General Information of Target

Target ID LDTP01026
Target Name Tyrosine-protein kinase JAK2 (JAK2)
Gene Name JAK2
Gene ID 3717
Synonyms
Tyrosine-protein kinase JAK2; EC 2.7.10.2; Janus kinase 2; JAK-2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSG
EYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYF
PRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLG
MAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQF
SQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSR
GKHKESETLTEQDLQLYCDFPNIIDVSIKQANQEGSNESRVVTIHKQDGKNLEIELSSLR
EALSFVSLIDGYYRLTADAHHYLCKEVAPPAVLENIQSNCHGPISMDFAISKLKKAGNQT
GLYVLRCSPKDFNKYFLTFAVERENVIEYKHCLITKNENEEYNLSGTKKNFSSLKDLLNC
YQMETVRSDNIIFQFTKCCPPKPKDKSNLLVFRTNGVSDVPTSPTLQRPTHMNQMVFHKI
RNEDLIFNESLGQGTFTKIFKGVRREVGDYGQLHETEVLLKVLDKAHRNYSESFFEAASM
MSKLSHKHLVLNYGVCVCGDENILVQEFVKFGSLDTYLKKNKNCINILWKLEVAKQLAWA
MHFLEENTLIHGNVCAKNILLIREEDRKTGNPPFIKLSDPGISITVLPKDILQERIPWVP
PECIENPKNLNLATDKWSFGTTLWEICSGGDKPLSALDSQRKLQFYEDRHQLPAPKWAEL
ANLINNCMDYEPDFRPSFRAIIRDLNSLFTPDYELLTENDMLPNMRIGALGFSGAFEDRD
PTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIE
ILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDHIKLLQYTSQI
CKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFW
YAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIE
LLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNMAG
Target Type
Successful
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Tyr protein kinase family, JAK subfamily
Subcellular location
Endomembrane system
Function
Non-receptor tyrosine kinase involved in various processes such as cell growth, development, differentiation or histone modifications. Mediates essential signaling events in both innate and adaptive immunity. In the cytoplasm, plays a pivotal role in signal transduction via its association with type I receptors such as growth hormone (GHR), prolactin (PRLR), leptin (LEPR), erythropoietin (EPOR), thrombopoietin (THPO); or type II receptors including IFN-alpha, IFN-beta, IFN-gamma and multiple interleukins. Following ligand-binding to cell surface receptors, phosphorylates specific tyrosine residues on the cytoplasmic tails of the receptor, creating docking sites for STATs proteins. Subsequently, phosphorylates the STATs proteins once they are recruited to the receptor. Phosphorylated STATs then form homodimer or heterodimers and translocate to the nucleus to activate gene transcription. For example, cell stimulation with erythropoietin (EPO) during erythropoiesis leads to JAK2 autophosphorylation, activation, and its association with erythropoietin receptor (EPOR) that becomes phosphorylated in its cytoplasmic domain. Then, STAT5 (STAT5A or STAT5B) is recruited, phosphorylated and activated by JAK2. Once activated, dimerized STAT5 translocates into the nucleus and promotes the transcription of several essential genes involved in the modulation of erythropoiesis. Part of a signaling cascade that is activated by increased cellular retinol and that leads to the activation of STAT5 (STAT5A or STAT5B). In addition, JAK2 mediates angiotensin-2-induced ARHGEF1 phosphorylation. Plays a role in cell cycle by phosphorylating CDKN1B. Cooperates with TEC through reciprocal phosphorylation to mediate cytokine-driven activation of FOS transcription. In the nucleus, plays a key role in chromatin by specifically mediating phosphorylation of 'Tyr-41' of histone H3 (H3Y41ph), a specific tag that promotes exclusion of CBX5 (HP1 alpha) from chromatin.
TTD ID
T08391
Uniprot ID
O60674
DrugMap ID
TT0F5HE
Ensemble ID
ENST00000381652.4
HGNC ID
HGNC:6192
ChEMBL ID
CHEMBL2971

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IA-alkyne
 Probe Info 
C243(13.34)  LDD0513  [1]
DBIA
 Probe Info 
C125(5.79)  LDD0080  [2]
NAIA_5
 Probe Info 
N.A.  LDD2224  [3]
IPM
 Probe Info 
N.A.  LDD0147  [4]
TFBX
 Probe Info 
N.A.  LDD0148  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HCT 116 C125(1.64); C243(1.12)  LDD0531  [2]
 LDCM0215  AC10 HCT 116 C125(1.72)  LDD0532  [2]
 LDCM0216  AC100 HCT 116 C243(0.93)  LDD0533  [2]
 LDCM0217  AC101 HCT 116 C243(0.87)  LDD0534  [2]
 LDCM0218  AC102 HCT 116 C243(0.82)  LDD0535  [2]
 LDCM0219  AC103 HCT 116 C243(0.98)  LDD0536  [2]
 LDCM0220  AC104 HCT 116 C243(0.96)  LDD0537  [2]
 LDCM0221  AC105 HCT 116 C243(0.94)  LDD0538  [2]
 LDCM0222  AC106 HCT 116 C243(0.86)  LDD0539  [2]
 LDCM0223  AC107 HCT 116 C243(1.04)  LDD0540  [2]
 LDCM0224  AC108 HCT 116 C243(0.78)  LDD0541  [2]
 LDCM0225  AC109 HCT 116 C243(0.83)  LDD0542  [2]
 LDCM0226  AC11 HCT 116 C125(2.28)  LDD0543  [2]
 LDCM0227  AC110 HCT 116 C243(0.79)  LDD0544  [2]
 LDCM0228  AC111 HCT 116 C243(0.81)  LDD0545  [2]
 LDCM0229  AC112 HCT 116 C243(0.90)  LDD0546  [2]
 LDCM0230  AC113 HCT 116 C125(0.95)  LDD0547  [2]
 LDCM0231  AC114 HCT 116 C125(1.11)  LDD0548  [2]
 LDCM0232  AC115 HCT 116 C125(1.30)  LDD0549  [2]
 LDCM0233  AC116 HCT 116 C125(1.15)  LDD0550  [2]
 LDCM0234  AC117 HCT 116 C125(1.06)  LDD0551  [2]
 LDCM0235  AC118 HCT 116 C125(1.01)  LDD0552  [2]
 LDCM0236  AC119 HCT 116 C125(0.85)  LDD0553  [2]
 LDCM0237  AC12 HCT 116 C125(1.38)  LDD0554  [2]
 LDCM0238  AC120 HCT 116 C125(1.29)  LDD0555  [2]
 LDCM0239  AC121 HCT 116 C125(0.92)  LDD0556  [2]
 LDCM0240  AC122 HCT 116 C125(0.91)  LDD0557  [2]
 LDCM0241  AC123 HCT 116 C125(0.86)  LDD0558  [2]
 LDCM0242  AC124 HCT 116 C125(0.91)  LDD0559  [2]
 LDCM0243  AC125 HCT 116 C125(1.03)  LDD0560  [2]
 LDCM0244  AC126 HCT 116 C125(1.19)  LDD0561  [2]
 LDCM0245  AC127 HCT 116 C125(1.17)  LDD0562  [2]
 LDCM0246  AC128 HCT 116 C125(0.82)  LDD0563  [2]
 LDCM0247  AC129 HCT 116 C125(1.10)  LDD0564  [2]
 LDCM0249  AC130 HCT 116 C125(1.05)  LDD0566  [2]
 LDCM0250  AC131 HCT 116 C125(0.79)  LDD0567  [2]
 LDCM0251  AC132 HCT 116 C125(1.15)  LDD0568  [2]
 LDCM0252  AC133 HCT 116 C125(0.88)  LDD0569  [2]
 LDCM0253  AC134 HCT 116 C125(1.11)  LDD0570  [2]
 LDCM0254  AC135 HCT 116 C125(1.20)  LDD0571  [2]
 LDCM0255  AC136 HCT 116 C125(1.16)  LDD0572  [2]
 LDCM0256  AC137 HCT 116 C125(0.94)  LDD0573  [2]
 LDCM0257  AC138 HCT 116 C125(1.33)  LDD0574  [2]
 LDCM0258  AC139 HCT 116 C125(1.35)  LDD0575  [2]
 LDCM0259  AC14 HCT 116 C125(2.05)  LDD0576  [2]
 LDCM0260  AC140 HCT 116 C125(1.50)  LDD0577  [2]
 LDCM0261  AC141 HCT 116 C125(1.48)  LDD0578  [2]
 LDCM0262  AC142 HCT 116 C125(1.37)  LDD0579  [2]
 LDCM0263  AC143 HCT 116 C125(1.25)  LDD0580  [2]
 LDCM0264  AC144 HCT 116 C125(2.17)  LDD0581  [2]
 LDCM0265  AC145 HCT 116 C125(1.93)  LDD0582  [2]
 LDCM0266  AC146 HCT 116 C125(2.67)  LDD0583  [2]
 LDCM0267  AC147 HCT 116 C125(1.35)  LDD0584  [2]
 LDCM0268  AC148 HCT 116 C125(2.43)  LDD0585  [2]
 LDCM0269  AC149 HCT 116 C125(1.84)  LDD0586  [2]
 LDCM0270  AC15 HCT 116 C125(2.08)  LDD0587  [2]
 LDCM0271  AC150 HCT 116 C125(1.11)  LDD0588  [2]
 LDCM0272  AC151 HCT 116 C125(1.36)  LDD0589  [2]
 LDCM0273  AC152 HCT 116 C125(1.81)  LDD0590  [2]
 LDCM0274  AC153 HCT 116 C125(2.69)  LDD0591  [2]
 LDCM0621  AC154 HCT 116 C125(2.09)  LDD2158  [2]
 LDCM0622  AC155 HCT 116 C125(2.19)  LDD2159  [2]
 LDCM0623  AC156 HCT 116 C125(1.53)  LDD2160  [2]
 LDCM0624  AC157 HCT 116 C125(1.12)  LDD2161  [2]
 LDCM0276  AC17 HEK-293T C125(1.38)  LDD0874  [2]
 LDCM0277  AC18 HEK-293T C125(1.06)  LDD0875  [2]
 LDCM0278  AC19 HEK-293T C125(1.33)  LDD0876  [2]
 LDCM0279  AC2 HCT 116 C243(0.99); C125(1.31)  LDD0596  [2]
 LDCM0280  AC20 HEK-293T C125(1.62)  LDD0878  [2]
 LDCM0281  AC21 HEK-293T C125(1.06)  LDD0879  [2]
 LDCM0282  AC22 HEK-293T C125(1.31)  LDD0880  [2]
 LDCM0283  AC23 HEK-293T C125(1.23)  LDD0881  [2]
 LDCM0284  AC24 HEK-293T C125(1.10)  LDD0882  [2]
 LDCM0285  AC25 HCT 116 C125(0.90); C243(0.92); C917(1.04)  LDD0602  [2]
 LDCM0286  AC26 HCT 116 C125(0.99); C917(1.09); C243(1.41)  LDD0603  [2]
 LDCM0287  AC27 HCT 116 C125(0.85); C243(1.03); C917(1.06)  LDD0604  [2]
 LDCM0288  AC28 HCT 116 C125(1.17); C243(1.26); C917(1.56)  LDD0605  [2]
 LDCM0289  AC29 HCT 116 C125(1.04); C917(1.41); C243(1.45)  LDD0606  [2]
 LDCM0290  AC3 HCT 116 C243(1.16); C125(1.24)  LDD0607  [2]
 LDCM0291  AC30 HCT 116 C243(1.19); C125(1.30); C917(1.66)  LDD0608  [2]
 LDCM0292  AC31 HCT 116 C125(0.97); C243(1.12); C917(1.61)  LDD0609  [2]
 LDCM0293  AC32 HCT 116 C917(1.13); C243(1.33); C125(1.46)  LDD0610  [2]
 LDCM0294  AC33 HCT 116 C125(1.03); C243(1.03); C917(1.61)  LDD0611  [2]
 LDCM0295  AC34 HCT 116 C243(1.07); C125(1.11); C917(1.93)  LDD0612  [2]
 LDCM0296  AC35 HCT 116 C243(0.92); C125(1.14)  LDD0613  [2]
 LDCM0297  AC36 HCT 116 C125(0.80); C243(1.05)  LDD0614  [2]
 LDCM0298  AC37 HCT 116 C243(0.87); C125(0.93)  LDD0615  [2]
 LDCM0299  AC38 HCT 116 C125(1.03); C243(1.05)  LDD0616  [2]
 LDCM0300  AC39 HCT 116 C243(1.00); C125(1.15)  LDD0617  [2]
 LDCM0301  AC4 HCT 116 C243(0.98); C125(1.76)  LDD0618  [2]
 LDCM0302  AC40 HCT 116 C243(1.20); C125(1.29)  LDD0619  [2]
 LDCM0303  AC41 HCT 116 C243(1.04); C125(1.07)  LDD0620  [2]
 LDCM0304  AC42 HCT 116 C125(0.99); C243(1.15)  LDD0621  [2]
 LDCM0305  AC43 HCT 116 C125(1.02); C243(1.27)  LDD0622  [2]
 LDCM0306  AC44 HCT 116 C243(0.85); C125(1.19)  LDD0623  [2]
 LDCM0307  AC45 HCT 116 C243(1.04); C125(1.14)  LDD0624  [2]
 LDCM0308  AC46 HCT 116 C125(1.02); C243(1.10); C917(1.28)  LDD0625  [2]
 LDCM0309  AC47 HCT 116 C243(1.00); C917(1.04); C125(1.15)  LDD0626  [2]
 LDCM0310  AC48 HCT 116 C243(0.88); C917(1.14); C125(1.21)  LDD0627  [2]
 LDCM0311  AC49 HCT 116 C243(0.87); C125(1.36); C917(1.80)  LDD0628  [2]
 LDCM0312  AC5 HCT 116 C243(0.95); C125(1.43)  LDD0629  [2]
 LDCM0313  AC50 HCT 116 C243(1.10); C917(1.18); C125(1.27)  LDD0630  [2]
 LDCM0314  AC51 HCT 116 C243(0.83); C125(1.09); C917(1.15)  LDD0631  [2]
 LDCM0315  AC52 HCT 116 C243(0.89); C125(1.00); C917(1.15)  LDD0632  [2]
 LDCM0316  AC53 HCT 116 C125(1.17); C243(1.20); C917(1.47)  LDD0633  [2]
 LDCM0317  AC54 HCT 116 C243(0.81); C125(1.32); C917(1.43)  LDD0634  [2]
 LDCM0318  AC55 HCT 116 C243(1.04); C125(1.29); C917(1.74)  LDD0635  [2]
 LDCM0319  AC56 HCT 116 C243(0.95); C917(1.54); C125(1.72)  LDD0636  [2]
 LDCM0320  AC57 HCT 116 C243(1.03); C125(1.13)  LDD0637  [2]
 LDCM0321  AC58 HCT 116 C243(1.00); C125(1.03)  LDD0638  [2]
 LDCM0322  AC59 HCT 116 C125(1.12); C243(1.19)  LDD0639  [2]
 LDCM0323  AC6 HCT 116 C125(1.77)  LDD0640  [2]
 LDCM0324  AC60 HCT 116 C125(1.05); C243(1.25)  LDD0641  [2]
 LDCM0325  AC61 HCT 116 C243(0.92); C125(1.07)  LDD0642  [2]
 LDCM0326  AC62 HCT 116 C243(1.08); C125(1.14)  LDD0643  [2]
 LDCM0327  AC63 HCT 116 C125(0.78); C243(1.23)  LDD0644  [2]
 LDCM0328  AC64 HCT 116 C125(0.74); C243(1.23)  LDD0645  [2]
 LDCM0329  AC65 HCT 116 C125(0.93); C243(1.17)  LDD0646  [2]
 LDCM0330  AC66 HCT 116 C125(0.89); C243(0.94)  LDD0647  [2]
 LDCM0331  AC67 HCT 116 C125(0.80); C243(1.10)  LDD0648  [2]
 LDCM0332  AC68 HCT 116 C243(0.89); C125(1.01)  LDD0649  [2]
 LDCM0333  AC69 HCT 116 C243(0.79); C125(1.20)  LDD0650  [2]
 LDCM0334  AC7 HCT 116 C125(1.72)  LDD0651  [2]
 LDCM0335  AC70 HCT 116 C243(0.93); C125(1.39)  LDD0652  [2]
 LDCM0336  AC71 HCT 116 C243(0.84); C125(1.17)  LDD0653  [2]
 LDCM0337  AC72 HCT 116 C243(1.03); C125(1.13)  LDD0654  [2]
 LDCM0338  AC73 HCT 116 C243(1.01); C125(1.40)  LDD0655  [2]
 LDCM0339  AC74 HCT 116 C243(0.99); C125(1.56)  LDD0656  [2]
 LDCM0340  AC75 HCT 116 C243(1.07); C125(1.70)  LDD0657  [2]
 LDCM0341  AC76 HCT 116 C243(0.89); C125(1.16)  LDD0658  [2]
 LDCM0342  AC77 HCT 116 C243(0.87); C125(1.30)  LDD0659  [2]
 LDCM0343  AC78 HCT 116 C125(0.98); C243(0.98)  LDD0660  [2]
 LDCM0344  AC79 HCT 116 C243(0.94); C125(1.04)  LDD0661  [2]
 LDCM0345  AC8 HCT 116 C125(1.90)  LDD0662  [2]
 LDCM0346  AC80 HCT 116 C243(0.94); C125(1.18)  LDD0663  [2]
 LDCM0347  AC81 HCT 116 C243(0.85); C125(0.95)  LDD0664  [2]
 LDCM0348  AC82 HCT 116 C243(1.08); C125(1.71)  LDD0665  [2]
 LDCM0349  AC83 HCT 116 C125(1.97)  LDD0666  [2]
 LDCM0350  AC84 HCT 116 C125(2.06)  LDD0667  [2]
 LDCM0351  AC85 HCT 116 C125(1.47)  LDD0668  [2]
 LDCM0352  AC86 HCT 116 C125(1.48)  LDD0669  [2]
 LDCM0353  AC87 HCT 116 C125(1.06)  LDD0670  [2]
 LDCM0354  AC88 HCT 116 C125(1.97)  LDD0671  [2]
 LDCM0355  AC89 HCT 116 C125(1.41)  LDD0672  [2]
 LDCM0357  AC90 HCT 116 C125(1.15)  LDD0674  [2]
 LDCM0358  AC91 HCT 116 C125(1.94)  LDD0675  [2]
 LDCM0359  AC92 HCT 116 C125(1.97)  LDD0676  [2]
 LDCM0360  AC93 HCT 116 C125(1.47)  LDD0677  [2]
 LDCM0361  AC94 HCT 116 C125(1.55)  LDD0678  [2]
 LDCM0362  AC95 HCT 116 C125(1.24)  LDD0679  [2]
 LDCM0363  AC96 HCT 116 C125(1.88)  LDD0680  [2]
 LDCM0364  AC97 HCT 116 C125(2.38)  LDD0681  [2]
 LDCM0365  AC98 HCT 116 C243(0.99)  LDD0682  [2]
 LDCM0366  AC99 HCT 116 C243(0.87)  LDD0683  [2]
 LDCM0248  AKOS034007472 HCT 116 C125(1.55)  LDD0565  [2]
 LDCM0356  AKOS034007680 HCT 116 C125(1.46)  LDD0673  [2]
 LDCM0275  AKOS034007705 HCT 116 C125(2.42)  LDD0592  [2]
 LDCM0020  ARS-1620 HCC44 C125(0.92)  LDD2171  [2]
 LDCM0367  CL1 HCT 116 C243(1.25)  LDD0684  [2]
 LDCM0368  CL10 HCT 116 C243(1.36)  LDD0685  [2]
 LDCM0369  CL100 HCT 116 C243(1.28); C125(1.43)  LDD0686  [2]
 LDCM0370  CL101 HCT 116 C125(2.50)  LDD0687  [2]
 LDCM0371  CL102 HCT 116 C125(1.52)  LDD0688  [2]
 LDCM0372  CL103 HCT 116 C125(1.78)  LDD0689  [2]
 LDCM0373  CL104 HCT 116 C125(1.73)  LDD0690  [2]
 LDCM0374  CL105 HEK-293T C125(0.96)  LDD0972  [2]
 LDCM0375  CL106 HEK-293T C125(1.21)  LDD0973  [2]
 LDCM0376  CL107 HEK-293T C125(1.01)  LDD0974  [2]
 LDCM0377  CL108 HEK-293T C125(1.29)  LDD0975  [2]
 LDCM0378  CL109 HEK-293T C125(1.05)  LDD0976  [2]
 LDCM0379  CL11 HCT 116 C243(1.31)  LDD0696  [2]
 LDCM0380  CL110 HEK-293T C125(1.10)  LDD0978  [2]
 LDCM0381  CL111 HEK-293T C125(1.10)  LDD0979  [2]
 LDCM0382  CL112 HCT 116 C917(0.78); C125(1.13); C243(1.31)  LDD0699  [2]
 LDCM0383  CL113 HCT 116 C243(1.20); C125(1.22); C917(1.26)  LDD0700  [2]
 LDCM0384  CL114 HCT 116 C125(1.16); C917(1.45); C243(1.80)  LDD0701  [2]
 LDCM0385  CL115 HCT 116 C125(1.00); C243(1.18); C917(1.39)  LDD0702  [2]
 LDCM0386  CL116 HCT 116 C125(0.98); C917(1.09); C243(1.11)  LDD0703  [2]
 LDCM0387  CL117 HCT 116 C243(1.11); C125(1.40)  LDD0704  [2]
 LDCM0388  CL118 HCT 116 C125(0.90); C243(1.26)  LDD0705  [2]
 LDCM0389  CL119 HCT 116 C125(1.04); C243(1.18)  LDD0706  [2]
 LDCM0390  CL12 HCT 116 C243(1.17)  LDD0707  [2]
 LDCM0391  CL120 HCT 116 C125(0.84); C243(1.05)  LDD0708  [2]
 LDCM0392  CL121 HCT 116 C125(0.76); C243(1.00); C917(1.48)  LDD0709  [2]
 LDCM0393  CL122 HCT 116 C243(0.85); C917(1.15); C125(1.29)  LDD0710  [2]
 LDCM0394  CL123 HCT 116 C243(1.10); C125(1.51); C917(2.69)  LDD0711  [2]
 LDCM0395  CL124 HCT 116 C243(0.92); C125(1.54); C917(1.63)  LDD0712  [2]
 LDCM0396  CL125 HCT 116 C243(1.18); C125(1.29)  LDD0713  [2]
 LDCM0397  CL126 HCT 116 C125(1.20); C243(1.31)  LDD0714  [2]
 LDCM0398  CL127 HCT 116 C125(1.01); C243(1.19)  LDD0715  [2]
 LDCM0399  CL128 HCT 116 C125(0.98); C243(1.06)  LDD0716  [2]
 LDCM0400  CL13 HCT 116 C243(1.35)  LDD0717  [2]
 LDCM0401  CL14 HCT 116 C243(1.47)  LDD0718  [2]
 LDCM0402  CL15 HCT 116 C243(1.46)  LDD0719  [2]
 LDCM0403  CL16 HCT 116 C917(1.10)  LDD0720  [2]
 LDCM0404  CL17 HCT 116 C917(1.36)  LDD0721  [2]
 LDCM0405  CL18 HCT 116 C917(1.31)  LDD0722  [2]
 LDCM0406  CL19 HCT 116 C917(1.02)  LDD0723  [2]
 LDCM0407  CL2 HCT 116 C243(1.17)  LDD0724  [2]
 LDCM0408  CL20 HCT 116 C917(0.99)  LDD0725  [2]
 LDCM0409  CL21 HCT 116 C917(1.40)  LDD0726  [2]
 LDCM0410  CL22 HCT 116 C917(2.29)  LDD0727  [2]
 LDCM0411  CL23 HCT 116 C917(2.37)  LDD0728  [2]
 LDCM0412  CL24 HCT 116 C917(1.65)  LDD0729  [2]
 LDCM0413  CL25 HCT 116 C917(0.94)  LDD0730  [2]
 LDCM0414  CL26 HCT 116 C917(1.26)  LDD0731  [2]
 LDCM0415  CL27 HCT 116 C917(1.54)  LDD0732  [2]
 LDCM0416  CL28 HCT 116 C917(1.48)  LDD0733  [2]
 LDCM0417  CL29 HCT 116 C917(1.79)  LDD0734  [2]
 LDCM0418  CL3 HCT 116 C243(1.12)  LDD0735  [2]
 LDCM0419  CL30 HCT 116 C917(1.35)  LDD0736  [2]
 LDCM0420  CL31 HCT 116 C917(0.81)  LDD0737  [2]
 LDCM0421  CL32 HCT 116 C917(1.10)  LDD0738  [2]
 LDCM0422  CL33 HCT 116 C917(1.08)  LDD0739  [2]
 LDCM0423  CL34 HCT 116 C917(0.64)  LDD0740  [2]
 LDCM0424  CL35 HCT 116 C917(0.68)  LDD0741  [2]
 LDCM0425  CL36 HCT 116 C917(0.91)  LDD0742  [2]
 LDCM0426  CL37 HCT 116 C917(0.80)  LDD0743  [2]
 LDCM0428  CL39 HCT 116 C917(0.80)  LDD0745  [2]
 LDCM0429  CL4 HCT 116 C243(1.18)  LDD0746  [2]
 LDCM0430  CL40 HCT 116 C917(0.71)  LDD0747  [2]
 LDCM0431  CL41 HCT 116 C917(0.83)  LDD0748  [2]
 LDCM0432  CL42 HCT 116 C917(0.67)  LDD0749  [2]
 LDCM0433  CL43 HCT 116 C917(0.89)  LDD0750  [2]
 LDCM0434  CL44 HCT 116 C917(0.90)  LDD0751  [2]
 LDCM0435  CL45 HCT 116 C917(1.14)  LDD0752  [2]
 LDCM0440  CL5 HCT 116 C243(1.05)  LDD0757  [2]
 LDCM0451  CL6 HCT 116 C243(1.20)  LDD0768  [2]
 LDCM0453  CL61 HCT 116 C243(1.24)  LDD0770  [2]
 LDCM0454  CL62 HCT 116 C243(1.19)  LDD0771  [2]
 LDCM0455  CL63 HCT 116 C243(1.94)  LDD0772  [2]
 LDCM0456  CL64 HCT 116 C243(1.17)  LDD0773  [2]
 LDCM0457  CL65 HCT 116 C243(1.17)  LDD0774  [2]
 LDCM0458  CL66 HCT 116 C243(1.16)  LDD0775  [2]
 LDCM0459  CL67 HCT 116 C243(1.09)  LDD0776  [2]
 LDCM0460  CL68 HCT 116 C243(1.24)  LDD0777  [2]
 LDCM0461  CL69 HCT 116 C243(1.35)  LDD0778  [2]
 LDCM0462  CL7 HCT 116 C243(1.15)  LDD0779  [2]
 LDCM0463  CL70 HCT 116 C243(1.04)  LDD0780  [2]
 LDCM0464  CL71 HCT 116 C243(1.60)  LDD0781  [2]
 LDCM0465  CL72 HCT 116 C243(1.12)  LDD0782  [2]
 LDCM0466  CL73 HCT 116 C243(1.66)  LDD0783  [2]
 LDCM0467  CL74 HCT 116 C243(1.12)  LDD0784  [2]
 LDCM0469  CL76 HCT 116 C243(1.06)  LDD0786  [2]
 LDCM0470  CL77 HCT 116 C243(1.14)  LDD0787  [2]
 LDCM0471  CL78 HCT 116 C243(1.01)  LDD0788  [2]
 LDCM0472  CL79 HCT 116 C243(1.06)  LDD0789  [2]
 LDCM0473  CL8 HCT 116 C243(1.20)  LDD0790  [2]
 LDCM0474  CL80 HCT 116 C243(1.06)  LDD0791  [2]
 LDCM0475  CL81 HCT 116 C243(1.10)  LDD0792  [2]
 LDCM0476  CL82 HCT 116 C243(1.01)  LDD0793  [2]
 LDCM0477  CL83 HCT 116 C243(1.90)  LDD0794  [2]
 LDCM0478  CL84 HCT 116 C243(1.22)  LDD0795  [2]
 LDCM0479  CL85 HCT 116 C243(0.98)  LDD0796  [2]
 LDCM0480  CL86 HCT 116 C243(0.92)  LDD0797  [2]
 LDCM0481  CL87 HCT 116 C243(0.96)  LDD0798  [2]
 LDCM0482  CL88 HCT 116 C243(1.27)  LDD0799  [2]
 LDCM0483  CL89 HCT 116 C243(1.00)  LDD0800  [2]
 LDCM0484  CL9 HCT 116 C243(1.24)  LDD0801  [2]
 LDCM0485  CL90 HCT 116 C243(1.41)  LDD0802  [2]
 LDCM0486  CL91 HCT 116 C125(1.39); C243(1.07)  LDD0803  [2]
 LDCM0487  CL92 HCT 116 C125(1.37); C243(1.20)  LDD0804  [2]
 LDCM0488  CL93 HCT 116 C125(1.16); C243(1.06)  LDD0805  [2]
 LDCM0489  CL94 HCT 116 C125(1.99); C243(1.10)  LDD0806  [2]
 LDCM0490  CL95 HCT 116 C125(2.66); C243(2.01)  LDD0807  [2]
 LDCM0491  CL96 HCT 116 C125(1.39); C243(1.19)  LDD0808  [2]
 LDCM0492  CL97 HCT 116 C125(1.30); C243(1.58)  LDD0809  [2]
 LDCM0493  CL98 HCT 116 C125(1.79); C243(1.18)  LDD0810  [2]
 LDCM0494  CL99 HCT 116 C125(1.26); C243(1.20)  LDD0811  [2]
 LDCM0198  Dimethyl Fumarate(DMF) T cell C243(13.34)  LDD0513  [1]
 LDCM0468  Fragment33 HCT 116 C243(1.24)  LDD0785  [2]
 LDCM0427  Fragment51 HCT 116 C917(0.58)  LDD0744  [2]
 LDCM0022  KB02 HCT 116 C125(5.79)  LDD0080  [2]
 LDCM0023  KB03 HCT 116 C125(2.02)  LDD0081  [2]
 LDCM0024  KB05 HCT 116 C125(2.68)  LDD0082  [2]
 LDCM0021  THZ1 HCT 116 C125(0.92)  LDD2173  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Rho-associated protein kinase 2 (ROCK2) AGC Ser/Thr protein kinase family O75116
Non-receptor tyrosine-protein kinase TYK2 (TYK2) Tyr protein kinase family P29597
Tyrosine-protein kinase JAK1 (JAK1) Tyr protein kinase family P23458
Tyrosine-protein kinase JAK2 (JAK2) Tyr protein kinase family O60674
Tyrosine-protein phosphatase non-receptor type 1 (PTPN1) Protein-tyrosine phosphatase family P18031
Cytokine and receptor
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Thrombopoietin receptor (MPL) Type I cytokine receptor family P40238
Cytokine receptor common subunit beta (CSF2RB) Type I cytokine receptor family P32927
Interleukin-5 receptor subunit alpha (IL5RA) Type I cytokine receptor family Q01344
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
SH2/SH3 adapter protein NCK1 (NCK1) . P16333

The Drug(s) Related To This Target

Approved
Click To Hide/Show 9 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Baricitinib Small molecular drug D0Y7IC
Entrectinib Small molecular drug DB11986
Fedratinib Small molecular drug D0G8BM
Fostamatinib Small molecular drug DB12010
Ruxolitinib Small molecular drug D04LKS
Tofacitinib Small molecular drug DB08895
Abrocitinib . DB14973
Pralsetinib . DB15822
Zanubrutinib . DB15035
Phase 3
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Itf2357 Small molecular drug D0GH3Q
Momelotinib Small molecular drug D0D5ZJ
Pacritinib Small molecular drug D0PN8H
Xl019 Small molecular drug D05AJT
Phase 2
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Azd1480 Small molecular drug D0MP0X
Bms-911543 Small molecular drug D0DK8X
Ctp-543 Small molecular drug DU10JI
Incb039110 Small molecular drug D09AFI
Ly2784544 Small molecular drug D05TSJ
Ns-018 Small molecular drug D00MYW
Cerdulatinib . D0BI3N
Phase 1
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ac430 Small molecular drug D08CNP
Peginterferon Beta . D0S0NX
Sb-1578 . D00RYA
Investigative
Click To Hide/Show 17 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1,2,3,4,5,6-hexabromocyclohexane Small molecular drug DLW69V
2-tert-butyl-9-fluoro-16-dihydrobenzo[H]Imidazo[45-f]Isoquinolin-7-one Small molecular drug DB04716
5-phenyl-1h-indazol-3-amine Small molecular drug D0I3EY
Atropisomer 1 Small molecular drug D05MHL
Az960 Small molecular drug D0OP3D
Cmp-6 Small molecular drug D0IR6U
Nsc-1771 Small molecular drug D02UVS
Pmid21493067c1d Small molecular drug D02NNT
Pmid24359159c19a Small molecular drug D0US9O
Whi-p154 Small molecular drug D0E5IP
4-(3-amino-1h-indazol-5-yl)-n-tert-butylbenzenesulfonamide . DB07162
4-[(2-{4-[(Cyclopropylcarbamoyl)Amino]-1h-pyrazol-3-yl}-1h-benzimidazol-6-yl)Methyl]Morpholin-4-ium . DB08067
Amg-jak2-01 . D00MAM
Bvb-808 . D0N8CN
K-454 . D0I6QN
On-044580 . D0A7XQ
Sgi-1252 . D09VZR
Patented
Click To Hide/Show 76 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1,2,4-triazolo[1,5a]Pyridine Derivative 1 Small molecular drug D07XYI
1,2,4-triazolo[1,5a]Pyridine Derivative 2 Small molecular drug D0NP2W
Alkynyl-substituted Pyrimidinyl-pyrrole Derivative 1 Small molecular drug D0JZ2B
Aminooxazole Carboxamide Derivative 1 Small molecular drug D05AXE
Aminotriazolopyridine Derivative 1 Small molecular drug D09ALF
Aromatic Bicyclic Compound 1 Small molecular drug D0QD5Y
Aromatic Bicyclic Compound 2 Small molecular drug D0VI7E
Aromatic Bicyclic Compound 3 Small molecular drug D0M5AG
Aromatic Bicyclic Compound 4 Small molecular drug D0M9YZ
Aromatic Bicyclic Compound 5 Small molecular drug D0Q5JV
Aromatic Bicyclic Compound 6 Small molecular drug D09RTW
Benzimidazole Derivative 7 Small molecular drug D01CRX
Bis-aminopyrimidine Derivative 2 Small molecular drug D0LR6J
Bis-aminopyrimidine Derivative 3 Small molecular drug D0S6XT
Bis-aminopyrimidine Derivative 4 Small molecular drug D0SJ1Q
Bis-aminopyrimidine Derivative 5 Small molecular drug D0M2OK
Curcumin Analog 1 Small molecular drug D0WD1Z
Curcumin Analog 2 Small molecular drug D0IC8O
Cyanomethyl Pypazole Carboxamide Derivative 1 Small molecular drug D0K2RW
Cyclic Cyanoethypypazole Derivative 1 Small molecular drug D05GEL
Cycloalkyl Nitrile Pyrazole Carboxamide Derivative 1 Small molecular drug D0V0KI
Cycloalkyl Nitrile Pyrazolo Pyridone Derivative 1 Small molecular drug D0PB5X
Cycloalkyl Nitrile Pyrazolo Pyridone Derivative 2 Small molecular drug D0S4TH
Five-and-six-membered Heterocyclic Compound 1 Small molecular drug D08WPB
Geminally-substituted Cyanoethylpypazolo Pyridone Derivative 1 Small molecular drug D0H6XN
Geminally-substituted Cyanoethylpypazolo Pyridone Derivative 2 Small molecular drug D0KI5F
Imidazo[4,5-c]Pyridine Derivative 2 Small molecular drug D0VJ1R
Isoxazole Derivative 1 Small molecular drug D0G9MM
Isoxazole Derivative 2 Small molecular drug D0TX2G
N-(Cyanomethyl)-4-(2-(Phenylamino)Pyrimidin-4-yl)Benzamide Derivative 1 Small molecular drug D0Y2IM
Pmid27774822-compound-figure10compound12 Small molecular drug D0A8BV
Pmid27774822-compound-figure10compound4 Small molecular drug D0AE0M
Pmid27774822-compound-figure10example1 Small molecular drug D0GH8D
Pmid27774822-compound-figure10example19 Small molecular drug D0W8DN
Pmid27774822-compound-figure11example5 Small molecular drug D0RJ3W
Pmid27774822-compound-figure1example20 Small molecular drug D0M3CB
Pmid27774822-compound-figure2example1-1left Small molecular drug D0E2WK
Pmid27774822-compound-figure2example1-1right Small molecular drug D0IQ6G
Pmid27774822-compound-figure3compoundi-165 Small molecular drug D0NY6M
Pmid27774822-compound-figure7example63 Small molecular drug D04OCD
Pmid27774822-compound-figure8example5 Small molecular drug D0B9TH
Pmid27774824-compound-figure11example1up Small molecular drug D0YR8S
Pmid27774824-compound-figure2example4 Small molecular drug D0A6RG
Pmid27774824-compound-figure3example18 Small molecular drug D0U1HA
Pmid27774824-compound-figure6example12 Small molecular drug D0GB7G
Pmid27774824-compound-figure6example6 Small molecular drug D0F3BK
Pmid27774824-compound-figure8example22 Small molecular drug D0KF8H
Pmid27774824-compound-figure8example99 Small molecular drug D0HS2J
Pmid27774824-compound-figure9example2down Small molecular drug D01DBB
Pmid27774824-compound-figure9example2up Small molecular drug D0WZ8N
Pyrazolopyridine Derivative 3 Small molecular drug D03QAY
Pyrazolopyridine Derivative 6 Small molecular drug D02VGC
Pyrazolopyridine Derivative 7 Small molecular drug D0D1QH
Pyrimidopyridazinone Derivative 1 Small molecular drug D0CD6Y
Pyrimidopyridazinone Derivative 2 Small molecular drug D0WA1V
Pyrrole Derivative 7 Small molecular drug D0YJ4D
Pyrrole Six-membered Heteroaryl Ring Derivative 1 Small molecular drug D09UBE
Pyrrolo-pyridine Derivative 3 Small molecular drug D0VR6E
Pyrrolo-pyridone Derivative 1 Small molecular drug D06MQB
Pyrrolo-pyridone Derivative 2 Small molecular drug D03PBI
Pyrrolo[2,3-d]Pyrimidine Derivative 11 Small molecular drug D0VQ7P
Pyrrolo[2,3-d]Pyrimidine Derivative 6 Small molecular drug D0FQ4Z
Pyrrolo[2,3-d]Pyrimidine Derivative 7 Small molecular drug D0U5FZ
Pyrrolo[2,3-d]Pyrimidine Derivative 8 Small molecular drug D0KL3B
Ruxolitinib Derivative 2 Small molecular drug D01EYJ
Triazolo-pyridine Derivative 1 Small molecular drug D00JUI
Tricyclic Compound 1 Small molecular drug D0G0FK
Tricyclic Compound 11 Small molecular drug D0LS1O
Tricyclic Heterocycle Derivative 1 Small molecular drug D0X1FD
Tricyclic Heterocycle Derivative 2 Small molecular drug D03TEE
Tricyclic Heterocycle Derivative 5 Small molecular drug D0M2WA
Tricyclic Pyrrolopyridine Compound 1 Small molecular drug D04BOW
Bis-aminopyrimidine Derivative 1 . D01FVC
Pmid27774824-compound-figure7example10 . D0PM8K
Pyrazolopyridine Derivative 4 . D09RUN
Pyrazolo[4,3-c]Pyridine Derivative 2 . D09PIS
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ag490 Small molecular drug D0GZ7B

References

1 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.
2 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.
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 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