General Information of Target

Target ID LDTP04048
Target Name Tyrosine-protein kinase SYK (SYK)
Gene Name SYK
Gene ID 6850
Synonyms
Tyrosine-protein kinase SYK; EC 2.7.10.2; Spleen tyrosine kinase; p72-Syk
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MASSGMADSANHLPFFFGNITREEAEDYLVQGGMSDGLYLLRQSRNYLGGFALSVAHGRK
AHHYTIERELNGTYAIAGGRTHASPADLCHYHSQESDGLVCLLKKPFNRPQGVQPKTGPF
EDLKENLIREYVKQTWNLQGQALEQAIISQKPQLEKLIATTAHEKMPWFHGKISREESEQ
IVLIGSKTNGKFLIRARDNNGSYALCLLHEGKVLHYRIDKDKTGKLSIPEGKKFDTLWQL
VEHYSYKADGLLRVLTVPCQKIGTQGNVNFGGRPQLPGSHPATWSAGGIISRIKSYSFPK
PGHRKSSPAQGNRQESTVSFNPYEPELAPWAADKGPQREALPMDTEVYESPYADPEEIRP
KEVYLDRKLLTLEDKELGSGNFGTVKKGYYQMKKVVKTVAVKILKNEANDPALKDELLAE
ANVMQQLDNPYIVRMIGICEAESWMLVMEMAELGPLNKYLQQNRHVKDKNIIELVHQVSM
GMKYLEESNFVHRDLAARNVLLVTQHYAKISDFGLSKALRADENYYKAQTHGKWPVKWYA
PECINYYKFSSKSDVWSFGVLMWEAFSYGQKPYRGMKGSEVTAMLEKGERMGCPAGCPRE
MYDLMNLCWTYDVENRPGFAAVELRLRNYYYDVVN
Target Type
Successful
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Tyr protein kinase family, SYK/ZAP-70 subfamily
Subcellular location
Cell membrane
Function
Non-receptor tyrosine kinase which mediates signal transduction downstream of a variety of transmembrane receptors including classical immunoreceptors like the B-cell receptor (BCR). Regulates several biological processes including innate and adaptive immunity, cell adhesion, osteoclast maturation, platelet activation and vascular development. Assembles into signaling complexes with activated receptors at the plasma membrane via interaction between its SH2 domains and the receptor tyrosine-phosphorylated ITAM domains. The association with the receptor can also be indirect and mediated by adapter proteins containing ITAM or partial hemITAM domains. The phosphorylation of the ITAM domains is generally mediated by SRC subfamily kinases upon engagement of the receptor. More rarely signal transduction via SYK could be ITAM-independent. Direct downstream effectors phosphorylated by SYK include DEPTOR, VAV1, PLCG1, PI-3-kinase, LCP2 and BLNK. Initially identified as essential in B-cell receptor (BCR) signaling, it is necessary for the maturation of B-cells most probably at the pro-B to pre-B transition. Activated upon BCR engagement, it phosphorylates and activates BLNK an adapter linking the activated BCR to downstream signaling adapters and effectors. It also phosphorylates and activates PLCG1 and the PKC signaling pathway. It also phosphorylates BTK and regulates its activity in B-cell antigen receptor (BCR)-coupled signaling. In addition to its function downstream of BCR also plays a role in T-cell receptor signaling. Plays also a crucial role in the innate immune response to fungal, bacterial and viral pathogens. It is for instance activated by the membrane lectin CLEC7A. Upon stimulation by fungal proteins, CLEC7A together with SYK activates immune cells inducing the production of ROS. Also activates the inflammasome and NF-kappa-B-mediated transcription of chemokines and cytokines in presence of pathogens. Regulates neutrophil degranulation and phagocytosis through activation of the MAPK signaling cascade. Required for the stimulation of neutrophil phagocytosis by IL15. Also mediates the activation of dendritic cells by cell necrosis stimuli. Also involved in mast cells activation. Involved in interleukin-3/IL3-mediated signaling pathway in basophils. Also functions downstream of receptors mediating cell adhesion. Relays for instance, integrin-mediated neutrophils and macrophages activation and P-selectin receptor/SELPG-mediated recruitment of leukocytes to inflammatory loci. Also plays a role in non-immune processes. It is for instance involved in vascular development where it may regulate blood and lymphatic vascular separation. It is also required for osteoclast development and function. Functions in the activation of platelets by collagen, mediating PLCG2 phosphorylation and activation. May be coupled to the collagen receptor by the ITAM domain-containing FCER1G. Also activated by the membrane lectin CLEC1B that is required for activation of platelets by PDPN/podoplanin. Involved in platelet adhesion being activated by ITGB3 engaged by fibrinogen. Together with CEACAM20, enhances production of the cytokine CXCL8/IL-8 via the NFKB pathway and may thus have a role in the intestinal immune response.
TTD ID
T62431
Uniprot ID
P43405
DrugMap ID
TTOU65C
Ensemble ID
ENST00000375746.1
HGNC ID
HGNC:11491
ChEMBL ID
CHEMBL2599

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A2058 SNV: p.G578E .
CHL1 SNV: p.G588R .
DU145 SNV: p.V622A .
G415 SNV: p.D221E .
HUH7 SNV: p.K133E .
LNCaP clone FGC Deletion: p.G33AfsTer2 .
LS180 Insertion: p.M34HfsTer3 .
MDAMB468 SNV: p.T81P .
MEWO SNV: p.E315K .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Probe 1
 Probe Info 
Y390(27.60)  LDD3495  [1]
DBIA
 Probe Info 
C593(18.53); C593(19.87); C597(19.87)  LDD0209  [2]
IA-alkyne
 Probe Info 
C543(0.52); 3.02  LDD2182  [3]
AMP probe
 Probe Info 
N.A.  LDD0200  [4]
ATP probe
 Probe Info 
N.A.  LDD0199  [4]
NAIA_5
 Probe Info 
N.A.  LDD2223  [5]
PAL-AfBPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
VE-P
 Probe Info 
N.A.  LDD0396  [6]
DFG-out-4
 Probe Info 
0.00  LDD0075  [7]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HCT 116 C593(0.62); C597(0.62)  LDD0531  [8]
 LDCM0215  AC10 HEK-293T C543(0.87)  LDD0813  [8]
 LDCM0226  AC11 HEK-293T C543(0.92)  LDD0824  [8]
 LDCM0230  AC113 HEK-293T C543(0.96)  LDD0828  [8]
 LDCM0231  AC114 HEK-293T C543(1.07)  LDD0829  [8]
 LDCM0232  AC115 HEK-293T C543(1.05)  LDD0830  [8]
 LDCM0233  AC116 HEK-293T C543(1.12)  LDD0831  [8]
 LDCM0234  AC117 HEK-293T C543(0.85)  LDD0832  [8]
 LDCM0235  AC118 HEK-293T C543(0.88)  LDD0833  [8]
 LDCM0236  AC119 HEK-293T C543(0.76)  LDD0834  [8]
 LDCM0237  AC12 HEK-293T C543(0.94)  LDD0835  [8]
 LDCM0238  AC120 HEK-293T C543(0.82)  LDD0836  [8]
 LDCM0239  AC121 HEK-293T C543(0.83)  LDD0837  [8]
 LDCM0240  AC122 HEK-293T C543(0.52)  LDD0838  [8]
 LDCM0241  AC123 HEK-293T C543(0.49)  LDD0839  [8]
 LDCM0242  AC124 HEK-293T C543(0.84)  LDD0840  [8]
 LDCM0243  AC125 HEK-293T C543(0.48)  LDD0841  [8]
 LDCM0244  AC126 HEK-293T C543(0.49)  LDD0842  [8]
 LDCM0245  AC127 HEK-293T C543(0.49)  LDD0843  [8]
 LDCM0246  AC128 HCT 116 C593(1.11); C597(1.11)  LDD0563  [8]
 LDCM0247  AC129 HCT 116 C593(1.38); C597(1.38)  LDD0564  [8]
 LDCM0249  AC130 HCT 116 C593(1.23); C597(1.23)  LDD0566  [8]
 LDCM0250  AC131 HCT 116 C593(1.80); C597(1.80)  LDD0567  [8]
 LDCM0251  AC132 HCT 116 C593(1.50); C597(1.50)  LDD0568  [8]
 LDCM0252  AC133 HCT 116 C593(1.56); C597(1.56)  LDD0569  [8]
 LDCM0253  AC134 HCT 116 C593(1.46); C597(1.46)  LDD0570  [8]
 LDCM0254  AC135 HCT 116 C593(0.90); C597(0.90)  LDD0571  [8]
 LDCM0255  AC136 HCT 116 C593(1.19); C597(1.19)  LDD0572  [8]
 LDCM0256  AC137 HCT 116 C593(1.33); C597(1.33)  LDD0573  [8]
 LDCM0257  AC138 HCT 116 C593(1.71); C597(1.71)  LDD0574  [8]
 LDCM0258  AC139 HCT 116 C593(1.67); C597(1.67)  LDD0575  [8]
 LDCM0259  AC14 HEK-293T C543(0.81)  LDD0857  [8]
 LDCM0260  AC140 HCT 116 C593(1.14); C597(1.14)  LDD0577  [8]
 LDCM0261  AC141 HCT 116 C593(1.27); C597(1.27)  LDD0578  [8]
 LDCM0262  AC142 HCT 116 C593(0.91); C597(0.91)  LDD0579  [8]
 LDCM0263  AC143 HEK-293T C543(0.85)  LDD0861  [8]
 LDCM0264  AC144 HEK-293T C543(0.56)  LDD0862  [8]
 LDCM0265  AC145 HEK-293T C543(0.55)  LDD0863  [8]
 LDCM0266  AC146 HEK-293T C543(0.53)  LDD0864  [8]
 LDCM0267  AC147 HEK-293T C543(0.56)  LDD0865  [8]
 LDCM0268  AC148 HEK-293T C543(0.62)  LDD0866  [8]
 LDCM0269  AC149 HEK-293T C543(1.03)  LDD0867  [8]
 LDCM0270  AC15 HEK-293T C543(0.74)  LDD0868  [8]
 LDCM0271  AC150 HEK-293T C543(0.83)  LDD0869  [8]
 LDCM0272  AC151 HEK-293T C543(0.72)  LDD0870  [8]
 LDCM0273  AC152 HEK-293T C543(0.92)  LDD0871  [8]
 LDCM0274  AC153 HEK-293T C543(0.77)  LDD0872  [8]
 LDCM0621  AC154 HEK-293T C543(1.04)  LDD2162  [8]
 LDCM0622  AC155 HEK-293T C543(0.90)  LDD2163  [8]
 LDCM0623  AC156 HEK-293T C543(0.55)  LDD2164  [8]
 LDCM0624  AC157 HEK-293T C543(0.60)  LDD2165  [8]
 LDCM0276  AC17 HEK-293T C543(0.69)  LDD0874  [8]
 LDCM0277  AC18 HEK-293T C543(0.80)  LDD0875  [8]
 LDCM0278  AC19 HEK-293T C543(0.76)  LDD0876  [8]
 LDCM0279  AC2 HCT 116 C593(0.65); C597(0.65)  LDD0596  [8]
 LDCM0280  AC20 HEK-293T C543(0.86)  LDD0878  [8]
 LDCM0281  AC21 HEK-293T C543(0.65)  LDD0879  [8]
 LDCM0282  AC22 HEK-293T C543(0.68)  LDD0880  [8]
 LDCM0283  AC23 HEK-293T C543(0.64)  LDD0881  [8]
 LDCM0284  AC24 HEK-293T C543(0.87)  LDD0882  [8]
 LDCM0285  AC25 HEK-293T C543(1.04)  LDD0883  [8]
 LDCM0286  AC26 HEK-293T C543(0.89)  LDD0884  [8]
 LDCM0287  AC27 HEK-293T C543(0.89)  LDD0885  [8]
 LDCM0288  AC28 HEK-293T C543(0.91)  LDD0886  [8]
 LDCM0289  AC29 HEK-293T C543(0.81)  LDD0887  [8]
 LDCM0290  AC3 HCT 116 C593(0.72); C597(0.72)  LDD0607  [8]
 LDCM0291  AC30 HEK-293T C543(0.87)  LDD0889  [8]
 LDCM0292  AC31 HEK-293T C543(0.96)  LDD0890  [8]
 LDCM0293  AC32 HEK-293T C543(0.87)  LDD0891  [8]
 LDCM0294  AC33 HEK-293T C543(0.93)  LDD0892  [8]
 LDCM0295  AC34 HEK-293T C543(1.21)  LDD0893  [8]
 LDCM0301  AC4 HCT 116 C593(0.52); C597(0.52)  LDD0618  [8]
 LDCM0308  AC46 HEK-293T C543(0.82)  LDD0906  [8]
 LDCM0309  AC47 HEK-293T C543(0.89)  LDD0907  [8]
 LDCM0310  AC48 HEK-293T C543(0.89)  LDD0908  [8]
 LDCM0311  AC49 HEK-293T C543(1.04)  LDD0909  [8]
 LDCM0312  AC5 HCT 116 C593(0.49); C597(0.49)  LDD0629  [8]
 LDCM0313  AC50 HEK-293T C543(0.85)  LDD0911  [8]
 LDCM0314  AC51 HEK-293T C543(0.78)  LDD0912  [8]
 LDCM0315  AC52 HEK-293T C543(1.04)  LDD0913  [8]
 LDCM0316  AC53 HEK-293T C543(0.86)  LDD0914  [8]
 LDCM0317  AC54 HEK-293T C543(0.92)  LDD0915  [8]
 LDCM0318  AC55 HEK-293T C543(0.96)  LDD0916  [8]
 LDCM0319  AC56 HEK-293T C543(1.06)  LDD0917  [8]
 LDCM0320  AC57 HCT 116 C593(0.28); C597(0.28)  LDD0637  [8]
 LDCM0321  AC58 HCT 116 C593(0.32); C597(0.32)  LDD0638  [8]
 LDCM0322  AC59 HCT 116 C593(0.27); C597(0.27)  LDD0639  [8]
 LDCM0323  AC6 HEK-293T C543(0.92)  LDD0921  [8]
 LDCM0324  AC60 HCT 116 C593(0.32); C597(0.32)  LDD0641  [8]
 LDCM0325  AC61 HCT 116 C593(0.32); C597(0.32)  LDD0642  [8]
 LDCM0326  AC62 HCT 116 C593(0.25); C597(0.25)  LDD0643  [8]
 LDCM0327  AC63 HCT 116 C593(0.31); C597(0.31)  LDD0644  [8]
 LDCM0328  AC64 HCT 116 C593(0.31); C597(0.31)  LDD0645  [8]
 LDCM0329  AC65 HCT 116 C593(0.32); C597(0.32)  LDD0646  [8]
 LDCM0330  AC66 HCT 116 C593(0.36); C597(0.36)  LDD0647  [8]
 LDCM0331  AC67 HCT 116 C593(0.36); C597(0.36)  LDD0648  [8]
 LDCM0332  AC68 HCT 116 C593(0.42); C597(0.42)  LDD0649  [8]
 LDCM0333  AC69 HCT 116 C593(0.79); C597(0.79)  LDD0650  [8]
 LDCM0334  AC7 HEK-293T C543(0.84)  LDD0932  [8]
 LDCM0335  AC70 HCT 116 C593(0.58); C597(0.58)  LDD0652  [8]
 LDCM0336  AC71 HCT 116 C593(0.64); C597(0.64)  LDD0653  [8]
 LDCM0337  AC72 HCT 116 C593(0.37); C597(0.37)  LDD0654  [8]
 LDCM0338  AC73 HCT 116 C593(0.52); C597(0.52)  LDD0655  [8]
 LDCM0339  AC74 HCT 116 C593(0.53); C597(0.53)  LDD0656  [8]
 LDCM0340  AC75 HCT 116 C593(0.60); C597(0.60)  LDD0657  [8]
 LDCM0341  AC76 HCT 116 C593(0.41); C597(0.41)  LDD0658  [8]
 LDCM0342  AC77 HCT 116 C593(0.47); C597(0.47)  LDD0659  [8]
 LDCM0343  AC78 HCT 116 C593(0.85); C597(0.85)  LDD0660  [8]
 LDCM0344  AC79 HCT 116 C593(0.75); C597(0.75)  LDD0661  [8]
 LDCM0345  AC8 HEK-293T C543(0.76)  LDD0943  [8]
 LDCM0346  AC80 HCT 116 C593(0.37); C597(0.37)  LDD0663  [8]
 LDCM0347  AC81 HCT 116 C593(0.56); C597(0.56)  LDD0664  [8]
 LDCM0348  AC82 HCT 116 C593(0.72); C597(0.72)  LDD0665  [8]
 LDCM0349  AC83 HEK-293T C543(1.01)  LDD0947  [8]
 LDCM0350  AC84 HEK-293T C543(0.78)  LDD0948  [8]
 LDCM0351  AC85 HEK-293T C543(1.08)  LDD0949  [8]
 LDCM0352  AC86 HEK-293T C543(0.86)  LDD0950  [8]
 LDCM0353  AC87 HEK-293T C543(1.19)  LDD0951  [8]
 LDCM0354  AC88 HEK-293T C543(0.82)  LDD0952  [8]
 LDCM0355  AC89 HEK-293T C543(0.88)  LDD0953  [8]
 LDCM0357  AC90 HEK-293T C543(0.84)  LDD0955  [8]
 LDCM0358  AC91 HEK-293T C543(0.97)  LDD0956  [8]
 LDCM0359  AC92 HEK-293T C543(1.08)  LDD0957  [8]
 LDCM0360  AC93 HEK-293T C543(0.85)  LDD0958  [8]
 LDCM0361  AC94 HEK-293T C543(0.68)  LDD0959  [8]
 LDCM0362  AC95 HEK-293T C543(1.01)  LDD0960  [8]
 LDCM0363  AC96 HEK-293T C543(0.80)  LDD0961  [8]
 LDCM0364  AC97 HEK-293T C543(0.51)  LDD0962  [8]
 LDCM0248  AKOS034007472 HEK-293T C543(1.00)  LDD0846  [8]
 LDCM0356  AKOS034007680 HEK-293T C543(0.76)  LDD0954  [8]
 LDCM0275  AKOS034007705 HEK-293T C543(0.84)  LDD0873  [8]
 LDCM0367  CL1 HCT 116 C593(1.18); C597(1.18)  LDD0684  [8]
 LDCM0368  CL10 HCT 116 C593(0.49); C597(0.49)  LDD0685  [8]
 LDCM0369  CL100 HCT 116 C593(0.56); C597(0.56)  LDD0686  [8]
 LDCM0370  CL101 HEK-293T C543(0.63)  LDD0968  [8]
 LDCM0371  CL102 HEK-293T C543(0.63)  LDD0969  [8]
 LDCM0372  CL103 HEK-293T C543(0.81)  LDD0970  [8]
 LDCM0373  CL104 HEK-293T C543(0.85)  LDD0971  [8]
 LDCM0374  CL105 HEK-293T C543(0.88)  LDD0972  [8]
 LDCM0375  CL106 HEK-293T C543(0.91)  LDD0973  [8]
 LDCM0376  CL107 HEK-293T C543(0.80)  LDD0974  [8]
 LDCM0377  CL108 HEK-293T C543(0.86)  LDD0975  [8]
 LDCM0378  CL109 HEK-293T C543(0.74)  LDD0976  [8]
 LDCM0379  CL11 HCT 116 C593(0.60); C597(0.60)  LDD0696  [8]
 LDCM0380  CL110 HEK-293T C543(0.74)  LDD0978  [8]
 LDCM0381  CL111 HEK-293T C543(0.71)  LDD0979  [8]
 LDCM0382  CL112 HEK-293T C543(0.73)  LDD0980  [8]
 LDCM0383  CL113 HEK-293T C543(0.95)  LDD0981  [8]
 LDCM0384  CL114 HEK-293T C543(0.86)  LDD0982  [8]
 LDCM0385  CL115 HEK-293T C543(1.00)  LDD0983  [8]
 LDCM0386  CL116 HEK-293T C543(0.86)  LDD0984  [8]
 LDCM0390  CL12 HCT 116 C593(0.59); C597(0.59)  LDD0707  [8]
 LDCM0392  CL121 HEK-293T C543(0.77)  LDD0990  [8]
 LDCM0393  CL122 HEK-293T C543(0.89)  LDD0991  [8]
 LDCM0394  CL123 HEK-293T C543(0.84)  LDD0992  [8]
 LDCM0395  CL124 HEK-293T C543(0.93)  LDD0993  [8]
 LDCM0396  CL125 HCT 116 C593(0.48); C597(0.48)  LDD0713  [8]
 LDCM0397  CL126 HCT 116 C593(0.72); C597(0.72)  LDD0714  [8]
 LDCM0398  CL127 HCT 116 C593(0.61); C597(0.61)  LDD0715  [8]
 LDCM0399  CL128 HCT 116 C593(0.29); C597(0.29)  LDD0716  [8]
 LDCM0400  CL13 HCT 116 C593(0.50); C597(0.50)  LDD0717  [8]
 LDCM0401  CL14 HCT 116 C593(0.78); C597(0.78)  LDD0718  [8]
 LDCM0402  CL15 HCT 116 C593(0.72); C597(0.72)  LDD0719  [8]
 LDCM0407  CL2 HCT 116 C593(0.70); C597(0.70)  LDD0724  [8]
 LDCM0418  CL3 HCT 116 C593(0.69); C597(0.69)  LDD0735  [8]
 LDCM0420  CL31 HCT 116 C593(0.63); C597(0.63)  LDD0737  [8]
 LDCM0421  CL32 HCT 116 C593(0.55); C597(0.55)  LDD0738  [8]
 LDCM0422  CL33 HCT 116 C593(0.56); C597(0.56)  LDD0739  [8]
 LDCM0423  CL34 HCT 116 C593(0.47); C597(0.47)  LDD0740  [8]
 LDCM0424  CL35 HCT 116 C593(0.42); C597(0.42)  LDD0741  [8]
 LDCM0425  CL36 HCT 116 C593(0.44); C597(0.44)  LDD0742  [8]
 LDCM0426  CL37 HCT 116 C593(0.47); C597(0.47)  LDD0743  [8]
 LDCM0428  CL39 HCT 116 C593(0.48); C597(0.48)  LDD0745  [8]
 LDCM0429  CL4 HCT 116 C593(0.67); C597(0.67)  LDD0746  [8]
 LDCM0430  CL40 HCT 116 C593(0.43); C597(0.43)  LDD0747  [8]
 LDCM0431  CL41 HCT 116 C593(0.47); C597(0.47)  LDD0748  [8]
 LDCM0432  CL42 HCT 116 C593(0.64); C597(0.64)  LDD0749  [8]
 LDCM0433  CL43 HCT 116 C593(0.48); C597(0.48)  LDD0750  [8]
 LDCM0434  CL44 HCT 116 C593(0.47); C597(0.47)  LDD0751  [8]
 LDCM0435  CL45 HCT 116 C593(0.48); C597(0.48)  LDD0752  [8]
 LDCM0440  CL5 HCT 116 C593(0.70); C597(0.70)  LDD0757  [8]
 LDCM0451  CL6 HCT 116 C593(0.62); C597(0.62)  LDD0768  [8]
 LDCM0453  CL61 HCT 116 C593(1.07); C597(1.07)  LDD0770  [8]
 LDCM0454  CL62 HCT 116 C593(0.99); C597(0.99)  LDD0771  [8]
 LDCM0455  CL63 HCT 116 C593(0.93); C597(0.93)  LDD0772  [8]
 LDCM0456  CL64 HCT 116 C593(0.97); C597(0.97)  LDD0773  [8]
 LDCM0457  CL65 HCT 116 C593(1.13); C597(1.13)  LDD0774  [8]
 LDCM0458  CL66 HCT 116 C593(1.02); C597(1.02)  LDD0775  [8]
 LDCM0459  CL67 HCT 116 C593(1.03); C597(1.03)  LDD0776  [8]
 LDCM0460  CL68 HCT 116 C593(1.05); C597(1.05)  LDD0777  [8]
 LDCM0461  CL69 HCT 116 C593(0.90); C597(0.90)  LDD0778  [8]
 LDCM0462  CL7 HCT 116 C593(0.60); C597(0.60)  LDD0779  [8]
 LDCM0463  CL70 HCT 116 C593(1.11); C597(1.11)  LDD0780  [8]
 LDCM0464  CL71 HCT 116 C593(1.08); C597(1.08)  LDD0781  [8]
 LDCM0465  CL72 HCT 116 C593(1.00); C597(1.00)  LDD0782  [8]
 LDCM0466  CL73 HCT 116 C593(1.24); C597(1.24)  LDD0783  [8]
 LDCM0467  CL74 HCT 116 C593(1.01); C597(1.01)  LDD0784  [8]
 LDCM0469  CL76 HEK-293T C543(1.14)  LDD1067  [8]
 LDCM0470  CL77 HEK-293T C543(1.22)  LDD1068  [8]
 LDCM0471  CL78 HEK-293T C543(1.65)  LDD1069  [8]
 LDCM0472  CL79 HEK-293T C543(1.20)  LDD1070  [8]
 LDCM0473  CL8 HCT 116 C593(0.48); C597(0.48)  LDD0790  [8]
 LDCM0474  CL80 HEK-293T C543(1.32)  LDD1072  [8]
 LDCM0475  CL81 HEK-293T C543(0.98)  LDD1073  [8]
 LDCM0476  CL82 HEK-293T C543(0.92)  LDD1074  [8]
 LDCM0477  CL83 HEK-293T C543(0.83)  LDD1075  [8]
 LDCM0478  CL84 HEK-293T C543(1.18)  LDD1076  [8]
 LDCM0479  CL85 HEK-293T C543(1.18)  LDD1077  [8]
 LDCM0480  CL86 HEK-293T C543(1.31)  LDD1078  [8]
 LDCM0481  CL87 HEK-293T C543(1.05)  LDD1079  [8]
 LDCM0482  CL88 HEK-293T C543(0.99)  LDD1080  [8]
 LDCM0483  CL89 HEK-293T C543(0.96)  LDD1081  [8]
 LDCM0484  CL9 HCT 116 C593(0.55); C597(0.55)  LDD0801  [8]
 LDCM0485  CL90 HEK-293T C543(0.91)  LDD1083  [8]
 LDCM0486  CL91 HCT 116 C593(0.76); C597(0.76)  LDD0803  [8]
 LDCM0487  CL92 HCT 116 C593(0.65); C597(0.65)  LDD0804  [8]
 LDCM0488  CL93 HCT 116 C593(0.82); C597(0.82)  LDD0805  [8]
 LDCM0489  CL94 HCT 116 C593(0.62); C597(0.62)  LDD0806  [8]
 LDCM0490  CL95 HCT 116 C593(0.46); C597(0.46)  LDD0807  [8]
 LDCM0491  CL96 HCT 116 C593(0.62); C597(0.62)  LDD0808  [8]
 LDCM0492  CL97 HCT 116 C593(0.61); C597(0.61)  LDD0809  [8]
 LDCM0493  CL98 HCT 116 C593(0.54); C597(0.54)  LDD0810  [8]
 LDCM0494  CL99 HCT 116 C593(0.49); C597(0.49)  LDD0811  [8]
 LDCM0017  DFG-out-2 A431 0.00  LDD0075  [7]
 LDCM0625  F8 Ramos C543(0.69); 0.66  LDD2187  [3]
 LDCM0572  Fragment10 Ramos C543(0.75); 0.93  LDD2189  [3]
 LDCM0573  Fragment11 Ramos C543(0.22); 0.65  LDD2190  [3]
 LDCM0574  Fragment12 Ramos C543(0.82); 1.00  LDD2191  [3]
 LDCM0575  Fragment13 Ramos C543(1.35); 1.07  LDD2192  [3]
 LDCM0576  Fragment14 Ramos C543(0.79); 0.34  LDD2193  [3]
 LDCM0579  Fragment20 Ramos C543(0.84); 1.04  LDD2194  [3]
 LDCM0580  Fragment21 Ramos C543(0.83); 0.55  LDD2195  [3]
 LDCM0582  Fragment23 Ramos C543(0.31); 0.20  LDD2196  [3]
 LDCM0578  Fragment27 Ramos C543(0.92); 0.80  LDD2197  [3]
 LDCM0586  Fragment28 Ramos C543(0.57); 1.07  LDD2198  [3]
 LDCM0588  Fragment30 Ramos C543(0.87); 0.99  LDD2199  [3]
 LDCM0589  Fragment31 Ramos C543(0.85); 0.92  LDD2200  [3]
 LDCM0590  Fragment32 Ramos C543(0.58); 1.15  LDD2201  [3]
 LDCM0468  Fragment33 HCT 116 C593(1.25); C597(1.25)  LDD0785  [8]
 LDCM0596  Fragment38 Ramos C543(0.69); 0.43  LDD2203  [3]
 LDCM0566  Fragment4 Ramos C543(0.68); 1.01  LDD2184  [3]
 LDCM0427  Fragment51 HCT 116 C593(0.57); C597(0.57)  LDD0744  [8]
 LDCM0610  Fragment52 Ramos C543(0.89); 1.78  LDD2204  [3]
 LDCM0614  Fragment56 Ramos C543(0.76); 1.43  LDD2205  [3]
 LDCM0569  Fragment7 Ramos C543(0.57); 0.97  LDD2186  [3]
 LDCM0571  Fragment9 Ramos C543(0.61); 1.26  LDD2188  [3]
 LDCM0022  KB02 Ramos C543(0.52); 3.02  LDD2182  [3]
 LDCM0023  KB03 Jurkat C593(18.53); C593(19.87); C597(19.87)  LDD0209  [2]
 LDCM0024  KB05 MOLM-13 C543(1.73)  LDD3333  [9]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 15 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Bleomycin hydrolase (BLMH) Peptidase C1 family Q13867
Ubiquitin carboxyl-terminal hydrolase 25 (USP25) Peptidase C19 family Q9UHP3
Serine/threonine-protein phosphatase PP1-alpha catalytic subunit (PPP1CA) PPP phosphatase family P62136
Hepatocyte growth factor receptor (MET) Tyr protein kinase family P08581
Receptor-type tyrosine-protein kinase FLT3 (FLT3) Tyr protein kinase family P36888
Epidermal growth factor receptor (EGFR) Tyr protein kinase family P00533
Receptor tyrosine-protein kinase erbB-2 (ERBB2) Tyr protein kinase family P04626
Receptor tyrosine-protein kinase erbB-3 (ERBB3) Tyr protein kinase family P21860
Tyrosine-protein kinase Lck (LCK) Tyr protein kinase family P06239
Ras-related C3 botulinum toxin substrate 1 (RAC1) Rho family P63000
Terminal nucleotidyltransferase 5A (TENT5A) TENT family Q96IP4
TNF receptor-associated factor 6 (TRAF6) TNF receptor-associated factor family Q9Y4K3
1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1 (PLCG1) . P19174
E3 ubiquitin-protein ligase CBL (CBL) . P22681
Ubiquitin-associated and SH3 domain-containing protein B (UBASH3B) . Q8TF42
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid-beta precursor protein (APP) APP family P05067
T-cell surface glycoprotein CD3 epsilon chain (CD3E) . P07766
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Signal transducer and activator of transcription 3 (STAT3) Transcription factor STAT family P40763
Immunoglobulin
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
B-cell receptor CD22 (CD22) SIGLEC (sialic acid binding Ig-like lectin) family P20273
Other
Click To Hide/Show 9 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
High affinity immunoglobulin epsilon receptor subunit gamma (FCER1G) CD3Z/FCER1G family P30273
GRB2-associated-binding protein 1 (GAB1) GAB family Q13480
Heat shock 70 kDa protein 1A (HSPA1A) Heat shock protein 70 family P0DMV8
Alpha-2-macroglobulin (A2M) Protease inhibitor I39 (alpha-2-macroglobulin) family P01023
Leukocyte antigen CD37 (CD37) Tetraspanin (TM4SF) family P11049
Apoptosis-associated speck-like protein containing a CARD (PYCARD) . Q9ULZ3
Cysteine-rich C-terminal protein 1 (CRCT1) . Q9UGL9
SH2 domain-containing protein 2A (SH2D2A) . Q9NP31
Telomeric repeat-binding factor 1 (TERF1) . P54274

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 D0V8HJ
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Disodium . D00OPX
Phase 2
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gs-9973 Small molecular drug D0G9AW
Hm43239 Small molecular drug DI1VM3
Cerdulatinib . D0BI3N
Gs-9876 . D0BW6F
Tak-659 . D06KTJ
Phase 1
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Hmpl-523 Small molecular drug DODG42
Prt-062607 Small molecular drug D0R9IU
Gsk2646264 . D0H2HZ
Prt6207 . D0C0SZ
Ski-o-703 . D01IDW
Clinical trial
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tamatinib Small molecular drug D0S6TK
Investigative
Click To Hide/Show 17 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cg-103065 Small molecular drug D00EIL
Ellagic Acid Small molecular drug D0A1CM
Ellagic Acid Small molecular drug DB08846
Entospletinib Small molecular drug DB12121
K00592a Small molecular drug D0T4MJ
N-benzyl-4-(2,5-dihydroxy-benzylamino)-benzamide Small molecular drug D0C7AS
Pmid17600705c23 Small molecular drug D04TLI
Pmid23312943c21 Small molecular drug D0O6OH
Sbb007833 Small molecular drug D03YUW
Staurosporine Small molecular drug DB02010
Tamatinib Small molecular drug DB07159
2-{2-[(35-dimethylphenyl)Amino]Pyrimidin-4-yl}-n-[(1s)-2-hydroxy-1-methylethyl]-4-methyl-13-thiazole-5-carboxamide . DB07194
2-{[(1r2s)-2-aminocyclohexyl]Amino}-4-[(3-methylphenyl)Amino]Pyrimidine-5-carboxamide . DB08361
Dnx-2000 . D0J3FK
N-(2-hydroxy-11-dimethylethyl)-1-methyl-3-(1h-pyrrolo[23-b]Pyridin-2-yl)-1h-indole-5-carboxamide . DB06834
Prt-060318 . D09KEB
Vrt-750018 . D04LGK
Patented
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pyrimidopyridazinone Derivative 1 Small molecular drug D0CD6Y
Pyrimidopyridazinone Derivative 2 Small molecular drug D0WA1V
Pyrrolo-pyrazine Derivative 3 Small molecular drug D0JU1R
Pyrrolo-pyrazine Derivative 4 Small molecular drug D0Y6ON
Discontinued
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
R-343 Small molecular drug D08DBE
Pf-3526299 . D0Y2XQ

References

1 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.
2 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
3 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
4 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.
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 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.
7 Affinity-based probes based on type II kinase inhibitors. J Am Chem Soc. 2012 Nov 21;134(46):19017-25. doi: 10.1021/ja306035v. Epub 2012 Nov 6.
8 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.
9 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