcellular location
Nucleus
Function
Multidomain protein that acts as a key epigenetic regulator by bridging DNA methylation and chromatin modification. Specifically recognizes and binds hemimethylated DNA at replication forks via its YDG domain and recruits DNMT1 methyltransferase to ensure faithful propagation of the DNA methylation patterns through DNA replication. In addition to its role in maintenance of DNA methylation, also plays a key role in chromatin modification: through its tudor-like regions and PHD-type zinc fingers, specifically recognizes and binds histone H3 trimethylated at 'Lys-9' (H3K9me3) and unmethylated at 'Arg-2' (H3R2me0), respectively, and recruits chromatin proteins. Enriched in pericentric heterochromatin where it recruits different chromatin modifiers required for this chromatin replication. Also localizes to euchromatic regions where it negatively regulates transcription possibly by impacting DNA methylation and histone modifications. Has E3 ubiquitin-protein ligase activity by mediating the ubiquitination of target proteins such as histone H3 and PML. It is still unclear how E3 ubiquitin-protein ligase activity is related to its role in chromatin in vivo. Plays a role in DNA repair by cooperating with UHRF2 to ensure recruitment of FANCD2 to interstrand cross-links (ICLs) leading to FANCD2 activation. Acts as a critical player of proper spindle architecture by catalyzing the 'Lys-63'-linked ubiquitination of KIF11, thereby controlling KIF11 localization on the spindle.
Uniprot ID
Q96T88
Ensemble ID
ENST00000612630.4
HGNC ID
HGNC:12556
ChEMBL ID
CHEMBL2424510

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.V223I DBIA    Probe Info 
HUH1 SNV: p.G594R DBIA    Probe Info 
IGROV1 SNV: p.D556N DBIA    Probe Info 
J82 SNV: p.R270L DBIA    Probe Info 
JURKAT SNV: p.C344Y Compound 10    Probe Info 
MOLT4 SNV: p.V413I; p.A493V IA-alkyne    Probe Info 
NALM6 Deletion: p.S380QfsTer87 DBIA    Probe Info 
NUGC3 SNV: p.L698M DBIA    Probe Info 
RL952 SNV: p.D596Y DBIA    Probe Info 
SUPT1 SNV: p.R247H; p.D687G DBIA    Probe Info 
TOV21G SNV: p.R395L DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 25 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
CY-1
 Probe Info  		100.00  LDD0243  [2]
TH211
 Probe Info  		Y466(18.50); Y555(11.49)  LDD0257  [3]
STPyne
 Probe Info  		K303(10.00); K540(10.00); K563(5.89)  LDD0277  [4]
Probe 1
 Probe Info  		Y191(15.66)  LDD3495  [5]
P11
 Probe Info  		6.33  LDD0201  [6]
BTD
 Probe Info  		C318(1.97)  LDD1700  [7]
AHL-Pu-1
 Probe Info  		C97(3.18); C497(2.15)  LDD0168  [8]
DBIA
 Probe Info  		CAmbiguous(5.17); C403(25.03)  LDD0209  [9]
4-Iodoacetamidophenylacetylene
 Probe Info  		C512(0.00); C170(0.00); C410(0.00); C403(0.00)  LDD0038  [10]
IA-alkyne
 Probe Info  		C410(0.00); C759(0.00); C512(0.00); C497(0.00)  LDD0032  [11]
Lodoacetamide azide
 Probe Info  		C512(0.00); C170(0.00); C410(0.00); C403(0.00)  LDD0037  [10]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [12]
TFBX
 Probe Info  		N.A.  LDD0027  [12]
Compound 10
 Probe Info  		C170(0.00); C497(0.00); C512(0.00)  LDD2216  [13]
Compound 11
 Probe Info  		N.A.  LDD2213  [13]
IPM
 Probe Info  		C321(0.00); C316(0.00); C403(0.00)  LDD0005  [14]
SF
 Probe Info  		N.A.  LDD0028  [15]
VSF
 Probe Info  		C97(0.00); C98(0.00); C170(0.00)  LDD0007  [14]
Phosphinate-6
 Probe Info  		C305(0.00); C170(0.00); C302(0.00); C497(0.00)  LDD0018  [16]
Acrolein
 Probe Info  		C512(0.00); C497(0.00); C316(0.00)  LDD0217  [17]
Crotonaldehyde
 Probe Info  		C497(0.00); C512(0.00)  LDD0219  [17]
Methacrolein
 Probe Info  		C512(0.00); C497(0.00)  LDD0218  [17]
W1
 Probe Info  		C512(0.00); C759(0.00); C762(0.00); C497(0.00)  LDD0236  [18]
NAIA_5
 Probe Info  		C305(0.00); C497(0.00)  LDD2223  [19]
PAL-AfBPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C353
 Probe Info  		6.59  LDD2014  [20]
VE-P
 Probe Info  		N.A.  LDD0396  [21]

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 C316(0.96)  LDD2142  [7]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C316(0.72)  LDD2112  [7]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C403(0.69)  LDD2130  [7]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C316(1.74); C403(1.04); C318(1.85); C762(0.90)  LDD2117  [7]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C316(1.23)  LDD2152  [7]
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C739(0.98)  LDD2103  [7]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C316(0.89)  LDD2132  [7]
 LDCM0025  4SU-RNA HEK-293T C97(3.18); C497(2.15)  LDD0168  [8]
 LDCM0026  4SU-RNA+native RNA HEK-293T C410(2.91); C403(2.26)  LDD0169  [8]
 LDCM0214  AC1 HEK-293T C170(1.08); C316(1.03)  LDD1507  [22]
 LDCM0215  AC10 HEK-293T C170(1.04); C410(0.88); C512(1.05); C497(1.05)  LDD1508  [22]
 LDCM0226  AC11 HEK-293T C170(1.04); C410(1.15); C316(0.99)  LDD1509  [22]
 LDCM0237  AC12 HEK-293T C170(1.10); C410(1.03); C512(1.05)  LDD1510  [22]
 LDCM0259  AC14 HEK-293T C170(0.90); C512(1.14); C497(1.19); C316(0.97)  LDD1512  [22]
 LDCM0270  AC15 HEK-293T C170(0.96); C512(0.85); C497(1.12); C316(0.96)  LDD1513  [22]
 LDCM0276  AC17 HEK-293T C170(1.07); C316(1.08)  LDD1515  [22]
 LDCM0277  AC18 HEK-293T C170(0.99); C410(0.84); C512(1.41); C497(1.19)  LDD1516  [22]
 LDCM0278  AC19 HEK-293T C170(0.97); C410(1.30); C316(1.27)  LDD1517  [22]
 LDCM0279  AC2 HEK-293T C170(1.04); C410(0.94); C512(0.86); C497(1.18)  LDD1518  [22]
 LDCM0280  AC20 HEK-293T C170(1.07); C410(1.02); C512(1.18)  LDD1519  [22]
 LDCM0281  AC21 HEK-293T C170(1.01); C410(1.13); C316(1.05); C726(0.95)  LDD1520  [22]
 LDCM0282  AC22 HEK-293T C170(0.91); C512(1.02); C497(1.11); C316(0.95)  LDD1521  [22]
 LDCM0283  AC23 HEK-293T C170(0.95); C512(0.95); C497(1.13); C316(0.93)  LDD1522  [22]
 LDCM0284  AC24 HEK-293T C170(0.98); C410(1.08); C497(1.06); C316(0.99)  LDD1523  [22]
 LDCM0285  AC25 HEK-293T C170(1.06); C316(1.06)  LDD1524  [22]
 LDCM0286  AC26 HEK-293T C170(1.05); C410(0.98); C512(1.03); C497(1.24)  LDD1525  [22]
 LDCM0287  AC27 HEK-293T C170(1.03); C410(1.04); C316(1.03)  LDD1526  [22]
 LDCM0288  AC28 HEK-293T C170(1.04); C410(1.07); C512(1.38)  LDD1527  [22]
 LDCM0289  AC29 HEK-293T C170(0.92); C410(0.93); C316(0.92); C726(0.94)  LDD1528  [22]
 LDCM0290  AC3 HEK-293T C170(1.07); C410(0.99); C316(1.08)  LDD1529  [22]
 LDCM0291  AC30 HEK-293T C170(1.05); C512(1.03); C497(0.88); C316(0.97)  LDD1530  [22]
 LDCM0292  AC31 HEK-293T C170(0.93); C512(0.88); C497(1.10); C316(1.02)  LDD1531  [22]
 LDCM0293  AC32 HEK-293T C170(1.00); C410(1.03); C497(1.19); C316(0.97)  LDD1532  [22]
 LDCM0294  AC33 HEK-293T C170(1.02); C316(1.10)  LDD1533  [22]
 LDCM0295  AC34 HEK-293T C170(1.01); C410(0.80); C512(0.99); C497(1.32)  LDD1534  [22]
 LDCM0296  AC35 HEK-293T C170(0.96); C410(1.04); C316(1.02)  LDD1535  [22]
 LDCM0297  AC36 HEK-293T C170(1.03); C410(0.98); C512(1.11)  LDD1536  [22]
 LDCM0298  AC37 HEK-293T C170(0.98); C410(1.14); C316(0.92); C726(1.07)  LDD1537  [22]
 LDCM0299  AC38 HEK-293T C170(0.89); C512(1.09); C497(1.00); C316(1.00)  LDD1538  [22]
 LDCM0300  AC39 HEK-293T C170(1.04); C512(0.81); C497(1.09); C316(0.98)  LDD1539  [22]
 LDCM0301  AC4 HEK-293T C170(1.00); C410(1.22); C512(1.03)  LDD1540  [22]
 LDCM0302  AC40 HEK-293T C170(0.89); C410(1.06); C497(0.95); C316(1.03)  LDD1541  [22]
 LDCM0303  AC41 HEK-293T C170(1.06); C316(1.08)  LDD1542  [22]
 LDCM0304  AC42 HEK-293T C170(1.10); C410(0.96); C512(0.84); C497(1.24)  LDD1543  [22]
 LDCM0305  AC43 HEK-293T C170(1.01); C410(0.98); C316(1.08)  LDD1544  [22]
 LDCM0306  AC44 HEK-293T C170(1.17); C410(0.98); C512(0.99)  LDD1545  [22]
 LDCM0307  AC45 HEK-293T C170(0.90); C410(1.23); C316(0.94); C726(0.85)  LDD1546  [22]
 LDCM0308  AC46 HEK-293T C170(0.95); C512(1.07); C497(1.15); C316(0.98)  LDD1547  [22]
 LDCM0309  AC47 HEK-293T C170(1.03); C512(0.86); C497(1.04); C316(1.04)  LDD1548  [22]
 LDCM0310  AC48 HEK-293T C170(0.99); C410(0.94); C497(0.86); C316(0.93)  LDD1549  [22]
 LDCM0311  AC49 HEK-293T C170(1.08); C316(1.15)  LDD1550  [22]
 LDCM0312  AC5 HEK-293T C170(1.02); C410(1.34); C316(0.95); C726(0.95)  LDD1551  [22]
 LDCM0313  AC50 HEK-293T C170(1.00); C410(0.92); C512(1.11); C497(1.11)  LDD1552  [22]
 LDCM0314  AC51 HEK-293T C170(0.96); C410(1.04); C316(1.00)  LDD1553  [22]
 LDCM0315  AC52 HEK-293T C170(1.03); C410(1.26); C512(1.07)  LDD1554  [22]
 LDCM0316  AC53 HEK-293T C170(0.91); C410(1.00); C316(0.99); C726(1.00)  LDD1555  [22]
 LDCM0317  AC54 HEK-293T C170(0.98); C512(1.03); C497(0.98); C316(0.98)  LDD1556  [22]
 LDCM0318  AC55 HEK-293T C170(1.01); C512(1.09); C497(1.10); C316(1.02)  LDD1557  [22]
 LDCM0319  AC56 HEK-293T C170(0.96); C410(1.01); C497(0.85); C316(1.06)  LDD1558  [22]
 LDCM0320  AC57 HEK-293T C170(1.11); C316(0.99)  LDD1559  [22]
 LDCM0321  AC58 HEK-293T C170(1.02); C410(0.96); C512(1.17); C497(1.02)  LDD1560  [22]
 LDCM0322  AC59 HEK-293T C170(1.05); C410(0.98); C316(1.02)  LDD1561  [22]
 LDCM0323  AC6 HEK-293T C170(1.00); C512(1.16); C497(0.87); C316(1.04)  LDD1562  [22]
 LDCM0324  AC60 HEK-293T C170(1.06); C410(1.15); C512(0.87)  LDD1563  [22]
 LDCM0325  AC61 HEK-293T C170(1.03); C410(0.89); C316(0.98); C726(0.96)  LDD1564  [22]
 LDCM0326  AC62 HEK-293T C170(0.87); C512(1.05); C497(0.83); C316(1.04)  LDD1565  [22]
 LDCM0327  AC63 HEK-293T C170(0.95); C512(1.14); C497(1.02); C316(1.04)  LDD1566  [22]
 LDCM0328  AC64 HEK-293T C170(1.06); C410(0.86); C497(0.76); C316(0.99)  LDD1567  [22]
 LDCM0334  AC7 HEK-293T C170(0.98); C512(0.88); C497(1.05); C316(1.01)  LDD1568  [22]
 LDCM0345  AC8 HEK-293T C170(1.03); C410(1.02); C497(0.76); C316(1.01)  LDD1569  [22]
 LDCM0520  AKOS000195272 MDA-MB-231 C316(1.11)  LDD2113  [7]
 LDCM0248  AKOS034007472 HEK-293T C170(0.93); C410(1.08); C316(1.02); C726(0.92)  LDD1511  [22]
 LDCM0356  AKOS034007680 HEK-293T C170(1.08); C316(1.02)  LDD1570  [22]
 LDCM0275  AKOS034007705 HEK-293T C170(0.96); C410(1.10); C497(1.11); C316(1.02)  LDD1514  [22]
 LDCM0156  Aniline NCI-H1299 11.79  LDD0403  [1]
 LDCM0498  BS-3668 MDA-MB-231 C305(0.80)  LDD2091  [7]
 LDCM0088  C45 HEK-293T 6.33  LDD0201  [6]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [17]
 LDCM0367  CL1 HEK-293T C170(0.94); C410(0.97); C512(1.04); C316(0.97)  LDD1571  [22]
 LDCM0368  CL10 HEK-293T C170(0.82); C512(0.85); C497(0.73); C316(0.80)  LDD1572  [22]
 LDCM0369  CL100 HEK-293T C170(1.03); C410(0.96); C512(1.09); C497(0.96)  LDD1573  [22]
 LDCM0370  CL101 HEK-293T C170(1.05); C410(1.18); C512(0.94); C316(1.01)  LDD1574  [22]
 LDCM0371  CL102 HEK-293T C170(0.96); C410(0.86); C512(1.20); C497(1.05)  LDD1575  [22]
 LDCM0372  CL103 HEK-293T C170(0.92); C410(1.24); C316(0.95)  LDD1576  [22]
 LDCM0373  CL104 HEK-293T C170(1.04); C410(1.16); C512(1.32); C497(1.19)  LDD1577  [22]
 LDCM0374  CL105 HEK-293T C170(0.99); C410(1.06); C512(0.91); C316(0.95)  LDD1578  [22]
 LDCM0375  CL106 HEK-293T C170(0.95); C410(0.95); C512(1.06); C497(1.17)  LDD1579  [22]
 LDCM0376  CL107 HEK-293T C170(0.92); C410(1.13); C316(1.02)  LDD1580  [22]
 LDCM0377  CL108 HEK-293T C170(0.99); C410(0.89); C512(1.11); C497(0.88)  LDD1581  [22]
 LDCM0378  CL109 HEK-293T C170(1.02); C410(1.16); C512(1.00); C316(0.91)  LDD1582  [22]
 LDCM0379  CL11 HEK-293T C170(1.01); C512(0.74); C497(0.90); C316(0.99)  LDD1583  [22]
 LDCM0380  CL110 HEK-293T C170(0.99); C410(0.85); C512(0.85); C497(0.78)  LDD1584  [22]
 LDCM0381  CL111 HEK-293T C170(0.87); C410(1.32); C316(0.87)  LDD1585  [22]
 LDCM0382  CL112 HEK-293T C170(1.12); C410(1.06); C512(1.56); C497(1.04)  LDD1586  [22]
 LDCM0383  CL113 HEK-293T C170(1.05); C410(1.16); C512(1.05); C316(0.99)  LDD1587  [22]
 LDCM0384  CL114 HEK-293T C170(0.97); C410(1.09); C512(0.82); C497(0.86)  LDD1588  [22]
 LDCM0385  CL115 HEK-293T C170(0.86); C410(1.16); C316(0.96)  LDD1589  [22]
 LDCM0386  CL116 HEK-293T C170(0.98); C410(1.06); C512(1.06); C497(1.00)  LDD1590  [22]
 LDCM0387  CL117 HEK-293T C170(1.02); C410(1.47); C512(1.01); C316(1.01)  LDD1591  [22]
 LDCM0388  CL118 HEK-293T C170(0.99); C410(1.15); C512(1.20); C497(0.95)  LDD1592  [22]
 LDCM0389  CL119 HEK-293T C170(0.89); C410(1.08); C316(0.98)  LDD1593  [22]
 LDCM0390  CL12 HEK-293T C170(0.99); C410(0.86); C497(0.60); C316(0.96)  LDD1594  [22]
 LDCM0391  CL120 HEK-293T C170(1.06); C410(1.15); C512(1.06); C497(0.86)  LDD1595  [22]
 LDCM0392  CL121 HEK-293T C170(1.01); C410(1.18); C512(1.01); C316(1.01)  LDD1596  [22]
 LDCM0393  CL122 HEK-293T C170(0.96); C410(0.87); C512(1.09); C497(1.23)  LDD1597  [22]
 LDCM0394  CL123 HEK-293T C170(0.89); C410(1.12); C316(0.88)  LDD1598  [22]
 LDCM0395  CL124 HEK-293T C170(1.03); C410(0.95); C512(1.17); C497(1.00)  LDD1599  [22]
 LDCM0396  CL125 HEK-293T C170(0.99); C410(1.12); C512(1.16); C316(1.03)  LDD1600  [22]
 LDCM0397  CL126 HEK-293T C170(0.95); C410(0.92); C512(1.33); C497(0.91)  LDD1601  [22]
 LDCM0398  CL127 HEK-293T C170(0.99); C410(1.04); C316(1.03)  LDD1602  [22]
 LDCM0399  CL128 HEK-293T C170(1.04); C410(1.15); C512(0.96); C497(0.87)  LDD1603  [22]
 LDCM0400  CL13 HEK-293T C170(1.02); C410(1.23); C512(0.98); C316(0.98)  LDD1604  [22]
 LDCM0401  CL14 HEK-293T C170(0.97); C410(1.09); C512(1.44); C497(1.29)  LDD1605  [22]
 LDCM0402  CL15 HEK-293T C170(0.81); C410(1.20); C316(0.86)  LDD1606  [22]
 LDCM0403  CL16 HEK-293T C170(1.06); C410(1.06); C512(1.08); C497(1.05)  LDD1607  [22]
 LDCM0404  CL17 HEK-293T C170(0.98); C316(1.01)  LDD1608  [22]
 LDCM0405  CL18 HEK-293T C170(1.02); C410(0.99); C512(1.78); C497(1.14)  LDD1609  [22]
 LDCM0406  CL19 HEK-293T C170(0.96); C410(0.86); C316(0.97)  LDD1610  [22]
 LDCM0407  CL2 HEK-293T C170(1.01); C410(1.01); C512(1.06); C497(0.99)  LDD1611  [22]
 LDCM0408  CL20 HEK-293T C170(1.20); C410(1.08); C512(1.07)  LDD1612  [22]
 LDCM0409  CL21 HEK-293T C170(0.90); C410(0.97); C316(0.84); C726(0.76)  LDD1613  [22]
 LDCM0410  CL22 HEK-293T C170(0.96); C512(1.00); C497(1.08); C316(0.90)  LDD1614  [22]
 LDCM0411  CL23 HEK-293T C170(1.05); C512(0.86); C497(0.85); C316(0.96)  LDD1615  [22]
 LDCM0412  CL24 HEK-293T C170(1.05); C410(1.03); C497(0.79); C316(0.99)  LDD1616  [22]
 LDCM0413  CL25 HEK-293T C170(0.92); C410(1.05); C512(0.98); C316(0.91)  LDD1617  [22]
 LDCM0414  CL26 HEK-293T C170(0.95); C410(1.00); C512(0.92); C497(1.27)  LDD1618  [22]
 LDCM0415  CL27 HEK-293T C170(1.00); C410(1.46); C316(0.92)  LDD1619  [22]
 LDCM0416  CL28 HEK-293T C170(1.02); C410(1.07); C512(1.22); C497(0.92)  LDD1620  [22]
 LDCM0417  CL29 HEK-293T C170(1.02); C316(0.90)  LDD1621  [22]
 LDCM0418  CL3 HEK-293T C170(0.88); C410(1.00); C316(0.95)  LDD1622  [22]
 LDCM0419  CL30 HEK-293T C170(1.05); C410(0.92); C512(1.25); C497(1.22)  LDD1623  [22]
 LDCM0420  CL31 HEK-293T C170(0.99); C410(0.96); C316(0.97)  LDD1624  [22]
 LDCM0421  CL32 HEK-293T C170(1.11); C410(1.00); C512(1.03)  LDD1625  [22]
 LDCM0422  CL33 HEK-293T C170(0.84); C410(0.96); C316(0.82); C726(0.77)  LDD1626  [22]
 LDCM0423  CL34 HEK-293T C170(0.90); C512(0.91); C497(0.81); C316(0.90)  LDD1627  [22]
 LDCM0424  CL35 HEK-293T C170(1.01); C512(0.95); C497(0.83); C316(0.99)  LDD1628  [22]
 LDCM0425  CL36 HEK-293T C170(0.97); C410(0.94); C497(0.63); C316(1.05)  LDD1629  [22]
 LDCM0426  CL37 HEK-293T C170(0.53); C410(1.27); C512(1.09); C316(0.91)  LDD1630  [22]
 LDCM0428  CL39 HEK-293T C170(0.87); C410(1.06); C316(0.86)  LDD1632  [22]
 LDCM0429  CL4 HEK-293T C170(1.03); C410(1.12); C512(1.15); C497(0.86)  LDD1633  [22]
 LDCM0430  CL40 HEK-293T C170(0.95); C410(1.04); C512(1.23); C497(0.83)  LDD1634  [22]
 LDCM0431  CL41 HEK-293T C170(0.98); C316(0.99)  LDD1635  [22]
 LDCM0432  CL42 HEK-293T C170(1.06); C410(1.04); C512(1.25); C497(1.09)  LDD1636  [22]
 LDCM0433  CL43 HEK-293T C170(0.88); C410(1.14); C316(0.89)  LDD1637  [22]
 LDCM0434  CL44 HEK-293T C170(1.12); C410(1.17); C512(0.93)  LDD1638  [22]
 LDCM0435  CL45 HEK-293T C170(0.92); C410(1.23); C316(1.02); C726(0.71)  LDD1639  [22]
 LDCM0436  CL46 HEK-293T C170(0.83); C512(1.05); C497(0.99); C316(0.93)  LDD1640  [22]
 LDCM0437  CL47 HEK-293T C170(1.04); C512(0.69); C497(0.83); C316(0.93)  LDD1641  [22]
 LDCM0438  CL48 HEK-293T C170(0.91); C410(0.93); C497(0.61); C316(1.05)  LDD1642  [22]
 LDCM0439  CL49 HEK-293T C170(1.02); C410(1.30); C512(0.98); C316(0.98)  LDD1643  [22]
 LDCM0440  CL5 HEK-293T C170(1.16); C316(1.08)  LDD1644  [22]
 LDCM0441  CL50 HEK-293T C170(0.91); C410(0.98); C512(1.03); C497(1.11)  LDD1645  [22]
 LDCM0443  CL52 HEK-293T C170(1.08); C410(1.07); C512(1.21); C497(0.82)  LDD1646  [22]
 LDCM0444  CL53 HEK-293T C170(0.97); C316(0.97)  LDD1647  [22]
 LDCM0445  CL54 HEK-293T C170(0.91); C410(0.86); C512(0.79); C497(1.08)  LDD1648  [22]
 LDCM0446  CL55 HEK-293T C170(0.98); C410(1.12); C316(1.01)  LDD1649  [22]
 LDCM0447  CL56 HEK-293T C170(1.20); C410(0.82); C512(1.11)  LDD1650  [22]
 LDCM0448  CL57 HEK-293T C170(0.88); C410(1.07); C316(1.04); C726(0.74)  LDD1651  [22]
 LDCM0449  CL58 HEK-293T C170(0.88); C512(0.96); C497(1.01); C316(0.97)  LDD1652  [22]
 LDCM0450  CL59 HEK-293T C170(0.97); C512(1.01); C497(0.86); C316(0.95)  LDD1653  [22]
 LDCM0451  CL6 HEK-293T C170(0.98); C410(0.82); C512(0.90); C497(0.97)  LDD1654  [22]
 LDCM0452  CL60 HEK-293T C170(0.85); C410(0.95); C497(0.89); C316(0.99)  LDD1655  [22]
 LDCM0453  CL61 HEK-293T C170(1.11); C410(1.01); C512(0.86); C316(1.05)  LDD1656  [22]
 LDCM0454  CL62 HEK-293T C170(1.01); C410(1.22); C512(0.71); C497(0.87)  LDD1657  [22]
 LDCM0455  CL63 HEK-293T C170(0.91); C410(0.97); C316(0.97)  LDD1658  [22]
 LDCM0456  CL64 HEK-293T C170(0.88); C410(1.06); C512(0.94); C497(1.26)  LDD1659  [22]
 LDCM0457  CL65 HEK-293T C170(1.07); C316(1.03)  LDD1660  [22]
 LDCM0458  CL66 HEK-293T C170(1.00); C410(0.98); C512(1.27); C497(1.05)  LDD1661  [22]
 LDCM0459  CL67 HEK-293T C170(1.01); C410(1.02); C316(0.93)  LDD1662  [22]
 LDCM0460  CL68 HEK-293T C170(1.10); C410(1.02); C512(1.32)  LDD1663  [22]
 LDCM0461  CL69 HEK-293T C170(0.98); C410(0.87); C316(0.93); C726(0.84)  LDD1664  [22]
 LDCM0462  CL7 HEK-293T C170(0.99); C410(0.98); C316(0.91)  LDD1665  [22]
 LDCM0463  CL70 HEK-293T C170(0.92); C512(1.07); C497(1.05); C316(0.95)  LDD1666  [22]
 LDCM0464  CL71 HEK-293T C170(1.01); C512(0.78); C497(0.84); C316(0.93)  LDD1667  [22]
 LDCM0465  CL72 HEK-293T C170(0.92); C410(1.00); C497(0.64); C316(1.04)  LDD1668  [22]
 LDCM0466  CL73 HEK-293T C170(0.99); C410(1.07); C512(1.00); C316(0.99)  LDD1669  [22]
 LDCM0467  CL74 HEK-293T C170(1.01); C410(0.91); C512(1.23); C497(0.98)  LDD1670  [22]
 LDCM0469  CL76 HEK-293T C170(1.02); C410(1.05); C512(1.43); C497(0.74)  LDD1672  [22]
 LDCM0470  CL77 HEK-293T C170(1.02); C316(1.01)  LDD1673  [22]
 LDCM0471  CL78 HEK-293T C170(1.03); C410(1.01); C512(1.51); C497(1.29)  LDD1674  [22]
 LDCM0472  CL79 HEK-293T C170(0.98); C410(1.02); C316(0.93)  LDD1675  [22]
 LDCM0473  CL8 HEK-293T C170(0.89); C410(1.12); C512(1.20)  LDD1676  [22]
 LDCM0474  CL80 HEK-293T C170(1.06); C410(1.03); C512(1.44)  LDD1677  [22]
 LDCM0475  CL81 HEK-293T C170(0.97); C410(0.94); C316(0.99); C726(0.81)  LDD1678  [22]
 LDCM0476  CL82 HEK-293T C170(0.88); C512(0.98); C497(1.01); C316(0.92)  LDD1679  [22]
 LDCM0477  CL83 HEK-293T C170(0.98); C512(0.78); C497(0.88); C316(0.94)  LDD1680  [22]
 LDCM0478  CL84 HEK-293T C170(0.97); C410(1.00); C497(0.64); C316(1.03)  LDD1681  [22]
 LDCM0479  CL85 HEK-293T C170(0.98); C410(0.95); C512(1.02); C316(1.00)  LDD1682  [22]
 LDCM0480  CL86 HEK-293T C170(0.96); C410(0.80); C512(0.98); C497(0.80)  LDD1683  [22]
 LDCM0481  CL87 HEK-293T C170(1.13); C410(1.11); C316(0.97)  LDD1684  [22]
 LDCM0482  CL88 HEK-293T C170(1.05); C410(0.94); C512(0.94); C497(0.72)  LDD1685  [22]
 LDCM0483  CL89 HEK-293T C170(1.14); C316(1.11)  LDD1686  [22]
 LDCM0484  CL9 HEK-293T C170(0.97); C410(1.02); C316(0.96); C726(0.84)  LDD1687  [22]
 LDCM0485  CL90 HEK-293T C170(0.83); C410(0.84); C512(0.89); C497(0.94)  LDD1688  [22]
 LDCM0486  CL91 HEK-293T C170(0.96); C410(0.83); C316(0.94)  LDD1689  [22]
 LDCM0487  CL92 HEK-293T C170(1.04); C410(0.97); C512(1.06)  LDD1690  [22]
 LDCM0488  CL93 HEK-293T C170(0.92); C410(0.88); C316(0.94); C726(0.69)  LDD1691  [22]
 LDCM0489  CL94 HEK-293T C170(0.92); C512(1.07); C497(0.77); C316(0.89)  LDD1692  [22]
 LDCM0490  CL95 HEK-293T C170(0.90); C512(0.79); C497(0.71); C316(0.77)  LDD1693  [22]
 LDCM0491  CL96 HEK-293T C170(0.95); C410(0.81); C497(0.50); C316(0.98)  LDD1694  [22]
 LDCM0492  CL97 HEK-293T C170(0.97); C410(0.85); C512(0.87); C316(0.95)  LDD1695  [22]
 LDCM0493  CL98 HEK-293T C170(0.98); C410(1.07); C512(1.39); C497(1.60)  LDD1696  [22]
 LDCM0494  CL99 HEK-293T C170(0.94); C410(1.23); C316(0.96)  LDD1697  [22]
 LDCM0495  E2913 HEK-293T C170(0.80); C410(1.45); C316(0.96)  LDD1698  [22]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C512(2.22); C410(1.52); C403(1.38); C759(1.26)  LDD1702  [7]
 LDCM0573  Fragment11 Ramos C497(1.87)  LDD2190  [23]
 LDCM0574  Fragment12 Ramos C497(0.59)  LDD2191  [23]
 LDCM0575  Fragment13 Ramos C497(0.91)  LDD2192  [23]
 LDCM0576  Fragment14 Ramos C497(0.73)  LDD2193  [23]
 LDCM0579  Fragment20 Ramos C497(0.49)  LDD2194  [23]
 LDCM0580  Fragment21 Ramos C497(0.78)  LDD2195  [23]
 LDCM0582  Fragment23 Ramos C497(0.70)  LDD2196  [23]
 LDCM0578  Fragment27 Ramos C497(1.02)  LDD2197  [23]
 LDCM0586  Fragment28 Ramos C497(0.66)  LDD2198  [23]
 LDCM0588  Fragment30 Ramos C497(1.08)  LDD2199  [23]
 LDCM0589  Fragment31 Ramos C497(0.53)  LDD2200  [23]
 LDCM0590  Fragment32 Ramos C497(0.74)  LDD2201  [23]
 LDCM0468  Fragment33 HEK-293T C170(0.92); C410(0.93); C316(0.95)  LDD1671  [22]
 LDCM0596  Fragment38 Ramos C497(0.41)  LDD2203  [23]
 LDCM0427  Fragment51 HEK-293T C170(1.02); C410(1.08); C512(0.86); C497(0.99)  LDD1631  [22]
 LDCM0610  Fragment52 Ramos C497(0.85)  LDD2204  [23]
 LDCM0107  IAA HeLa N.A.  LDD0221  [17]
 LDCM0022  KB02 HEK-293T C170(0.90); C410(1.00); C316(1.06)  LDD1492  [22]
 LDCM0023  KB03 Jurkat CAmbiguous(5.17); C403(25.03)  LDD0209  [9]
 LDCM0024  KB05 COLO792 C510(1.75)  LDD3310  [24]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C739(0.54)  LDD2102  [7]
 LDCM0109  NEM HeLa N.A.  LDD0223  [17]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C170(1.25)  LDD2090  [7]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C316(0.65); C170(1.11)  LDD2092  [7]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C316(1.21); C403(1.15)  LDD2093  [7]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C170(1.75)  LDD2094  [7]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C170(1.10)  LDD2098  [7]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C403(1.15); C497(1.08)  LDD2099  [7]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C739(0.74)  LDD2100  [7]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C316(1.36)  LDD2101  [7]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C316(0.89); C739(0.66)  LDD2104  [7]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C739(0.71)  LDD2105  [7]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C316(0.98); C403(0.93)  LDD2107  [7]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C316(0.78)  LDD2108  [7]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C403(1.00); C762(1.46)  LDD2109  [7]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C316(0.72); C739(0.64); C170(0.64)  LDD2114  [7]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C316(0.63)  LDD2115  [7]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C316(1.31)  LDD2119  [7]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C316(1.24); C739(0.96); C762(0.95); C759(1.02)  LDD2123  [7]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C305(0.78); C762(0.68); C759(0.70); C497(0.84)  LDD2125  [7]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C316(0.74); C403(0.89); C305(0.92); C762(1.07)  LDD2127  [7]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C316(1.03); C403(0.98)  LDD2129  [7]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C316(1.08)  LDD2134  [7]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C316(0.78); C403(1.10); C739(0.84)  LDD2135  [7]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C403(1.23); C759(1.26); C497(1.00)  LDD2136  [7]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C316(0.82); C403(0.85); C762(1.01); C759(0.98)  LDD2137  [7]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C318(1.97)  LDD1700  [7]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C403(0.91); C759(0.87); C497(1.00)  LDD2140  [7]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C739(0.56); C497(1.16)  LDD2141  [7]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C316(0.51)  LDD2143  [7]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C316(1.49)  LDD2144  [7]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C403(1.03); C305(0.56)  LDD2146  [7]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C316(0.80)  LDD2148  [7]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C403(0.23)  LDD2150  [7]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 3 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

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
3 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
4 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
5 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
6 Discovery of Potent and Selective Inhibitors against Protein-Derived Electrophilic Cofactors. J Am Chem Soc. 2022 Mar 30;144(12):5377-5388. doi: 10.1021/jacs.1c12748. Epub 2022 Mar 2.
7 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
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 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.
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 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
13 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
14 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
15 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
16 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
17 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.
18 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.
19 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
20 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
21 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.
22 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
23 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
24 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