Details of the Target

General Information of Target

Target ID LDTP05484
Target Name Proteasome activator complex subunit 1 (PSME1)
Gene Name PSME1
Gene ID 5720
Synonyms
IFI5111; Proteasome activator complex subunit 1; 11S regulator complex subunit alpha; REG-alpha; Activator of multicatalytic protease subunit 1; Interferon gamma up-regulated I-5111 protein; IGUP I-5111; Proteasome activator 28 subunit alpha; PA28a; PA28alpha
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAMLRVQPEAQAKVDVFREDLCTKTENLLGSYFPKKISELDAFLKEPALNEANLSNLKAP
LDIPVPDPVKEKEKEERKKQQEKEDKDEKKKGEDEDKGPPCGPVNCNEKIVVLLQRLKPE
IKDVIEQLNLVTTWLQLQIPRIEDGNNFGVAVQEKVFELMTSLHTKLEGFHTQISKYFSE
RGDAVTKAAKQPHVGDYRQLVHELDEAEYRDIRLMVMEIRNAYAVLYDIILKNFEKLKKP
RGETKGMIY
Target Bioclass
Other
Family
PA28 family
Function
Implicated in immunoproteasome assembly and required for efficient antigen processing. The PA28 activator complex enhances the generation of class I binding peptides by altering the cleavage pattern of the proteasome.
Uniprot ID
Q06323
Ensemble ID
ENST00000206451.11
HGNC ID
HGNC:9568
ChEMBL ID
CHEMBL4295804

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CAL78 SNV: p.G169V .
MOLT4 SNV: p.Y32C; p.C106Y IA-alkyne    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 39 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
P3
 Probe Info  		10.00  LDD0450  [2]
AZ-9
 Probe Info  		2.16  LDD0393  [3]
CY-1
 Probe Info  		100.00  LDD0243  [4]
SAA-alkyne
 Probe Info  		1.12  LDD0252  [5]
FBP2
 Probe Info  		2.63  LDD0323  [6]
YN-1
 Probe Info  		100.00  LDD0444  [7]
ONAyne
 Probe Info  		K13(9.82); K190(1.12)  LDD0274  [8]
STPyne
 Probe Info  		K13(8.20); K187(10.00); K190(4.48); K24(0.83)  LDD0277  [8]
Probe 1
 Probe Info  		Y197(19.19); Y209(32.98); Y227(10.85)  LDD3495  [9]
JZ128-DTB
 Probe Info  		C106(0.00); C101(0.00)  LDD0462  [10]
THZ1-DTB
 Probe Info  		C106(1.13); C101(1.08)  LDD0460  [10]
AHL-Pu-1
 Probe Info  		C22(2.10)  LDD0171  [11]
DBIA
 Probe Info  		C22(41.81); C22(90.86)  LDD0209  [12]
HHS-475
 Probe Info  		Y32(0.55)  LDD0264  [13]
HHS-465
 Probe Info  		Y32(6.21)  LDD2237  [14]
5E-2FA
 Probe Info  		H171(0.00); H202(0.00); H193(0.00); H164(0.00)  LDD2235  [15]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [16]
IA-alkyne
 Probe Info  		N.A.  LDD0032  [17]
IPIAA_L
 Probe Info  		N.A.  LDD0031  [18]
Lodoacetamide azide
 Probe Info  		C22(0.00); C101(0.00); C106(0.00)  LDD0037  [16]
ATP probe
 Probe Info  		N.A.  LDD0035  [19]
BTD
 Probe Info  		C106(0.00); C22(0.00)  LDD0004  [20]
NAIA_4
 Probe Info  		N.A.  LDD2226  [21]
WYneN
 Probe Info  		C106(0.00); C101(0.00)  LDD0021  [20]
aHNE
 Probe Info  		N.A.  LDD0001  [20]
Compound 10
 Probe Info  		N.A.  LDD2216  [22]
Compound 11
 Probe Info  		N.A.  LDD2213  [22]
IPM
 Probe Info  		N.A.  LDD0005  [20]
NHS
 Probe Info  		N.A.  LDD0010  [20]
PF-06672131
 Probe Info  		C22(0.00); C101(0.00)  LDD0017  [23]
TFBX
 Probe Info  		N.A.  LDD0148  [24]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [25]
1c-yne
 Probe Info  		N.A.  LDD0228  [26]
Acrolein
 Probe Info  		C22(0.00); C101(0.00); H164(0.00); C106(0.00)  LDD0217  [27]
Methacrolein
 Probe Info  		N.A.  LDD0218  [27]
W1
 Probe Info  		C101(0.00); C106(0.00)  LDD0236  [28]
AOyne
 Probe Info  		7.90  LDD0443  [29]
NAIA_5
 Probe Info  		C106(0.00); C101(0.00); C22(0.00)  LDD2223  [21]
PAL-AfBPP Probe
Click To Hide/Show 11 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C040
 Probe Info  		7.62  LDD1740  [30]
C284
 Probe Info  		29.04  LDD1954  [30]
C391
 Probe Info  		16.45  LDD2050  [30]
FFF probe13
 Probe Info  		8.52  LDD0475  [31]
FFF probe14
 Probe Info  		20.00  LDD0477  [31]
FFF probe2
 Probe Info  		14.33  LDD0463  [31]
FFF probe3
 Probe Info  		15.13  LDD0464  [31]
FFF probe6
 Probe Info  		20.00  LDD0482  [31]
Kambe_31
 Probe Info  		3.14  LDD0128  [32]
Staurosporine capture compound
 Probe Info  		3.17  LDD0083  [33]
STS-1
 Probe Info  		N.A.  LDD0068  [34]

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 C106(0.80); C22(0.61); C101(0.63)  LDD2142  [35]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C22(0.97); C101(0.63)  LDD2112  [35]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C22(0.83)  LDD2117  [35]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C22(1.30)  LDD2152  [35]
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C106(1.18); C22(0.91); C101(1.11)  LDD2103  [35]
 LDCM0025  4SU-RNA HEK-293T C22(2.35)  LDD0371  [11]
 LDCM0026  4SU-RNA+native RNA DM93 C22(2.10)  LDD0171  [11]
 LDCM0214  AC1 HEK-293T C22(1.19); C101(1.03)  LDD1507  [36]
 LDCM0215  AC10 HEK-293T C22(0.91); C101(0.96)  LDD1508  [36]
 LDCM0226  AC11 HEK-293T C22(0.83); C101(0.98); C106(1.29)  LDD1509  [36]
 LDCM0237  AC12 HEK-293T C22(0.73); C101(1.02)  LDD1510  [36]
 LDCM0259  AC14 HEK-293T C22(0.73); C101(0.99)  LDD1512  [36]
 LDCM0270  AC15 HEK-293T C22(0.98); C101(0.96)  LDD1513  [36]
 LDCM0276  AC17 HEK-293T C22(0.96); C101(1.00)  LDD1515  [36]
 LDCM0277  AC18 HEK-293T C22(1.01); C101(0.93)  LDD1516  [36]
 LDCM0278  AC19 HEK-293T C22(0.97); C101(0.72); C106(0.86)  LDD1517  [36]
 LDCM0279  AC2 HEK-293T C22(1.04); C101(0.85)  LDD1518  [36]
 LDCM0280  AC20 HEK-293T C22(0.92); C101(1.00)  LDD1519  [36]
 LDCM0281  AC21 HEK-293T C101(0.98)  LDD1520  [36]
 LDCM0282  AC22 HEK-293T C22(0.85); C101(1.03)  LDD1521  [36]
 LDCM0283  AC23 HEK-293T C22(0.93); C101(0.91)  LDD1522  [36]
 LDCM0284  AC24 HEK-293T C101(0.98)  LDD1523  [36]
 LDCM0285  AC25 HEK-293T C22(1.01); C101(1.08)  LDD1524  [36]
 LDCM0286  AC26 HEK-293T C22(0.96); C101(0.94)  LDD1525  [36]
 LDCM0287  AC27 HEK-293T C22(0.93); C101(1.02); C106(1.09)  LDD1526  [36]
 LDCM0288  AC28 HEK-293T C22(0.91); C101(1.03)  LDD1527  [36]
 LDCM0289  AC29 HEK-293T C101(1.01)  LDD1528  [36]
 LDCM0290  AC3 HEK-293T C22(1.05); C101(1.00); C106(1.10)  LDD1529  [36]
 LDCM0291  AC30 HEK-293T C22(1.04); C101(0.98)  LDD1530  [36]
 LDCM0292  AC31 HEK-293T C22(1.03); C101(0.92)  LDD1531  [36]
 LDCM0293  AC32 HEK-293T C101(1.02)  LDD1532  [36]
 LDCM0294  AC33 HEK-293T C22(0.98); C101(0.99)  LDD1533  [36]
 LDCM0295  AC34 HEK-293T C22(0.92); C101(1.01)  LDD1534  [36]
 LDCM0296  AC35 HEK-293T C22(0.83); C101(0.99); C106(1.27)  LDD1535  [36]
 LDCM0297  AC36 HEK-293T C22(0.86); C101(1.02)  LDD1536  [36]
 LDCM0298  AC37 HEK-293T C101(0.96)  LDD1537  [36]
 LDCM0299  AC38 HEK-293T C22(0.74); C101(0.94)  LDD1538  [36]
 LDCM0300  AC39 HEK-293T C22(0.88); C101(0.94)  LDD1539  [36]
 LDCM0301  AC4 HEK-293T C22(1.05); C101(1.00)  LDD1540  [36]
 LDCM0302  AC40 HEK-293T C101(1.13)  LDD1541  [36]
 LDCM0303  AC41 HEK-293T C22(0.98); C101(1.01)  LDD1542  [36]
 LDCM0304  AC42 HEK-293T C22(0.93); C101(0.98)  LDD1543  [36]
 LDCM0305  AC43 HEK-293T C22(0.84); C101(0.98); C106(1.30)  LDD1544  [36]
 LDCM0306  AC44 HEK-293T C22(0.87); C101(0.99)  LDD1545  [36]
 LDCM0307  AC45 HEK-293T C101(1.03)  LDD1546  [36]
 LDCM0308  AC46 HEK-293T C22(0.80); C101(1.02)  LDD1547  [36]
 LDCM0309  AC47 HEK-293T C22(0.85); C101(0.83)  LDD1548  [36]
 LDCM0310  AC48 HEK-293T C101(0.99)  LDD1549  [36]
 LDCM0311  AC49 HEK-293T C22(1.04); C101(0.94)  LDD1550  [36]
 LDCM0312  AC5 HEK-293T C101(0.98)  LDD1551  [36]
 LDCM0313  AC50 HEK-293T C22(0.98); C101(0.90)  LDD1552  [36]
 LDCM0314  AC51 HEK-293T C22(0.93); C101(0.90); C106(1.08)  LDD1553  [36]
 LDCM0315  AC52 HEK-293T C22(0.90); C101(1.01)  LDD1554  [36]
 LDCM0316  AC53 HEK-293T C101(1.01)  LDD1555  [36]
 LDCM0317  AC54 HEK-293T C22(0.88); C101(0.86)  LDD1556  [36]
 LDCM0318  AC55 HEK-293T C22(0.83); C101(1.01)  LDD1557  [36]
 LDCM0319  AC56 HEK-293T C101(1.04)  LDD1558  [36]
 LDCM0320  AC57 HEK-293T C22(1.04); C101(1.02)  LDD1559  [36]
 LDCM0321  AC58 HEK-293T C22(1.00); C101(0.95)  LDD1560  [36]
 LDCM0322  AC59 HEK-293T C22(0.94); C101(0.96); C106(1.26)  LDD1561  [36]
 LDCM0323  AC6 HEK-293T C22(1.09); C101(0.95)  LDD1562  [36]
 LDCM0324  AC60 HEK-293T C22(0.99); C101(1.00)  LDD1563  [36]
 LDCM0325  AC61 HEK-293T C101(0.95)  LDD1564  [36]
 LDCM0326  AC62 HEK-293T C22(1.05); C101(0.96)  LDD1565  [36]
 LDCM0327  AC63 HEK-293T C22(0.99); C101(0.99)  LDD1566  [36]
 LDCM0328  AC64 HEK-293T C101(1.03)  LDD1567  [36]
 LDCM0334  AC7 HEK-293T C22(0.91); C101(0.97)  LDD1568  [36]
 LDCM0345  AC8 HEK-293T C101(1.00)  LDD1569  [36]
 LDCM0520  AKOS000195272 MDA-MB-231 C106(0.79); C101(0.67)  LDD2113  [35]
 LDCM0248  AKOS034007472 HEK-293T C101(1.03)  LDD1511  [36]
 LDCM0356  AKOS034007680 HEK-293T C22(0.95); C101(1.02)  LDD1570  [36]
 LDCM0275  AKOS034007705 HEK-293T C101(1.06)  LDD1514  [36]
 LDCM0156  Aniline NCI-H1299 13.25  LDD0403  [1]
 LDCM0630  CCW28-3 231MFP C22(0.93)  LDD2214  [37]
 LDCM0108  Chloroacetamide HeLa H164(0.00); C22(0.00); H171(0.00); C101(0.00)  LDD0222  [27]
 LDCM0632  CL-Sc Hep-G2 C101(1.13); C101(0.90); C22(0.67); C22(0.43)  LDD2227  [21]
 LDCM0367  CL1 HEK-293T C22(0.86); C101(1.00)  LDD1571  [36]
 LDCM0368  CL10 HEK-293T C22(0.48); C101(1.64)  LDD1572  [36]
 LDCM0369  CL100 HEK-293T C22(1.02); C101(1.08)  LDD1573  [36]
 LDCM0370  CL101 HEK-293T C22(0.96); C101(1.03)  LDD1574  [36]
 LDCM0371  CL102 HEK-293T C22(0.88); C101(1.33)  LDD1575  [36]
 LDCM0372  CL103 HEK-293T C22(0.79); C101(0.94)  LDD1576  [36]
 LDCM0373  CL104 HEK-293T C22(0.90); C101(0.96)  LDD1577  [36]
 LDCM0374  CL105 HEK-293T C22(1.06); C101(1.04)  LDD1578  [36]
 LDCM0375  CL106 HEK-293T C22(0.91); C101(0.97)  LDD1579  [36]
 LDCM0376  CL107 HEK-293T C22(0.90); C101(0.99)  LDD1580  [36]
 LDCM0377  CL108 HEK-293T C22(0.97); C101(1.04)  LDD1581  [36]
 LDCM0378  CL109 HEK-293T C22(1.01); C101(1.10)  LDD1582  [36]
 LDCM0379  CL11 HEK-293T C22(0.53); C101(1.29)  LDD1583  [36]
 LDCM0380  CL110 HEK-293T C22(0.89); C101(1.33)  LDD1584  [36]
 LDCM0381  CL111 HEK-293T C22(0.87); C101(1.11)  LDD1585  [36]
 LDCM0382  CL112 HEK-293T C22(0.94); C101(1.20)  LDD1586  [36]
 LDCM0383  CL113 HEK-293T C22(0.92); C101(0.94)  LDD1587  [36]
 LDCM0384  CL114 HEK-293T C22(0.95); C101(1.31)  LDD1588  [36]
 LDCM0385  CL115 HEK-293T C22(0.91); C101(0.99)  LDD1589  [36]
 LDCM0386  CL116 HEK-293T C22(0.95); C101(1.02)  LDD1590  [36]
 LDCM0387  CL117 HEK-293T C22(0.96); C101(1.00)  LDD1591  [36]
 LDCM0388  CL118 HEK-293T C22(0.93); C101(0.89)  LDD1592  [36]
 LDCM0389  CL119 HEK-293T C22(0.81); C101(0.93)  LDD1593  [36]
 LDCM0390  CL12 HEK-293T C101(1.16)  LDD1594  [36]
 LDCM0391  CL120 HEK-293T C22(0.82); C101(0.91)  LDD1595  [36]
 LDCM0392  CL121 HEK-293T C22(1.08); C101(0.94)  LDD1596  [36]
 LDCM0393  CL122 HEK-293T C22(0.92); C101(1.01)  LDD1597  [36]
 LDCM0394  CL123 HEK-293T C22(0.97); C101(1.22)  LDD1598  [36]
 LDCM0395  CL124 HEK-293T C22(0.88); C101(0.99)  LDD1599  [36]
 LDCM0396  CL125 HEK-293T C22(1.39); C101(0.98)  LDD1600  [36]
 LDCM0397  CL126 HEK-293T C22(1.15); C101(1.07)  LDD1601  [36]
 LDCM0398  CL127 HEK-293T C22(1.14); C101(1.02)  LDD1602  [36]
 LDCM0399  CL128 HEK-293T C22(1.19); C101(1.05)  LDD1603  [36]
 LDCM0400  CL13 HEK-293T C22(0.98); C101(0.88)  LDD1604  [36]
 LDCM0401  CL14 HEK-293T C22(0.77); C101(1.13)  LDD1605  [36]
 LDCM0402  CL15 HEK-293T C22(0.68); C101(1.21)  LDD1606  [36]
 LDCM0403  CL16 HEK-293T C22(0.64); C101(1.00)  LDD1607  [36]
 LDCM0404  CL17 HEK-293T C22(0.73); C101(1.34)  LDD1608  [36]
 LDCM0405  CL18 HEK-293T C22(0.63); C101(1.06)  LDD1609  [36]
 LDCM0406  CL19 HEK-293T C22(0.57); C101(1.13); C106(1.20)  LDD1610  [36]
 LDCM0407  CL2 HEK-293T C22(0.75); C101(1.06)  LDD1611  [36]
 LDCM0408  CL20 HEK-293T C22(0.47); C101(1.11)  LDD1612  [36]
 LDCM0409  CL21 HEK-293T C101(1.53)  LDD1613  [36]
 LDCM0410  CL22 HEK-293T C22(0.38); C101(1.13)  LDD1614  [36]
 LDCM0411  CL23 HEK-293T C22(0.57); C101(1.09)  LDD1615  [36]
 LDCM0412  CL24 HEK-293T C101(1.15)  LDD1616  [36]
 LDCM0413  CL25 HEK-293T C22(1.27); C101(1.23)  LDD1617  [36]
 LDCM0414  CL26 HEK-293T C22(0.88); C101(1.06)  LDD1618  [36]
 LDCM0415  CL27 HEK-293T C22(0.78); C101(0.99)  LDD1619  [36]
 LDCM0416  CL28 HEK-293T C22(0.86); C101(1.04)  LDD1620  [36]
 LDCM0417  CL29 HEK-293T C22(0.74); C101(1.00)  LDD1621  [36]
 LDCM0418  CL3 HEK-293T C22(0.77); C101(1.04)  LDD1622  [36]
 LDCM0419  CL30 HEK-293T C22(0.70); C101(0.97)  LDD1623  [36]
 LDCM0420  CL31 HEK-293T C22(0.61); C101(1.14); C106(1.20)  LDD1624  [36]
 LDCM0421  CL32 HEK-293T C22(0.59); C101(1.11)  LDD1625  [36]
 LDCM0422  CL33 HEK-293T C101(1.59)  LDD1626  [36]
 LDCM0423  CL34 HEK-293T C22(0.42); C101(1.11)  LDD1627  [36]
 LDCM0424  CL35 HEK-293T C22(0.57); C101(1.10)  LDD1628  [36]
 LDCM0425  CL36 HEK-293T C101(1.26)  LDD1629  [36]
 LDCM0426  CL37 HEK-293T C22(1.17); C101(1.07)  LDD1630  [36]
 LDCM0428  CL39 HEK-293T C22(0.82); C101(1.21)  LDD1632  [36]
 LDCM0429  CL4 HEK-293T C22(0.84); C101(1.00)  LDD1633  [36]
 LDCM0430  CL40 HEK-293T C22(0.82); C101(0.96)  LDD1634  [36]
 LDCM0431  CL41 HEK-293T C22(0.75); C101(1.09)  LDD1635  [36]
 LDCM0432  CL42 HEK-293T C22(0.79); C101(0.96)  LDD1636  [36]
 LDCM0433  CL43 HEK-293T C22(0.58); C101(1.06); C106(1.21)  LDD1637  [36]
 LDCM0434  CL44 HEK-293T C22(0.60); C101(1.04)  LDD1638  [36]
 LDCM0435  CL45 HEK-293T C101(1.33)  LDD1639  [36]
 LDCM0436  CL46 HEK-293T C22(0.48); C101(1.09)  LDD1640  [36]
 LDCM0437  CL47 HEK-293T C22(0.57); C101(1.05)  LDD1641  [36]
 LDCM0438  CL48 HEK-293T C101(1.19)  LDD1642  [36]
 LDCM0439  CL49 HEK-293T C22(1.21); C101(0.94)  LDD1643  [36]
 LDCM0440  CL5 HEK-293T C22(0.86); C101(1.08)  LDD1644  [36]
 LDCM0441  CL50 HEK-293T C22(0.75); C101(1.03)  LDD1645  [36]
 LDCM0443  CL52 HEK-293T C22(0.76); C101(1.00)  LDD1646  [36]
 LDCM0444  CL53 HEK-293T C22(0.73); C101(1.17)  LDD1647  [36]
 LDCM0445  CL54 HEK-293T C22(0.72); C101(1.17)  LDD1648  [36]
 LDCM0446  CL55 HEK-293T C22(0.55); C101(1.07); C106(1.24)  LDD1649  [36]
 LDCM0447  CL56 HEK-293T C22(0.51); C101(1.20)  LDD1650  [36]
 LDCM0448  CL57 HEK-293T C101(1.18)  LDD1651  [36]
 LDCM0449  CL58 HEK-293T C22(0.41); C101(1.03)  LDD1652  [36]
 LDCM0450  CL59 HEK-293T C22(0.59); C101(1.06)  LDD1653  [36]
 LDCM0451  CL6 HEK-293T C22(0.80); C101(1.51)  LDD1654  [36]
 LDCM0452  CL60 HEK-293T C101(1.22)  LDD1655  [36]
 LDCM0453  CL61 HEK-293T C22(1.17); C101(0.91)  LDD1656  [36]
 LDCM0454  CL62 HEK-293T C22(0.86); C101(0.93)  LDD1657  [36]
 LDCM0455  CL63 HEK-293T C22(0.90); C101(0.94)  LDD1658  [36]
 LDCM0456  CL64 HEK-293T C22(0.79); C101(1.21)  LDD1659  [36]
 LDCM0457  CL65 HEK-293T C22(0.85); C101(1.06)  LDD1660  [36]
 LDCM0458  CL66 HEK-293T C22(0.74); C101(1.17)  LDD1661  [36]
 LDCM0459  CL67 HEK-293T C22(0.63); C101(1.08); C106(1.37)  LDD1662  [36]
 LDCM0460  CL68 HEK-293T C22(0.56); C101(1.21)  LDD1663  [36]
 LDCM0461  CL69 HEK-293T C101(1.23)  LDD1664  [36]
 LDCM0462  CL7 HEK-293T C22(0.63); C101(1.16); C106(1.26)  LDD1665  [36]
 LDCM0463  CL70 HEK-293T C22(0.45); C101(1.00)  LDD1666  [36]
 LDCM0464  CL71 HEK-293T C22(0.65); C101(1.00)  LDD1667  [36]
 LDCM0465  CL72 HEK-293T C101(1.20)  LDD1668  [36]
 LDCM0466  CL73 HEK-293T C22(1.21); C101(0.87)  LDD1669  [36]
 LDCM0467  CL74 HEK-293T C22(1.01); C101(1.06)  LDD1670  [36]
 LDCM0469  CL76 HEK-293T C22(0.86); C101(0.93)  LDD1672  [36]
 LDCM0470  CL77 HEK-293T C22(0.90); C101(1.16)  LDD1673  [36]
 LDCM0471  CL78 HEK-293T C22(0.75); C101(1.02)  LDD1674  [36]
 LDCM0472  CL79 HEK-293T C22(0.68); C101(1.01); C106(1.17)  LDD1675  [36]
 LDCM0473  CL8 HEK-293T C22(0.90); C101(2.16)  LDD1676  [36]
 LDCM0474  CL80 HEK-293T C22(0.59); C101(1.05)  LDD1677  [36]
 LDCM0475  CL81 HEK-293T C101(1.17)  LDD1678  [36]
 LDCM0476  CL82 HEK-293T C22(0.55); C101(1.05)  LDD1679  [36]
 LDCM0477  CL83 HEK-293T C22(0.69); C101(1.11)  LDD1680  [36]
 LDCM0478  CL84 HEK-293T C101(1.28)  LDD1681  [36]
 LDCM0479  CL85 HEK-293T C22(1.58); C101(0.91)  LDD1682  [36]
 LDCM0480  CL86 HEK-293T C22(1.37); C101(0.99)  LDD1683  [36]
 LDCM0481  CL87 HEK-293T C22(1.26); C101(1.05)  LDD1684  [36]
 LDCM0482  CL88 HEK-293T C22(1.05); C101(0.93)  LDD1685  [36]
 LDCM0483  CL89 HEK-293T C22(1.12); C101(1.05)  LDD1686  [36]
 LDCM0484  CL9 HEK-293T C101(1.22)  LDD1687  [36]
 LDCM0485  CL90 HEK-293T C22(0.67); C101(1.48)  LDD1688  [36]
 LDCM0486  CL91 HEK-293T C22(0.82); C101(1.09); C106(1.29)  LDD1689  [36]
 LDCM0487  CL92 HEK-293T C22(0.70); C101(1.21)  LDD1690  [36]
 LDCM0488  CL93 HEK-293T C101(1.20)  LDD1691  [36]
 LDCM0489  CL94 HEK-293T C22(0.57); C101(1.18)  LDD1692  [36]
 LDCM0490  CL95 HEK-293T C22(0.91); C101(1.98)  LDD1693  [36]
 LDCM0491  CL96 HEK-293T C101(1.27)  LDD1694  [36]
 LDCM0492  CL97 HEK-293T C22(1.06); C101(1.08)  LDD1695  [36]
 LDCM0493  CL98 HEK-293T C22(0.99); C101(1.07)  LDD1696  [36]
 LDCM0494  CL99 HEK-293T C22(1.06); C101(1.13)  LDD1697  [36]
 LDCM0189  Compound 16 HEK-293T 17.00  LDD0492  [31]
 LDCM0191  Compound 21 HEK-293T 6.31  LDD0493  [31]
 LDCM0190  Compound 34 HEK-293T 12.88  LDD0497  [31]
 LDCM0193  Compound 36 HEK-293T 3.50  LDD0494  [31]
 LDCM0196  Compound 39 HEK-293T 4.69  LDD0496  [31]
 LDCM0634  CY-0357 Hep-G2 C22(4.46)  LDD2228  [21]
 LDCM0495  E2913 HEK-293T C22(0.78); C101(1.10)  LDD1698  [36]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C106(7.17)  LDD1702  [35]
 LDCM0625  F8 Ramos C22(1.43)  LDD2187  [38]
 LDCM0572  Fragment10 MDA-MB-231 C22(1.36)  LDD1389  [39]
 LDCM0573  Fragment11 MDA-MB-231 C22(1.24)  LDD1391  [39]
 LDCM0574  Fragment12 MDA-MB-231 C22(1.39)  LDD1393  [39]
 LDCM0575  Fragment13 MDA-MB-231 C22(1.26)  LDD1395  [39]
 LDCM0576  Fragment14 MDA-MB-231 C22(2.28)  LDD1397  [39]
 LDCM0577  Fragment15 Ramos C22(1.16)  LDD1400  [39]
 LDCM0579  Fragment20 MDA-MB-231 C22(1.03)  LDD1402  [39]
 LDCM0580  Fragment21 MDA-MB-231 C22(1.23)  LDD1404  [39]
 LDCM0581  Fragment22 MDA-MB-231 C22(1.08)  LDD1406  [39]
 LDCM0582  Fragment23 MDA-MB-231 C22(0.96)  LDD1408  [39]
 LDCM0583  Fragment24 Ramos C22(1.07)  LDD1410  [39]
 LDCM0584  Fragment25 MDA-MB-231 C22(0.97)  LDD1411  [39]
 LDCM0585  Fragment26 Ramos C22(0.52)  LDD1412  [39]
 LDCM0578  Fragment27 MDA-MB-231 C22(0.94)  LDD1401  [39]
 LDCM0586  Fragment28 MDA-MB-231 C22(0.93)  LDD1415  [39]
 LDCM0587  Fragment29 MDA-MB-231 C22(1.34)  LDD1417  [39]
 LDCM0588  Fragment30 MDA-MB-231 C22(1.06)  LDD1419  [39]
 LDCM0589  Fragment31 Ramos C22(0.76)  LDD1422  [39]
 LDCM0590  Fragment32 MDA-MB-231 C22(2.43)  LDD1423  [39]
 LDCM0468  Fragment33 MDA-MB-231 C22(1.00)  LDD1425  [39]
 LDCM0592  Fragment34 MDA-MB-231 C22(0.47)  LDD1427  [39]
 LDCM0593  Fragment35 Ramos C22(0.70)  LDD1430  [39]
 LDCM0594  Fragment36 MDA-MB-231 C22(1.16)  LDD1431  [39]
 LDCM0595  Fragment37 Ramos C22(1.04)  LDD1432  [39]
 LDCM0596  Fragment38 MDA-MB-231 C22(1.11)  LDD1433  [39]
 LDCM0597  Fragment39 MDA-MB-231 C22(1.51)  LDD1435  [39]
 LDCM0566  Fragment4 MDA-MB-231 C22(0.97)  LDD1378  [39]
 LDCM0598  Fragment40 MDA-MB-231 C22(1.25)  LDD1436  [39]
 LDCM0599  Fragment41 MDA-MB-231 C22(1.67)  LDD1438  [39]
 LDCM0600  Fragment42 Ramos C22(0.88)  LDD1440  [39]
 LDCM0602  Fragment44 MDA-MB-231 C22(0.66)  LDD1443  [39]
 LDCM0603  Fragment45 MDA-MB-231 C22(3.03)  LDD1444  [39]
 LDCM0605  Fragment47 MDA-MB-231 C22(1.89)  LDD1446  [39]
 LDCM0607  Fragment49 MDA-MB-231 C22(3.73)  LDD1448  [39]
 LDCM0427  Fragment51 Ramos C22(1.07)  LDD1451  [39]
 LDCM0610  Fragment52 Ramos C22(1.77)  LDD1453  [39]
 LDCM0611  Fragment53 MDA-MB-231 C22(0.78)  LDD1454  [39]
 LDCM0612  Fragment54 MDA-MB-231 C22(1.27)  LDD1456  [39]
 LDCM0613  Fragment55 MDA-MB-231 C22(1.08)  LDD1457  [39]
 LDCM0614  Fragment56 MDA-MB-231 C22(0.95)  LDD1458  [39]
 LDCM0568  Fragment6 MDA-MB-231 C22(1.18)  LDD1382  [39]
 LDCM0569  Fragment7 MDA-MB-231 C22(0.74)  LDD1383  [39]
 LDCM0570  Fragment8 MDA-MB-231 C22(2.02)  LDD1385  [39]
 LDCM0571  Fragment9 MDA-MB-231 C22(1.26)  LDD1387  [39]
 LDCM0116  HHS-0101 DM93 Y32(0.55)  LDD0264  [13]
 LDCM0117  HHS-0201 DM93 Y32(0.49)  LDD0265  [13]
 LDCM0118  HHS-0301 DM93 Y32(0.43)  LDD0266  [13]
 LDCM0119  HHS-0401 DM93 Y32(0.56)  LDD0267  [13]
 LDCM0120  HHS-0701 DM93 Y32(0.45)  LDD0268  [13]
 LDCM0107  IAA HeLa H164(0.00); H193(0.00); H171(0.00)  LDD0221  [27]
 LDCM0179  JZ128 PC-3 C106(0.00); C101(0.00)  LDD0462  [10]
 LDCM0073  Kambe_cp3 PC-3 3.14  LDD0128  [32]
 LDCM0022  KB02 MDA-MB-231 C22(2.04)  LDD1374  [39]
 LDCM0023  KB03 Jurkat C22(41.81); C22(90.86)  LDD0209  [12]
 LDCM0024  KB05 IGR37 C22(12.07)  LDD3314  [40]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C106(0.90); C22(0.97); C101(1.04)  LDD2102  [35]
 LDCM0109  NEM HeLa H202(0.00); H164(0.00); H171(0.00); H193(0.00)  LDD0223  [27]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C106(1.44); C22(1.33); C101(1.33)  LDD2090  [35]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C106(0.89); C22(0.88); C101(1.00)  LDD2092  [35]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C106(1.20); C22(1.62); C101(1.25)  LDD2094  [35]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C106(1.27); C22(0.41)  LDD2096  [35]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C106(1.01); C22(0.65); C101(1.04)  LDD2097  [35]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C106(0.99); C22(0.84); C101(1.17)  LDD2098  [35]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C22(0.63); C101(0.80)  LDD2100  [35]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C106(1.09); C101(0.67)  LDD2101  [35]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C106(0.87); C22(0.86); C101(0.51)  LDD2104  [35]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C106(1.06); C22(1.53); C101(1.08)  LDD2105  [35]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C106(0.78); C22(0.79); C101(0.43)  LDD2106  [35]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C106(1.00); C22(0.88); C101(0.77)  LDD2108  [35]
 LDCM0517  Nucleophilic fragment 21b MDA-MB-231 C106(1.13); C101(0.77)  LDD2110  [35]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C22(0.82); C101(0.58)  LDD2114  [35]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C106(0.76); C22(0.93); C101(0.47)  LDD2115  [35]
 LDCM0523  Nucleophilic fragment 24b MDA-MB-231 C106(1.58); C101(0.83)  LDD2116  [35]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C106(1.11)  LDD2118  [35]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C106(0.82); C22(1.00); C101(0.74)  LDD2120  [35]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C106(1.42); C22(0.44); C101(1.39)  LDD2122  [35]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C22(0.72); C101(1.39)  LDD2124  [35]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C106(1.49); C22(0.55)  LDD2126  [35]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C106(0.95); C22(1.13); C101(0.93)  LDD2128  [35]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C106(0.92)  LDD2129  [35]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C106(0.79); C101(0.51)  LDD2133  [35]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C106(0.87); C22(1.43); C101(0.64)  LDD2134  [35]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C106(0.98); C22(0.68); C101(1.01)  LDD2141  [35]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C106(1.01); C22(0.97); C101(1.00)  LDD2143  [35]
 LDCM0553  Nucleophilic fragment 6b MDA-MB-231 C22(2.63); C101(3.10)  LDD2147  [35]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C106(0.75); C101(0.44)  LDD2148  [35]
 LDCM0555  Nucleophilic fragment 7b MDA-MB-231 C22(0.98)  LDD2149  [35]
 LDCM0557  Nucleophilic fragment 8b MDA-MB-231 C22(0.73)  LDD2151  [35]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C106(2.05); C101(1.46)  LDD2153  [35]
 LDCM0131  RA190 MM1.R C22(1.19)  LDD0304  [41]
 LDCM0019  Staurosporine Hep-G2 3.17  LDD0083  [33]
 LDCM0021  THZ1 HeLa S3 C106(1.13); C101(1.08)  LDD0460  [10]
 LDCM0112  W16 Hep-G2 C22(0.62)  LDD0239  [28]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Fibroblast growth factor receptor 3 (FGFR3) Tyr protein kinase family P22607
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Glutamate receptor ionotropic, NMDA 2C (GRIN2C) Glutamate-gated ion channel family Q14957
Junctophilin-3 (JPH3) Junctophilin family Q8WXH2
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Proteasome activator complex subunit 2 (PSME2) PA28 family Q9UL46
Torsin-1A-interacting protein 1 (TOR1AIP1) TOR1AIP family Q5JTV8
Gelsolin (GSN) Villin/gelsolin family P06396
Ubiquilin-1 (UBQLN1) . Q9UMX0

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
Copper . DB09130

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 Comparison of Different Competitive Proteome Profiling Approaches in Target Identification of Covalent Inhibitors. Chembiochem. 2022 Dec 16;23(24):e202200389. doi: 10.1002/cbic.202200389. Epub 2022 Nov 22.
3 2H-Azirine-Based Reagents for Chemoselective Bioconjugation at Carboxyl Residues Inside Live Cells. J Am Chem Soc. 2020 Apr 1;142(13):6051-6059. doi: 10.1021/jacs.9b12116. Epub 2020 Mar 23.
4 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.
5 Chemoproteomics and Phosphoproteomics Profiling Reveals Salvianolic Acid A as a Covalent Inhibitor of mTORC1. J Proteome Res. 2023 Jul 7;22(7):2450-2459. doi: 10.1021/acs.jproteome.3c00188. Epub 2023 Jun 22.
6 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580
7 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.
8 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
9 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.
10 A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. J Am Chem Soc. 2019 Jan 9;141(1):191-203. doi: 10.1021/jacs.8b07911. Epub 2018 Dec 20.
11 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
12 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.
13 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.
14 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.
15 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
16 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
17 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
18 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
19 Comparison of Quantitative Mass Spectrometry Platforms for Monitoring Kinase ATP Probe Uptake in Lung Cancer. J Proteome Res. 2018 Jan 5;17(1):63-75. doi: 10.1021/acs.jproteome.7b00329. Epub 2017 Nov 22.
Mass spectrometry data entry: PXD006095 , PXD006096
20 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
21 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
22 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
23 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
24 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
25 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
26 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.
27 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.
28 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.
29 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.
30 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
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Mass spectrometry data entry: PXD039908 , PXD029761
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Mass spectrometry data entry: PXD044402
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Mass spectrometry data entry: PXD027578
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Mass spectrometry data entry: PXD047840
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