Details of the Target

General Information of Target

Target ID LDTP06699
Target Name AP2-associated protein kinase 1 (AAK1)
Gene Name AAK1
Gene ID 22848
Synonyms
KIAA1048; AP2-associated protein kinase 1; EC 2.7.11.1; Adaptor-associated kinase 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MKKFFDSRREQGGSGLGSGSSGGGGSTSGLGSGYIGRVFGIGRQQVTVDEVLAEGGFAIV
FLVRTSNGMKCALKRMFVNNEHDLQVCKREIQIMRDLSGHKNIVGYIDSSINNVSSGDVW
EVLILMDFCRGGQVVNLMNQRLQTGFTENEVLQIFCDTCEAVARLHQCKTPIIHRDLKVE
NILLHDRGHYVLCDFGSATNKFQNPQTEGVNAVEDEIKKYTTLSYRAPEMVNLYSGKIIT
TKADIWALGCLLYKLCYFTLPFGESQVAICDGNFTIPDNSRYSQDMHCLIRYMLEPDPDK
RPDIYQVSYFSFKLLKKECPIPNVQNSPIPAKLPEPVKASEAAAKKTQPKARLTDPIPTT
ETSIAPRQRPKAGQTQPNPGILPIQPALTPRKRATVQPPPQAAGSSNQPGLLASVPQPKP
QAPPSQPLPQTQAKQPQAPPTPQQTPSTQAQGLPAQAQATPQHQQQLFLKQQQQQQQPPP
AQQQPAGTFYQQQQAQTQQFQAVHPATQKPAIAQFPVVSQGGSQQQLMQNFYQQQQQQQQ
QQQQQQLATALHQQQLMTQQAALQQKPTMAAGQQPQPQPAAAPQPAPAQEPAIQAPVRQQ
PKVQTTPPPAVQGQKVGSLTPPSSPKTQRAGHRRILSDVTHSAVFGVPASKSTQLLQAAA
AEASLNKSKSATTTPSGSPRTSQQNVYNPSEGSTWNPFDDDNFSKLTAEELLNKDFAKLG
EGKHPEKLGGSAESLIPGFQSTQGDAFATTSFSAGTAEKRKGGQTVDSGLPLLSVSDPFI
PLQVPDAPEKLIEGLKSPDTSLLLPDLLPMTDPFGSTSDAVIEKADVAVESLIPGLEPPV
PQRLPSQTESVTSNRTDSLTGEDSLLDCSLLSNPTTDLLEEFAPTAISAPVHKAAEDSNL
ISGFDVPEGSDKVAEDEFDPIPVLITKNPQGGHSRNSSGSSESSLPNLARSLLLVDQLID
L
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Ser/Thr protein kinase family
Subcellular location
Cell membrane
Function
Regulates clathrin-mediated endocytosis by phosphorylating the AP2M1/mu2 subunit of the adaptor protein complex 2 (AP-2) which ensures high affinity binding of AP-2 to cargo membrane proteins during the initial stages of endocytosis . Isoform 1 and isoform 2 display similar levels of kinase activity towards AP2M1. Preferentially, may phosphorylate substrates on threonine residues. Regulates phosphorylation of other AP-2 subunits as well as AP-2 localization and AP-2-mediated internalization of ligand complexes. Phosphorylates NUMB and regulates its cellular localization, promoting NUMB localization to endosomes. Binds to and stabilizes the activated form of NOTCH1, increases its localization in endosomes and regulates its transcriptional activity.; (Microbial infection) By regulating clathrin-mediated endocytosis, AAK1 plays a role in the entry of hepatitis C virus as well as for the lifecycle of other viruses such as Ebola and Dengue.
TTD ID
T32764
Uniprot ID
Q2M2I8
DrugMap ID
TTN9A16
Ensemble ID
ENST00000406297.7
HGNC ID
HGNC:19679
ChEMBL ID
CHEMBL3830

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.R634H DBIA    Probe Info 
LS180 Insertion: p.T885HfsTer9 .
MCC13 SNV: p.P330S DBIA    Probe Info 
NCIH1155 SNV: p.A163S DBIA    Probe Info 
SW403 Deletion: p.F312LfsTer26 .
TOV21G SNV: p.G939W .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 14 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
STPyne
 Probe Info  		K3(7.27); K714(4.17)  LDD0277  [2]
Probe 1
 Probe Info  		Y34(22.44)  LDD3495  [3]
Johansson_61
 Probe Info  		_(20.00)  LDD1489  [4]
HHS-475
 Probe Info  		Y34(0.60)  LDD0264  [5]
DBIA
 Probe Info  		C87(0.92)  LDD0531  [6]
4-Iodoacetamidophenylacetylene
 Probe Info  		C250(0.00); C319(0.00); C193(0.00); C87(0.00)  LDD0038  [7]
IA-alkyne
 Probe Info  		C250(0.00); C193(0.00); C87(0.00); C288(0.00)  LDD0036  [7]
Lodoacetamide azide
 Probe Info  		C250(0.00); C319(0.00); C193(0.00); C87(0.00)  LDD0037  [7]
IPM
 Probe Info  		C87(0.00); C193(0.00)  LDD2156  [8]
TFBX
 Probe Info  		N.A.  LDD0148  [9]
AOyne
 Probe Info  		10.90  LDD0443  [10]
NAIA_5
 Probe Info  		C250(0.00); C193(0.00); C168(0.00)  LDD2223  [11]
HHS-465
 Probe Info  		N.A.  LDD2240  [12]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HCT 116 C87(0.92)  LDD0531  [6]
 LDCM0215  AC10 HCT 116 C87(0.98)  LDD0532  [6]
 LDCM0226  AC11 HCT 116 C87(0.99)  LDD0543  [6]
 LDCM0230  AC113 HEK-293T C256(0.78); C87(1.29)  LDD0828  [6]
 LDCM0231  AC114 HEK-293T C256(1.03); C87(1.46)  LDD0829  [6]
 LDCM0232  AC115 HEK-293T C256(0.99); C87(1.25)  LDD0830  [6]
 LDCM0233  AC116 HEK-293T C256(1.01); C87(1.22)  LDD0831  [6]
 LDCM0234  AC117 HEK-293T C256(1.14); C87(1.23)  LDD0832  [6]
 LDCM0235  AC118 HEK-293T C256(0.79); C87(1.21)  LDD0833  [6]
 LDCM0236  AC119 HEK-293T C256(0.79); C87(1.13)  LDD0834  [6]
 LDCM0237  AC12 HCT 116 C87(1.05)  LDD0554  [6]
 LDCM0238  AC120 HEK-293T C256(0.95); C87(1.05)  LDD0836  [6]
 LDCM0239  AC121 HEK-293T C256(0.81); C87(1.16)  LDD0837  [6]
 LDCM0240  AC122 HEK-293T C256(0.53); C87(1.52)  LDD0838  [6]
 LDCM0241  AC123 HEK-293T C256(0.51); C87(1.30)  LDD0839  [6]
 LDCM0242  AC124 HEK-293T C256(0.81); C87(1.17)  LDD0840  [6]
 LDCM0243  AC125 HEK-293T C256(0.51); C87(1.12)  LDD0841  [6]
 LDCM0244  AC126 HEK-293T C256(0.31); C87(1.47)  LDD0842  [6]
 LDCM0245  AC127 HEK-293T C256(0.25); C87(1.07)  LDD0843  [6]
 LDCM0259  AC14 HCT 116 C87(1.04)  LDD0576  [6]
 LDCM0263  AC143 HEK-293T C270(0.75)  LDD0861  [6]
 LDCM0264  AC144 HEK-293T C270(1.13)  LDD0862  [6]
 LDCM0265  AC145 HEK-293T C270(0.73)  LDD0863  [6]
 LDCM0266  AC146 HEK-293T C270(1.03)  LDD0864  [6]
 LDCM0267  AC147 HEK-293T C270(0.96)  LDD0865  [6]
 LDCM0268  AC148 HEK-293T C270(1.76)  LDD0866  [6]
 LDCM0269  AC149 HEK-293T C270(1.09)  LDD0867  [6]
 LDCM0270  AC15 HCT 116 C87(1.11)  LDD0587  [6]
 LDCM0271  AC150 HEK-293T C270(1.21)  LDD0869  [6]
 LDCM0272  AC151 HEK-293T C270(0.92)  LDD0870  [6]
 LDCM0273  AC152 HEK-293T C270(1.03)  LDD0871  [6]
 LDCM0274  AC153 HEK-293T C270(0.84)  LDD0872  [6]
 LDCM0621  AC154 HEK-293T C270(0.95)  LDD2162  [6]
 LDCM0622  AC155 HEK-293T C270(0.93)  LDD2163  [6]
 LDCM0623  AC156 HEK-293T C270(1.42)  LDD2164  [6]
 LDCM0624  AC157 HEK-293T C270(0.72)  LDD2165  [6]
 LDCM0276  AC17 HCT 116 C87(0.83)  LDD0593  [6]
 LDCM0277  AC18 HCT 116 C87(0.85)  LDD0594  [6]
 LDCM0278  AC19 HCT 116 C87(0.70)  LDD0595  [6]
 LDCM0279  AC2 HCT 116 C87(0.84)  LDD0596  [6]
 LDCM0280  AC20 HCT 116 C87(0.87)  LDD0597  [6]
 LDCM0281  AC21 HCT 116 C87(0.92)  LDD0598  [6]
 LDCM0282  AC22 HCT 116 C87(0.98)  LDD0599  [6]
 LDCM0283  AC23 HCT 116 C87(0.96)  LDD0600  [6]
 LDCM0284  AC24 HCT 116 C87(0.67)  LDD0601  [6]
 LDCM0285  AC25 HCT 116 C87(1.01)  LDD0602  [6]
 LDCM0286  AC26 HCT 116 C87(1.03)  LDD0603  [6]
 LDCM0287  AC27 HCT 116 C87(1.02)  LDD0604  [6]
 LDCM0288  AC28 HCT 116 C87(0.97)  LDD0605  [6]
 LDCM0289  AC29 HCT 116 C87(0.99)  LDD0606  [6]
 LDCM0290  AC3 HCT 116 C87(0.90)  LDD0607  [6]
 LDCM0291  AC30 HCT 116 C87(1.04)  LDD0608  [6]
 LDCM0292  AC31 HCT 116 C87(1.00)  LDD0609  [6]
 LDCM0293  AC32 HCT 116 C87(1.07)  LDD0610  [6]
 LDCM0294  AC33 HCT 116 C87(0.99)  LDD0611  [6]
 LDCM0295  AC34 HCT 116 C87(1.04)  LDD0612  [6]
 LDCM0296  AC35 HCT 116 C87(0.93)  LDD0613  [6]
 LDCM0297  AC36 HCT 116 C87(0.89)  LDD0614  [6]
 LDCM0298  AC37 HCT 116 C87(0.83)  LDD0615  [6]
 LDCM0299  AC38 HCT 116 C87(0.95)  LDD0616  [6]
 LDCM0300  AC39 HCT 116 C87(0.96)  LDD0617  [6]
 LDCM0301  AC4 HCT 116 C87(0.87)  LDD0618  [6]
 LDCM0302  AC40 HCT 116 C87(0.85)  LDD0619  [6]
 LDCM0303  AC41 HCT 116 C87(0.95)  LDD0620  [6]
 LDCM0304  AC42 HCT 116 C87(0.96)  LDD0621  [6]
 LDCM0305  AC43 HCT 116 C87(0.87)  LDD0622  [6]
 LDCM0306  AC44 HCT 116 C87(0.86)  LDD0623  [6]
 LDCM0307  AC45 HCT 116 C87(0.86)  LDD0624  [6]
 LDCM0308  AC46 HCT 116 C87(0.84)  LDD0625  [6]
 LDCM0309  AC47 HCT 116 C87(0.91)  LDD0626  [6]
 LDCM0310  AC48 HCT 116 C87(1.00)  LDD0627  [6]
 LDCM0311  AC49 HCT 116 C87(0.87)  LDD0628  [6]
 LDCM0312  AC5 HCT 116 C87(1.11)  LDD0629  [6]
 LDCM0313  AC50 HCT 116 C87(1.03)  LDD0630  [6]
 LDCM0314  AC51 HCT 116 C87(0.97)  LDD0631  [6]
 LDCM0315  AC52 HCT 116 C87(1.19)  LDD0632  [6]
 LDCM0316  AC53 HCT 116 C87(0.76)  LDD0633  [6]
 LDCM0317  AC54 HCT 116 C87(1.09)  LDD0634  [6]
 LDCM0318  AC55 HCT 116 C87(0.95)  LDD0635  [6]
 LDCM0319  AC56 HCT 116 C87(1.05)  LDD0636  [6]
 LDCM0320  AC57 HCT 116 C87(1.02)  LDD0637  [6]
 LDCM0321  AC58 HCT 116 C87(1.03)  LDD0638  [6]
 LDCM0322  AC59 HCT 116 C87(1.03)  LDD0639  [6]
 LDCM0323  AC6 HCT 116 C87(1.11)  LDD0640  [6]
 LDCM0324  AC60 HCT 116 C87(0.96)  LDD0641  [6]
 LDCM0325  AC61 HCT 116 C87(0.98)  LDD0642  [6]
 LDCM0326  AC62 HCT 116 C87(0.88)  LDD0643  [6]
 LDCM0327  AC63 HCT 116 C87(0.72)  LDD0644  [6]
 LDCM0328  AC64 HCT 116 C87(0.92)  LDD0645  [6]
 LDCM0329  AC65 HCT 116 C87(1.11)  LDD0646  [6]
 LDCM0330  AC66 HCT 116 C87(0.94)  LDD0647  [6]
 LDCM0331  AC67 HCT 116 C87(0.95)  LDD0648  [6]
 LDCM0332  AC68 HEK-293T C270(1.00)  LDD0930  [6]
 LDCM0333  AC69 HEK-293T C270(0.91)  LDD0931  [6]
 LDCM0334  AC7 HCT 116 C87(1.08)  LDD0651  [6]
 LDCM0335  AC70 HEK-293T C270(1.20)  LDD0933  [6]
 LDCM0336  AC71 HEK-293T C270(0.95)  LDD0934  [6]
 LDCM0337  AC72 HEK-293T C270(1.08)  LDD0935  [6]
 LDCM0338  AC73 HEK-293T C270(1.07)  LDD0936  [6]
 LDCM0339  AC74 HEK-293T C270(1.06)  LDD0937  [6]
 LDCM0340  AC75 HEK-293T C270(1.03)  LDD0938  [6]
 LDCM0341  AC76 HEK-293T C270(1.50)  LDD0939  [6]
 LDCM0342  AC77 HEK-293T C270(1.00)  LDD0940  [6]
 LDCM0343  AC78 HEK-293T C270(1.42)  LDD0941  [6]
 LDCM0344  AC79 HEK-293T C270(1.32)  LDD0942  [6]
 LDCM0345  AC8 HCT 116 C87(1.11)  LDD0662  [6]
 LDCM0346  AC80 HEK-293T C270(1.27)  LDD0944  [6]
 LDCM0347  AC81 HEK-293T C270(1.13)  LDD0945  [6]
 LDCM0348  AC82 HEK-293T C270(1.37)  LDD0946  [6]
 LDCM0349  AC83 HEK-293T C256(0.87); C270(0.52)  LDD0947  [6]
 LDCM0350  AC84 HEK-293T C256(0.82); C270(0.86)  LDD0948  [6]
 LDCM0351  AC85 HEK-293T C256(1.01); C270(0.59)  LDD0949  [6]
 LDCM0352  AC86 HEK-293T C256(1.00); C270(0.71)  LDD0950  [6]
 LDCM0353  AC87 HEK-293T C256(0.93); C270(0.89)  LDD0951  [6]
 LDCM0354  AC88 HEK-293T C256(0.79); C270(0.88)  LDD0952  [6]
 LDCM0355  AC89 HEK-293T C256(0.67); C270(1.00)  LDD0953  [6]
 LDCM0357  AC90 HEK-293T C256(0.89); C270(1.18)  LDD0955  [6]
 LDCM0358  AC91 HEK-293T C256(0.74); C270(0.43)  LDD0956  [6]
 LDCM0359  AC92 HEK-293T C256(0.81); C270(0.63)  LDD0957  [6]
 LDCM0360  AC93 HEK-293T C256(0.87); C270(0.86)  LDD0958  [6]
 LDCM0361  AC94 HEK-293T C256(0.58); C270(0.96)  LDD0959  [6]
 LDCM0362  AC95 HEK-293T C256(0.78); C270(0.78)  LDD0960  [6]
 LDCM0363  AC96 HEK-293T C256(1.18); C270(0.58)  LDD0961  [6]
 LDCM0364  AC97 HEK-293T C256(0.21); C270(0.67)  LDD0962  [6]
 LDCM0248  AKOS034007472 HCT 116 C87(0.98)  LDD0565  [6]
 LDCM0356  AKOS034007680 HCT 116 C87(0.98)  LDD0673  [6]
 LDCM0275  AKOS034007705 HCT 116 C87(1.20)  LDD0592  [6]
 LDCM0367  CL1 HCT 116 C87(0.73)  LDD0684  [6]
 LDCM0368  CL10 HCT 116 C87(0.73)  LDD0685  [6]
 LDCM0369  CL100 HCT 116 C87(0.99)  LDD0686  [6]
 LDCM0370  CL101 HCT 116 C87(0.88)  LDD0687  [6]
 LDCM0371  CL102 HCT 116 C87(0.93)  LDD0688  [6]
 LDCM0372  CL103 HCT 116 C87(0.98)  LDD0689  [6]
 LDCM0373  CL104 HCT 116 C87(1.01)  LDD0690  [6]
 LDCM0374  CL105 HCT 116 C87(0.77)  LDD0691  [6]
 LDCM0375  CL106 HCT 116 C87(0.77)  LDD0692  [6]
 LDCM0376  CL107 HCT 116 C87(0.92)  LDD0693  [6]
 LDCM0377  CL108 HCT 116 C87(0.98)  LDD0694  [6]
 LDCM0378  CL109 HCT 116 C87(0.94)  LDD0695  [6]
 LDCM0379  CL11 HCT 116 C87(0.68)  LDD0696  [6]
 LDCM0380  CL110 HCT 116 C87(0.79)  LDD0697  [6]
 LDCM0381  CL111 HCT 116 C87(0.79)  LDD0698  [6]
 LDCM0382  CL112 HCT 116 C87(0.99)  LDD0699  [6]
 LDCM0383  CL113 HCT 116 C87(0.92)  LDD0700  [6]
 LDCM0384  CL114 HCT 116 C87(0.91)  LDD0701  [6]
 LDCM0385  CL115 HCT 116 C87(0.93)  LDD0702  [6]
 LDCM0386  CL116 HCT 116 C87(1.02)  LDD0703  [6]
 LDCM0387  CL117 HCT 116 C87(1.00)  LDD0704  [6]
 LDCM0388  CL118 HCT 116 C87(0.94)  LDD0705  [6]
 LDCM0389  CL119 HCT 116 C87(1.00)  LDD0706  [6]
 LDCM0390  CL12 HCT 116 C87(0.89)  LDD0707  [6]
 LDCM0391  CL120 HCT 116 C87(0.98)  LDD0708  [6]
 LDCM0392  CL121 HCT 116 C87(1.04)  LDD0709  [6]
 LDCM0393  CL122 HCT 116 C87(0.93)  LDD0710  [6]
 LDCM0394  CL123 HCT 116 C87(1.03)  LDD0711  [6]
 LDCM0395  CL124 HCT 116 C87(0.86)  LDD0712  [6]
 LDCM0396  CL125 HCT 116 C87(1.08)  LDD0713  [6]
 LDCM0397  CL126 HCT 116 C87(0.60)  LDD0714  [6]
 LDCM0398  CL127 HCT 116 C87(0.88)  LDD0715  [6]
 LDCM0399  CL128 HCT 116 C87(1.06)  LDD0716  [6]
 LDCM0400  CL13 HCT 116 C87(0.80)  LDD0717  [6]
 LDCM0401  CL14 HCT 116 C87(0.86)  LDD0718  [6]
 LDCM0402  CL15 HCT 116 C87(0.96)  LDD0719  [6]
 LDCM0403  CL16 PaTu 8988t C87(0.83); C256(1.28); C270(1.28)  LDD1282  [6]
 LDCM0404  CL17 HCT 116 C87(0.98)  LDD0721  [6]
 LDCM0405  CL18 HCT 116 C87(1.13)  LDD0722  [6]
 LDCM0406  CL19 HCT 116 C87(1.13)  LDD0723  [6]
 LDCM0407  CL2 HCT 116 C87(0.78)  LDD0724  [6]
 LDCM0408  CL20 HCT 116 C87(1.04)  LDD0725  [6]
 LDCM0409  CL21 HCT 116 C87(1.02)  LDD0726  [6]
 LDCM0410  CL22 HCT 116 C87(0.80)  LDD0727  [6]
 LDCM0411  CL23 HCT 116 C87(0.83)  LDD0728  [6]
 LDCM0412  CL24 HCT 116 C87(1.06)  LDD0729  [6]
 LDCM0413  CL25 HCT 116 C87(1.03)  LDD0730  [6]
 LDCM0414  CL26 HCT 116 C87(0.85)  LDD0731  [6]
 LDCM0415  CL27 HCT 116 C87(0.88)  LDD0732  [6]
 LDCM0416  CL28 HCT 116 C87(0.86)  LDD0733  [6]
 LDCM0417  CL29 HCT 116 C87(0.83)  LDD0734  [6]
 LDCM0418  CL3 HCT 116 C87(0.95)  LDD0735  [6]
 LDCM0419  CL30 HCT 116 C87(0.87)  LDD0736  [6]
 LDCM0420  CL31 HCT 116 C87(1.05)  LDD0737  [6]
 LDCM0421  CL32 HEK-293T C256(1.05)  LDD1019  [6]
 LDCM0422  CL33 HEK-293T C256(0.80)  LDD1020  [6]
 LDCM0423  CL34 HEK-293T C256(0.85)  LDD1021  [6]
 LDCM0424  CL35 HEK-293T C256(1.04)  LDD1022  [6]
 LDCM0425  CL36 HEK-293T C256(0.87)  LDD1023  [6]
 LDCM0426  CL37 HEK-293T C256(0.88)  LDD1024  [6]
 LDCM0428  CL39 HEK-293T C256(0.35)  LDD1026  [6]
 LDCM0429  CL4 HCT 116 C87(0.69)  LDD0746  [6]
 LDCM0430  CL40 HEK-293T C256(0.74)  LDD1028  [6]
 LDCM0431  CL41 HEK-293T C256(0.47)  LDD1029  [6]
 LDCM0432  CL42 HEK-293T C256(0.38)  LDD1030  [6]
 LDCM0433  CL43 HEK-293T C256(0.40)  LDD1031  [6]
 LDCM0434  CL44 HEK-293T C256(0.98)  LDD1032  [6]
 LDCM0435  CL45 HEK-293T C256(0.50)  LDD1033  [6]
 LDCM0436  CL46 PaTu 8988t C156(0.65); C159(0.65); C87(0.82)  LDD1315  [6]
 LDCM0437  CL47 PaTu 8988t C156(0.56); C159(0.56); C87(1.00)  LDD1316  [6]
 LDCM0438  CL48 PaTu 8988t C156(1.22); C159(1.22); C87(0.84)  LDD1317  [6]
 LDCM0439  CL49 PaTu 8988t C156(0.87); C159(0.87); C87(0.93)  LDD1318  [6]
 LDCM0440  CL5 HCT 116 C87(0.93)  LDD0757  [6]
 LDCM0441  CL50 PaTu 8988t C156(1.12); C159(1.12); C87(1.05)  LDD1320  [6]
 LDCM0442  CL51 PaTu 8988t C156(0.82); C159(0.82); C87(0.88)  LDD1321  [6]
 LDCM0443  CL52 PaTu 8988t C156(0.71); C159(0.71); C87(0.79)  LDD1322  [6]
 LDCM0444  CL53 PaTu 8988t C156(0.84); C159(0.84); C87(0.88)  LDD1323  [6]
 LDCM0445  CL54 PaTu 8988t C156(0.93); C159(0.93); C87(1.31)  LDD1324  [6]
 LDCM0446  CL55 PaTu 8988t C156(0.75); C159(0.75); C87(0.89)  LDD1325  [6]
 LDCM0447  CL56 PaTu 8988t C156(0.71); C159(0.71); C87(0.70)  LDD1326  [6]
 LDCM0448  CL57 PaTu 8988t C156(1.08); C159(1.08); C87(1.02)  LDD1327  [6]
 LDCM0449  CL58 PaTu 8988t C156(0.84); C159(0.84); C87(0.88)  LDD1328  [6]
 LDCM0450  CL59 PaTu 8988t C156(0.95); C159(0.95); C87(0.94)  LDD1329  [6]
 LDCM0451  CL6 HCT 116 C87(0.81)  LDD0768  [6]
 LDCM0452  CL60 PaTu 8988t C156(0.88); C159(0.88); C87(0.81)  LDD1331  [6]
 LDCM0453  CL61 HEK-293T C87(1.06)  LDD1051  [6]
 LDCM0454  CL62 HEK-293T C87(0.97)  LDD1052  [6]
 LDCM0455  CL63 HEK-293T C87(1.06)  LDD1053  [6]
 LDCM0456  CL64 HEK-293T C87(0.95)  LDD1054  [6]
 LDCM0457  CL65 HEK-293T C87(0.94)  LDD1055  [6]
 LDCM0458  CL66 HEK-293T C87(1.11)  LDD1056  [6]
 LDCM0459  CL67 HEK-293T C87(1.10)  LDD1057  [6]
 LDCM0460  CL68 HEK-293T C87(1.05)  LDD1058  [6]
 LDCM0461  CL69 HEK-293T C87(1.03)  LDD1059  [6]
 LDCM0462  CL7 HCT 116 C87(0.82)  LDD0779  [6]
 LDCM0463  CL70 HEK-293T C87(1.01)  LDD1061  [6]
 LDCM0464  CL71 HEK-293T C87(1.14)  LDD1062  [6]
 LDCM0465  CL72 HEK-293T C87(1.21)  LDD1063  [6]
 LDCM0466  CL73 HEK-293T C87(0.94)  LDD1064  [6]
 LDCM0467  CL74 HEK-293T C87(1.01)  LDD1065  [6]
 LDCM0469  CL76 HCT 116 C87(0.85)  LDD0786  [6]
 LDCM0470  CL77 HCT 116 C87(0.95)  LDD0787  [6]
 LDCM0471  CL78 HCT 116 C87(0.99)  LDD0788  [6]
 LDCM0472  CL79 HCT 116 C87(1.03)  LDD0789  [6]
 LDCM0473  CL8 HCT 116 C87(0.89)  LDD0790  [6]
 LDCM0474  CL80 HCT 116 C87(1.09)  LDD0791  [6]
 LDCM0475  CL81 HCT 116 C87(0.94)  LDD0792  [6]
 LDCM0476  CL82 HCT 116 C87(0.94)  LDD0793  [6]
 LDCM0477  CL83 HCT 116 C87(0.88)  LDD0794  [6]
 LDCM0478  CL84 HCT 116 C87(1.23)  LDD0795  [6]
 LDCM0479  CL85 HCT 116 C87(0.97)  LDD0796  [6]
 LDCM0480  CL86 HCT 116 C87(1.00)  LDD0797  [6]
 LDCM0481  CL87 HCT 116 C87(0.99)  LDD0798  [6]
 LDCM0482  CL88 HCT 116 C87(1.00)  LDD0799  [6]
 LDCM0483  CL89 HCT 116 C87(0.99)  LDD0800  [6]
 LDCM0484  CL9 HCT 116 C87(0.75)  LDD0801  [6]
 LDCM0485  CL90 HCT 116 C87(0.79)  LDD0802  [6]
 LDCM0486  CL91 HCT 116 C87(1.12)  LDD0803  [6]
 LDCM0487  CL92 HCT 116 C87(0.96)  LDD0804  [6]
 LDCM0488  CL93 HCT 116 C87(0.96)  LDD0805  [6]
 LDCM0489  CL94 HCT 116 C87(0.96)  LDD0806  [6]
 LDCM0490  CL95 HCT 116 C87(1.02)  LDD0807  [6]
 LDCM0491  CL96 HCT 116 C87(1.16)  LDD0808  [6]
 LDCM0492  CL97 HCT 116 C87(1.04)  LDD0809  [6]
 LDCM0493  CL98 HCT 116 C87(1.04)  LDD0810  [6]
 LDCM0494  CL99 HCT 116 C87(1.11)  LDD0811  [6]
 LDCM0468  Fragment33 HEK-293T C87(0.97)  LDD1066  [6]
 LDCM0427  Fragment51 HEK-293T C256(1.13)  LDD1025  [6]
 LDCM0616  Fragment61 Jurkat _(20.00)  LDD1489  [4]
 LDCM0116  HHS-0101 DM93 Y34(0.60)  LDD0264  [5]
 LDCM0117  HHS-0201 DM93 Y34(0.49)  LDD0265  [5]
 LDCM0118  HHS-0301 DM93 Y34(0.49)  LDD0266  [5]
 LDCM0119  HHS-0401 DM93 Y34(0.58)  LDD0267  [5]
 LDCM0120  HHS-0701 DM93 Y34(0.80)  LDD0268  [5]
 LDCM0022  KB02 22RV1 C319(2.01)  LDD2243  [13]
 LDCM0023  KB03 22RV1 C319(3.41)  LDD2660  [13]
 LDCM0024  KB05 COLO792 C193(2.27)  LDD3310  [13]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Polyamine-transporting ATPase 13A2 (ATP13A2) Cation transport ATPase (P-type) (TC 3.A.3) family Q9NQ11

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Lx9211 . D05IQI

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 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
3 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.
4 Proteome-wide covalent ligand discovery in native biological systems. Nature. 2016 Jun 23;534(7608):570-4. doi: 10.1038/nature18002. Epub 2016 Jun 15.
5 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
6 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.
7 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
8 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
9 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
10 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.
11 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
12 Global profiling identifies a stress-responsive tyrosine site on EDC3 regulating biomolecular condensate formation. Cell Chem Biol. 2022 Dec 15;29(12):1709-1720.e7. doi: 10.1016/j.chembiol.2022.11.008. Epub 2022 Dec 6.
Mass spectrometry data entry: PXD038010
13 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