Details of the Target

General Information of Target

Target ID LDTP01228
Target Name Serine/threonine-protein kinase/endoribonuclease IRE1 (ERN1)
Gene Name ERN1
Gene ID 2081
Synonyms
IRE1; Serine/threonine-protein kinase/endoribonuclease IRE1; Endoplasmic reticulum-to-nucleus signaling 1; Inositol-requiring protein 1; hIRE1p; Ire1-alpha; IRE1a) [Includes: Serine/threonine-protein kinase; EC 2.7.11.1; Endoribonuclease; EC 3.1.26.-)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPARRLLLLLTLLLPGLGIFGSTSTVTLPETLLFVSTLDGSLHAVSKRTGSIKWTLKEDP
VLQVPTHVEEPAFLPDPNDGSLYTLGSKNNEGLTKLPFTIPELVQASPCRSSDGILYMGK
KQDIWYVIDLLTGEKQQTLSSAFADSLCPSTSLLYLGRTEYTITMYDTKTRELRWNATYF
DYAASLPEDDVDYKMSHFVSNGDGLVVTVDSESGDVLWIQNYASPVVAFYVWQREGLRKV
MHINVAVETLRYLTFMSGEVGRITKWKYPFPKETEAKSKLTPTLYVGKYSTSLYASPSMV
HEGVAVVPRGSTLPLLEGPQTDGVTIGDKGECVITPSTDVKFDPGLKSKNKLNYLRNYWL
LIGHHETPLSASTKMLERFPNNLPKHRENVIPADSEKKSFEEVINLVDQTSENAPTTVSR
DVEEKPAHAPARPEAPVDSMLKDMATIILSTFLLIGWVAFIITYPLSMHQQQQLQHQQFQ
KELEKIQLLQQQQQQLPFHPPGDTAQDGELLDTSGPYSESSGTSSPSTSPRASNHSLCSG
SSASKAGSSPSLEQDDGDEETSVVIVGKISFCPKDVLGHGAEGTIVYRGMFDNRDVAVKR
ILPECFSFADREVQLLRESDEHPNVIRYFCTEKDRQFQYIAIELCAATLQEYVEQKDFAH
LGLEPITLLQQTTSGLAHLHSLNIVHRDLKPHNILISMPNAHGKIKAMISDFGLCKKLAV
GRHSFSRRSGVPGTEGWIAPEMLSEDCKENPTYTVDIFSAGCVFYYVISEGSHPFGKSLQ
RQANILLGACSLDCLHPEKHEDVIARELIEKMIAMDPQKRPSAKHVLKHPFFWSLEKQLQ
FFQDVSDRIEKESLDGPIVKQLERGGRAVVKMDWRENITVPLQTDLRKFRTYKGGSVRDL
LRAMRNKKHHYRELPAEVRETLGSLPDDFVCYFTSRFPHLLAHTYRAMELCSHERLFQPY
YFHEPPEPQPPVTPDAL
Target Type
Clinical trial
Target Bioclass
Transporter and channel
Family
Protein kinase superfamily, Ser/Thr protein kinase family
Subcellular location
Endoplasmic reticulum membrane
Function
Serine/threonine-protein kinase and endoribonuclease that acts as a key sensor for the endoplasmic reticulum unfolded protein response (UPR). In unstressed cells, the endoplasmic reticulum luminal domain is maintained in its inactive monomeric state by binding to the endoplasmic reticulum chaperone HSPA5/BiP. Accumulation of misfolded proteins in the endoplasmic reticulum causes release of HSPA5/BiP, allowing the luminal domain to homodimerize, promoting autophosphorylation of the kinase domain and subsequent activation of the endoribonuclease activity. The endoribonuclease activity is specific for XBP1 mRNA and excises 26 nucleotides from XBP1 mRNA. The resulting spliced transcript of XBP1 encodes a transcriptional activator protein that up-regulates expression of UPR target genes. Acts as an upstream signal for ER stress-induced GORASP2-mediated unconventional (ER/Golgi-independent) trafficking of CFTR to cell membrane by modulating the expression and localization of SEC16A.
TTD ID
T01003
Uniprot ID
O75460
DrugMap ID
TTOJ9QL
Ensemble ID
ENST00000433197.4
HGNC ID
HGNC:3449
ChEMBL ID
CHEMBL1163101

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
DU145 SNV: p.R728L DBIA    Probe Info 
EFO27 SNV: p.P830T DBIA    Probe Info 
JHH7 SNV: p.Y911C .
KPNYN SNV: p.A789S .
LNCaP clone FGC SNV: p.S549G DBIA    Probe Info 
MCC13 SNV: p.P392S .
MELJUSO SNV: p.L8R DBIA    Probe Info 
MEWO SNV: p.W737Ter; p.P926S DBIA    Probe Info 
MM1S SNV: p.D816Y .
MOLT4 SNV: p.R728Q; p.P959L .
NCIH1155 SNV: p.R912Q DBIA    Probe Info 
NCIH1792 SNV: p.S337G DBIA    Probe Info 
OVK18 SNV: p.R627C .
RKO SNV: p.S107P DBIA    Probe Info 
SNU1 SNV: p.P187H .
SUPT1 Insertion: p.D555RfsTer5 DBIA    Probe Info 
TOV21G SNV: p.R912L .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 9 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IPM
 Probe Info  		N.A.  LDD0241  [1]
AHL-Pu-1
 Probe Info  		C538(3.16)  LDD0171  [2]
DBIA
 Probe Info  		C605(1.01)  LDD0531  [3]
IA-alkyne
 Probe Info  		N.A.  LDD0162  [4]
NAIA_4
 Probe Info  		C715(0.00); C931(0.00)  LDD2226  [5]
NAIA_5
 Probe Info  		N.A.  LDD2224  [5]
DA-P3
 Probe Info  		N.A.  LDD0178  [6]
TFBX
 Probe Info  		N.A.  LDD0148  [7]
YN-1
 Probe Info  		N.A.  LDD0447  [8]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0026  4SU-RNA+native RNA DM93 C538(3.16)  LDD0171  [2]
 LDCM0214  AC1 HCT 116 C605(1.01)  LDD0531  [3]
 LDCM0215  AC10 HCT 116 C605(1.07)  LDD0532  [3]
 LDCM0226  AC11 HCT 116 C605(1.09)  LDD0543  [3]
 LDCM0230  AC113 HCT 116 C605(1.09)  LDD0547  [3]
 LDCM0231  AC114 HCT 116 C605(0.95)  LDD0548  [3]
 LDCM0232  AC115 HCT 116 C605(1.17)  LDD0549  [3]
 LDCM0233  AC116 HCT 116 C605(1.12)  LDD0550  [3]
 LDCM0234  AC117 HCT 116 C605(1.17)  LDD0551  [3]
 LDCM0235  AC118 HCT 116 C605(1.20)  LDD0552  [3]
 LDCM0236  AC119 HCT 116 C605(1.24)  LDD0553  [3]
 LDCM0237  AC12 HCT 116 C605(1.17)  LDD0554  [3]
 LDCM0238  AC120 HCT 116 C605(1.07)  LDD0555  [3]
 LDCM0239  AC121 HCT 116 C605(1.13)  LDD0556  [3]
 LDCM0240  AC122 HCT 116 C605(1.03)  LDD0557  [3]
 LDCM0241  AC123 HCT 116 C605(1.10)  LDD0558  [3]
 LDCM0242  AC124 HCT 116 C605(1.26)  LDD0559  [3]
 LDCM0243  AC125 HCT 116 C605(1.26)  LDD0560  [3]
 LDCM0244  AC126 HCT 116 C605(1.08)  LDD0561  [3]
 LDCM0245  AC127 HCT 116 C605(1.18)  LDD0562  [3]
 LDCM0259  AC14 HCT 116 C605(1.02)  LDD0576  [3]
 LDCM0270  AC15 HCT 116 C605(1.09)  LDD0587  [3]
 LDCM0276  AC17 HEK-293T C951(0.82); C148(0.91)  LDD1515  [9]
 LDCM0277  AC18 HEK-293T C951(0.96)  LDD1516  [9]
 LDCM0278  AC19 HEK-293T C951(1.20)  LDD1517  [9]
 LDCM0279  AC2 HCT 116 C605(1.02)  LDD0596  [3]
 LDCM0280  AC20 HEK-293T C951(1.09); C148(0.92)  LDD1519  [9]
 LDCM0281  AC21 HEK-293T C951(1.07)  LDD1520  [9]
 LDCM0282  AC22 HEK-293T C951(1.02); C605(1.12)  LDD1521  [9]
 LDCM0283  AC23 HEK-293T C951(1.05); C148(1.09); C605(1.24)  LDD1522  [9]
 LDCM0284  AC24 HEK-293T C951(0.98); C715(0.99)  LDD1523  [9]
 LDCM0285  AC25 HCT 116 C605(0.89)  LDD0602  [3]
 LDCM0286  AC26 HCT 116 C605(0.96)  LDD0603  [3]
 LDCM0287  AC27 HCT 116 C605(0.86)  LDD0604  [3]
 LDCM0288  AC28 HCT 116 C605(1.01)  LDD0605  [3]
 LDCM0289  AC29 HCT 116 C605(0.96)  LDD0606  [3]
 LDCM0290  AC3 HCT 116 C605(1.08)  LDD0607  [3]
 LDCM0291  AC30 HCT 116 C605(0.79)  LDD0608  [3]
 LDCM0292  AC31 HCT 116 C605(0.83)  LDD0609  [3]
 LDCM0293  AC32 HCT 116 C605(0.85)  LDD0610  [3]
 LDCM0294  AC33 HCT 116 C605(0.76)  LDD0611  [3]
 LDCM0295  AC34 HCT 116 C605(0.94)  LDD0612  [3]
 LDCM0296  AC35 HCT 116 C605(0.87)  LDD0613  [3]
 LDCM0297  AC36 HCT 116 C605(0.97)  LDD0614  [3]
 LDCM0298  AC37 HCT 116 C605(0.95)  LDD0615  [3]
 LDCM0299  AC38 HCT 116 C605(1.01)  LDD0616  [3]
 LDCM0300  AC39 HCT 116 C605(0.84)  LDD0617  [3]
 LDCM0301  AC4 HCT 116 C605(1.02)  LDD0618  [3]
 LDCM0302  AC40 HCT 116 C605(0.88)  LDD0619  [3]
 LDCM0303  AC41 HCT 116 C605(1.02)  LDD0620  [3]
 LDCM0304  AC42 HCT 116 C605(1.11)  LDD0621  [3]
 LDCM0305  AC43 HCT 116 C605(0.94)  LDD0622  [3]
 LDCM0306  AC44 HCT 116 C605(0.89)  LDD0623  [3]
 LDCM0307  AC45 HCT 116 C605(0.96)  LDD0624  [3]
 LDCM0308  AC46 HEK-293T C951(0.93); C605(1.09)  LDD1547  [9]
 LDCM0309  AC47 HEK-293T C951(1.15); C148(1.07); C605(1.35)  LDD1548  [9]
 LDCM0310  AC48 HEK-293T C951(0.98); C715(0.99)  LDD1549  [9]
 LDCM0311  AC49 HEK-293T C951(0.94); C148(1.06)  LDD1550  [9]
 LDCM0312  AC5 HCT 116 C605(1.09)  LDD0629  [3]
 LDCM0313  AC50 HEK-293T C951(1.00)  LDD1552  [9]
 LDCM0314  AC51 HEK-293T C951(0.91)  LDD1553  [9]
 LDCM0315  AC52 HEK-293T C951(1.04); C148(0.97)  LDD1554  [9]
 LDCM0316  AC53 HEK-293T C951(1.09)  LDD1555  [9]
 LDCM0317  AC54 HEK-293T C951(0.93); C605(1.05)  LDD1556  [9]
 LDCM0318  AC55 HEK-293T C951(1.11); C148(0.96); C605(1.40)  LDD1557  [9]
 LDCM0319  AC56 HEK-293T C951(0.87); C715(0.93)  LDD1558  [9]
 LDCM0320  AC57 HEK-293T C951(0.86); C148(1.12)  LDD1559  [9]
 LDCM0321  AC58 HEK-293T C951(1.05)  LDD1560  [9]
 LDCM0322  AC59 HEK-293T C951(0.90)  LDD1561  [9]
 LDCM0323  AC6 HCT 116 C605(1.12)  LDD0640  [3]
 LDCM0324  AC60 HEK-293T C951(1.03); C148(1.04)  LDD1563  [9]
 LDCM0325  AC61 HEK-293T C951(0.95)  LDD1564  [9]
 LDCM0326  AC62 HEK-293T C951(1.06); C605(0.99)  LDD1565  [9]
 LDCM0327  AC63 HEK-293T C951(1.02); C148(1.25); C605(1.11)  LDD1566  [9]
 LDCM0328  AC64 HEK-293T C951(1.00); C715(1.19)  LDD1567  [9]
 LDCM0334  AC7 HCT 116 C605(1.05)  LDD0651  [3]
 LDCM0345  AC8 HCT 116 C605(1.15)  LDD0662  [3]
 LDCM0248  AKOS034007472 HCT 116 C605(1.19)  LDD0565  [3]
 LDCM0356  AKOS034007680 HCT 116 C605(1.02)  LDD0673  [3]
 LDCM0275  AKOS034007705 HCT 116 C605(1.13)  LDD0592  [3]
 LDCM0367  CL1 HEK-293T C951(0.98)  LDD1571  [9]
 LDCM0368  CL10 HEK-293T C951(1.42); C605(1.20)  LDD1572  [9]
 LDCM0369  CL100 HCT 116 C605(0.96)  LDD0686  [3]
 LDCM0370  CL101 HCT 116 C605(1.10)  LDD0687  [3]
 LDCM0371  CL102 HCT 116 C605(1.00)  LDD0688  [3]
 LDCM0372  CL103 HCT 116 C605(1.20)  LDD0689  [3]
 LDCM0373  CL104 HCT 116 C605(1.16)  LDD0690  [3]
 LDCM0374  CL105 HEK-293T C951(1.00)  LDD1578  [9]
 LDCM0375  CL106 HEK-293T C951(0.99); C148(0.89)  LDD1579  [9]
 LDCM0376  CL107 HEK-293T C951(0.96); C605(1.00)  LDD1580  [9]
 LDCM0377  CL108 HEK-293T C951(0.88); C605(1.09)  LDD1581  [9]
 LDCM0378  CL109 HEK-293T C951(0.97)  LDD1582  [9]
 LDCM0379  CL11 HEK-293T C951(1.01); C148(1.16); C605(1.01)  LDD1583  [9]
 LDCM0380  CL110 HEK-293T C951(1.25); C148(0.94)  LDD1584  [9]
 LDCM0381  CL111 HEK-293T C951(0.95); C605(1.04)  LDD1585  [9]
 LDCM0382  CL112 HCT 116 C605(0.79)  LDD0699  [3]
 LDCM0383  CL113 HCT 116 C605(0.90)  LDD0700  [3]
 LDCM0384  CL114 HCT 116 C605(0.88)  LDD0701  [3]
 LDCM0385  CL115 HCT 116 C605(0.97)  LDD0702  [3]
 LDCM0386  CL116 HCT 116 C605(1.07)  LDD0703  [3]
 LDCM0387  CL117 HCT 116 C605(0.96)  LDD0704  [3]
 LDCM0388  CL118 HCT 116 C605(0.96)  LDD0705  [3]
 LDCM0389  CL119 HCT 116 C605(0.92)  LDD0706  [3]
 LDCM0390  CL12 HEK-293T C951(1.02); C715(1.24)  LDD1594  [9]
 LDCM0391  CL120 HCT 116 C605(0.82)  LDD0708  [3]
 LDCM0392  CL121 HEK-293T C951(1.07)  LDD1596  [9]
 LDCM0393  CL122 HEK-293T C951(1.05); C148(0.89)  LDD1597  [9]
 LDCM0394  CL123 HEK-293T C951(0.92); C605(1.14)  LDD1598  [9]
 LDCM0395  CL124 HEK-293T C951(1.00); C605(1.27)  LDD1599  [9]
 LDCM0396  CL125 HEK-293T C951(1.08)  LDD1600  [9]
 LDCM0397  CL126 HEK-293T C951(1.19); C148(0.82)  LDD1601  [9]
 LDCM0398  CL127 HEK-293T C951(0.93); C605(1.21)  LDD1602  [9]
 LDCM0399  CL128 HEK-293T C951(0.93); C605(1.19)  LDD1603  [9]
 LDCM0400  CL13 HEK-293T C951(0.99)  LDD1604  [9]
 LDCM0401  CL14 HEK-293T C951(0.98); C148(1.20)  LDD1605  [9]
 LDCM0402  CL15 HEK-293T C951(1.14); C605(1.24)  LDD1606  [9]
 LDCM0403  CL16 HCT 116 C605(1.07)  LDD0720  [3]
 LDCM0404  CL17 HCT 116 C605(0.86)  LDD0721  [3]
 LDCM0405  CL18 HCT 116 C605(0.95)  LDD0722  [3]
 LDCM0406  CL19 HCT 116 C605(0.91)  LDD0723  [3]
 LDCM0407  CL2 HEK-293T C951(1.28); C148(0.97)  LDD1611  [9]
 LDCM0408  CL20 HCT 116 C605(0.97)  LDD0725  [3]
 LDCM0409  CL21 HCT 116 C605(0.80)  LDD0726  [3]
 LDCM0410  CL22 HCT 116 C605(0.90)  LDD0727  [3]
 LDCM0411  CL23 HCT 116 C605(1.00)  LDD0728  [3]
 LDCM0412  CL24 HCT 116 C605(0.89)  LDD0729  [3]
 LDCM0413  CL25 HCT 116 C605(0.91)  LDD0730  [3]
 LDCM0414  CL26 HCT 116 C605(0.89)  LDD0731  [3]
 LDCM0415  CL27 HCT 116 C605(0.85)  LDD0732  [3]
 LDCM0416  CL28 HCT 116 C605(1.03)  LDD0733  [3]
 LDCM0417  CL29 HCT 116 C605(0.91)  LDD0734  [3]
 LDCM0418  CL3 HEK-293T C951(1.03); C605(1.05)  LDD1622  [9]
 LDCM0419  CL30 HCT 116 C605(0.92)  LDD0736  [3]
 LDCM0420  CL31 HEK-293T C951(0.84)  LDD1624  [9]
 LDCM0421  CL32 HEK-293T C951(1.06); C148(0.86)  LDD1625  [9]
 LDCM0422  CL33 HEK-293T C951(1.02)  LDD1626  [9]
 LDCM0423  CL34 HEK-293T C951(1.05); C605(1.00)  LDD1627  [9]
 LDCM0424  CL35 HEK-293T C951(1.03); C148(0.78); C605(1.28)  LDD1628  [9]
 LDCM0425  CL36 HEK-293T C951(1.06); C715(1.06)  LDD1629  [9]
 LDCM0426  CL37 HEK-293T C951(0.95)  LDD1630  [9]
 LDCM0428  CL39 HEK-293T C951(0.89); C605(1.05)  LDD1632  [9]
 LDCM0429  CL4 HEK-293T C951(1.41); C605(1.17)  LDD1633  [9]
 LDCM0430  CL40 HEK-293T C951(0.90); C605(1.14)  LDD1634  [9]
 LDCM0431  CL41 HEK-293T C951(0.88); C148(0.83)  LDD1635  [9]
 LDCM0432  CL42 HEK-293T C951(0.93)  LDD1636  [9]
 LDCM0433  CL43 HEK-293T C951(0.84)  LDD1637  [9]
 LDCM0434  CL44 HEK-293T C951(1.01); C148(1.00)  LDD1638  [9]
 LDCM0435  CL45 HEK-293T C951(1.41)  LDD1639  [9]
 LDCM0436  CL46 HEK-293T C951(1.13); C605(1.02)  LDD1640  [9]
 LDCM0437  CL47 HEK-293T C951(1.34); C148(0.72); C605(1.28)  LDD1641  [9]
 LDCM0438  CL48 HEK-293T C951(0.96); C715(1.15)  LDD1642  [9]
 LDCM0439  CL49 HEK-293T C951(0.96)  LDD1643  [9]
 LDCM0440  CL5 HEK-293T C951(0.94); C148(1.11)  LDD1644  [9]
 LDCM0441  CL50 HEK-293T C951(1.07); C148(1.07)  LDD1645  [9]
 LDCM0443  CL52 HEK-293T C951(1.02); C605(1.05)  LDD1646  [9]
 LDCM0444  CL53 HEK-293T C951(0.91); C148(0.86)  LDD1647  [9]
 LDCM0445  CL54 HEK-293T C951(1.01)  LDD1648  [9]
 LDCM0446  CL55 HEK-293T C951(0.93)  LDD1649  [9]
 LDCM0447  CL56 HEK-293T C951(0.99); C148(1.00)  LDD1650  [9]
 LDCM0448  CL57 HEK-293T C951(1.24)  LDD1651  [9]
 LDCM0449  CL58 HEK-293T C951(1.25); C605(1.17)  LDD1652  [9]
 LDCM0450  CL59 HEK-293T C951(0.96); C148(0.82); C605(1.32)  LDD1653  [9]
 LDCM0451  CL6 HEK-293T C951(0.86)  LDD1654  [9]
 LDCM0452  CL60 HEK-293T C951(1.06); C715(1.14)  LDD1655  [9]
 LDCM0453  CL61 HEK-293T C951(0.88)  LDD1656  [9]
 LDCM0454  CL62 HEK-293T C951(0.99); C148(0.98)  LDD1657  [9]
 LDCM0455  CL63 HEK-293T C951(0.92); C605(1.13)  LDD1658  [9]
 LDCM0456  CL64 HEK-293T C951(1.10); C605(1.05)  LDD1659  [9]
 LDCM0457  CL65 HEK-293T C951(0.90); C148(0.87)  LDD1660  [9]
 LDCM0458  CL66 HEK-293T C951(1.04)  LDD1661  [9]
 LDCM0459  CL67 HEK-293T C951(0.89)  LDD1662  [9]
 LDCM0460  CL68 HEK-293T C951(1.06); C148(0.75)  LDD1663  [9]
 LDCM0461  CL69 HEK-293T C951(1.20)  LDD1664  [9]
 LDCM0462  CL7 HEK-293T C951(0.84)  LDD1665  [9]
 LDCM0463  CL70 HEK-293T C951(1.17); C605(0.97)  LDD1666  [9]
 LDCM0464  CL71 HEK-293T C951(1.28); C148(1.01); C605(1.37)  LDD1667  [9]
 LDCM0465  CL72 HEK-293T C951(1.07); C715(0.99)  LDD1668  [9]
 LDCM0466  CL73 HEK-293T C951(1.08)  LDD1669  [9]
 LDCM0467  CL74 HEK-293T C951(1.22); C148(0.86)  LDD1670  [9]
 LDCM0469  CL76 HEK-293T C951(1.05); C605(1.15)  LDD1672  [9]
 LDCM0470  CL77 HEK-293T C951(0.95); C148(0.86)  LDD1673  [9]
 LDCM0471  CL78 HEK-293T C951(0.88)  LDD1674  [9]
 LDCM0472  CL79 HEK-293T C951(0.77)  LDD1675  [9]
 LDCM0473  CL8 HEK-293T C951(1.08); C148(0.70)  LDD1676  [9]
 LDCM0474  CL80 HEK-293T C951(1.11); C148(0.94)  LDD1677  [9]
 LDCM0475  CL81 HEK-293T C951(1.00)  LDD1678  [9]
 LDCM0476  CL82 HEK-293T C951(1.12); C605(1.04)  LDD1679  [9]
 LDCM0477  CL83 HEK-293T C951(1.27); C148(0.96); C605(1.20)  LDD1680  [9]
 LDCM0478  CL84 HEK-293T C951(0.98); C715(1.06)  LDD1681  [9]
 LDCM0479  CL85 HEK-293T C951(1.00)  LDD1682  [9]
 LDCM0480  CL86 HEK-293T C951(1.07); C148(1.00)  LDD1683  [9]
 LDCM0481  CL87 HEK-293T C951(0.82); C605(1.13)  LDD1684  [9]
 LDCM0482  CL88 HEK-293T C951(0.90); C605(1.13)  LDD1685  [9]
 LDCM0483  CL89 HEK-293T C951(0.85); C148(1.08)  LDD1686  [9]
 LDCM0484  CL9 HEK-293T C951(0.90)  LDD1687  [9]
 LDCM0485  CL90 HEK-293T C951(1.44)  LDD1688  [9]
 LDCM0486  CL91 HCT 116 C605(0.86)  LDD0803  [3]
 LDCM0487  CL92 HCT 116 C605(1.00)  LDD0804  [3]
 LDCM0488  CL93 HCT 116 C605(1.09)  LDD0805  [3]
 LDCM0489  CL94 HCT 116 C605(1.12)  LDD0806  [3]
 LDCM0490  CL95 HCT 116 C605(0.99)  LDD0807  [3]
 LDCM0491  CL96 HCT 116 C605(1.06)  LDD0808  [3]
 LDCM0492  CL97 HCT 116 C605(1.05)  LDD0809  [3]
 LDCM0493  CL98 HCT 116 C605(1.04)  LDD0810  [3]
 LDCM0494  CL99 HCT 116 C605(1.02)  LDD0811  [3]
 LDCM0495  E2913 HEK-293T C951(0.89); C605(1.06)  LDD1698  [9]
 LDCM0573  Fragment11 Ramos C951(2.79)  LDD2190  [10]
 LDCM0576  Fragment14 Ramos C951(1.84)  LDD2193  [10]
 LDCM0468  Fragment33 HEK-293T C951(0.86); C605(1.15)  LDD1671  [9]
 LDCM0566  Fragment4 Ramos C951(0.83)  LDD2184  [10]
 LDCM0427  Fragment51 HEK-293T C951(1.19); C148(1.10)  LDD1631  [9]
 LDCM0022  KB02 HEK-293T C951(0.97)  LDD1492  [9]
 LDCM0023  KB03 HEK-293T C951(1.00)  LDD1497  [9]
 LDCM0024  KB05 G361 C951(1.77); C109(1.69)  LDD3311  [11]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 9 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Adenylate kinase 8 (AK8) Adenylate kinase family Q96MA6
DNA polymerase alpha subunit B (POLA2) DNA polymerase alpha subunit B family Q14181
Endoplasmic reticulum chaperone BiP (HSPA5) Heat shock protein 70 family P11021
E3 ubiquitin-protein ligase synoviolin (SYVN1) HRD1 family Q86TM6
Serine/threonine-protein kinase TAO3 (TAOK3) STE Ser/Thr protein kinase family Q9H2K8
Zinc-regulated GTPase metalloprotein activator 1A (ZNG1A) SIMIBI class G3E GTPase family Q9BRT8
TNF receptor-associated factor 2 (TRAF2) TNF receptor-associated factor family Q12933
Ubiquitin-conjugating enzyme E2 A (UBE2A) Ubiquitin-conjugating enzyme family P49459
Set1/Ash2 histone methyltransferase complex subunit ASH2 (ASH2L) . Q9UBL3
Transporter and channel
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Large neutral amino acids transporter small subunit 2 (SLC7A8) L-type amino acid transporter (LAT) (TC 2.A.3.8) family Q9UHI5
Apoptosis regulator BAX (BAX) Bcl-2 family Q07812
Protein OS-9 (OS9) OS-9 family Q13438
Serine/threonine-protein kinase/endoribonuclease IRE1 (ERN1) Ser/Thr protein kinase family O75460
Protein sel-1 homolog 1 (SEL1L) Sel-1 family Q9UBV2
Other
Click To Hide/Show 10 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cyclin-dependent kinase inhibitor 1 (CDKN1A) CDI family P38936
Protein INCA1 (INCA1) INCA family Q0VD86
Transcription initiation factor IIA subunit 1 (GTF2A1) TFIIA subunit 1 family P52655
Protein YIPF5 (YIPF5) YIP1 family Q969M3
Bromo adjacent homology domain-containing 1 protein (BAHD1) . Q8TBE0
La-related protein 4B (LARP4B) . Q92615
Period circadian protein homolog 1 (PER1) . O15534
Spermatogenesis-associated serine-rich protein 1 (SPATS1) . Q496A3
Suppressor of cytokine signaling 6 (SOCS6) . O14544
WW domain binding protein 1-like (WBP1L) . Q9NX94

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
Fostamatinib Small molecular drug DB12010
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Orin1001 Small interfering RNA DK3QD9
Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Apy29 Small molecular drug D1BCW8
N~2~-1h-benzimidazol-5-yl-n~4~-(3-cyclopropyl-1h-pyrazol-5-yl)Pyrimidine-24-diamine Small molecular drug DB07382
Pmid24749861c34 Small molecular drug D0E3CB
Patented
Click To Hide/Show 11 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
879325-11-8 Small molecular drug D0KF0D
Ac1le05k Small molecular drug D0M2TO
Bb 0223767 Small molecular drug D0VP7R
T8361 Small molecular drug D01UPA
Us8614253, 29-1 Small molecular drug D0AV6X
Us8614253, 29-19 Small molecular drug D0GK1K
Us8614253, 32-4 Small molecular drug D0TA9C
Us8614253, 32-5 Small molecular drug D0DV4H
Us9040714, 155 Small molecular drug D0ZP0G
Us9040714, 7 Small molecular drug D00OUG
Us9241942, 32-12 Small molecular drug D0XX5N

References

1 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.
2 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
3 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
4 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
5 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
6 A chemical probe unravels the reactive proteome of health-associated catechols. Chem Sci. 2023 Jul 22;14(32):8635-8643. doi: 10.1039/d3sc00888f. eCollection 2023 Aug 16.
Mass spectrometry data entry: PXD043348
7 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
8 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.
9 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
10 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
11 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