Details of the Target

General Information of Target

Target ID LDTP08198
Target Name Dipeptidyl peptidase 9 (DPP9)
Gene Name DPP9
Gene ID 91039
Synonyms
DPRP2; Dipeptidyl peptidase 9; DP9; EC 3.4.14.5; Dipeptidyl peptidase IV-related protein 2; DPRP-2; Dipeptidyl peptidase IX; DPP IX; Dipeptidyl peptidase-like protein 9; DPLP9
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MATTGTPTADRGDAAATDDPAARFQVQKHSWDGLRSIIHGSRKYSGLIVNKAPHDFQFVQ
KTDESGPHSHRLYYLGMPYGSRENSLLYSEIPKKVRKEALLLLSWKQMLDHFQATPHHGV
YSREEELLRERKRLGVFGITSYDFHSESGLFLFQASNSLFHCRDGGKNGFMVSPMKPLEI
KTQCSGPRMDPKICPADPAFFSFINNSDLWVANIETGEERRLTFCHQGLSNVLDDPKSAG
VATFVIQEEFDRFTGYWWCPTASWEGSEGLKTLRILYEEVDESEVEVIHVPSPALEERKT
DSYRYPRTGSKNPKIALKLAEFQTDSQGKIVSTQEKELVQPFSSLFPKVEYIARAGWTRD
GKYAWAMFLDRPQQWLQLVLLPPALFIPSTENEEQRLASARAVPRNVQPYVVYEEVTNVW
INVHDIFYPFPQSEGEDELCFLRANECKTGFCHLYKVTAVLKSQGYDWSEPFSPGEDEFK
CPIKEEIALTSGEWEVLARHGSKIWVNEETKLVYFQGTKDTPLEHHLYVVSYEAAGEIVR
LTTPGFSHSCSMSQNFDMFVSHYSSVSTPPCVHVYKLSGPDDDPLHKQPRFWASMMEAAS
CPPDYVPPEIFHFHTRSDVRLYGMIYKPHALQPGKKHPTVLFVYGGPQVQLVNNSFKGIK
YLRLNTLASLGYAVVVIDGRGSCQRGLRFEGALKNQMGQVEIEDQVEGLQFVAEKYGFID
LSRVAIHGWSYGGFLSLMGLIHKPQVFKVAIAGAPVTVWMAYDTGYTERYMDVPENNQHG
YEAGSVALHVEKLPNEPNRLLILHGFLDENVHFFHTNFLVSQLIRAGKPYQLQIYPNERH
SIRCPESGEHYEVTLLHFLQEYL
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Peptidase S9B family, DPPIV subfamily
Subcellular location
Nucleus; Cytoplasm, cytosol
Function
Dipeptidyl peptidase that cleaves off N-terminal dipeptides from proteins having a Pro or Ala residue at position 2. Acts as a key inhibitor of caspase-1-dependent monocyte and macrophage pyroptosis in resting cells by preventing activation of NLRP1 and CARD8. Sequesters the cleaved C-terminal part of NLRP1 and CARD8, which respectively constitute the active part of the NLRP1 and CARD8 inflammasomes, in a ternary complex, thereby preventing their oligomerization and activation. The dipeptidyl peptidase activity is required to suppress NLRP1 and CARD8; however, neither NLRP1 nor CARD8 are bona fide substrates of DPP9, suggesting the existence of substrate(s) required for NLRP1 and CARD8 inhibition.
TTD ID
T66252
Uniprot ID
Q86TI2
DrugMap ID
TTNDUL7
Ensemble ID
ENST00000262960.14
HGNC ID
HGNC:18648
ChEMBL ID
CHEMBL4793

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 17 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		14.93  LDD0402  [1]
STPyne
 Probe Info  		K43(3.68); K660(3.85)  LDD0277  [2]
Probe 1
 Probe Info  		Y466(10.41)  LDD3495  [3]
DBIA
 Probe Info  		C213(1.36)  LDD3318  [4]
BTD
 Probe Info  		C184(1.01)  LDD1700  [5]
HHS-475
 Probe Info  		Y44(0.73); Y79(0.96)  LDD0264  [6]
IPM
 Probe Info  		C184(1.42)  LDD1702  [5]
Acrolein
 Probe Info  		N.A.  LDD0225  [7]
ATP probe
 Probe Info  		K43(0.00); K51(0.00); K61(0.00)  LDD0199  [8]
4-Iodoacetamidophenylacetylene
 Probe Info  		C259(0.00); C225(0.00); C481(0.00); C184(0.00)  LDD0038  [9]
IA-alkyne
 Probe Info  		C601(0.00); C194(0.00); C225(0.00); C844(0.00)  LDD0036  [9]
Lodoacetamide azide
 Probe Info  		C844(0.00); C259(0.00); C601(0.00); C225(0.00)  LDD0037  [9]
NAIA_4
 Probe Info  		N.A.  LDD2226  [10]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [11]
AOyne
 Probe Info  		11.40  LDD0443  [12]
NAIA_5
 Probe Info  		N.A.  LDD2223  [10]
HHS-482
 Probe Info  		Y44(1.10)  LDD2239  [13]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STS-1
 Probe Info  		N.A.  LDD0137  [14]

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 C225(1.34)  LDD2117  [5]
 LDCM0214  AC1 HEK-293T C184(1.01); C601(1.22)  LDD1507  [15]
 LDCM0215  AC10 HEK-293T C184(1.12); C844(1.02); C601(1.05)  LDD1508  [15]
 LDCM0226  AC11 HEK-293T C844(0.71); C601(1.02)  LDD1509  [15]
 LDCM0237  AC12 HEK-293T C844(1.00); C601(0.96); C194(1.28)  LDD1510  [15]
 LDCM0259  AC14 HEK-293T C844(1.00); C601(1.00)  LDD1512  [15]
 LDCM0270  AC15 HEK-293T C184(1.15); C844(1.01); C601(0.98)  LDD1513  [15]
 LDCM0276  AC17 HEK-293T C184(0.97); C601(1.00)  LDD1515  [15]
 LDCM0277  AC18 HEK-293T C184(1.11); C844(0.95); C601(0.98)  LDD1516  [15]
 LDCM0278  AC19 HEK-293T C844(1.28); C601(1.06)  LDD1517  [15]
 LDCM0279  AC2 HEK-293T C184(1.10); C844(0.93); C601(1.04)  LDD1518  [15]
 LDCM0280  AC20 HEK-293T C844(0.97); C601(1.13); C194(0.86)  LDD1519  [15]
 LDCM0281  AC21 HEK-293T C184(0.99); C844(0.95); C601(1.12)  LDD1520  [15]
 LDCM0282  AC22 HEK-293T C844(0.79); C601(0.97)  LDD1521  [15]
 LDCM0283  AC23 HEK-293T C184(1.14); C844(1.06); C601(1.03)  LDD1522  [15]
 LDCM0284  AC24 HEK-293T C194(1.08)  LDD1523  [15]
 LDCM0285  AC25 HEK-293T C184(1.03); C601(1.02)  LDD1524  [15]
 LDCM0286  AC26 HEK-293T C184(1.23); C844(0.98); C601(1.04)  LDD1525  [15]
 LDCM0287  AC27 HEK-293T C844(1.03); C601(1.02)  LDD1526  [15]
 LDCM0288  AC28 HEK-293T C844(1.26); C601(1.05); C194(1.05)  LDD1527  [15]
 LDCM0289  AC29 HEK-293T C184(1.05); C844(1.24); C601(1.04)  LDD1528  [15]
 LDCM0290  AC3 HEK-293T C844(0.97); C601(1.03)  LDD1529  [15]
 LDCM0291  AC30 HEK-293T C844(0.86); C601(0.94)  LDD1530  [15]
 LDCM0292  AC31 HEK-293T C184(1.11); C844(0.86); C601(1.06)  LDD1531  [15]
 LDCM0293  AC32 HEK-293T C194(1.08)  LDD1532  [15]
 LDCM0294  AC33 HEK-293T C184(1.06); C601(1.13)  LDD1533  [15]
 LDCM0295  AC34 HEK-293T C184(1.18); C844(0.94); C601(1.01)  LDD1534  [15]
 LDCM0296  AC35 HEK-293T C844(1.31); C601(1.00)  LDD1535  [15]
 LDCM0297  AC36 HEK-293T C844(1.12); C601(1.00); C194(1.03)  LDD1536  [15]
 LDCM0298  AC37 HEK-293T C184(0.97); C844(1.07); C601(1.13)  LDD1537  [15]
 LDCM0299  AC38 HEK-293T C844(0.94); C601(1.08)  LDD1538  [15]
 LDCM0300  AC39 HEK-293T C184(1.02); C844(0.98); C601(1.04)  LDD1539  [15]
 LDCM0301  AC4 HEK-293T C844(0.89); C601(0.98); C194(1.27)  LDD1540  [15]
 LDCM0302  AC40 HEK-293T C194(1.06)  LDD1541  [15]
 LDCM0303  AC41 HEK-293T C184(0.88); C601(1.15)  LDD1542  [15]
 LDCM0304  AC42 HEK-293T C184(1.18); C844(1.05); C601(1.07)  LDD1543  [15]
 LDCM0305  AC43 HEK-293T C844(0.95); C601(1.17)  LDD1544  [15]
 LDCM0306  AC44 HEK-293T C844(1.11); C601(1.06); C194(1.06)  LDD1545  [15]
 LDCM0307  AC45 HEK-293T C184(0.98); C844(0.89); C601(1.10)  LDD1546  [15]
 LDCM0308  AC46 HEK-293T C844(1.04); C601(1.21)  LDD1547  [15]
 LDCM0309  AC47 HEK-293T C184(1.06); C844(1.09); C601(1.13)  LDD1548  [15]
 LDCM0310  AC48 HEK-293T C194(1.20)  LDD1549  [15]
 LDCM0311  AC49 HEK-293T C184(1.14); C601(1.13)  LDD1550  [15]
 LDCM0312  AC5 HEK-293T C184(1.13); C844(0.88); C601(1.13)  LDD1551  [15]
 LDCM0313  AC50 HEK-293T C184(1.19); C844(1.04); C601(1.01)  LDD1552  [15]
 LDCM0314  AC51 HEK-293T C844(0.92); C601(1.00)  LDD1553  [15]
 LDCM0315  AC52 HEK-293T C844(0.96); C601(1.08); C194(0.81)  LDD1554  [15]
 LDCM0316  AC53 HEK-293T C184(0.96); C844(0.89); C601(1.14)  LDD1555  [15]
 LDCM0317  AC54 HEK-293T C844(0.93); C601(1.04)  LDD1556  [15]
 LDCM0318  AC55 HEK-293T C184(0.94); C844(0.96); C601(1.09)  LDD1557  [15]
 LDCM0319  AC56 HEK-293T C194(0.99)  LDD1558  [15]
 LDCM0320  AC57 HEK-293T C184(1.11); C601(1.07)  LDD1559  [15]
 LDCM0321  AC58 HEK-293T C184(1.18); C844(0.93); C601(0.97)  LDD1560  [15]
 LDCM0322  AC59 HEK-293T C844(1.13); C601(1.07)  LDD1561  [15]
 LDCM0323  AC6 HEK-293T C844(0.95); C601(1.02)  LDD1562  [15]
 LDCM0324  AC60 HEK-293T C844(1.13); C601(1.03); C194(0.97)  LDD1563  [15]
 LDCM0325  AC61 HEK-293T C184(1.06); C844(1.18); C601(1.17)  LDD1564  [15]
 LDCM0326  AC62 HEK-293T C844(0.73); C601(0.97)  LDD1565  [15]
 LDCM0327  AC63 HEK-293T C184(1.01); C844(0.92); C601(1.08)  LDD1566  [15]
 LDCM0328  AC64 HEK-293T C194(1.03)  LDD1567  [15]
 LDCM0334  AC7 HEK-293T C184(1.02); C844(1.03); C601(1.02)  LDD1568  [15]
 LDCM0345  AC8 HEK-293T C194(1.04)  LDD1569  [15]
 LDCM0520  AKOS000195272 MDA-MB-231 C184(0.79)  LDD2113  [5]
 LDCM0248  AKOS034007472 HEK-293T C184(1.10); C844(0.98); C601(1.08)  LDD1511  [15]
 LDCM0356  AKOS034007680 HEK-293T C184(0.96); C601(1.14)  LDD1570  [15]
 LDCM0275  AKOS034007705 HEK-293T C194(1.23)  LDD1514  [15]
 LDCM0156  Aniline NCI-H1299 12.59  LDD0403  [1]
 LDCM0498  BS-3668 MDA-MB-231 C184(0.43)  LDD2091  [5]
 LDCM0367  CL1 HEK-293T C184(0.99); C601(1.63)  LDD1571  [15]
 LDCM0368  CL10 HEK-293T C844(1.37); C601(1.66)  LDD1572  [15]
 LDCM0369  CL100 HEK-293T C184(0.90); C844(1.11); C601(1.19)  LDD1573  [15]
 LDCM0370  CL101 HEK-293T C184(0.99); C601(1.14)  LDD1574  [15]
 LDCM0371  CL102 HEK-293T C184(0.98); C844(1.14); C601(0.92)  LDD1575  [15]
 LDCM0372  CL103 HEK-293T C184(1.07); C601(1.28)  LDD1576  [15]
 LDCM0373  CL104 HEK-293T C184(1.00); C844(1.03); C601(1.24)  LDD1577  [15]
 LDCM0374  CL105 HEK-293T C184(1.03); C601(1.07)  LDD1578  [15]
 LDCM0375  CL106 HEK-293T C184(1.01); C844(1.19); C601(1.14)  LDD1579  [15]
 LDCM0376  CL107 HEK-293T C184(1.06); C601(1.11)  LDD1580  [15]
 LDCM0377  CL108 HEK-293T C184(0.90); C844(1.17); C601(1.04)  LDD1581  [15]
 LDCM0378  CL109 HEK-293T C184(1.01); C601(1.18)  LDD1582  [15]
 LDCM0379  CL11 HEK-293T C184(1.06); C844(1.23); C601(1.15)  LDD1583  [15]
 LDCM0380  CL110 HEK-293T C184(0.88); C844(1.21); C601(1.22)  LDD1584  [15]
 LDCM0381  CL111 HEK-293T C184(1.09); C601(1.22)  LDD1585  [15]
 LDCM0382  CL112 HEK-293T C184(1.01); C844(1.14); C601(1.08)  LDD1586  [15]
 LDCM0383  CL113 HEK-293T C184(1.04); C601(1.04)  LDD1587  [15]
 LDCM0384  CL114 HEK-293T C184(0.98); C844(0.75); C601(1.32)  LDD1588  [15]
 LDCM0385  CL115 HEK-293T C184(1.08); C601(1.26)  LDD1589  [15]
 LDCM0386  CL116 HEK-293T C184(1.20); C844(0.97); C601(1.14)  LDD1590  [15]
 LDCM0387  CL117 HEK-293T C184(1.02); C601(1.33)  LDD1591  [15]
 LDCM0388  CL118 HEK-293T C184(1.10); C844(1.17); C601(0.97)  LDD1592  [15]
 LDCM0389  CL119 HEK-293T C184(1.03); C601(1.25)  LDD1593  [15]
 LDCM0390  CL12 HEK-293T C194(1.40)  LDD1594  [15]
 LDCM0391  CL120 HEK-293T C184(1.04); C844(0.81); C601(1.21)  LDD1595  [15]
 LDCM0392  CL121 HEK-293T C184(0.99); C601(1.11)  LDD1596  [15]
 LDCM0393  CL122 HEK-293T C184(1.02); C844(0.97); C601(1.07)  LDD1597  [15]
 LDCM0394  CL123 HEK-293T C184(0.98); C601(1.80)  LDD1598  [15]
 LDCM0395  CL124 HEK-293T C184(0.92); C844(1.39); C601(1.41)  LDD1599  [15]
 LDCM0396  CL125 HEK-293T C184(1.04); C601(1.09)  LDD1600  [15]
 LDCM0397  CL126 HEK-293T C184(1.00); C844(1.20); C601(1.16)  LDD1601  [15]
 LDCM0398  CL127 HEK-293T C184(1.03); C601(1.29)  LDD1602  [15]
 LDCM0399  CL128 HEK-293T C184(0.99); C844(0.94); C601(1.08)  LDD1603  [15]
 LDCM0400  CL13 HEK-293T C184(0.89); C601(1.11)  LDD1604  [15]
 LDCM0401  CL14 HEK-293T C184(0.97); C844(1.21); C601(1.21)  LDD1605  [15]
 LDCM0402  CL15 HEK-293T C184(0.81); C601(1.32)  LDD1606  [15]
 LDCM0403  CL16 HEK-293T C184(1.07); C844(1.03); C601(1.19)  LDD1607  [15]
 LDCM0404  CL17 HEK-293T C184(0.78); C601(1.32)  LDD1608  [15]
 LDCM0405  CL18 HEK-293T C184(0.99); C844(1.03); C601(1.10)  LDD1609  [15]
 LDCM0406  CL19 HEK-293T C844(1.07); C601(1.14)  LDD1610  [15]
 LDCM0407  CL2 HEK-293T C184(1.00); C844(1.11); C601(1.09)  LDD1611  [15]
 LDCM0408  CL20 HEK-293T C844(1.07); C601(1.04); C194(1.03)  LDD1612  [15]
 LDCM0409  CL21 HEK-293T C184(0.92); C844(1.09); C601(1.65)  LDD1613  [15]
 LDCM0410  CL22 HEK-293T C844(0.99); C601(1.00)  LDD1614  [15]
 LDCM0411  CL23 HEK-293T C184(1.07); C844(1.09); C601(1.04)  LDD1615  [15]
 LDCM0412  CL24 HEK-293T C194(1.23)  LDD1616  [15]
 LDCM0413  CL25 HEK-293T C184(0.95); C601(1.47)  LDD1617  [15]
 LDCM0414  CL26 HEK-293T C184(0.89); C844(0.92); C601(1.10)  LDD1618  [15]
 LDCM0415  CL27 HEK-293T C184(1.10); C601(1.07)  LDD1619  [15]
 LDCM0416  CL28 HEK-293T C184(0.96); C844(0.86); C601(1.37)  LDD1620  [15]
 LDCM0417  CL29 HEK-293T C184(1.16); C601(1.03)  LDD1621  [15]
 LDCM0418  CL3 HEK-293T C184(0.99); C601(1.25)  LDD1622  [15]
 LDCM0419  CL30 HEK-293T C184(1.09); C844(1.01); C601(0.98)  LDD1623  [15]
 LDCM0420  CL31 HEK-293T C844(0.97); C601(1.20)  LDD1624  [15]
 LDCM0421  CL32 HEK-293T C844(0.82); C601(1.30); C194(0.86)  LDD1625  [15]
 LDCM0422  CL33 HEK-293T C184(0.92); C844(0.93); C601(1.50)  LDD1626  [15]
 LDCM0423  CL34 HEK-293T C844(0.84); C601(1.11)  LDD1627  [15]
 LDCM0424  CL35 HEK-293T C184(1.15); C844(1.03); C601(1.06)  LDD1628  [15]
 LDCM0425  CL36 HEK-293T C194(1.30)  LDD1629  [15]
 LDCM0426  CL37 HEK-293T C184(0.95); C601(1.49)  LDD1630  [15]
 LDCM0428  CL39 HEK-293T C184(0.99); C601(1.16)  LDD1632  [15]
 LDCM0429  CL4 HEK-293T C184(0.97); C844(1.06); C601(1.41)  LDD1633  [15]
 LDCM0430  CL40 HEK-293T C184(0.94); C844(0.91); C601(0.96)  LDD1634  [15]
 LDCM0431  CL41 HEK-293T C184(0.97); C601(1.15)  LDD1635  [15]
 LDCM0432  CL42 HEK-293T C184(1.03); C844(1.02); C601(0.97)  LDD1636  [15]
 LDCM0433  CL43 HEK-293T C844(1.37); C601(0.91)  LDD1637  [15]
 LDCM0434  CL44 HEK-293T C844(0.77); C601(1.09); C194(0.86)  LDD1638  [15]
 LDCM0435  CL45 HEK-293T C184(0.99); C844(1.54); C601(1.25)  LDD1639  [15]
 LDCM0436  CL46 HEK-293T C844(0.97); C601(1.14)  LDD1640  [15]
 LDCM0437  CL47 HEK-293T C184(1.14); C844(1.16); C601(1.00)  LDD1641  [15]
 LDCM0438  CL48 HEK-293T C194(1.28)  LDD1642  [15]
 LDCM0439  CL49 HEK-293T C184(0.89); C601(1.19)  LDD1643  [15]
 LDCM0440  CL5 HEK-293T C184(0.78); C601(1.00)  LDD1644  [15]
 LDCM0441  CL50 HEK-293T C184(0.95); C844(1.08); C601(1.16)  LDD1645  [15]
 LDCM0443  CL52 HEK-293T C184(1.04); C844(1.26); C601(1.26)  LDD1646  [15]
 LDCM0444  CL53 HEK-293T C184(0.94); C601(1.36)  LDD1647  [15]
 LDCM0445  CL54 HEK-293T C184(1.01); C844(1.16); C601(1.39)  LDD1648  [15]
 LDCM0446  CL55 HEK-293T C844(0.85); C601(1.01)  LDD1649  [15]
 LDCM0447  CL56 HEK-293T C844(1.22); C601(1.05); C194(0.73)  LDD1650  [15]
 LDCM0448  CL57 HEK-293T C184(1.00); C844(1.48); C601(1.43)  LDD1651  [15]
 LDCM0449  CL58 HEK-293T C844(0.70); C601(1.30)  LDD1652  [15]
 LDCM0450  CL59 HEK-293T C184(1.11); C844(0.98); C601(1.16)  LDD1653  [15]
 LDCM0451  CL6 HEK-293T C184(0.96); C844(1.18); C601(1.12)  LDD1654  [15]
 LDCM0452  CL60 HEK-293T C194(1.24)  LDD1655  [15]
 LDCM0453  CL61 HEK-293T C184(1.10); C601(1.02)  LDD1656  [15]
 LDCM0454  CL62 HEK-293T C184(1.00); C844(1.11); C601(1.15)  LDD1657  [15]
 LDCM0455  CL63 HEK-293T C184(1.05); C601(1.07)  LDD1658  [15]
 LDCM0456  CL64 HEK-293T C184(1.01); C844(1.31); C601(1.41)  LDD1659  [15]
 LDCM0457  CL65 HEK-293T C184(1.04); C601(1.10)  LDD1660  [15]
 LDCM0458  CL66 HEK-293T C184(1.10); C844(1.01); C601(1.00)  LDD1661  [15]
 LDCM0459  CL67 HEK-293T C844(0.94); C601(0.98)  LDD1662  [15]
 LDCM0460  CL68 HEK-293T C844(1.01); C601(1.27); C194(1.24)  LDD1663  [15]
 LDCM0461  CL69 HEK-293T C184(1.05); C844(1.19); C601(1.23)  LDD1664  [15]
 LDCM0462  CL7 HEK-293T C844(1.11); C601(1.18)  LDD1665  [15]
 LDCM0463  CL70 HEK-293T C844(0.80); C601(1.04)  LDD1666  [15]
 LDCM0464  CL71 HEK-293T C184(0.99); C844(1.17); C601(1.05)  LDD1667  [15]
 LDCM0465  CL72 HEK-293T C194(1.00)  LDD1668  [15]
 LDCM0466  CL73 HEK-293T C184(0.95); C601(1.23)  LDD1669  [15]
 LDCM0467  CL74 HEK-293T C184(1.04); C844(1.10); C601(1.11)  LDD1670  [15]
 LDCM0469  CL76 HEK-293T C184(0.96); C844(1.01); C601(1.06)  LDD1672  [15]
 LDCM0470  CL77 HEK-293T C184(0.91); C601(1.40)  LDD1673  [15]
 LDCM0471  CL78 HEK-293T C184(1.04); C844(1.13); C601(1.02)  LDD1674  [15]
 LDCM0472  CL79 HEK-293T C844(1.20); C601(1.14)  LDD1675  [15]
 LDCM0473  CL8 HEK-293T C844(1.01); C601(1.43); C194(0.58)  LDD1676  [15]
 LDCM0474  CL80 HEK-293T C844(1.13); C601(1.04); C194(0.96)  LDD1677  [15]
 LDCM0475  CL81 HEK-293T C184(0.98); C844(0.91); C601(1.23)  LDD1678  [15]
 LDCM0476  CL82 HEK-293T C844(0.79); C601(1.12)  LDD1679  [15]
 LDCM0477  CL83 HEK-293T C184(1.03); C844(1.06); C601(1.25)  LDD1680  [15]
 LDCM0478  CL84 HEK-293T C194(1.25)  LDD1681  [15]
 LDCM0479  CL85 HEK-293T C184(1.04); C601(1.11)  LDD1682  [15]
 LDCM0480  CL86 HEK-293T C184(1.03); C844(1.06); C601(1.12)  LDD1683  [15]
 LDCM0481  CL87 HEK-293T C184(0.95); C601(1.16)  LDD1684  [15]
 LDCM0482  CL88 HEK-293T C184(1.11); C844(0.95); C601(1.09)  LDD1685  [15]
 LDCM0483  CL89 HEK-293T C184(1.09); C601(1.19)  LDD1686  [15]
 LDCM0484  CL9 HEK-293T C184(0.89); C844(0.96); C601(1.19)  LDD1687  [15]
 LDCM0485  CL90 HEK-293T C184(1.02); C844(1.23); C601(1.20)  LDD1688  [15]
 LDCM0486  CL91 HEK-293T C844(1.21); C601(1.11)  LDD1689  [15]
 LDCM0487  CL92 HEK-293T C844(1.27); C601(1.27); C194(0.73)  LDD1690  [15]
 LDCM0488  CL93 HEK-293T C184(0.96); C844(0.93); C601(1.40)  LDD1691  [15]
 LDCM0489  CL94 HEK-293T C844(0.85); C601(1.03)  LDD1692  [15]
 LDCM0490  CL95 HEK-293T C184(1.06); C844(1.20); C601(0.37)  LDD1693  [15]
 LDCM0491  CL96 HEK-293T C194(0.99)  LDD1694  [15]
 LDCM0492  CL97 HEK-293T C184(0.96); C601(1.30)  LDD1695  [15]
 LDCM0493  CL98 HEK-293T C184(0.97); C844(1.17); C601(1.41)  LDD1696  [15]
 LDCM0494  CL99 HEK-293T C184(1.09); C601(1.21)  LDD1697  [15]
 LDCM0495  E2913 HEK-293T C184(0.91); C601(1.05)  LDD1698  [15]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C184(1.42)  LDD1702  [5]
 LDCM0468  Fragment33 HEK-293T C184(0.93); C601(1.63)  LDD1671  [15]
 LDCM0427  Fragment51 HEK-293T C184(1.02); C844(1.14); C601(1.17)  LDD1631  [15]
 LDCM0116  HHS-0101 DM93 Y44(0.73); Y79(0.96)  LDD0264  [6]
 LDCM0117  HHS-0201 DM93 Y44(0.74); Y79(1.05)  LDD0265  [6]
 LDCM0118  HHS-0301 DM93 Y79(0.47); Y44(0.93)  LDD0266  [6]
 LDCM0119  HHS-0401 DM93 Y44(1.07); Y79(1.16)  LDD0267  [6]
 LDCM0120  HHS-0701 DM93 Y44(0.67); Y79(1.09)  LDD0268  [6]
 LDCM0022  KB02 HEK-293T C184(0.91); C601(1.12); C844(0.98)  LDD1492  [15]
 LDCM0023  KB03 HEK-293T C184(0.86); C601(1.05); C844(0.99)  LDD1497  [15]
 LDCM0024  KB05 MELHO C213(1.36)  LDD3318  [4]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C184(1.84)  LDD2121  [5]
 LDCM0109  NEM HeLa N.A.  LDD0225  [7]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C184(0.65)  LDD2093  [5]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C184(0.14); C225(0.29)  LDD2096  [5]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C184(0.88)  LDD2097  [5]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C184(0.57)  LDD2099  [5]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C184(1.00)  LDD2101  [5]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C184(0.60)  LDD2107  [5]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C184(0.50)  LDD2109  [5]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C184(0.68)  LDD2111  [5]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C184(0.58)  LDD2115  [5]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C184(0.22)  LDD2118  [5]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C184(0.91)  LDD2120  [5]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C225(0.26)  LDD2122  [5]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C184(1.63)  LDD2123  [5]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C225(0.31)  LDD2124  [5]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C184(0.63); C225(0.98)  LDD2125  [5]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C225(0.83)  LDD2126  [5]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C184(0.80)  LDD2127  [5]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C184(0.96)  LDD2128  [5]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C184(0.78)  LDD2129  [5]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C184(0.71)  LDD2133  [5]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C184(0.50)  LDD2134  [5]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C184(0.86)  LDD2135  [5]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C184(0.86)  LDD2136  [5]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C184(0.91)  LDD2137  [5]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C184(1.01)  LDD1700  [5]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C184(1.11)  LDD2140  [5]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C184(0.56)  LDD2141  [5]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C184(1.17)  LDD2143  [5]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C184(1.66)  LDD2145  [5]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C184(0.74)  LDD2146  [5]
 LDCM0553  Nucleophilic fragment 6b MDA-MB-231 C184(4.02)  LDD2147  [5]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C184(0.54)  LDD2148  [5]
 LDCM0555  Nucleophilic fragment 7b MDA-MB-231 C225(0.40)  LDD2149  [5]
 LDCM0557  Nucleophilic fragment 8b MDA-MB-231 C225(0.39)  LDD2151  [5]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
CMP-N-acetylneuraminate-beta-1,4-galactoside alpha-2,3-sialyltransferase (ST3GAL3) Glycosyltransferase 29 family Q11203
Dipeptidyl peptidase 9 (DPP9) Peptidase S9B family Q86TI2
Peroxiredoxin-1 (PRDX1) Peroxiredoxin family Q06830
Cytochrome b-c1 complex subunit 7 (UQCRB) UQCRB/QCR7 family P14927
Transporter and channel
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Nucleoporin p58/p45 (NUP58) NUP58 family Q9BVL2
Signal recognition particle 9 kDa protein (SRP9) SRP9 family P49458
Optineurin (OPTN) . Q96CV9
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Krueppel-like factor 11 (KLF11) Sp1 C2H2-type zinc-finger protein family O14901
Other
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein BRICK1 (BRK1) BRK1 family Q8WUW1
Axonemal dynein light intermediate polypeptide 1 (DNALI1) Inner dynein arm light chain family O14645
Protein Dr1 (DR1) NC2 beta/DR1 family Q01658
General transcription factor 3C polypeptide 3 (GTF3C3) . Q9Y5Q9
TAR DNA-binding protein 43 (TARDBP) . Q13148

The Drug(s) Related To This Target

Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Talabostat Small molecular drug D0FQ2U
Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1g244 Small molecular drug D0CP1J
Pmid20684603c24dd Small molecular drug D08NMS
Patented
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Thiomorpholine Derivative 1 Small molecular drug D06HJX
Thiomorpholine Derivative 2 Small molecular drug D0D4BP

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 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.
4 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
5 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
6 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
7 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.
8 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
9 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
10 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
11 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
12 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.
13 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.
14 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.
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