Details of the Target

General Information of Target

Target ID LDTP04685
Target Name Caspase-7 (CASP7)
Gene Name CASP7
Gene ID 840
Synonyms
MCH3; Caspase-7; CASP-7; EC 3.4.22.60; Apoptotic protease Mch-3; CMH-1; ICE-like apoptotic protease 3; ICE-LAP3) [Cleaved into: Caspase-7 subunit p20; Caspase-7 subunit p11]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MADDQGCIEEQGVEDSANEDSVDAKPDRSSFVPSLFSKKKKNVTMRSIKTTRDRVPTYQY
NMNFEKLGKCIIINNKNFDKVTGMGVRNGTDKDAEALFKCFRSLGFDVIVYNDCSCAKMQ
DLLKKASEEDHTNAACFACILLSHGEENVIYGKDGVTPIKDLTAHFRGDRCKTLLEKPKL
FFIQACRGTELDDGIQADSGPINDTDANPRYKIPVEADFLFAYSTVPGYYSWRSPGRGSW
FVQALCSILEEHGKDLEIMQILTRVNDRVARHFESQSDDPHFHEKKQIPCVVSMLTKELY
FSQ
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Peptidase C14A family
Subcellular location
Cytoplasm, cytosol
Function
Thiol protease involved in different programmed cell death processes, such as apoptosis, pyroptosis or granzyme-mediated programmed cell death, by proteolytically cleaving target proteins. Has a marked preference for Asp-Glu-Val-Asp (DEVD) consensus sequences, with some plasticity for alternate non-canonical sequences. Its involvement in the different programmed cell death processes is probably determined by upstream proteases that activate CASP7. Acts as an effector caspase involved in the execution phase of apoptosis: following cleavage and activation by initiator caspases (CASP8, CASP9 and/or CASP10), mediates execution of apoptosis by catalyzing cleavage of proteins, such as CLSPN, PARP1, PTGES3 and YY1. Compared to CASP3, acts as a minor executioner caspase and cleaves a limited set of target proteins. Acts as a key regulator of the inflammatory response in response to bacterial infection by catalyzing cleavage and activation of the sphingomyelin phosphodiesterase SMPD1 in the extracellular milieu, thereby promoting membrane repair. Regulates pyroptosis in intestinal epithelial cells: cleaved and activated by CASP1 in response to S.typhimurium infection, promoting its secretion to the extracellular milieu, where it catalyzes activation of SMPD1, generating ceramides that repair membranes and counteract the action of gasdermin-D (GSDMD) pores. Regulates granzyme-mediated programmed cell death in hepatocytes: cleaved and activated by granzyme B (GZMB) in response to bacterial infection, promoting its secretion to the extracellular milieu, where it catalyzes activation of SMPD1, generating ceramides that repair membranes and counteract the action of perforin (PRF1) pores. Following cleavage by CASP1 in response to inflammasome activation, catalyzes processing and inactivation of PARP1, alleviating the transcription repressor activity of PARP1. Acts as an inhibitor of type I interferon production during virus-induced apoptosis by mediating cleavage of antiviral proteins CGAS, IRF3 and MAVS, thereby preventing cytokine overproduction. Cleaves and activates sterol regulatory element binding proteins (SREBPs). Cleaves phospholipid scramblase proteins XKR4, XKR8 and XKR9. In case of infection, catalyzes cleavage of Kaposi sarcoma-associated herpesvirus protein ORF57, thereby preventing expression of viral lytic genes.; [Isoform Beta]: Lacks enzymatic activity.
TTD ID
T72252
Uniprot ID
P55210
DrugMap ID
TTM7Y45
Ensemble ID
ENST00000345633.8
HGNC ID
HGNC:1508
ChEMBL ID
CHEMBL3468

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
KPNYN SNV: p.C136Ter .
SNU1196 SNV: p.N148I DBIA    Probe Info 

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
STPyne
 Probe Info  		K38(0.90)  LDD0277  [1]
Probe 1
 Probe Info  		Y60(16.92)  LDD3495  [2]
m-APA
 Probe Info  		13.48  LDD0403  [3]
DBIA
 Probe Info  		C323(2.27)  LDD3310  [4]
HHS-465
 Probe Info  		Y58(5.56)  LDD2237  [5]
Acrolein
 Probe Info  		N.A.  LDD0222  [6]
ATP probe
 Probe Info  		N.A.  LDD0199  [7]
1d-yne
 Probe Info  		N.A.  LDD0358  [8]
4-Iodoacetamidophenylacetylene
 Probe Info  		C70(0.00); C246(0.00); C186(0.00); C290(0.00)  LDD0038  [9]
IA-alkyne
 Probe Info  		N.A.  LDD0032  [10]
Lodoacetamide azide
 Probe Info  		C70(0.00); C246(0.00); C186(0.00); C290(0.00)  LDD0037  [9]
TFBX
 Probe Info  		N.A.  LDD0027  [11]
WYneN
 Probe Info  		N.A.  LDD0021  [12]
Compound 10
 Probe Info  		C186(0.00); C290(0.00)  LDD2216  [13]
Compound 11
 Probe Info  		N.A.  LDD2213  [13]
IPM
 Probe Info  		N.A.  LDD0005  [12]
Phosphinate-6
 Probe Info  		C186(0.00); C7(0.00); C290(0.00)  LDD0018  [14]
Methacrolein
 Probe Info  		N.A.  LDD0218  [6]
W1
 Probe Info  		N.A.  LDD0236  [15]
AOyne
 Probe Info  		15.00  LDD0443  [16]
NAIA_5
 Probe Info  		C70(0.00); C246(0.00); C290(0.00); C186(0.00)  LDD2223  [17]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C290(1.06); C186(0.92); C246(1.05); C70(1.08)  LDD1507  [18]
 LDCM0215  AC10 HEK-293T C290(1.23); C186(1.04); C246(0.95); C70(1.01)  LDD1508  [18]
 LDCM0226  AC11 HEK-293T C290(1.06); C186(0.94); C246(0.87); C116(0.83)  LDD1509  [18]
 LDCM0237  AC12 HEK-293T C290(1.07); C186(0.88); C246(1.02); C70(1.05)  LDD1510  [18]
 LDCM0259  AC14 HEK-293T C290(1.06); C186(0.93); C246(1.15); C70(0.99)  LDD1512  [18]
 LDCM0270  AC15 HEK-293T C290(1.07); C186(0.96); C70(1.19); C116(0.90)  LDD1513  [18]
 LDCM0276  AC17 HEK-293T C290(1.28); C186(0.94); C246(1.11); C70(1.12)  LDD1515  [18]
 LDCM0277  AC18 HEK-293T C290(1.09); C186(0.91); C246(0.98); C70(1.05)  LDD1516  [18]
 LDCM0278  AC19 HEK-293T C290(0.93); C186(0.94); C246(0.76); C116(0.86)  LDD1517  [18]
 LDCM0279  AC2 HEK-293T C290(1.13); C186(0.95); C246(0.91); C70(1.12)  LDD1518  [18]
 LDCM0280  AC20 HEK-293T C290(1.23); C186(0.99); C246(0.98); C70(1.04)  LDD1519  [18]
 LDCM0281  AC21 HEK-293T C290(1.06); C186(0.99); C246(1.07); C70(0.98)  LDD1520  [18]
 LDCM0282  AC22 HEK-293T C290(1.21); C186(1.27); C246(0.95); C70(1.04)  LDD1521  [18]
 LDCM0283  AC23 HEK-293T C290(1.13); C186(1.01); C70(1.09); C116(1.01)  LDD1522  [18]
 LDCM0284  AC24 HEK-293T C290(1.10); C186(0.98); C246(1.02); C70(1.12)  LDD1523  [18]
 LDCM0285  AC25 HEK-293T C290(1.27); C186(0.89); C246(0.92); C70(1.19)  LDD1524  [18]
 LDCM0286  AC26 HEK-293T C290(1.13); C186(0.95); C246(0.89); C70(1.06)  LDD1525  [18]
 LDCM0287  AC27 HEK-293T C290(1.17); C186(0.90); C246(0.89); C116(0.93)  LDD1526  [18]
 LDCM0288  AC28 HEK-293T C290(1.18); C186(0.92); C246(0.88); C70(1.03)  LDD1527  [18]
 LDCM0289  AC29 HEK-293T C290(1.08); C186(1.04); C246(1.13); C70(0.90)  LDD1528  [18]
 LDCM0290  AC3 HEK-293T C290(1.10); C186(0.95); C246(0.90); C116(0.84)  LDD1529  [18]
 LDCM0291  AC30 HEK-293T C290(1.13); C186(1.00); C246(0.96); C70(0.91)  LDD1530  [18]
 LDCM0292  AC31 HEK-293T C290(1.09); C186(0.95); C70(1.07); C116(1.06)  LDD1531  [18]
 LDCM0293  AC32 HEK-293T C290(1.03); C186(0.99); C246(1.05); C70(1.11)  LDD1532  [18]
 LDCM0294  AC33 HEK-293T C290(1.25); C186(0.94); C246(1.02); C70(1.05)  LDD1533  [18]
 LDCM0295  AC34 HEK-293T C290(1.19); C186(0.94); C246(0.92); C70(1.17)  LDD1534  [18]
 LDCM0296  AC35 HEK-293T C290(1.25); C186(0.92); C246(0.82); C116(0.86)  LDD1535  [18]
 LDCM0297  AC36 HEK-293T C290(1.19); C186(0.96); C246(0.96); C70(1.08)  LDD1536  [18]
 LDCM0298  AC37 HEK-293T C290(1.10); C186(1.04); C246(1.24); C70(1.06)  LDD1537  [18]
 LDCM0299  AC38 HEK-293T C290(1.09); C186(1.03); C246(0.98); C70(0.94)  LDD1538  [18]
 LDCM0300  AC39 HEK-293T C290(1.11); C186(1.00); C70(1.15); C116(0.96)  LDD1539  [18]
 LDCM0301  AC4 HEK-293T C290(1.17); C186(0.99); C246(0.91); C70(0.98)  LDD1540  [18]
 LDCM0302  AC40 HEK-293T C290(1.27); C186(1.02); C246(1.03); C70(1.18)  LDD1541  [18]
 LDCM0303  AC41 HEK-293T C290(1.14); C186(0.96); C246(1.13); C70(1.04)  LDD1542  [18]
 LDCM0304  AC42 HEK-293T C290(1.17); C186(0.91); C246(0.87); C70(0.97)  LDD1543  [18]
 LDCM0305  AC43 HEK-293T C290(1.07); C186(0.91); C246(0.91); C116(0.83)  LDD1544  [18]
 LDCM0306  AC44 HEK-293T C290(1.10); C186(0.94); C246(1.03); C70(1.05)  LDD1545  [18]
 LDCM0307  AC45 HEK-293T C290(1.08); C186(1.06); C246(1.21); C70(1.14)  LDD1546  [18]
 LDCM0308  AC46 HEK-293T C290(1.03); C186(1.04); C246(0.98); C70(1.05)  LDD1547  [18]
 LDCM0309  AC47 HEK-293T C290(1.20); C186(0.99); C70(1.05); C116(1.11)  LDD1548  [18]
 LDCM0310  AC48 HEK-293T C290(1.13); C186(1.02); C246(1.04); C70(1.16)  LDD1549  [18]
 LDCM0311  AC49 HEK-293T C290(1.23); C186(0.92); C246(1.05); C70(1.09)  LDD1550  [18]
 LDCM0312  AC5 HEK-293T C290(1.16); C186(1.07); C246(1.12); C70(1.02)  LDD1551  [18]
 LDCM0313  AC50 HEK-293T C290(1.16); C186(0.95); C246(0.89); C70(1.16)  LDD1552  [18]
 LDCM0314  AC51 HEK-293T C290(1.09); C186(0.97); C246(0.85); C116(0.89)  LDD1553  [18]
 LDCM0315  AC52 HEK-293T C290(1.14); C186(0.97); C246(1.09); C70(1.06)  LDD1554  [18]
 LDCM0316  AC53 HEK-293T C290(1.09); C186(1.02); C246(1.14); C70(0.93)  LDD1555  [18]
 LDCM0317  AC54 HEK-293T C290(1.12); C186(1.01); C246(1.04); C70(0.96)  LDD1556  [18]
 LDCM0318  AC55 HEK-293T C290(1.06); C186(0.99); C70(1.02); C116(1.02)  LDD1557  [18]
 LDCM0319  AC56 HEK-293T C290(1.11); C186(0.93); C246(1.00); C70(1.08)  LDD1558  [18]
 LDCM0320  AC57 HEK-293T C290(1.26); C186(0.92); C246(0.98); C70(0.95)  LDD1559  [18]
 LDCM0321  AC58 HEK-293T C290(1.13); C186(0.94); C246(0.91); C70(1.07)  LDD1560  [18]
 LDCM0322  AC59 HEK-293T C290(1.10); C186(0.98); C246(0.91); C116(0.95)  LDD1561  [18]
 LDCM0323  AC6 HEK-293T C290(1.05); C186(1.07); C246(0.94); C70(0.86)  LDD1562  [18]
 LDCM0324  AC60 HEK-293T C290(1.23); C186(0.98); C246(0.95); C70(1.01)  LDD1563  [18]
 LDCM0325  AC61 HEK-293T C290(1.13); C186(1.07); C246(1.17); C70(0.99)  LDD1564  [18]
 LDCM0326  AC62 HEK-293T C290(1.12); C186(1.00); C246(1.02); C70(0.89)  LDD1565  [18]
 LDCM0327  AC63 HEK-293T C290(1.11); C186(1.00); C70(1.06); C116(1.05)  LDD1566  [18]
 LDCM0328  AC64 HEK-293T C290(1.10); C186(0.95); C246(0.95); C70(1.03)  LDD1567  [18]
 LDCM0334  AC7 HEK-293T C290(1.13); C186(1.04); C70(1.08); C116(1.07)  LDD1568  [18]
 LDCM0345  AC8 HEK-293T C290(1.14); C186(0.92); C246(1.03); C70(1.16)  LDD1569  [18]
 LDCM0248  AKOS034007472 HEK-293T C290(1.06); C186(1.03); C246(1.10); C70(1.09)  LDD1511  [18]
 LDCM0356  AKOS034007680 HEK-293T C290(1.28); C186(0.93); C246(1.03); C70(0.95)  LDD1570  [18]
 LDCM0275  AKOS034007705 HEK-293T C290(1.03); C186(0.98); C246(1.07); C70(1.11)  LDD1514  [18]
 LDCM0156  Aniline NCI-H1299 13.48  LDD0403  [3]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [6]
 LDCM0632  CL-Sc Hep-G2 C290(20.00); C186(1.26); C290(1.26)  LDD2227  [17]
 LDCM0367  CL1 HEK-293T C290(1.10); C186(0.97); C116(0.99)  LDD1571  [18]
 LDCM0368  CL10 HEK-293T C290(0.84); C186(0.72); C246(1.63); C70(0.62)  LDD1572  [18]
 LDCM0369  CL100 HEK-293T C290(1.12); C186(0.93); C246(0.95); C70(0.98)  LDD1573  [18]
 LDCM0370  CL101 HEK-293T C290(1.03); C186(0.96); C116(0.98)  LDD1574  [18]
 LDCM0371  CL102 HEK-293T C290(1.04); C186(0.86); C246(0.84); C70(1.08)  LDD1575  [18]
 LDCM0372  CL103 HEK-293T C290(1.25); C186(0.85); C246(0.99); C70(1.05)  LDD1576  [18]
 LDCM0373  CL104 HEK-293T C290(1.10); C186(0.99); C246(0.96); C70(1.15)  LDD1577  [18]
 LDCM0374  CL105 HEK-293T C290(1.07); C186(1.02); C116(0.85)  LDD1578  [18]
 LDCM0375  CL106 HEK-293T C290(0.99); C186(0.92); C246(0.94); C70(1.06)  LDD1579  [18]
 LDCM0376  CL107 HEK-293T C290(1.27); C186(0.95); C246(0.98); C70(1.09)  LDD1580  [18]
 LDCM0377  CL108 HEK-293T C290(1.15); C186(0.96); C246(0.90); C70(1.11)  LDD1581  [18]
 LDCM0378  CL109 HEK-293T C290(1.07); C186(0.95); C116(0.98)  LDD1582  [18]
 LDCM0379  CL11 HEK-293T C290(0.68); C186(0.84); C70(0.94); C116(1.02)  LDD1583  [18]
 LDCM0380  CL110 HEK-293T C290(1.04); C186(0.87); C246(0.79); C70(0.95)  LDD1584  [18]
 LDCM0381  CL111 HEK-293T C290(1.24); C186(0.90); C246(0.88); C70(0.98)  LDD1585  [18]
 LDCM0382  CL112 HEK-293T C290(1.20); C186(0.91); C246(0.89); C70(0.92)  LDD1586  [18]
 LDCM0383  CL113 HEK-293T C290(1.08); C186(0.97); C116(1.03)  LDD1587  [18]
 LDCM0384  CL114 HEK-293T C290(1.04); C186(0.86); C246(0.80); C70(0.95)  LDD1588  [18]
 LDCM0385  CL115 HEK-293T C290(1.22); C186(0.94); C246(0.98); C70(1.07)  LDD1589  [18]
 LDCM0386  CL116 HEK-293T C290(1.20); C186(0.95); C246(1.05); C70(1.01)  LDD1590  [18]
 LDCM0387  CL117 HEK-293T C290(1.10); C186(0.97); C116(0.90)  LDD1591  [18]
 LDCM0388  CL118 HEK-293T C290(1.01); C186(0.97); C246(0.97); C70(1.10)  LDD1592  [18]
 LDCM0389  CL119 HEK-293T C290(1.04); C186(0.96); C246(1.03); C70(1.10)  LDD1593  [18]
 LDCM0390  CL12 HEK-293T C290(0.68); C186(1.02); C246(1.30); C70(1.13)  LDD1594  [18]
 LDCM0391  CL120 HEK-293T C290(1.06); C186(1.01); C246(0.93); C70(1.11)  LDD1595  [18]
 LDCM0392  CL121 HEK-293T C290(1.11); C186(1.02); C116(0.91)  LDD1596  [18]
 LDCM0393  CL122 HEK-293T C290(1.07); C186(0.97); C246(0.97); C70(1.18)  LDD1597  [18]
 LDCM0394  CL123 HEK-293T C290(1.36); C186(0.88); C246(0.85); C70(0.95)  LDD1598  [18]
 LDCM0395  CL124 HEK-293T C290(1.07); C186(0.87); C246(0.93); C70(1.02)  LDD1599  [18]
 LDCM0396  CL125 HEK-293T C290(1.13); C186(0.98); C116(0.96)  LDD1600  [18]
 LDCM0397  CL126 HEK-293T C290(1.06); C186(0.95); C246(0.81); C70(0.96)  LDD1601  [18]
 LDCM0398  CL127 HEK-293T C290(1.34); C186(0.94); C246(0.94); C70(0.97)  LDD1602  [18]
 LDCM0399  CL128 HEK-293T C290(1.17); C186(0.98); C246(0.95); C70(0.99)  LDD1603  [18]
 LDCM0400  CL13 HEK-293T C290(1.06); C186(0.96); C116(0.89)  LDD1604  [18]
 LDCM0401  CL14 HEK-293T C290(0.96); C186(0.95); C246(0.97); C70(1.18)  LDD1605  [18]
 LDCM0402  CL15 HEK-293T C290(0.90); C186(0.76); C246(0.83); C70(1.08)  LDD1606  [18]
 LDCM0403  CL16 HEK-293T C290(1.02); C186(0.95); C246(0.98); C70(1.19)  LDD1607  [18]
 LDCM0404  CL17 HEK-293T C290(1.25); C186(0.78); C246(1.12); C70(1.07)  LDD1608  [18]
 LDCM0405  CL18 HEK-293T C290(1.01); C186(0.90); C246(1.07); C70(1.14)  LDD1609  [18]
 LDCM0406  CL19 HEK-293T C290(0.85); C186(0.94); C246(0.88); C116(0.86)  LDD1610  [18]
 LDCM0407  CL2 HEK-293T C290(1.04); C186(0.83); C246(0.91); C70(1.14)  LDD1611  [18]
 LDCM0408  CL20 HEK-293T C290(0.77); C186(0.93); C246(1.60); C70(1.10)  LDD1612  [18]
 LDCM0409  CL21 HEK-293T C290(0.71); C186(1.04); C246(1.55); C70(0.91)  LDD1613  [18]
 LDCM0410  CL22 HEK-293T C290(0.70); C186(0.96); C246(1.93); C70(0.91)  LDD1614  [18]
 LDCM0411  CL23 HEK-293T C290(0.59); C186(0.89); C70(1.03); C116(1.06)  LDD1615  [18]
 LDCM0412  CL24 HEK-293T C290(0.72); C186(0.98); C246(1.29); C70(1.13)  LDD1616  [18]
 LDCM0413  CL25 HEK-293T C290(1.14); C186(0.95); C116(0.86)  LDD1617  [18]
 LDCM0414  CL26 HEK-293T C290(1.01); C186(0.94); C246(0.96); C70(1.26)  LDD1618  [18]
 LDCM0415  CL27 HEK-293T C290(1.13); C186(0.91); C246(0.95); C70(1.18)  LDD1619  [18]
 LDCM0416  CL28 HEK-293T C290(1.12); C186(0.85); C246(1.00); C70(0.97)  LDD1620  [18]
 LDCM0417  CL29 HEK-293T C290(1.09); C186(0.93); C246(1.22); C70(1.38)  LDD1621  [18]
 LDCM0418  CL3 HEK-293T C290(1.13); C186(0.92); C246(0.93); C70(1.20)  LDD1622  [18]
 LDCM0419  CL30 HEK-293T C290(0.98); C186(1.03); C246(1.00); C70(1.21)  LDD1623  [18]
 LDCM0420  CL31 HEK-293T C290(0.91); C186(0.85); C246(0.77); C116(0.85)  LDD1624  [18]
 LDCM0421  CL32 HEK-293T C290(0.76); C186(0.83); C246(1.52); C70(1.09)  LDD1625  [18]
 LDCM0422  CL33 HEK-293T C290(1.18); C186(0.89); C246(1.60); C70(1.14)  LDD1626  [18]
 LDCM0423  CL34 HEK-293T C290(0.70); C186(0.87); C246(1.76); C70(0.89)  LDD1627  [18]
 LDCM0424  CL35 HEK-293T C290(0.55); C186(0.90); C70(1.20); C116(1.02)  LDD1628  [18]
 LDCM0425  CL36 HEK-293T C290(0.65); C186(0.98); C246(1.23); C70(0.94)  LDD1629  [18]
 LDCM0426  CL37 HEK-293T C290(1.18); C186(1.00); C116(0.80)  LDD1630  [18]
 LDCM0428  CL39 HEK-293T C290(1.14); C186(0.92); C246(1.03); C70(1.18)  LDD1632  [18]
 LDCM0429  CL4 HEK-293T C290(1.00); C186(0.84); C246(0.98); C70(1.15)  LDD1633  [18]
 LDCM0430  CL40 HEK-293T C290(1.10); C186(1.01); C246(0.98); C70(1.14)  LDD1634  [18]
 LDCM0431  CL41 HEK-293T C290(1.26); C186(0.87); C246(1.18); C70(1.08)  LDD1635  [18]
 LDCM0432  CL42 HEK-293T C290(0.86); C186(0.91); C246(0.94); C70(1.14)  LDD1636  [18]
 LDCM0433  CL43 HEK-293T C290(0.83); C186(0.91); C246(0.92); C116(0.89)  LDD1637  [18]
 LDCM0434  CL44 HEK-293T C290(0.78); C186(0.86); C246(1.35); C70(1.01)  LDD1638  [18]
 LDCM0435  CL45 HEK-293T C290(0.97); C186(0.96); C246(1.64); C70(0.77)  LDD1639  [18]
 LDCM0436  CL46 HEK-293T C290(0.71); C186(0.90); C246(1.61); C70(0.99)  LDD1640  [18]
 LDCM0437  CL47 HEK-293T C290(0.61); C186(0.85); C70(0.99); C116(1.02)  LDD1641  [18]
 LDCM0438  CL48 HEK-293T C290(0.62); C186(1.04); C246(1.18); C70(0.94)  LDD1642  [18]
 LDCM0439  CL49 HEK-293T C290(1.14); C186(1.00); C116(0.86)  LDD1643  [18]
 LDCM0440  CL5 HEK-293T C290(1.09); C186(0.94); C246(1.19); C70(1.15)  LDD1644  [18]
 LDCM0441  CL50 HEK-293T C290(1.07); C186(0.88); C246(1.04); C70(1.17)  LDD1645  [18]
 LDCM0443  CL52 HEK-293T C290(1.07); C186(0.94); C246(1.05); C70(1.26)  LDD1646  [18]
 LDCM0444  CL53 HEK-293T C290(1.22); C186(0.80); C246(1.18); C70(1.03)  LDD1647  [18]
 LDCM0445  CL54 HEK-293T C290(1.17); C186(0.80); C246(0.84); C70(0.88)  LDD1648  [18]
 LDCM0446  CL55 HEK-293T C290(0.78); C186(1.00); C246(0.85); C116(0.87)  LDD1649  [18]
 LDCM0447  CL56 HEK-293T C290(0.75); C186(0.88); C246(1.50); C70(1.11)  LDD1650  [18]
 LDCM0448  CL57 HEK-293T C290(0.85); C186(0.97); C246(1.70); C70(0.73)  LDD1651  [18]
 LDCM0449  CL58 HEK-293T C290(0.65); C186(0.86); C246(1.69); C70(0.81)  LDD1652  [18]
 LDCM0450  CL59 HEK-293T C290(0.62); C186(0.89); C70(1.08); C116(1.11)  LDD1653  [18]
 LDCM0451  CL6 HEK-293T C290(1.00); C186(0.84); C246(0.97); C70(1.03)  LDD1654  [18]
 LDCM0452  CL60 HEK-293T C290(0.67); C186(1.00); C246(1.30); C70(1.06)  LDD1655  [18]
 LDCM0453  CL61 HEK-293T C290(1.22); C186(0.97); C116(0.88)  LDD1656  [18]
 LDCM0454  CL62 HEK-293T C290(1.08); C186(0.99); C246(1.06); C70(1.22)  LDD1657  [18]
 LDCM0455  CL63 HEK-293T C290(1.16); C186(0.94); C246(0.95); C70(1.13)  LDD1658  [18]
 LDCM0456  CL64 HEK-293T C290(1.06); C186(0.86); C246(0.92); C70(1.14)  LDD1659  [18]
 LDCM0457  CL65 HEK-293T C290(1.18); C186(0.95); C246(1.20); C70(1.11)  LDD1660  [18]
 LDCM0458  CL66 HEK-293T C290(1.02); C186(0.90); C246(1.02); C70(1.11)  LDD1661  [18]
 LDCM0459  CL67 HEK-293T C290(0.87); C186(0.94); C246(0.89); C116(0.84)  LDD1662  [18]
 LDCM0460  CL68 HEK-293T C290(0.75); C186(0.84); C246(1.33); C70(1.05)  LDD1663  [18]
 LDCM0461  CL69 HEK-293T C290(0.77); C186(1.07); C246(1.55); C70(1.10)  LDD1664  [18]
 LDCM0462  CL7 HEK-293T C290(0.94); C186(0.96); C246(0.93); C116(0.86)  LDD1665  [18]
 LDCM0463  CL70 HEK-293T C290(0.74); C186(0.90); C246(1.56); C70(0.92)  LDD1666  [18]
 LDCM0464  CL71 HEK-293T C290(0.63); C186(0.95); C70(1.13); C116(1.03)  LDD1667  [18]
 LDCM0465  CL72 HEK-293T C290(0.69); C186(1.06); C246(1.37); C70(1.12)  LDD1668  [18]
 LDCM0466  CL73 HEK-293T C290(1.17); C186(0.99); C116(0.89)  LDD1669  [18]
 LDCM0467  CL74 HEK-293T C290(1.00); C186(0.94); C246(0.96); C70(1.22)  LDD1670  [18]
 LDCM0469  CL76 HEK-293T C290(1.04); C186(0.97); C246(1.00); C70(1.16)  LDD1672  [18]
 LDCM0470  CL77 HEK-293T C290(1.11); C186(0.90); C246(1.05); C70(0.88)  LDD1673  [18]
 LDCM0471  CL78 HEK-293T C290(1.01); C186(0.94); C246(1.00); C70(1.23)  LDD1674  [18]
 LDCM0472  CL79 HEK-293T C290(0.87); C186(0.97); C246(0.88); C116(0.88)  LDD1675  [18]
 LDCM0473  CL8 HEK-293T C290(1.41); C186(0.66); C246(1.11); C70(0.72)  LDD1676  [18]
 LDCM0474  CL80 HEK-293T C290(0.80); C186(0.97); C246(1.20); C70(1.32)  LDD1677  [18]
 LDCM0475  CL81 HEK-293T C290(0.76); C186(1.04); C246(1.63); C70(1.09)  LDD1678  [18]
 LDCM0476  CL82 HEK-293T C290(0.78); C186(0.89); C246(1.23); C70(1.07)  LDD1679  [18]
 LDCM0477  CL83 HEK-293T C290(0.65); C186(0.92); C70(0.92); C116(1.03)  LDD1680  [18]
 LDCM0478  CL84 HEK-293T C290(0.75); C186(1.01); C246(1.15); C70(1.12)  LDD1681  [18]
 LDCM0479  CL85 HEK-293T C290(1.31); C186(1.02); C116(0.90)  LDD1682  [18]
 LDCM0480  CL86 HEK-293T C290(1.14); C186(0.88); C246(1.06); C70(1.17)  LDD1683  [18]
 LDCM0481  CL87 HEK-293T C290(1.22); C186(0.94); C246(0.92); C70(1.03)  LDD1684  [18]
 LDCM0482  CL88 HEK-293T C290(1.13); C186(0.97); C246(0.95); C70(1.18)  LDD1685  [18]
 LDCM0483  CL89 HEK-293T C290(1.23); C186(0.90); C246(1.04); C70(1.51)  LDD1686  [18]
 LDCM0484  CL9 HEK-293T C290(0.69); C186(1.09); C246(1.80); C70(0.87)  LDD1687  [18]
 LDCM0485  CL90 HEK-293T C290(2.00); C186(0.78); C246(0.87); C70(1.36)  LDD1688  [18]
 LDCM0486  CL91 HEK-293T C290(0.96); C186(0.93); C246(1.00); C116(0.82)  LDD1689  [18]
 LDCM0487  CL92 HEK-293T C290(0.96); C186(0.85); C246(1.02); C70(0.99)  LDD1690  [18]
 LDCM0488  CL93 HEK-293T C290(0.91); C186(0.98); C246(1.46); C70(0.94)  LDD1691  [18]
 LDCM0489  CL94 HEK-293T C290(0.81); C186(0.93); C246(1.24); C70(0.82)  LDD1692  [18]
 LDCM0490  CL95 HEK-293T C290(1.17); C186(0.80); C70(0.71); C116(0.96)  LDD1693  [18]
 LDCM0491  CL96 HEK-293T C290(0.95); C186(0.99); C246(1.05); C70(0.93)  LDD1694  [18]
 LDCM0492  CL97 HEK-293T C290(1.07); C186(0.97); C116(0.94)  LDD1695  [18]
 LDCM0493  CL98 HEK-293T C290(1.07); C186(0.90); C246(0.86); C70(1.09)  LDD1696  [18]
 LDCM0494  CL99 HEK-293T C290(1.05); C186(0.95); C246(0.98); C70(0.98)  LDD1697  [18]
 LDCM0634  CY-0357 Hep-G2 C7(0.67)  LDD2228  [17]
 LDCM0495  E2913 HEK-293T C290(1.03); C186(1.10); C246(1.05); C70(1.21)  LDD1698  [18]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C290(1.39); C186(1.31)  LDD1702  [19]
 LDCM0625  F8 Ramos C186(1.52); C290(0.87); C70(0.36)  LDD2187  [20]
 LDCM0572  Fragment10 Ramos C186(0.86); C290(2.20); C70(0.38)  LDD2189  [20]
 LDCM0573  Fragment11 Ramos C186(2.06); C290(0.62); C70(3.57)  LDD2190  [20]
 LDCM0574  Fragment12 Ramos C186(0.92); C290(3.61); C70(0.93)  LDD2191  [20]
 LDCM0575  Fragment13 Ramos C186(1.12); C290(1.24); C70(1.14)  LDD2192  [20]
 LDCM0576  Fragment14 Ramos C186(0.79); C290(0.67); C70(0.39)  LDD2193  [20]
 LDCM0579  Fragment20 Ramos C186(0.59); C290(1.94); C70(0.53)  LDD2194  [20]
 LDCM0580  Fragment21 Ramos C186(0.95); C290(1.35); C70(0.83)  LDD2195  [20]
 LDCM0582  Fragment23 Ramos C186(1.05); C290(0.90); C70(0.97)  LDD2196  [20]
 LDCM0578  Fragment27 Ramos C186(0.95); C290(1.00); C70(1.39)  LDD2197  [20]
 LDCM0586  Fragment28 Ramos C186(1.00); C290(1.32); C70(0.34)  LDD2198  [20]
 LDCM0588  Fragment30 Ramos C186(0.75); C290(1.99); C70(1.43)  LDD2199  [20]
 LDCM0589  Fragment31 Ramos C186(1.05); C290(1.43); C70(1.09)  LDD2200  [20]
 LDCM0590  Fragment32 Ramos C186(0.80); C290(3.39); C70(0.40)  LDD2201  [20]
 LDCM0468  Fragment33 HEK-293T C290(1.10); C186(0.91); C246(0.96); C70(1.14)  LDD1671  [18]
 LDCM0596  Fragment38 Ramos C186(0.70); C290(1.27); C70(2.62)  LDD2203  [20]
 LDCM0566  Fragment4 Ramos C186(1.04); C290(1.26); C70(0.35)  LDD2184  [20]
 LDCM0427  Fragment51 HEK-293T C290(1.02); C186(1.05); C246(1.07); C70(1.27)  LDD1631  [18]
 LDCM0610  Fragment52 Ramos C186(0.71); C290(1.42); C70(0.78)  LDD2204  [20]
 LDCM0614  Fragment56 Ramos C186(0.78); C290(1.18); C70(0.62)  LDD2205  [20]
 LDCM0569  Fragment7 Ramos C186(1.38); C290(1.17); C70(0.39)  LDD2186  [20]
 LDCM0571  Fragment9 Ramos C186(0.86); C290(2.05); C70(0.51)  LDD2188  [20]
 LDCM0022  KB02 HEK-293T C70(0.90); C290(0.96); C186(0.95); C246(1.15)  LDD1492  [18]
 LDCM0023  KB03 Jurkat C290(12.77)  LDD0315  [10]
 LDCM0024  KB05 COLO792 C323(2.27)  LDD3310  [4]
 LDCM0131  RA190 MM1.R C186(1.08)  LDD0304  [21]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Diamine acetyltransferase 1 (SAT1) Acetyltransferase family P21673
Sphingomyelin phosphodiesterase (SMPD1) Acid sphingomyelinase family P17405
NIF3-like protein 1 (NIF3L1) GTP cyclohydrolase I type 2/NIF3 family Q9GZT8
Baculoviral IAP repeat-containing protein 2 (BIRC2) IAP family Q13490
E3 ubiquitin-protein ligase XIAP (XIAP) IAP family P98170
Serine protease HTRA4 (HTRA4) Peptidase S1C family P83105
Serine/threonine-protein kinase PAK 2 (PAK2) STE Ser/Thr protein kinase family Q13177
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Huntingtin (HTT) Huntingtin family P42858
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Nuclear factor erythroid 2-related factor 2 (NFE2L2) BZIP family Q16236
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Melanoma-associated antigen 11 (MAGEA11) . P43364

The Drug(s) Related To This Target

Clinical trial
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Isatin Sulfonamide 34 Small molecular drug D0J3SU
Investigative
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
M826 Small molecular drug D00YNW
Emricasan . DB05408
Fica . DB03384
Incadronic Acid . DB06255

References

1 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
2 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.
3 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
4 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 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.
6 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.
7 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.
8 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.
9 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
10 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
11 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
12 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
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 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
15 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.
16 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.
17 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
18 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
19 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
20 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
21 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.