Details of the Target

General Information of Target

Target ID LDTP02232
Target Name Tyrosine-protein kinase Lyn (LYN)
Gene Name LYN
Gene ID 4067
Synonyms
JTK8; Tyrosine-protein kinase Lyn; EC 2.7.10.2; Lck/Yes-related novel protein tyrosine kinase; V-yes-1 Yamaguchi sarcoma viral related oncogene homolog; p53Lyn; p56Lyn
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MGCIKSKGKDSLSDDGVDLKTQPVRNTERTIYVRDPTSNKQQRPVPESQLLPGQRFQTKD
PEEQGDIVVALYPYDGIHPDDLSFKKGEKMKVLEEHGEWWKAKSLLTKKEGFIPSNYVAK
LNTLETEEWFFKDITRKDAERQLLAPGNSAGAFLIRESETLKGSFSLSVRDFDPVHGDVI
KHYKIRSLDNGGYYISPRITFPCISDMIKHYQKQADGLCRRLEKACISPKPQKPWDKDAW
EIPRESIKLVKRLGAGQFGEVWMGYYNNSTKVAVKTLKPGTMSVQAFLEEANLMKTLQHD
KLVRLYAVVTREEPIYIITEYMAKGSLLDFLKSDEGGKVLLPKLIDFSAQIAEGMAYIER
KNYIHRDLRAANVLVSESLMCKIADFGLARVIEDNEYTAREGAKFPIKWTAPEAINFGCF
TIKSDVWSFGILLYEIVTYGKIPYPGRTNADVMTALSQGYRMPRVENCPDELYDIMKMCW
KEKAEERPTFDYLQSVLDDFYTATEGQYQQQP
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Tyr protein kinase family, SRC subfamily
Subcellular location
Cell membrane
Function
Non-receptor tyrosine-protein kinase that transmits signals from cell surface receptors and plays an important role in the regulation of innate and adaptive immune responses, hematopoiesis, responses to growth factors and cytokines, integrin signaling, but also responses to DNA damage and genotoxic agents. Functions primarily as negative regulator, but can also function as activator, depending on the context. Required for the initiation of the B-cell response, but also for its down-regulation and termination. Plays an important role in the regulation of B-cell differentiation, proliferation, survival and apoptosis, and is important for immune self-tolerance. Acts downstream of several immune receptors, including the B-cell receptor, CD79A, CD79B, CD5, CD19, CD22, FCER1, FCGR2, FCGR1A, TLR2 and TLR4. Plays a role in the inflammatory response to bacterial lipopolysaccharide. Mediates the responses to cytokines and growth factors in hematopoietic progenitors, platelets, erythrocytes, and in mature myeloid cells, such as dendritic cells, neutrophils and eosinophils. Acts downstream of EPOR, KIT, MPL, the chemokine receptor CXCR4, as well as the receptors for IL3, IL5 and CSF2. Plays an important role in integrin signaling. Regulates cell proliferation, survival, differentiation, migration, adhesion, degranulation, and cytokine release. Involved in the regulation of endothelial activation, neutrophil adhesion and transendothelial migration. Down-regulates signaling pathways by phosphorylation of immunoreceptor tyrosine-based inhibitory motifs (ITIM), that then serve as binding sites for phosphatases, such as PTPN6/SHP-1, PTPN11/SHP-2 and INPP5D/SHIP-1, that modulate signaling by dephosphorylation of kinases and their substrates. Phosphorylates LIME1 in response to CD22 activation. Phosphorylates BTK, CBL, CD5, CD19, CD72, CD79A, CD79B, CSF2RB, DOK1, HCLS1, LILRB3/PIR-B, MS4A2/FCER1B, SYK and TEC. Promotes phosphorylation of SIRPA, PTPN6/SHP-1, PTPN11/SHP-2 and INPP5D/SHIP-1. Mediates phosphorylation of the BCR-ABL fusion protein. Required for rapid phosphorylation of FER in response to FCER1 activation. Mediates KIT phosphorylation. Acts as an effector of EPOR (erythropoietin receptor) in controlling KIT expression and may play a role in erythroid differentiation during the switch between proliferation and maturation. Depending on the context, activates or inhibits several signaling cascades. Regulates phosphatidylinositol 3-kinase activity and AKT1 activation. Regulates activation of the MAP kinase signaling cascade, including activation of MAP2K1/MEK1, MAPK1/ERK2, MAPK3/ERK1, MAPK8/JNK1 and MAPK9/JNK2. Mediates activation of STAT5A and/or STAT5B. Phosphorylates LPXN on 'Tyr-72'. Kinase activity facilitates TLR4-TLR6 heterodimerization and signal initiation. Phosphorylates SCIMP on 'Tyr-107'; this enhances binding of SCIMP to TLR4, promoting the phosphorylation of TLR4, and a selective cytokine response to lipopolysaccharide in macrophages. Phosphorylates CLNK. Phosphorylates BCAR1/CAS and NEDD9/HEF1.
TTD ID
T68163
Uniprot ID
P07948
DrugMap ID
TT1RWNJ
Ensemble ID
ENST00000519728.6
HGNC ID
HGNC:6735
ChEMBL ID
CHEMBL3905

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
KMS12BM Deletion: p.R25del DBIA    Probe Info 
LS180 SNV: p.F130V DBIA    Probe Info 
MFE319 SNV: p.K271N DBIA    Probe Info 
NCIH1155 SNV: p.V118M DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 16 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		12.31  LDD0402  [1]
Probe 1
 Probe Info  		Y397(14.85)  LDD3495  [2]
Dasatinib-CA-4PAP
 Probe Info  		27.67  LDD0270  [3]
BTD
 Probe Info  		C226(0.65)  LDD2099  [4]
DBIA
 Probe Info  		C419(1.00); C203(1.70)  LDD0080  [5]
IA-alkyne
 Probe Info  		C381(0.00); C219(0.00); C226(0.00); C203(0.00)  LDD0162  [6]
WYneN
 Probe Info  		C219(0.00); C203(0.00)  LDD0021  [7]
IPM
 Probe Info  		N.A.  LDD0005  [7]
PF-06672131
 Probe Info  		N.A.  LDD0152  [8]
SF
 Probe Info  		N.A.  LDD0028  [9]
TFBX
 Probe Info  		N.A.  LDD0148  [10]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [11]
Acrolein
 Probe Info  		N.A.  LDD0217  [12]
W1
 Probe Info  		N.A.  LDD0236  [13]
AOyne
 Probe Info  		8.70  LDD0443  [14]
NAIA_5
 Probe Info  		N.A.  LDD2223  [15]
PAL-AfBPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe11
 Probe Info  		8.15  LDD0472  [16]
FFF probe3
 Probe Info  		12.16  LDD0465  [16]
STS-2
 Probe Info  		N.A.  LDD0139  [17]
VE-P
 Probe Info  		N.A.  LDD0396  [18]
Dasatinib-CA-3PAP
 Probe Info  		N.A.  LDD0365  [3]
DA-2
 Probe Info  		N.A.  LDD0072  [19]

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 C226(0.57)  LDD2117  [4]
 LDCM0214  AC1 HCT 116 C203(1.23)  LDD0531  [5]
 LDCM0215  AC10 HCT 116 C203(1.50)  LDD0532  [5]
 LDCM0216  AC100 HCT 116 C203(0.99)  LDD0533  [5]
 LDCM0217  AC101 HCT 116 C203(1.03)  LDD0534  [5]
 LDCM0218  AC102 HCT 116 C203(1.06)  LDD0535  [5]
 LDCM0219  AC103 HCT 116 C203(1.35)  LDD0536  [5]
 LDCM0220  AC104 HCT 116 C203(1.20)  LDD0537  [5]
 LDCM0221  AC105 HCT 116 C203(1.24)  LDD0538  [5]
 LDCM0222  AC106 HCT 116 C203(1.25)  LDD0539  [5]
 LDCM0223  AC107 HCT 116 C203(1.34)  LDD0540  [5]
 LDCM0224  AC108 HCT 116 C203(0.82)  LDD0541  [5]
 LDCM0225  AC109 HCT 116 C203(0.83)  LDD0542  [5]
 LDCM0226  AC11 HCT 116 C203(1.27)  LDD0543  [5]
 LDCM0227  AC110 HCT 116 C203(0.79)  LDD0544  [5]
 LDCM0228  AC111 HCT 116 C203(0.80)  LDD0545  [5]
 LDCM0229  AC112 HCT 116 C203(1.03)  LDD0546  [5]
 LDCM0230  AC113 HCT 116 C203(1.05)  LDD0547  [5]
 LDCM0231  AC114 HCT 116 C203(1.04)  LDD0548  [5]
 LDCM0232  AC115 HCT 116 C203(1.20)  LDD0549  [5]
 LDCM0233  AC116 HCT 116 C203(1.34)  LDD0550  [5]
 LDCM0234  AC117 HCT 116 C203(1.09)  LDD0551  [5]
 LDCM0235  AC118 HCT 116 C203(1.05)  LDD0552  [5]
 LDCM0236  AC119 HCT 116 C203(1.27)  LDD0553  [5]
 LDCM0237  AC12 HCT 116 C203(1.19)  LDD0554  [5]
 LDCM0238  AC120 HCT 116 C203(1.17)  LDD0555  [5]
 LDCM0239  AC121 HCT 116 C203(0.99)  LDD0556  [5]
 LDCM0240  AC122 HCT 116 C203(1.16)  LDD0557  [5]
 LDCM0241  AC123 HCT 116 C203(1.01)  LDD0558  [5]
 LDCM0242  AC124 HCT 116 C203(1.01)  LDD0559  [5]
 LDCM0243  AC125 HCT 116 C203(1.07)  LDD0560  [5]
 LDCM0244  AC126 HCT 116 C203(1.24)  LDD0561  [5]
 LDCM0245  AC127 HCT 116 C203(1.23)  LDD0562  [5]
 LDCM0246  AC128 HEK-293T C203(0.87)  LDD0844  [5]
 LDCM0247  AC129 HEK-293T C203(1.20)  LDD0845  [5]
 LDCM0249  AC130 HEK-293T C203(1.21)  LDD0847  [5]
 LDCM0250  AC131 HEK-293T C203(1.13)  LDD0848  [5]
 LDCM0251  AC132 HEK-293T C203(1.27)  LDD0849  [5]
 LDCM0252  AC133 HEK-293T C203(1.33)  LDD0850  [5]
 LDCM0253  AC134 HEK-293T C203(1.47)  LDD0851  [5]
 LDCM0254  AC135 HEK-293T C203(1.32)  LDD0852  [5]
 LDCM0255  AC136 HEK-293T C203(1.35)  LDD0853  [5]
 LDCM0256  AC137 HEK-293T C203(1.29)  LDD0854  [5]
 LDCM0257  AC138 HEK-293T C203(1.40)  LDD0855  [5]
 LDCM0258  AC139 HEK-293T C203(1.32)  LDD0856  [5]
 LDCM0259  AC14 HCT 116 C203(1.23)  LDD0576  [5]
 LDCM0260  AC140 HEK-293T C203(1.32)  LDD0858  [5]
 LDCM0261  AC141 HEK-293T C203(1.59)  LDD0859  [5]
 LDCM0262  AC142 HEK-293T C203(1.51)  LDD0860  [5]
 LDCM0263  AC143 HCT 116 C203(1.03)  LDD0580  [5]
 LDCM0264  AC144 HCT 116 C203(1.03)  LDD0581  [5]
 LDCM0265  AC145 HCT 116 C203(0.85)  LDD0582  [5]
 LDCM0266  AC146 HCT 116 C203(0.86)  LDD0583  [5]
 LDCM0267  AC147 HCT 116 C203(1.05)  LDD0584  [5]
 LDCM0268  AC148 HCT 116 C203(0.77)  LDD0585  [5]
 LDCM0269  AC149 HCT 116 C203(0.76)  LDD0586  [5]
 LDCM0270  AC15 HCT 116 C203(1.48)  LDD0587  [5]
 LDCM0271  AC150 HCT 116 C203(1.01)  LDD0588  [5]
 LDCM0272  AC151 HCT 116 C203(1.00)  LDD0589  [5]
 LDCM0273  AC152 HCT 116 C203(1.02)  LDD0590  [5]
 LDCM0274  AC153 HCT 116 C203(0.82)  LDD0591  [5]
 LDCM0621  AC154 HCT 116 C203(0.82)  LDD2158  [5]
 LDCM0622  AC155 HCT 116 C203(0.95)  LDD2159  [5]
 LDCM0623  AC156 HCT 116 C203(1.07)  LDD2160  [5]
 LDCM0624  AC157 HCT 116 C203(0.97)  LDD2161  [5]
 LDCM0276  AC17 HCT 116 C203(1.03)  LDD0593  [5]
 LDCM0277  AC18 HCT 116 C203(1.73)  LDD0594  [5]
 LDCM0278  AC19 HCT 116 C203(1.10)  LDD0595  [5]
 LDCM0279  AC2 HCT 116 C203(1.21)  LDD0596  [5]
 LDCM0280  AC20 HCT 116 C203(1.00)  LDD0597  [5]
 LDCM0281  AC21 HCT 116 C203(1.07)  LDD0598  [5]
 LDCM0282  AC22 HCT 116 C203(0.90)  LDD0599  [5]
 LDCM0283  AC23 HCT 116 C203(0.96)  LDD0600  [5]
 LDCM0284  AC24 HCT 116 C203(0.93)  LDD0601  [5]
 LDCM0285  AC25 HCT 116 C203(1.07)  LDD0602  [5]
 LDCM0286  AC26 HCT 116 C203(1.14)  LDD0603  [5]
 LDCM0287  AC27 HCT 116 C203(1.15)  LDD0604  [5]
 LDCM0288  AC28 HCT 116 C203(1.12)  LDD0605  [5]
 LDCM0289  AC29 HCT 116 C203(1.13)  LDD0606  [5]
 LDCM0290  AC3 HCT 116 C203(1.12)  LDD0607  [5]
 LDCM0291  AC30 HCT 116 C203(1.16)  LDD0608  [5]
 LDCM0292  AC31 HCT 116 C203(1.11)  LDD0609  [5]
 LDCM0293  AC32 HCT 116 C203(1.37)  LDD0610  [5]
 LDCM0294  AC33 HCT 116 C203(1.15)  LDD0611  [5]
 LDCM0295  AC34 HCT 116 C203(1.31)  LDD0612  [5]
 LDCM0296  AC35 HCT 116 C203(1.01)  LDD0613  [5]
 LDCM0297  AC36 HCT 116 C203(1.20)  LDD0614  [5]
 LDCM0298  AC37 HCT 116 C203(1.02)  LDD0615  [5]
 LDCM0299  AC38 HCT 116 C203(1.10)  LDD0616  [5]
 LDCM0300  AC39 HCT 116 C203(1.19)  LDD0617  [5]
 LDCM0301  AC4 HCT 116 C203(1.26)  LDD0618  [5]
 LDCM0302  AC40 HCT 116 C203(1.39)  LDD0619  [5]
 LDCM0303  AC41 HCT 116 C203(1.23)  LDD0620  [5]
 LDCM0304  AC42 HCT 116 C203(1.19)  LDD0621  [5]
 LDCM0305  AC43 HCT 116 C203(1.19)  LDD0622  [5]
 LDCM0306  AC44 HCT 116 C203(1.37)  LDD0623  [5]
 LDCM0307  AC45 HCT 116 C203(1.44)  LDD0624  [5]
 LDCM0308  AC46 HCT 116 C203(1.28)  LDD0625  [5]
 LDCM0309  AC47 HCT 116 C203(1.07)  LDD0626  [5]
 LDCM0310  AC48 HCT 116 C203(1.28)  LDD0627  [5]
 LDCM0311  AC49 HCT 116 C203(1.35)  LDD0628  [5]
 LDCM0312  AC5 HCT 116 C203(1.33)  LDD0629  [5]
 LDCM0313  AC50 HCT 116 C203(1.27)  LDD0630  [5]
 LDCM0314  AC51 HCT 116 C203(1.25)  LDD0631  [5]
 LDCM0315  AC52 HCT 116 C203(1.23)  LDD0632  [5]
 LDCM0316  AC53 HCT 116 C203(1.07)  LDD0633  [5]
 LDCM0317  AC54 HCT 116 C203(1.19)  LDD0634  [5]
 LDCM0318  AC55 HCT 116 C203(0.95)  LDD0635  [5]
 LDCM0319  AC56 HCT 116 C203(1.30)  LDD0636  [5]
 LDCM0320  AC57 HCT 116 C203(0.79)  LDD0637  [5]
 LDCM0321  AC58 HCT 116 C203(1.15)  LDD0638  [5]
 LDCM0322  AC59 HCT 116 C203(1.05)  LDD0639  [5]
 LDCM0323  AC6 HCT 116 C203(1.13)  LDD0640  [5]
 LDCM0324  AC60 HCT 116 C203(1.40)  LDD0641  [5]
 LDCM0325  AC61 HCT 116 C203(0.61)  LDD0642  [5]
 LDCM0326  AC62 HCT 116 C203(1.15)  LDD0643  [5]
 LDCM0327  AC63 HCT 116 C203(1.32)  LDD0644  [5]
 LDCM0328  AC64 HCT 116 C203(1.10)  LDD0645  [5]
 LDCM0329  AC65 HCT 116 C203(0.87)  LDD0646  [5]
 LDCM0330  AC66 HCT 116 C203(1.22)  LDD0647  [5]
 LDCM0331  AC67 HCT 116 C203(1.14)  LDD0648  [5]
 LDCM0332  AC68 PaTu 8988t C203(0.99)  LDD1211  [5]
 LDCM0333  AC69 PaTu 8988t C203(1.01)  LDD1212  [5]
 LDCM0334  AC7 HCT 116 C203(1.07)  LDD0651  [5]
 LDCM0335  AC70 PaTu 8988t C203(0.95)  LDD1214  [5]
 LDCM0336  AC71 PaTu 8988t C203(0.96)  LDD1215  [5]
 LDCM0337  AC72 PaTu 8988t C203(0.86)  LDD1216  [5]
 LDCM0338  AC73 PaTu 8988t C203(0.87)  LDD1217  [5]
 LDCM0339  AC74 PaTu 8988t C203(0.93)  LDD1218  [5]
 LDCM0340  AC75 PaTu 8988t C203(1.03)  LDD1219  [5]
 LDCM0341  AC76 PaTu 8988t C203(0.96)  LDD1220  [5]
 LDCM0342  AC77 PaTu 8988t C203(1.02)  LDD1221  [5]
 LDCM0343  AC78 PaTu 8988t C203(0.99)  LDD1222  [5]
 LDCM0344  AC79 PaTu 8988t C203(1.02)  LDD1223  [5]
 LDCM0345  AC8 HCT 116 C203(1.44)  LDD0662  [5]
 LDCM0346  AC80 PaTu 8988t C203(0.95)  LDD1225  [5]
 LDCM0347  AC81 PaTu 8988t C203(0.90)  LDD1226  [5]
 LDCM0348  AC82 PaTu 8988t C203(0.93)  LDD1227  [5]
 LDCM0349  AC83 HEK-293T C203(1.06)  LDD0947  [5]
 LDCM0350  AC84 HEK-293T C203(1.37)  LDD0948  [5]
 LDCM0351  AC85 HEK-293T C203(1.27)  LDD0949  [5]
 LDCM0352  AC86 HEK-293T C203(1.48)  LDD0950  [5]
 LDCM0353  AC87 HEK-293T C203(1.63)  LDD0951  [5]
 LDCM0354  AC88 HEK-293T C203(1.21)  LDD0952  [5]
 LDCM0355  AC89 HEK-293T C203(1.45)  LDD0953  [5]
 LDCM0357  AC90 HEK-293T C203(1.35)  LDD0955  [5]
 LDCM0358  AC91 HEK-293T C203(1.10)  LDD0956  [5]
 LDCM0359  AC92 HEK-293T C203(1.07)  LDD0957  [5]
 LDCM0360  AC93 HEK-293T C203(0.84)  LDD0958  [5]
 LDCM0361  AC94 HEK-293T C203(1.46)  LDD0959  [5]
 LDCM0362  AC95 HEK-293T C203(1.39)  LDD0960  [5]
 LDCM0363  AC96 HEK-293T C203(1.64)  LDD0961  [5]
 LDCM0364  AC97 HEK-293T C203(1.46)  LDD0962  [5]
 LDCM0365  AC98 HCT 116 C203(1.65)  LDD0682  [5]
 LDCM0366  AC99 HCT 116 C203(0.94)  LDD0683  [5]
 LDCM0248  AKOS034007472 HCT 116 C203(1.09)  LDD0565  [5]
 LDCM0356  AKOS034007680 HCT 116 C203(1.24)  LDD0673  [5]
 LDCM0275  AKOS034007705 HCT 116 C203(1.92)  LDD0592  [5]
 LDCM0020  ARS-1620 HCC44 C419(1.23)  LDD2171  [5]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [12]
 LDCM0367  CL1 HCT 116 C203(0.96)  LDD0684  [5]
 LDCM0368  CL10 HCT 116 C203(1.23)  LDD0685  [5]
 LDCM0369  CL100 HCT 116 C203(1.38)  LDD0686  [5]
 LDCM0370  CL101 HCT 116 C203(1.38)  LDD0687  [5]
 LDCM0371  CL102 HCT 116 C203(0.95)  LDD0688  [5]
 LDCM0372  CL103 HCT 116 C203(1.20)  LDD0689  [5]
 LDCM0373  CL104 HCT 116 C203(1.21)  LDD0690  [5]
 LDCM0374  CL105 HCT 116 C203(1.37)  LDD0691  [5]
 LDCM0375  CL106 HCT 116 C203(1.85)  LDD0692  [5]
 LDCM0376  CL107 HCT 116 C203(1.49)  LDD0693  [5]
 LDCM0377  CL108 HCT 116 C203(1.69)  LDD0694  [5]
 LDCM0378  CL109 HCT 116 C203(1.27)  LDD0695  [5]
 LDCM0379  CL11 HCT 116 C203(1.47)  LDD0696  [5]
 LDCM0380  CL110 HCT 116 C203(1.49)  LDD0697  [5]
 LDCM0381  CL111 HCT 116 C203(1.15)  LDD0698  [5]
 LDCM0382  CL112 HCT 116 C203(1.09)  LDD0699  [5]
 LDCM0383  CL113 HCT 116 C203(1.21)  LDD0700  [5]
 LDCM0384  CL114 HCT 116 C203(1.14)  LDD0701  [5]
 LDCM0385  CL115 HCT 116 C203(1.19)  LDD0702  [5]
 LDCM0386  CL116 HCT 116 C203(1.15)  LDD0703  [5]
 LDCM0387  CL117 HCT 116 C203(1.64)  LDD0704  [5]
 LDCM0388  CL118 HCT 116 C203(1.29)  LDD0705  [5]
 LDCM0389  CL119 HCT 116 C203(1.30)  LDD0706  [5]
 LDCM0390  CL12 HCT 116 C203(1.30)  LDD0707  [5]
 LDCM0391  CL120 HCT 116 C203(1.24)  LDD0708  [5]
 LDCM0392  CL121 HCT 116 C203(1.15)  LDD0709  [5]
 LDCM0393  CL122 HCT 116 C203(1.21)  LDD0710  [5]
 LDCM0394  CL123 HCT 116 C203(0.98)  LDD0711  [5]
 LDCM0395  CL124 HCT 116 C203(1.17)  LDD0712  [5]
 LDCM0396  CL125 HCT 116 C203(1.14)  LDD0713  [5]
 LDCM0397  CL126 HCT 116 C203(1.31)  LDD0714  [5]
 LDCM0398  CL127 HCT 116 C203(1.32)  LDD0715  [5]
 LDCM0399  CL128 HCT 116 C203(1.01)  LDD0716  [5]
 LDCM0400  CL13 HCT 116 C203(1.16)  LDD0717  [5]
 LDCM0401  CL14 HCT 116 C203(1.03)  LDD0718  [5]
 LDCM0402  CL15 HCT 116 C203(1.12)  LDD0719  [5]
 LDCM0403  CL16 HCT 116 C203(1.00)  LDD0720  [5]
 LDCM0404  CL17 HCT 116 C203(1.07)  LDD0721  [5]
 LDCM0405  CL18 HCT 116 C203(1.13)  LDD0722  [5]
 LDCM0406  CL19 HCT 116 C203(1.07)  LDD0723  [5]
 LDCM0407  CL2 HCT 116 C203(1.00)  LDD0724  [5]
 LDCM0408  CL20 HCT 116 C203(1.20)  LDD0725  [5]
 LDCM0409  CL21 HCT 116 C203(1.76)  LDD0726  [5]
 LDCM0410  CL22 HCT 116 C203(1.66)  LDD0727  [5]
 LDCM0411  CL23 HCT 116 C203(1.09)  LDD0728  [5]
 LDCM0412  CL24 HCT 116 C203(1.38)  LDD0729  [5]
 LDCM0413  CL25 HCT 116 C203(2.32)  LDD0730  [5]
 LDCM0414  CL26 HCT 116 C203(1.08)  LDD0731  [5]
 LDCM0415  CL27 HCT 116 C203(1.09)  LDD0732  [5]
 LDCM0416  CL28 HCT 116 C203(1.20)  LDD0733  [5]
 LDCM0417  CL29 HCT 116 C203(1.18)  LDD0734  [5]
 LDCM0418  CL3 HCT 116 C203(0.97)  LDD0735  [5]
 LDCM0419  CL30 HCT 116 C203(1.01)  LDD0736  [5]
 LDCM0420  CL31 HCT 116 C203(1.15)  LDD0737  [5]
 LDCM0421  CL32 HCT 116 C203(1.12)  LDD0738  [5]
 LDCM0422  CL33 HCT 116 C203(1.05)  LDD0739  [5]
 LDCM0423  CL34 HCT 116 C203(1.27)  LDD0740  [5]
 LDCM0424  CL35 HCT 116 C203(1.18)  LDD0741  [5]
 LDCM0425  CL36 HCT 116 C203(1.13)  LDD0742  [5]
 LDCM0426  CL37 HCT 116 C203(1.27)  LDD0743  [5]
 LDCM0428  CL39 HCT 116 C203(1.22)  LDD0745  [5]
 LDCM0429  CL4 HCT 116 C203(1.02)  LDD0746  [5]
 LDCM0430  CL40 HCT 116 C203(1.16)  LDD0747  [5]
 LDCM0431  CL41 HCT 116 C203(1.14)  LDD0748  [5]
 LDCM0432  CL42 HCT 116 C203(1.44)  LDD0749  [5]
 LDCM0433  CL43 HCT 116 C203(1.28)  LDD0750  [5]
 LDCM0434  CL44 HCT 116 C203(1.32)  LDD0751  [5]
 LDCM0435  CL45 HCT 116 C203(1.31)  LDD0752  [5]
 LDCM0436  CL46 HCT 116 C203(0.80)  LDD0753  [5]
 LDCM0437  CL47 HCT 116 C203(0.73)  LDD0754  [5]
 LDCM0438  CL48 HCT 116 C203(0.74)  LDD0755  [5]
 LDCM0439  CL49 HCT 116 C203(0.82)  LDD0756  [5]
 LDCM0440  CL5 HCT 116 C203(0.97)  LDD0757  [5]
 LDCM0441  CL50 HCT 116 C203(0.82)  LDD0758  [5]
 LDCM0442  CL51 HCT 116 C203(0.75)  LDD0759  [5]
 LDCM0443  CL52 HCT 116 C203(0.81)  LDD0760  [5]
 LDCM0444  CL53 HCT 116 C203(0.74)  LDD0761  [5]
 LDCM0445  CL54 HCT 116 C203(0.72)  LDD0762  [5]
 LDCM0446  CL55 HCT 116 C203(0.72)  LDD0763  [5]
 LDCM0447  CL56 HCT 116 C203(0.90)  LDD0764  [5]
 LDCM0448  CL57 HCT 116 C203(0.82)  LDD0765  [5]
 LDCM0449  CL58 HCT 116 C203(0.77)  LDD0766  [5]
 LDCM0450  CL59 HCT 116 C203(0.87)  LDD0767  [5]
 LDCM0451  CL6 HCT 116 C203(1.14)  LDD0768  [5]
 LDCM0452  CL60 HCT 116 C203(0.85)  LDD0769  [5]
 LDCM0453  CL61 HCT 116 C203(1.06)  LDD0770  [5]
 LDCM0454  CL62 HCT 116 C203(1.11)  LDD0771  [5]
 LDCM0455  CL63 HCT 116 C203(1.13)  LDD0772  [5]
 LDCM0456  CL64 HCT 116 C203(1.25)  LDD0773  [5]
 LDCM0457  CL65 HCT 116 C203(1.07)  LDD0774  [5]
 LDCM0458  CL66 HCT 116 C203(1.36)  LDD0775  [5]
 LDCM0459  CL67 HCT 116 C203(1.12)  LDD0776  [5]
 LDCM0460  CL68 HCT 116 C203(1.17)  LDD0777  [5]
 LDCM0461  CL69 HCT 116 C203(1.05)  LDD0778  [5]
 LDCM0462  CL7 HCT 116 C203(1.21)  LDD0779  [5]
 LDCM0463  CL70 HCT 116 C203(1.06)  LDD0780  [5]
 LDCM0464  CL71 HCT 116 C203(1.20)  LDD0781  [5]
 LDCM0465  CL72 HCT 116 C203(1.09)  LDD0782  [5]
 LDCM0466  CL73 HCT 116 C203(1.10)  LDD0783  [5]
 LDCM0467  CL74 HCT 116 C203(1.07)  LDD0784  [5]
 LDCM0469  CL76 HCT 116 C203(1.12)  LDD0786  [5]
 LDCM0470  CL77 HCT 116 C203(1.09)  LDD0787  [5]
 LDCM0471  CL78 HCT 116 C203(1.14)  LDD0788  [5]
 LDCM0472  CL79 HCT 116 C203(1.32)  LDD0789  [5]
 LDCM0473  CL8 HCT 116 C203(1.44)  LDD0790  [5]
 LDCM0474  CL80 HCT 116 C203(1.10)  LDD0791  [5]
 LDCM0475  CL81 HCT 116 C203(1.14)  LDD0792  [5]
 LDCM0476  CL82 HCT 116 C203(1.55)  LDD0793  [5]
 LDCM0477  CL83 HCT 116 C203(1.51)  LDD0794  [5]
 LDCM0478  CL84 HCT 116 C203(1.86)  LDD0795  [5]
 LDCM0479  CL85 HCT 116 C203(1.22)  LDD0796  [5]
 LDCM0480  CL86 HCT 116 C203(1.15)  LDD0797  [5]
 LDCM0481  CL87 HCT 116 C203(1.28)  LDD0798  [5]
 LDCM0482  CL88 HCT 116 C203(1.47)  LDD0799  [5]
 LDCM0483  CL89 HCT 116 C203(2.03)  LDD0800  [5]
 LDCM0484  CL9 HCT 116 C203(1.11)  LDD0801  [5]
 LDCM0485  CL90 HCT 116 C203(1.06)  LDD0802  [5]
 LDCM0486  CL91 HCT 116 C203(1.14)  LDD0803  [5]
 LDCM0487  CL92 HCT 116 C203(1.13)  LDD0804  [5]
 LDCM0488  CL93 HCT 116 C203(1.08)  LDD0805  [5]
 LDCM0489  CL94 HCT 116 C203(1.40)  LDD0806  [5]
 LDCM0490  CL95 HCT 116 C203(1.51)  LDD0807  [5]
 LDCM0491  CL96 HCT 116 C203(1.17)  LDD0808  [5]
 LDCM0492  CL97 HCT 116 C203(1.22)  LDD0809  [5]
 LDCM0493  CL98 HCT 116 C203(1.35)  LDD0810  [5]
 LDCM0494  CL99 HCT 116 C203(1.27)  LDD0811  [5]
 LDCM0097  Dasatinib K562 27.67  LDD0270  [3]
 LDCM0495  E2913 HEK-293T C219(1.09); C381(0.91); C203(1.03); C419(0.87)  LDD1698  [20]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C226(2.00)  LDD1702  [4]
 LDCM0625  F8 Ramos C468(0.89); C381(0.70); C203(0.32); C419(0.58)  LDD2187  [21]
 LDCM0572  Fragment10 Ramos C468(1.11); C381(1.00); C203(1.63)  LDD2189  [21]
 LDCM0573  Fragment11 Ramos C468(1.12); C381(0.18); C203(0.10); C419(5.69)  LDD2190  [21]
 LDCM0574  Fragment12 Ramos C468(1.85); C381(1.55); C203(0.99); C419(0.72)  LDD2191  [21]
 LDCM0575  Fragment13 Ramos C468(0.89); C381(1.26); C203(1.01)  LDD2192  [21]
 LDCM0576  Fragment14 Ramos C468(0.86); C381(1.39); C203(0.83); C419(0.67)  LDD2193  [21]
 LDCM0579  Fragment20 Ramos C468(2.39); C381(1.70); C203(0.74)  LDD2194  [21]
 LDCM0580  Fragment21 Ramos C468(0.88); C381(0.92); C203(0.84); C419(0.78)  LDD2195  [21]
 LDCM0582  Fragment23 Ramos C468(1.93); C381(1.46); C203(0.59)  LDD2196  [21]
 LDCM0578  Fragment27 Ramos C468(0.82); C381(1.23); C203(0.90)  LDD2197  [21]
 LDCM0586  Fragment28 Ramos C468(0.42); C381(1.08); C203(0.36)  LDD2198  [21]
 LDCM0588  Fragment30 Ramos C468(1.08); C381(0.67); C203(0.82); C419(1.14)  LDD2199  [21]
 LDCM0589  Fragment31 Ramos C468(0.93); C381(1.45); C203(1.08)  LDD2200  [21]
 LDCM0590  Fragment32 Ramos C468(1.65); C381(0.90); C203(6.09)  LDD2201  [21]
 LDCM0468  Fragment33 HCT 116 C203(1.10)  LDD0785  [5]
 LDCM0596  Fragment38 Ramos C468(0.94); C381(0.82); C203(0.39)  LDD2203  [21]
 LDCM0566  Fragment4 Ramos C468(1.68); C381(1.27); C203(0.59); C419(0.91)  LDD2184  [21]
 LDCM0427  Fragment51 HCT 116 C203(1.32)  LDD0744  [5]
 LDCM0610  Fragment52 Ramos C468(1.24); C381(1.28); C203(1.05); C419(1.07)  LDD2204  [21]
 LDCM0614  Fragment56 Ramos C468(1.05); C381(0.78); C203(1.71); C419(0.73)  LDD2205  [21]
 LDCM0569  Fragment7 Ramos C468(1.44); C381(1.12); C203(1.48); C419(0.41)  LDD2186  [21]
 LDCM0571  Fragment9 Ramos C468(2.30); C381(0.96); C203(0.54)  LDD2188  [21]
 LDCM0022  KB02 HCT 116 C419(1.00); C203(1.70)  LDD0080  [5]
 LDCM0023  KB03 HCT 116 C419(0.83); C203(1.03)  LDD0081  [5]
 LDCM0024  KB05 HCT 116 C419(1.06); C203(1.02)  LDD0082  [5]
 LDCM0109  NEM HeLa N.A.  LDD0229  [12]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C226(0.65)  LDD2099  [4]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C226(1.41)  LDD2100  [4]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C226(0.54); C219(0.90)  LDD2109  [4]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C219(1.05)  LDD2127  [4]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C219(1.31)  LDD2136  [4]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C226(0.71)  LDD2140  [4]
 LDCM0628  OTUB2-COV-1 HEK-293T C468(1.50)  LDD2207  [22]
 LDCM0021  THZ1 HCT 116 C419(1.23)  LDD2173  [5]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
DNA replication licensing factor MCM7 (MCM7) MCM family P33993
MAP/microtubule affinity-regulating kinase 4 (MARK4) CAMK Ser/Thr protein kinase family Q96L34
Hepatocyte growth factor receptor (MET) Tyr protein kinase family P08581
Mast/stem cell growth factor receptor Kit (KIT) Tyr protein kinase family P10721
Epidermal growth factor receptor (EGFR) Tyr protein kinase family P00533
Proto-oncogene tyrosine-protein kinase Src (SRC) Tyr protein kinase family P12931
Disintegrin and metalloproteinase domain-containing protein 12 (ADAM12) . O43184
Disintegrin and metalloproteinase domain-containing protein 15 (ADAM15) . Q13444
Transporter and channel
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid-beta precursor protein (APP) APP family P05067
Platelet glycoprotein 4 (CD36) CD36 family P16671
Heat shock protein HSP 90-beta (HSP90AB1) Heat shock protein 90 family P08238
Integrin beta-1 (ITGB1) Integrin beta chain family P05556
Alpha-synuclein (SNCA) Synuclein family P37840
Small ribosomal subunit protein RACK1 (RACK1) WD repeat G protein beta family P63244
Prosaposin (PSAP) . P07602
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Androgen receptor (AR) Nuclear hormone receptor family P10275
Immunoglobulin
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Brevican core protein (BCAN) Aggrecan/versican proteoglycan family Q96GW7
B-cell receptor CD22 (CD22) SIGLEC (sialic acid binding Ig-like lectin) family P20273
Platelet glycoprotein VI (GP6) . Q9HCN6
Other
Click To Hide/Show 11 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Signal transducer CD24 (CD24) CD24 family P25063
Cyclin-dependent kinase inhibitor 1B (CDKN1B) CDI family P46527
GRB2-associated-binding protein 1 (GAB1) GAB family Q13480
Alpha-2-macroglobulin (A2M) Protease inhibitor I39 (alpha-2-macroglobulin) family P01023
Leukocyte antigen CD37 (CD37) Tetraspanin (TM4SF) family P11049
B-cell scaffold protein with ankyrin repeats (BANK1) . Q8NDB2
Endoplasmic reticulum resident protein 44 (ERP44) . Q9BS26
Methyl-CpG-binding protein 2 (MECP2) . P51608
Phosphoprotein associated with glycosphingolipid-enriched microdomains 1 (PAG1) . Q9NWQ8
SLP adapter and CSK-interacting membrane protein (SCIMP) . Q6UWF3
Sprouty-related, EVH1 domain-containing protein 1 (SPRED1) . Q7Z699

The Drug(s) Related To This Target

Approved
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bosutinib Small molecular drug DB06616
Dasatinib Small molecular drug DB01254
Fostamatinib Small molecular drug DB12010
Nintedanib Small molecular drug DB09079
Ponatinib Small molecular drug DB08901
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bafetinib Small molecular drug D0G0VV
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Jnj-26483327 . D0U3XL
Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ng-25 Small molecular drug D0X7IC
Pmid17600705c23 Small molecular drug D04TLI
1-tert-butyl-3-(4-chloro-phenyl)-1h-pyrazolo[34-d]Pyrimidin-4-ylamine . DB03023
Patented
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Alkynyl-substituted Pyrimidinyl-pyrrole Derivative 1 Small molecular drug D0JZ2B

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 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 Streamlined Target Deconvolution Approach Utilizing a Single Photoreactive Chloroalkane Capture Tag. ACS Chem Biol. 2021 Feb 19;16(2):404-413. doi: 10.1021/acschembio.0c00987. Epub 2021 Feb 5.
4 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
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 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
7 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
8 Site-Specific Activity-Based Protein Profiling Using Phosphonate Handles. Mol Cell Proteomics. 2023 Jan;22(1):100455. doi: 10.1016/j.mcpro.2022.100455. Epub 2022 Nov 24.
Mass spectrometry data entry: PXD036569
9 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
10 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
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 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.
13 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.
14 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.
15 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
16 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
17 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.
18 Pharmacological Targeting of Vacuolar H(+)-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Nov 19;27(11):1359-1370.e8. doi: 10.1016/j.chembiol.2020.06.011. Epub 2020 Jul 9.
19 Cell-based proteome profiling of potential dasatinib targets by use of affinity-based probes. J Am Chem Soc. 2012 Feb 15;134(6):3001-14. doi: 10.1021/ja208518u. Epub 2012 Feb 1.
20 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
21 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
22 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.