Details of the Target

General Information of Target

Target ID LDTP12744
Target Name Interleukin-1 receptor-associated kinase 4 (IRAK4)
Gene Name IRAK4
Gene ID 51135
Synonyms
Interleukin-1 receptor-associated kinase 4; IRAK-4; EC 2.7.11.1; Renal carcinoma antigen NY-REN-64
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MVGGGGKRRPGGEGPQCEKTTDVKKSKFCEADVSSDLRKEVENHYKLSLPEDFYHFWKFC
EELDPEKPSDSLSASLGLQLVGPYDILAGKHKTKKKSTGLNFNLHWRFYYDPPEFQTIII
GDNKTQYHMGYFRDSPDEFPVYVGINEAKKNCIIVPNGDNVFAAVKLFLTKKLREITDKK
KINLLKNIDEKLTEAARELGYSLEQRTVKMKQRDKKVVTKTFHGAGLVVPVDKNDVGYRE
LPETDADLKRICKTIVEAASDEERLKAFAPIQEMMTFVQFANDECDYGMGLELGMDLFCY
GSHYFHKVAGQLLPLAYNLLKRNLFAEIIEEHLANRSQENIDQLAA
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, TKL Ser/Thr protein kinase family, Pelle subfamily
Subcellular location
Cytoplasm
Function
Serine/threonine-protein kinase that plays a critical role in initiating innate immune response against foreign pathogens. Involved in Toll-like receptor (TLR) and IL-1R signaling pathways. Is rapidly recruited by MYD88 to the receptor-signaling complex upon TLR activation to form the Myddosome together with IRAK2. Phosphorylates initially IRAK1, thus stimulating the kinase activity and intensive autophosphorylation of IRAK1. Phosphorylates E3 ubiquitin ligases Pellino proteins (PELI1, PELI2 and PELI3) to promote pellino-mediated polyubiquitination of IRAK1. Then, the ubiquitin-binding domain of IKBKG/NEMO binds to polyubiquitinated IRAK1 bringing together the IRAK1-MAP3K7/TAK1-TRAF6 complex and the NEMO-IKKA-IKKB complex. In turn, MAP3K7/TAK1 activates IKKs (CHUK/IKKA and IKBKB/IKKB) leading to NF-kappa-B nuclear translocation and activation. Alternatively, phosphorylates TIRAP to promote its ubiquitination and subsequent degradation. Phosphorylates NCF1 and regulates NADPH oxidase activation after LPS stimulation suggesting a similar mechanism during microbial infections.
TTD ID
T55398
Uniprot ID
Q9NWZ3
DrugMap ID
TTKFVXR
Ensemble ID
ENST00000440781.6
HGNC ID
HGNC:17967
ChEMBL ID
CHEMBL3778

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
IGROV1 SNV: p.A238S DBIA    Probe Info 
KMCH1 SNV: p.K400Q DBIA    Probe Info 
MDST8 SNV: p.M218I DBIA    Probe Info 
SUPT1 SNV: p.A38V DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 11 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
Backus_15
 Probe Info  		3.19  LDD0423  [2]
NAIA_5
 Probe Info  		C13(1.13)  LDD2227  [3]
IA-alkyne
 Probe Info  		C13(6.51)  LDD0513  [4]
DBIA
 Probe Info  		C13(0.98)  LDD0078  [5]
AMP probe
 Probe Info  		K213(0.00); K214(0.00)  LDD0200  [6]
ATP probe
 Probe Info  		K213(0.00); K214(0.00); K313(0.00)  LDD0199  [6]
KY-26
 Probe Info  		N.A.  LDD0301  [7]
IPM
 Probe Info  		N.A.  LDD0005  [8]
NPM
 Probe Info  		N.A.  LDD0016  [8]
AOyne
 Probe Info  		15.00  LDD0443  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HCT 116 C128(0.90); C13(1.09)  LDD0531  [5]
 LDCM0215  AC10 HCT 116 C13(0.80)  LDD0532  [5]
 LDCM0226  AC11 HCT 116 C13(0.88)  LDD0543  [5]
 LDCM0237  AC12 HCT 116 C13(0.85)  LDD0554  [5]
 LDCM0259  AC14 HCT 116 C13(0.63)  LDD0576  [5]
 LDCM0270  AC15 HCT 116 C13(0.56)  LDD0587  [5]
 LDCM0276  AC17 HCT 116 C13(1.08)  LDD0593  [5]
 LDCM0277  AC18 HCT 116 C13(1.22)  LDD0594  [5]
 LDCM0278  AC19 HCT 116 C13(1.32)  LDD0595  [5]
 LDCM0279  AC2 HCT 116 C13(0.86); C128(0.94)  LDD0596  [5]
 LDCM0280  AC20 HCT 116 C13(1.14)  LDD0597  [5]
 LDCM0281  AC21 HCT 116 C13(1.10)  LDD0598  [5]
 LDCM0282  AC22 HCT 116 C13(1.04)  LDD0599  [5]
 LDCM0283  AC23 HCT 116 C13(1.17)  LDD0600  [5]
 LDCM0284  AC24 HCT 116 C13(1.12)  LDD0601  [5]
 LDCM0285  AC25 HCT 116 C13(1.07)  LDD0602  [5]
 LDCM0286  AC26 HCT 116 C13(1.55)  LDD0603  [5]
 LDCM0287  AC27 HCT 116 C13(1.09)  LDD0604  [5]
 LDCM0288  AC28 HCT 116 C13(1.46)  LDD0605  [5]
 LDCM0289  AC29 HCT 116 C13(1.38)  LDD0606  [5]
 LDCM0290  AC3 HCT 116 C128(0.91); C13(1.11)  LDD0607  [5]
 LDCM0291  AC30 HCT 116 C13(1.39)  LDD0608  [5]
 LDCM0292  AC31 HCT 116 C13(1.56)  LDD0609  [5]
 LDCM0293  AC32 HCT 116 C13(2.35)  LDD0610  [5]
 LDCM0294  AC33 HCT 116 C13(1.55)  LDD0611  [5]
 LDCM0295  AC34 HCT 116 C13(1.02)  LDD0612  [5]
 LDCM0296  AC35 HCT 116 C13(1.01)  LDD0613  [5]
 LDCM0297  AC36 HCT 116 C13(1.20)  LDD0614  [5]
 LDCM0298  AC37 HCT 116 C13(0.82)  LDD0615  [5]
 LDCM0299  AC38 HCT 116 C13(1.26)  LDD0616  [5]
 LDCM0300  AC39 HCT 116 C13(1.35)  LDD0617  [5]
 LDCM0301  AC4 HCT 116 C128(0.84); C13(1.24)  LDD0618  [5]
 LDCM0302  AC40 HCT 116 C13(1.19)  LDD0619  [5]
 LDCM0303  AC41 HCT 116 C13(0.78)  LDD0620  [5]
 LDCM0304  AC42 HCT 116 C13(0.79)  LDD0621  [5]
 LDCM0305  AC43 HCT 116 C13(0.71)  LDD0622  [5]
 LDCM0306  AC44 HCT 116 C13(0.53)  LDD0623  [5]
 LDCM0307  AC45 HCT 116 C13(0.73)  LDD0624  [5]
 LDCM0308  AC46 HCT 116 C13(1.22)  LDD0625  [5]
 LDCM0309  AC47 HCT 116 C13(1.20)  LDD0626  [5]
 LDCM0310  AC48 HCT 116 C13(1.12)  LDD0627  [5]
 LDCM0311  AC49 HCT 116 C13(1.23)  LDD0628  [5]
 LDCM0312  AC5 HCT 116 C128(0.77); C13(1.20)  LDD0629  [5]
 LDCM0313  AC50 HCT 116 C13(0.91)  LDD0630  [5]
 LDCM0314  AC51 HCT 116 C13(1.05)  LDD0631  [5]
 LDCM0315  AC52 HCT 116 C13(1.16)  LDD0632  [5]
 LDCM0316  AC53 HCT 116 C13(1.16)  LDD0633  [5]
 LDCM0317  AC54 HCT 116 C13(1.22)  LDD0634  [5]
 LDCM0318  AC55 HCT 116 C13(1.02)  LDD0635  [5]
 LDCM0319  AC56 HCT 116 C13(1.12)  LDD0636  [5]
 LDCM0320  AC57 HEK-293T C13(1.11); C128(1.16)  LDD1559  [10]
 LDCM0321  AC58 HEK-293T C13(0.95); C128(1.15)  LDD1560  [10]
 LDCM0322  AC59 HEK-293T C13(0.97); C128(1.10)  LDD1561  [10]
 LDCM0323  AC6 HCT 116 C13(0.69)  LDD0640  [5]
 LDCM0324  AC60 HEK-293T C13(1.00); C128(1.10)  LDD1563  [10]
 LDCM0325  AC61 HEK-293T C13(1.02); C128(1.13)  LDD1564  [10]
 LDCM0326  AC62 HEK-293T C13(1.05); C128(1.15)  LDD1565  [10]
 LDCM0327  AC63 HEK-293T C13(1.00); C128(1.08)  LDD1566  [10]
 LDCM0328  AC64 HEK-293T C13(1.01); C128(1.12)  LDD1567  [10]
 LDCM0334  AC7 HCT 116 C13(0.68)  LDD0651  [5]
 LDCM0345  AC8 HCT 116 C13(0.78)  LDD0662  [5]
 LDCM0349  AC83 HCT 116 C128(1.48)  LDD0666  [5]
 LDCM0350  AC84 HCT 116 C128(1.28)  LDD0667  [5]
 LDCM0351  AC85 HCT 116 C128(1.30)  LDD0668  [5]
 LDCM0352  AC86 HCT 116 C128(1.41)  LDD0669  [5]
 LDCM0353  AC87 HCT 116 C128(1.39)  LDD0670  [5]
 LDCM0354  AC88 HCT 116 C128(1.45)  LDD0671  [5]
 LDCM0355  AC89 HCT 116 C128(1.32)  LDD0672  [5]
 LDCM0357  AC90 HCT 116 C128(1.53)  LDD0674  [5]
 LDCM0358  AC91 HCT 116 C128(1.16)  LDD0675  [5]
 LDCM0359  AC92 HCT 116 C128(1.29)  LDD0676  [5]
 LDCM0360  AC93 HCT 116 C128(1.22)  LDD0677  [5]
 LDCM0361  AC94 HCT 116 C128(1.08)  LDD0678  [5]
 LDCM0362  AC95 HCT 116 C128(1.33)  LDD0679  [5]
 LDCM0363  AC96 HCT 116 C128(1.02)  LDD0680  [5]
 LDCM0364  AC97 HCT 116 C128(1.45)  LDD0681  [5]
 LDCM0248  AKOS034007472 HCT 116 C13(0.90)  LDD0565  [5]
 LDCM0356  AKOS034007680 HCT 116 C13(0.89)  LDD0673  [5]
 LDCM0275  AKOS034007705 HCT 116 C13(0.89)  LDD0592  [5]
 LDCM0156  Aniline NCI-H1299 12.41  LDD0403  [1]
 LDCM0020  ARS-1620 HCC44 C13(0.98)  LDD0078  [5]
 LDCM0632  CL-Sc Hep-G2 C13(1.13)  LDD2227  [3]
 LDCM0367  CL1 HEK-293T C13(0.91); C128(0.91)  LDD1571  [10]
 LDCM0368  CL10 HEK-293T C13(1.04); C128(0.89)  LDD1572  [10]
 LDCM0369  CL100 HCT 116 C128(0.93); C13(1.08)  LDD0686  [5]
 LDCM0370  CL101 HCT 116 C13(0.77)  LDD0687  [5]
 LDCM0371  CL102 HCT 116 C13(0.67)  LDD0688  [5]
 LDCM0372  CL103 HCT 116 C13(0.63)  LDD0689  [5]
 LDCM0373  CL104 HCT 116 C13(0.86)  LDD0690  [5]
 LDCM0374  CL105 HCT 116 C13(0.97)  LDD0691  [5]
 LDCM0375  CL106 HCT 116 C13(1.09)  LDD0692  [5]
 LDCM0376  CL107 HCT 116 C13(1.05)  LDD0693  [5]
 LDCM0377  CL108 HCT 116 C13(1.13)  LDD0694  [5]
 LDCM0378  CL109 HCT 116 C13(1.09)  LDD0695  [5]
 LDCM0379  CL11 HEK-293T C13(1.08); C128(0.78)  LDD1583  [10]
 LDCM0380  CL110 HCT 116 C13(1.51)  LDD0697  [5]
 LDCM0381  CL111 HCT 116 C13(1.11)  LDD0698  [5]
 LDCM0382  CL112 HCT 116 C13(0.93)  LDD0699  [5]
 LDCM0383  CL113 HCT 116 C13(1.11)  LDD0700  [5]
 LDCM0384  CL114 HCT 116 C13(1.82)  LDD0701  [5]
 LDCM0385  CL115 HCT 116 C13(1.70)  LDD0702  [5]
 LDCM0386  CL116 HCT 116 C13(1.13)  LDD0703  [5]
 LDCM0387  CL117 HCT 116 C13(1.20)  LDD0704  [5]
 LDCM0388  CL118 HCT 116 C13(0.66)  LDD0705  [5]
 LDCM0389  CL119 HCT 116 C13(0.60)  LDD0706  [5]
 LDCM0390  CL12 HEK-293T C13(1.00); C128(0.82)  LDD1594  [10]
 LDCM0391  CL120 HCT 116 C13(0.80)  LDD0708  [5]
 LDCM0392  CL121 HCT 116 C13(1.37)  LDD0709  [5]
 LDCM0393  CL122 HCT 116 C13(1.25)  LDD0710  [5]
 LDCM0394  CL123 HCT 116 C13(1.04)  LDD0711  [5]
 LDCM0395  CL124 HCT 116 C13(1.16)  LDD0712  [5]
 LDCM0396  CL125 HEK-293T C13(1.04); C128(1.03)  LDD1600  [10]
 LDCM0397  CL126 HEK-293T C13(1.02); C128(1.14)  LDD1601  [10]
 LDCM0398  CL127 HEK-293T C13(1.05); C128(1.06)  LDD1602  [10]
 LDCM0399  CL128 HEK-293T C128(1.16)  LDD1603  [10]
 LDCM0400  CL13 HEK-293T C13(0.99); C128(1.06)  LDD1604  [10]
 LDCM0401  CL14 HEK-293T C13(0.81); C128(1.15)  LDD1605  [10]
 LDCM0402  CL15 HEK-293T C13(0.79); C128(0.86)  LDD1606  [10]
 LDCM0403  CL16 HCT 116 C128(0.95)  LDD0720  [5]
 LDCM0404  CL17 HCT 116 C128(0.84)  LDD0721  [5]
 LDCM0405  CL18 HCT 116 C128(1.15)  LDD0722  [5]
 LDCM0406  CL19 HCT 116 C128(0.97)  LDD0723  [5]
 LDCM0407  CL2 HEK-293T C13(0.97); C128(1.19)  LDD1611  [10]
 LDCM0408  CL20 HCT 116 C128(0.80)  LDD0725  [5]
 LDCM0409  CL21 HCT 116 C128(0.83)  LDD0726  [5]
 LDCM0410  CL22 HCT 116 C128(0.84)  LDD0727  [5]
 LDCM0411  CL23 HCT 116 C128(0.78)  LDD0728  [5]
 LDCM0412  CL24 HCT 116 C128(0.82)  LDD0729  [5]
 LDCM0413  CL25 HCT 116 C128(0.72)  LDD0730  [5]
 LDCM0414  CL26 HCT 116 C128(0.83)  LDD0731  [5]
 LDCM0415  CL27 HCT 116 C128(0.75)  LDD0732  [5]
 LDCM0416  CL28 HCT 116 C128(0.74)  LDD0733  [5]
 LDCM0417  CL29 HCT 116 C128(0.70)  LDD0734  [5]
 LDCM0418  CL3 HEK-293T C13(0.91); C128(0.79)  LDD1622  [10]
 LDCM0419  CL30 HCT 116 C128(0.75)  LDD0736  [5]
 LDCM0420  CL31 HCT 116 C128(0.83); C13(1.18)  LDD0737  [5]
 LDCM0421  CL32 HCT 116 C128(0.92); C13(1.23)  LDD0738  [5]
 LDCM0422  CL33 HCT 116 C128(0.85); C13(1.23)  LDD0739  [5]
 LDCM0423  CL34 HCT 116 C128(0.98); C13(0.98)  LDD0740  [5]
 LDCM0424  CL35 HCT 116 C128(0.88); C13(1.08)  LDD0741  [5]
 LDCM0425  CL36 HCT 116 C128(0.90); C13(1.29)  LDD0742  [5]
 LDCM0426  CL37 HCT 116 C128(0.93); C13(1.13)  LDD0743  [5]
 LDCM0428  CL39 HCT 116 C128(0.91); C13(1.19)  LDD0745  [5]
 LDCM0429  CL4 HEK-293T C128(0.99)  LDD1633  [10]
 LDCM0430  CL40 HCT 116 C128(0.80); C13(0.89)  LDD0747  [5]
 LDCM0431  CL41 HCT 116 C128(0.83); C13(1.15)  LDD0748  [5]
 LDCM0432  CL42 HCT 116 C128(0.85); C13(1.18)  LDD0749  [5]
 LDCM0433  CL43 HCT 116 C128(0.82); C13(1.13)  LDD0750  [5]
 LDCM0434  CL44 HCT 116 C128(0.81); C13(1.12)  LDD0751  [5]
 LDCM0435  CL45 HCT 116 C128(0.78); C13(1.38)  LDD0752  [5]
 LDCM0436  CL46 HCT 116 C13(1.04)  LDD0753  [5]
 LDCM0437  CL47 HCT 116 C13(1.15)  LDD0754  [5]
 LDCM0438  CL48 HCT 116 C13(0.87)  LDD0755  [5]
 LDCM0439  CL49 HCT 116 C13(0.87)  LDD0756  [5]
 LDCM0440  CL5 HEK-293T C13(1.04); C128(1.07)  LDD1644  [10]
 LDCM0441  CL50 HCT 116 C13(0.99)  LDD0758  [5]
 LDCM0442  CL51 HCT 116 C13(1.12)  LDD0759  [5]
 LDCM0443  CL52 HCT 116 C13(1.05)  LDD0760  [5]
 LDCM0444  CL53 HCT 116 C13(1.04)  LDD0761  [5]
 LDCM0445  CL54 HCT 116 C13(1.06)  LDD0762  [5]
 LDCM0446  CL55 HCT 116 C13(0.89)  LDD0763  [5]
 LDCM0447  CL56 HCT 116 C13(1.12)  LDD0764  [5]
 LDCM0448  CL57 HCT 116 C13(1.20)  LDD0765  [5]
 LDCM0449  CL58 HCT 116 C13(1.12)  LDD0766  [5]
 LDCM0450  CL59 HCT 116 C13(1.00)  LDD0767  [5]
 LDCM0451  CL6 HEK-293T C13(0.94); C128(1.07)  LDD1654  [10]
 LDCM0452  CL60 HCT 116 C13(1.31)  LDD0769  [5]
 LDCM0453  CL61 HEK-293T C13(0.95); C128(1.19)  LDD1656  [10]
 LDCM0454  CL62 HEK-293T C13(1.01); C128(1.10)  LDD1657  [10]
 LDCM0455  CL63 HEK-293T C13(1.05); C128(1.05)  LDD1658  [10]
 LDCM0456  CL64 HEK-293T C128(1.05)  LDD1659  [10]
 LDCM0457  CL65 HEK-293T C13(1.07); C128(1.12)  LDD1660  [10]
 LDCM0458  CL66 HEK-293T C13(1.01); C128(1.13)  LDD1661  [10]
 LDCM0459  CL67 HEK-293T C13(1.00); C128(1.06)  LDD1662  [10]
 LDCM0460  CL68 HEK-293T C13(1.01); C128(0.90)  LDD1663  [10]
 LDCM0461  CL69 HEK-293T C13(0.92); C128(0.89)  LDD1664  [10]
 LDCM0462  CL7 HEK-293T C13(0.96); C128(0.96)  LDD1665  [10]
 LDCM0463  CL70 HEK-293T C13(1.16); C128(0.89)  LDD1666  [10]
 LDCM0464  CL71 HEK-293T C13(0.98); C128(0.82)  LDD1667  [10]
 LDCM0465  CL72 HEK-293T C13(1.11); C128(0.84)  LDD1668  [10]
 LDCM0466  CL73 HEK-293T C13(0.98); C128(1.20)  LDD1669  [10]
 LDCM0467  CL74 HEK-293T C13(1.07); C128(1.13)  LDD1670  [10]
 LDCM0469  CL76 HEK-293T C128(1.10)  LDD1672  [10]
 LDCM0470  CL77 HEK-293T C13(1.04); C128(1.07)  LDD1673  [10]
 LDCM0471  CL78 HEK-293T C13(1.06); C128(1.06)  LDD1674  [10]
 LDCM0472  CL79 HEK-293T C13(0.95); C128(1.02)  LDD1675  [10]
 LDCM0473  CL8 HEK-293T C13(0.85); C128(0.74)  LDD1676  [10]
 LDCM0474  CL80 HEK-293T C13(1.00); C128(0.88)  LDD1677  [10]
 LDCM0475  CL81 HEK-293T C13(1.05); C128(0.93)  LDD1678  [10]
 LDCM0476  CL82 HEK-293T C13(1.13); C128(0.88)  LDD1679  [10]
 LDCM0477  CL83 HEK-293T C13(0.93); C128(0.77)  LDD1680  [10]
 LDCM0478  CL84 HEK-293T C13(0.92); C128(0.86)  LDD1681  [10]
 LDCM0479  CL85 HEK-293T C13(0.86); C128(1.32)  LDD1682  [10]
 LDCM0480  CL86 HEK-293T C13(0.93); C128(1.17)  LDD1683  [10]
 LDCM0481  CL87 HEK-293T C13(0.94); C128(1.18)  LDD1684  [10]
 LDCM0482  CL88 HEK-293T C128(1.16)  LDD1685  [10]
 LDCM0483  CL89 HEK-293T C13(0.96); C128(1.15)  LDD1686  [10]
 LDCM0484  CL9 HEK-293T C13(0.95); C128(0.95)  LDD1687  [10]
 LDCM0485  CL90 HEK-293T C13(0.84); C128(0.98)  LDD1688  [10]
 LDCM0486  CL91 HCT 116 C128(1.00); C13(0.76)  LDD0803  [5]
 LDCM0487  CL92 HCT 116 C128(0.89); C13(0.95)  LDD0804  [5]
 LDCM0488  CL93 HCT 116 C128(0.81); C13(1.24)  LDD0805  [5]
 LDCM0489  CL94 HCT 116 C128(1.00); C13(1.22)  LDD0806  [5]
 LDCM0490  CL95 HCT 116 C128(0.93); C13(0.92)  LDD0807  [5]
 LDCM0491  CL96 HCT 116 C128(0.81); C13(1.30)  LDD0808  [5]
 LDCM0492  CL97 HCT 116 C128(0.90); C13(1.16)  LDD0809  [5]
 LDCM0493  CL98 HCT 116 C128(1.00); C13(0.81)  LDD0810  [5]
 LDCM0494  CL99 HCT 116 C128(0.96); C13(0.96)  LDD0811  [5]
 LDCM0198  Dimethyl Fumarate(DMF) T cell C13(6.51)  LDD0513  [4]
 LDCM0495  E2913 HEK-293T C13(0.98); C128(1.15)  LDD1698  [10]
 LDCM0625  F8 Ramos C13(1.00)  LDD2187  [11]
 LDCM0572  Fragment10 Ramos C13(1.30)  LDD2189  [11]
 LDCM0574  Fragment12 Ramos C13(1.04)  LDD2191  [11]
 LDCM0575  Fragment13 Ramos C13(1.08)  LDD2192  [11]
 LDCM0576  Fragment14 Ramos C13(0.71)  LDD2193  [11]
 LDCM0579  Fragment20 Ramos C13(1.06)  LDD2194  [11]
 LDCM0580  Fragment21 Ramos C13(0.89)  LDD2195  [11]
 LDCM0582  Fragment23 Ramos C13(1.42)  LDD2196  [11]
 LDCM0578  Fragment27 Ramos C13(0.95)  LDD2197  [11]
 LDCM0586  Fragment28 Ramos C13(0.94)  LDD2198  [11]
 LDCM0588  Fragment30 Ramos C13(1.17)  LDD2199  [11]
 LDCM0589  Fragment31 Ramos C13(0.90)  LDD2200  [11]
 LDCM0590  Fragment32 Ramos C13(1.30)  LDD2201  [11]
 LDCM0468  Fragment33 HEK-293T C13(1.31); C128(0.99)  LDD1671  [10]
 LDCM0596  Fragment38 Ramos C13(0.95)  LDD2203  [11]
 LDCM0566  Fragment4 Ramos C13(0.97)  LDD2184  [11]
 LDCM0427  Fragment51 HCT 116 C128(0.90); C13(1.34)  LDD0744  [5]
 LDCM0610  Fragment52 Ramos C13(1.38)  LDD2204  [11]
 LDCM0614  Fragment56 Ramos C13(1.10)  LDD2205  [11]
 LDCM0569  Fragment7 Ramos C13(1.11)  LDD2186  [11]
 LDCM0571  Fragment9 Ramos C13(1.20)  LDD2188  [11]
 LDCM0167  HOIPIN 11a HEK-293T 3.19  LDD0423  [2]
 LDCM0022  KB02 HEK-293T C128(1.02); C13(0.79)  LDD1492  [10]
 LDCM0023  KB03 HEK-293T C128(0.94); C13(0.98)  LDD1497  [10]
 LDCM0024  KB05 G361 C13(2.70)  LDD3311  [12]

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
E3 ubiquitin-protein ligase pellino homolog 1 (PELI1) Pellino family Q96FA3
E3 ubiquitin-protein ligase pellino homolog 2 (PELI2) Pellino family Q9HAT8
Interleukin-1 receptor-associated kinase-like 2 (IRAK2) TKL Ser/Thr protein kinase family O43187
E3 ubiquitin-protein ligase TRIM7 (TRIM7) TRIM/RBCC family Q9C029
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Toll/interleukin-1 receptor domain-containing adapter protein (TIRAP) . P58753
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Zinc finger protein 597 (ZNF597) Krueppel C2H2-type zinc-finger protein family Q96LX8
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Interleukin-36 receptor antagonist protein (IL36RN) IL-1 family Q9UBH0
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Myeloid differentiation primary response protein MyD88 (MYD88) . Q99836

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
Investigative
Click To Hide/Show 12 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Isis 156449 Antisense drug D0B2EL
Isis 156451 Antisense drug D06DVW
Isis 156452 Antisense drug D02AMI
Isis 156453 Antisense drug D02JBK
Isis 156471 Antisense drug D0U9JR
Isis 156472 Antisense drug D0N4TF
Isis 156473 Antisense drug D06LVL
Isis 156474 Antisense drug D0B5OL
Isis 156475 Antisense drug D0F5SD
N-(1h-benzo[D]Imidazol-2-yl)-3-cyanobenzamide Small molecular drug D0LY5S
N-(1h-benzo[D]Imidazol-2-yl)-3-nitrobenzamide Small molecular drug D02JIL
1-(3-hydroxypropyl)-2-[(3-nitrobenzoyl)Amino]-1h-benzimidazol-5-yl Pivalate . DB08590

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 Fragment-Based Covalent Ligand Screening Enables Rapid Discovery of Inhibitors for the RBR E3 Ubiquitin Ligase HOIP. J Am Chem Soc. 2019 Feb 13;141(6):2703-2712. doi: 10.1021/jacs.8b13193. Epub 2019 Feb 4.
3 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
4 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
5 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.
6 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.
7 Direct Target Site Identification of a Sulfonyl-Triazole Covalent Kinase Probe by LC-MS Chemical Proteomics. Anal Chem. 2021 Sep 7;93(35):11946-11955. doi: 10.1021/acs.analchem.1c01591. Epub 2021 Aug 25.
8 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
9 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.
10 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
11 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
12 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