Details of the Target

General Information of Target

Target ID LDTP05137
Target Name Disintegrin and metalloproteinase domain-containing protein 17 (ADAM17)
Gene Name ADAM17
Gene ID 6868
Synonyms
CSVP; TACE; Disintegrin and metalloproteinase domain-containing protein 17; ADAM 17; EC 3.4.24.86; Snake venom-like protease; TNF-alpha convertase; TNF-alpha-converting enzyme; CD antigen CD156b
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MRQSLLFLTSVVPFVLAPRPPDDPGFGPHQRLEKLDSLLSDYDILSLSNIQQHSVRKRDL
QTSTHVETLLTFSALKRHFKLYLTSSTERFSQNFKVVVVDGKNESEYTVKWQDFFTGHVV
GEPDSRVLAHIRDDDVIIRINTDGAEYNIEPLWRFVNDTKDKRMLVYKSEDIKNVSRLQS
PKVCGYLKVDNEELLPKGLVDREPPEELVHRVKRRADPDPMKNTCKLLVVADHRFYRYMG
RGEESTTTNYLIELIDRVDDIYRNTSWDNAGFKGYGIQIEQIRILKSPQEVKPGEKHYNM
AKSYPNEEKDAWDVKMLLEQFSFDIAEEASKVCLAHLFTYQDFDMGTLGLAYVGSPRANS
HGGVCPKAYYSPVGKKNIYLNSGLTSTKNYGKTILTKEADLVTTHELGHNFGAEHDPDGL
AECAPNEDQGGKYVMYPIAVSGDHENNKMFSNCSKQSIYKTIESKAQECFQERSNKVCGN
SRVDEGEECDPGIMYLNNDTCCNSDCTLKEGVQCSDRNSPCCKNCQFETAQKKCQEAINA
TCKGVSYCTGNSSECPPPGNAEDDTVCLDLGKCKDGKCIPFCEREQQLESCACNETDNSC
KVCCRDLSGRCVPYVDAEQKNLFLRKGKPCTVGFCDMNGKCEKRVQDVIERFWDFIDQLS
INTFGKFLADNIVGSVLVFSLIFWIPFSILVHCVDKKLDKQYESLSLFHPSNVEMLSSMD
SASVRIIKPFPAPQTPGRLQPAPVIPSAPAAPKLDHQRMDTIQEDPSTDSHMDEDGFEKD
PFPNSSTAAKSFEDLTDHPVTRSEKAASFKLQRQNRVDSKETEC
Target Type
Clinical trial
Target Bioclass
Enzyme
Subcellular location
Membrane
Function
Cleaves the membrane-bound precursor of TNF-alpha to its mature soluble form. Responsible for the proteolytical release of soluble JAM3 from endothelial cells surface. Responsible for the proteolytic release of several other cell-surface proteins, including p75 TNF-receptor, interleukin 1 receptor type II, p55 TNF-receptor, transforming growth factor-alpha, L-selectin, growth hormone receptor, MUC1 and the amyloid precursor protein. Acts as an activator of Notch pathway by mediating cleavage of Notch, generating the membrane-associated intermediate fragment called Notch extracellular truncation (NEXT). Plays a role in the proteolytic processing of ACE2. Plays a role in hemostasis through shedding of GP1BA, the platelet glycoprotein Ib alpha chain. Mediates the proteolytic cleavage of LAG3, leading to release the secreted form of LAG3. Mediates the proteolytic cleavage of IL6R, leading to the release of secreted form of IL6R. Mediates the proteolytic cleavage and shedding of FCGR3A upon NK cell stimulation, a mechanism that allows for increased NK cell motility and detachment from opsonized target cells.
TTD ID
T82393
Uniprot ID
P78536
DrugMap ID
TT6AZXG
Ensemble ID
ENST00000310823.8
HGNC ID
HGNC:195
ChEMBL ID
CHEMBL3706

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
ABC1 SNV: p.E583Ter DBIA    Probe Info 
CAL33 SNV: p.G242E DBIA    Probe Info 
COLO800 SNV: p.S40P .
EFO27 SNV: p.E583K DBIA    Probe Info 
JVM3 SNV: p.C423Y .
KMS11 SNV: p.K820R .
MKN45 SNV: p.S546F .
NCIH23 SNV: p.H336L .
NUGC3 SNV: p.N447S DBIA    Probe Info 
WM1552C SNV: p.Q763H .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 10 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FBPP2
 Probe Info  		2.86  LDD0318  [1]
STPyne
 Probe Info  		K810(6.67)  LDD0277  [2]
IPM
 Probe Info  		N.A.  LDD0241  [3]
Probe 1
 Probe Info  		Y369(24.92)  LDD3495  [4]
BTD
 Probe Info  		C365(0.55)  LDD2089  [5]
DBIA
 Probe Info  		C469(0.99)  LDD0078  [6]
IA-alkyne
 Probe Info  		C365(0.00); C469(0.00); C514(0.00); C525(0.00)  LDD0162  [7]
WYneO
 Probe Info  		C469(0.00); C365(0.00)  LDD0022  [8]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [9]
NAIA_5
 Probe Info  		C365(0.00); C611(0.00); C478(0.00)  LDD2223  [10]
PAL-AfBPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C056
 Probe Info  		16.68  LDD1753  [11]
C112
 Probe Info  		26.54  LDD1799  [11]
C407
 Probe Info  		15.03  LDD2064  [11]

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 C469(0.76)  LDD2117  [5]
 LDCM0214  AC1 HCT 116 C365(0.92); C469(1.39)  LDD0531  [6]
 LDCM0215  AC10 HCT 116 C365(1.29); C469(1.05)  LDD0532  [6]
 LDCM0216  AC100 HCT 116 C469(1.08)  LDD0533  [6]
 LDCM0217  AC101 HCT 116 C469(1.09)  LDD0534  [6]
 LDCM0218  AC102 HCT 116 C469(0.93)  LDD0535  [6]
 LDCM0219  AC103 HCT 116 C469(0.97)  LDD0536  [6]
 LDCM0220  AC104 HCT 116 C469(1.03)  LDD0537  [6]
 LDCM0221  AC105 HCT 116 C469(1.20)  LDD0538  [6]
 LDCM0222  AC106 HCT 116 C469(1.05)  LDD0539  [6]
 LDCM0223  AC107 HCT 116 C469(1.13)  LDD0540  [6]
 LDCM0224  AC108 HCT 116 C469(0.90)  LDD0541  [6]
 LDCM0225  AC109 HCT 116 C469(0.95)  LDD0542  [6]
 LDCM0226  AC11 HCT 116 C365(1.32); C469(1.57)  LDD0543  [6]
 LDCM0227  AC110 HCT 116 C469(1.09)  LDD0544  [6]
 LDCM0228  AC111 HCT 116 C469(1.36)  LDD0545  [6]
 LDCM0229  AC112 HCT 116 C469(1.16)  LDD0546  [6]
 LDCM0230  AC113 HCT 116 C469(0.70)  LDD0547  [6]
 LDCM0231  AC114 HCT 116 C469(0.73)  LDD0548  [6]
 LDCM0232  AC115 HCT 116 C469(0.92)  LDD0549  [6]
 LDCM0233  AC116 HCT 116 C469(0.74)  LDD0550  [6]
 LDCM0234  AC117 HCT 116 C469(0.71)  LDD0551  [6]
 LDCM0235  AC118 HCT 116 C469(0.54)  LDD0552  [6]
 LDCM0236  AC119 HCT 116 C469(0.63)  LDD0553  [6]
 LDCM0237  AC12 HCT 116 C365(0.97); C469(1.04)  LDD0554  [6]
 LDCM0238  AC120 HCT 116 C469(0.78)  LDD0555  [6]
 LDCM0239  AC121 HCT 116 C469(0.63)  LDD0556  [6]
 LDCM0240  AC122 HCT 116 C469(0.74)  LDD0557  [6]
 LDCM0241  AC123 HCT 116 C469(0.65)  LDD0558  [6]
 LDCM0242  AC124 HCT 116 C469(0.64)  LDD0559  [6]
 LDCM0243  AC125 HCT 116 C469(0.86)  LDD0560  [6]
 LDCM0244  AC126 HCT 116 C469(0.62)  LDD0561  [6]
 LDCM0245  AC127 HCT 116 C469(0.61)  LDD0562  [6]
 LDCM0246  AC128 HCT 116 C365(1.12); C469(0.59)  LDD0563  [6]
 LDCM0247  AC129 HCT 116 C365(0.80); C469(0.44)  LDD0564  [6]
 LDCM0249  AC130 HCT 116 C365(1.15); C469(0.43)  LDD0566  [6]
 LDCM0250  AC131 HCT 116 C365(0.85); C469(0.50)  LDD0567  [6]
 LDCM0251  AC132 HCT 116 C365(0.87); C469(0.72)  LDD0568  [6]
 LDCM0252  AC133 HCT 116 C365(0.99); C469(0.49)  LDD0569  [6]
 LDCM0253  AC134 HCT 116 C365(1.05); C469(0.49)  LDD0570  [6]
 LDCM0254  AC135 HCT 116 C365(1.05); C469(0.67)  LDD0571  [6]
 LDCM0255  AC136 HCT 116 C365(1.05); C469(0.50)  LDD0572  [6]
 LDCM0256  AC137 HCT 116 C365(1.07); C469(0.65)  LDD0573  [6]
 LDCM0257  AC138 HCT 116 C365(0.99); C469(0.72)  LDD0574  [6]
 LDCM0258  AC139 HCT 116 C365(1.04); C469(0.68)  LDD0575  [6]
 LDCM0259  AC14 HCT 116 C365(1.11); C469(1.27)  LDD0576  [6]
 LDCM0260  AC140 HCT 116 C365(1.07); C469(0.64)  LDD0577  [6]
 LDCM0261  AC141 HCT 116 C365(1.01); C469(0.83)  LDD0578  [6]
 LDCM0262  AC142 HCT 116 C365(0.88); C469(0.49)  LDD0579  [6]
 LDCM0263  AC143 HCT 116 C469(1.07)  LDD0580  [6]
 LDCM0264  AC144 HCT 116 C469(0.88)  LDD0581  [6]
 LDCM0265  AC145 HCT 116 C469(0.78)  LDD0582  [6]
 LDCM0266  AC146 HCT 116 C469(0.90)  LDD0583  [6]
 LDCM0267  AC147 HCT 116 C469(0.87)  LDD0584  [6]
 LDCM0268  AC148 HCT 116 C469(0.69)  LDD0585  [6]
 LDCM0269  AC149 HCT 116 C469(0.76)  LDD0586  [6]
 LDCM0270  AC15 HCT 116 C469(1.04); C365(1.26)  LDD0587  [6]
 LDCM0271  AC150 HCT 116 C469(0.78)  LDD0588  [6]
 LDCM0272  AC151 HCT 116 C469(0.72)  LDD0589  [6]
 LDCM0273  AC152 HCT 116 C469(0.79)  LDD0590  [6]
 LDCM0274  AC153 HCT 116 C469(0.58)  LDD0591  [6]
 LDCM0621  AC154 HCT 116 C469(0.74)  LDD2158  [6]
 LDCM0622  AC155 HCT 116 C469(0.78)  LDD2159  [6]
 LDCM0623  AC156 HCT 116 C469(0.78)  LDD2160  [6]
 LDCM0624  AC157 HCT 116 C469(0.67)  LDD2161  [6]
 LDCM0276  AC17 HCT 116 C469(1.27)  LDD0593  [6]
 LDCM0277  AC18 HCT 116 C469(1.04)  LDD0594  [6]
 LDCM0278  AC19 HCT 116 C469(1.24)  LDD0595  [6]
 LDCM0279  AC2 HCT 116 C365(0.91); C469(1.22)  LDD0596  [6]
 LDCM0280  AC20 HCT 116 C469(1.32)  LDD0597  [6]
 LDCM0281  AC21 HCT 116 C469(1.41)  LDD0598  [6]
 LDCM0282  AC22 HCT 116 C469(1.44)  LDD0599  [6]
 LDCM0283  AC23 HCT 116 C469(1.26)  LDD0600  [6]
 LDCM0284  AC24 HCT 116 C469(1.14)  LDD0601  [6]
 LDCM0285  AC25 HCT 116 C469(0.99)  LDD0602  [6]
 LDCM0286  AC26 HCT 116 C469(0.84)  LDD0603  [6]
 LDCM0287  AC27 HCT 116 C469(0.65)  LDD0604  [6]
 LDCM0288  AC28 HCT 116 C469(0.70)  LDD0605  [6]
 LDCM0289  AC29 HCT 116 C469(0.72)  LDD0606  [6]
 LDCM0290  AC3 HCT 116 C365(0.81); C469(1.16)  LDD0607  [6]
 LDCM0291  AC30 HCT 116 C469(0.78)  LDD0608  [6]
 LDCM0292  AC31 HCT 116 C469(0.63)  LDD0609  [6]
 LDCM0293  AC32 HCT 116 C469(1.01)  LDD0610  [6]
 LDCM0294  AC33 HCT 116 C469(0.74)  LDD0611  [6]
 LDCM0295  AC34 HCT 116 C469(1.14)  LDD0612  [6]
 LDCM0296  AC35 HCT 116 C469(1.30)  LDD0613  [6]
 LDCM0297  AC36 HCT 116 C469(1.30)  LDD0614  [6]
 LDCM0298  AC37 HCT 116 C469(1.57)  LDD0615  [6]
 LDCM0299  AC38 HCT 116 C469(1.70)  LDD0616  [6]
 LDCM0300  AC39 HCT 116 C469(0.86)  LDD0617  [6]
 LDCM0301  AC4 HCT 116 C365(0.96); C469(1.29)  LDD0618  [6]
 LDCM0302  AC40 HCT 116 C469(1.29)  LDD0619  [6]
 LDCM0303  AC41 HCT 116 C469(1.92)  LDD0620  [6]
 LDCM0304  AC42 HCT 116 C469(1.78)  LDD0621  [6]
 LDCM0305  AC43 HCT 116 C469(1.19)  LDD0622  [6]
 LDCM0306  AC44 HCT 116 C469(1.23)  LDD0623  [6]
 LDCM0307  AC45 HCT 116 C469(1.73)  LDD0624  [6]
 LDCM0308  AC46 HEK-293T C469(1.12)  LDD0906  [6]
 LDCM0309  AC47 HEK-293T C469(1.19)  LDD0907  [6]
 LDCM0310  AC48 HEK-293T C469(1.37)  LDD0908  [6]
 LDCM0311  AC49 HEK-293T C469(1.32)  LDD0909  [6]
 LDCM0312  AC5 HCT 116 C365(0.96); C469(1.34)  LDD0629  [6]
 LDCM0313  AC50 HEK-293T C469(1.20)  LDD0911  [6]
 LDCM0314  AC51 HEK-293T C469(1.59)  LDD0912  [6]
 LDCM0315  AC52 HEK-293T C469(1.64)  LDD0913  [6]
 LDCM0316  AC53 HEK-293T C469(1.07)  LDD0914  [6]
 LDCM0317  AC54 HEK-293T C469(1.47)  LDD0915  [6]
 LDCM0318  AC55 HEK-293T C469(1.40)  LDD0916  [6]
 LDCM0319  AC56 HEK-293T C469(1.23)  LDD0917  [6]
 LDCM0320  AC57 HCT 116 C469(1.63)  LDD0637  [6]
 LDCM0321  AC58 HCT 116 C469(1.43)  LDD0638  [6]
 LDCM0322  AC59 HCT 116 C469(1.23)  LDD0639  [6]
 LDCM0323  AC6 HCT 116 C365(1.05); C469(1.57)  LDD0640  [6]
 LDCM0324  AC60 HCT 116 C469(1.51)  LDD0641  [6]
 LDCM0325  AC61 HCT 116 C469(1.67)  LDD0642  [6]
 LDCM0326  AC62 HCT 116 C469(1.28)  LDD0643  [6]
 LDCM0327  AC63 HCT 116 C469(1.61)  LDD0644  [6]
 LDCM0328  AC64 HCT 116 C469(1.22)  LDD0645  [6]
 LDCM0329  AC65 HCT 116 C469(1.42)  LDD0646  [6]
 LDCM0330  AC66 HCT 116 C469(1.42)  LDD0647  [6]
 LDCM0331  AC67 HCT 116 C469(1.29)  LDD0648  [6]
 LDCM0332  AC68 HCT 116 C469(1.04)  LDD0649  [6]
 LDCM0333  AC69 HCT 116 C469(1.09)  LDD0650  [6]
 LDCM0334  AC7 HCT 116 C365(1.07); C469(1.26)  LDD0651  [6]
 LDCM0335  AC70 HCT 116 C469(1.40)  LDD0652  [6]
 LDCM0336  AC71 HCT 116 C469(0.95)  LDD0653  [6]
 LDCM0337  AC72 HCT 116 C469(1.29)  LDD0654  [6]
 LDCM0338  AC73 HCT 116 C469(1.35)  LDD0655  [6]
 LDCM0339  AC74 HCT 116 C469(1.01)  LDD0656  [6]
 LDCM0340  AC75 HCT 116 C469(1.34)  LDD0657  [6]
 LDCM0341  AC76 HCT 116 C469(0.91)  LDD0658  [6]
 LDCM0342  AC77 HCT 116 C469(1.14)  LDD0659  [6]
 LDCM0343  AC78 HCT 116 C469(1.20)  LDD0660  [6]
 LDCM0344  AC79 HCT 116 C469(1.35)  LDD0661  [6]
 LDCM0345  AC8 HCT 116 C469(1.22); C365(1.23)  LDD0662  [6]
 LDCM0346  AC80 HCT 116 C469(0.98)  LDD0663  [6]
 LDCM0347  AC81 HCT 116 C469(1.10)  LDD0664  [6]
 LDCM0348  AC82 HCT 116 C469(1.09)  LDD0665  [6]
 LDCM0349  AC83 HCT 116 C469(1.41)  LDD0666  [6]
 LDCM0350  AC84 HCT 116 C469(1.37)  LDD0667  [6]
 LDCM0351  AC85 HCT 116 C469(1.49)  LDD0668  [6]
 LDCM0352  AC86 HCT 116 C469(1.33)  LDD0669  [6]
 LDCM0353  AC87 HCT 116 C469(1.09)  LDD0670  [6]
 LDCM0354  AC88 HCT 116 C469(1.07)  LDD0671  [6]
 LDCM0355  AC89 HCT 116 C469(0.93)  LDD0672  [6]
 LDCM0357  AC90 HCT 116 C469(1.09)  LDD0674  [6]
 LDCM0358  AC91 HCT 116 C469(1.24)  LDD0675  [6]
 LDCM0359  AC92 HCT 116 C469(1.15)  LDD0676  [6]
 LDCM0360  AC93 HCT 116 C469(1.24)  LDD0677  [6]
 LDCM0361  AC94 HCT 116 C469(1.08)  LDD0678  [6]
 LDCM0362  AC95 HCT 116 C469(1.02)  LDD0679  [6]
 LDCM0363  AC96 HCT 116 C469(1.46)  LDD0680  [6]
 LDCM0364  AC97 HCT 116 C469(1.08)  LDD0681  [6]
 LDCM0365  AC98 HCT 116 C469(1.02)  LDD0682  [6]
 LDCM0366  AC99 HCT 116 C469(0.92)  LDD0683  [6]
 LDCM0248  AKOS034007472 HCT 116 C365(0.99); C469(1.00)  LDD0565  [6]
 LDCM0356  AKOS034007680 HCT 116 C365(1.04); C469(1.06)  LDD0673  [6]
 LDCM0275  AKOS034007705 HCT 116 C365(1.34); C469(1.85)  LDD0592  [6]
 LDCM0020  ARS-1620 HCC44 C469(0.99)  LDD0078  [6]
 LDCM0367  CL1 HCT 116 C469(0.77); C365(0.91)  LDD0684  [6]
 LDCM0368  CL10 HCT 116 C469(0.59); C365(0.85)  LDD0685  [6]
 LDCM0369  CL100 HCT 116 C365(0.96); C469(1.46)  LDD0686  [6]
 LDCM0370  CL101 HCT 116 C469(1.45); C365(1.46)  LDD0687  [6]
 LDCM0371  CL102 HCT 116 C365(1.03); C469(1.50)  LDD0688  [6]
 LDCM0372  CL103 HCT 116 C365(1.12); C469(1.86)  LDD0689  [6]
 LDCM0373  CL104 HCT 116 C365(1.14); C469(1.80)  LDD0690  [6]
 LDCM0374  CL105 HCT 116 C469(1.28)  LDD0691  [6]
 LDCM0375  CL106 HCT 116 C469(1.51)  LDD0692  [6]
 LDCM0376  CL107 HCT 116 C469(1.15)  LDD0693  [6]
 LDCM0377  CL108 HCT 116 C469(1.63)  LDD0694  [6]
 LDCM0378  CL109 HCT 116 C469(1.12)  LDD0695  [6]
 LDCM0379  CL11 HCT 116 C365(0.89); C469(1.91)  LDD0696  [6]
 LDCM0380  CL110 HCT 116 C469(1.04)  LDD0697  [6]
 LDCM0381  CL111 HCT 116 C469(1.20)  LDD0698  [6]
 LDCM0382  CL112 HCT 116 C469(1.45)  LDD0699  [6]
 LDCM0383  CL113 HCT 116 C469(0.68)  LDD0700  [6]
 LDCM0384  CL114 HCT 116 C469(1.02)  LDD0701  [6]
 LDCM0385  CL115 HCT 116 C469(0.72)  LDD0702  [6]
 LDCM0386  CL116 HCT 116 C469(0.88)  LDD0703  [6]
 LDCM0387  CL117 HCT 116 C469(1.11)  LDD0704  [6]
 LDCM0388  CL118 HCT 116 C469(1.26)  LDD0705  [6]
 LDCM0389  CL119 HCT 116 C469(2.26)  LDD0706  [6]
 LDCM0390  CL12 HCT 116 C469(0.66); C365(0.72)  LDD0707  [6]
 LDCM0391  CL120 HCT 116 C469(0.87)  LDD0708  [6]
 LDCM0392  CL121 HEK-293T C469(1.32)  LDD0990  [6]
 LDCM0393  CL122 HEK-293T C469(1.22)  LDD0991  [6]
 LDCM0394  CL123 HEK-293T C469(1.39)  LDD0992  [6]
 LDCM0395  CL124 HEK-293T C469(1.19)  LDD0993  [6]
 LDCM0396  CL125 HCT 116 C469(1.49)  LDD0713  [6]
 LDCM0397  CL126 HCT 116 C469(1.36)  LDD0714  [6]
 LDCM0398  CL127 HCT 116 C469(1.23)  LDD0715  [6]
 LDCM0399  CL128 HCT 116 C469(1.68)  LDD0716  [6]
 LDCM0400  CL13 HCT 116 C469(0.53); C365(0.77)  LDD0717  [6]
 LDCM0401  CL14 HCT 116 C469(0.57); C365(0.76)  LDD0718  [6]
 LDCM0402  CL15 HCT 116 C469(0.72); C365(0.75)  LDD0719  [6]
 LDCM0403  CL16 HCT 116 C469(1.07)  LDD0720  [6]
 LDCM0404  CL17 HCT 116 C469(1.02)  LDD0721  [6]
 LDCM0405  CL18 HCT 116 C469(1.21)  LDD0722  [6]
 LDCM0406  CL19 HCT 116 C469(1.07)  LDD0723  [6]
 LDCM0407  CL2 HCT 116 C469(0.83); C365(0.93)  LDD0724  [6]
 LDCM0408  CL20 HCT 116 C469(1.22)  LDD0725  [6]
 LDCM0409  CL21 HCT 116 C469(1.16)  LDD0726  [6]
 LDCM0410  CL22 HCT 116 C469(1.42)  LDD0727  [6]
 LDCM0411  CL23 HCT 116 C469(0.93)  LDD0728  [6]
 LDCM0412  CL24 HCT 116 C469(1.15)  LDD0729  [6]
 LDCM0413  CL25 HCT 116 C469(1.04)  LDD0730  [6]
 LDCM0414  CL26 HCT 116 C469(1.16)  LDD0731  [6]
 LDCM0415  CL27 HCT 116 C469(1.41)  LDD0732  [6]
 LDCM0416  CL28 HCT 116 C469(1.27)  LDD0733  [6]
 LDCM0417  CL29 HCT 116 C469(1.12)  LDD0734  [6]
 LDCM0418  CL3 HCT 116 C365(0.84); C469(0.90)  LDD0735  [6]
 LDCM0419  CL30 HCT 116 C469(1.07)  LDD0736  [6]
 LDCM0420  CL31 HCT 116 C365(0.98); C469(0.70)  LDD0737  [6]
 LDCM0421  CL32 HCT 116 C365(1.08); C469(1.00)  LDD0738  [6]
 LDCM0422  CL33 HCT 116 C365(1.12); C469(1.19)  LDD0739  [6]
 LDCM0423  CL34 HCT 116 C365(1.05); C469(0.99)  LDD0740  [6]
 LDCM0424  CL35 HCT 116 C365(1.05); C469(0.99)  LDD0741  [6]
 LDCM0425  CL36 HCT 116 C365(1.09); C469(0.60)  LDD0742  [6]
 LDCM0426  CL37 HCT 116 C365(0.95); C469(0.73)  LDD0743  [6]
 LDCM0428  CL39 HCT 116 C365(1.00); C469(1.01)  LDD0745  [6]
 LDCM0429  CL4 HCT 116 C365(1.00); C469(0.68)  LDD0746  [6]
 LDCM0430  CL40 HCT 116 C365(0.97); C469(0.76)  LDD0747  [6]
 LDCM0431  CL41 HCT 116 C365(0.97); C469(0.97)  LDD0748  [6]
 LDCM0432  CL42 HCT 116 C365(1.05); C469(0.89)  LDD0749  [6]
 LDCM0433  CL43 HCT 116 C365(1.05); C469(0.93)  LDD0750  [6]
 LDCM0434  CL44 HCT 116 C365(1.09); C469(0.76)  LDD0751  [6]
 LDCM0435  CL45 HCT 116 C365(0.97); C469(0.89)  LDD0752  [6]
 LDCM0436  CL46 HCT 116 C365(1.05); C469(1.41)  LDD0753  [6]
 LDCM0437  CL47 HCT 116 C365(1.02); C469(1.29)  LDD0754  [6]
 LDCM0438  CL48 HCT 116 C365(1.01); C469(1.20)  LDD0755  [6]
 LDCM0439  CL49 HCT 116 C365(1.01); C469(0.98)  LDD0756  [6]
 LDCM0440  CL5 HCT 116 C365(0.74); C469(0.55)  LDD0757  [6]
 LDCM0441  CL50 HCT 116 C365(0.93); C469(1.24)  LDD0758  [6]
 LDCM0442  CL51 HCT 116 C365(1.05); C469(1.06)  LDD0759  [6]
 LDCM0443  CL52 HCT 116 C365(0.94); C469(1.10)  LDD0760  [6]
 LDCM0444  CL53 HCT 116 C365(0.91); C469(1.12)  LDD0761  [6]
 LDCM0445  CL54 HCT 116 C365(1.00); C469(0.96)  LDD0762  [6]
 LDCM0446  CL55 HCT 116 C365(0.96); C469(0.87)  LDD0763  [6]
 LDCM0447  CL56 HCT 116 C365(0.86); C469(0.89)  LDD0764  [6]
 LDCM0448  CL57 HCT 116 C365(0.89); C469(0.95)  LDD0765  [6]
 LDCM0449  CL58 HCT 116 C365(0.89); C469(0.88)  LDD0766  [6]
 LDCM0450  CL59 HCT 116 C365(0.91); C469(0.79)  LDD0767  [6]
 LDCM0451  CL6 HCT 116 C365(0.82); C469(0.81)  LDD0768  [6]
 LDCM0452  CL60 HCT 116 C365(0.91); C469(1.09)  LDD0769  [6]
 LDCM0453  CL61 HCT 116 C469(0.55)  LDD0770  [6]
 LDCM0454  CL62 HCT 116 C469(0.92)  LDD0771  [6]
 LDCM0455  CL63 HCT 116 C469(0.89)  LDD0772  [6]
 LDCM0456  CL64 HCT 116 C469(0.56)  LDD0773  [6]
 LDCM0457  CL65 HCT 116 C469(0.51)  LDD0774  [6]
 LDCM0458  CL66 HCT 116 C469(0.62)  LDD0775  [6]
 LDCM0459  CL67 HCT 116 C469(1.41)  LDD0776  [6]
 LDCM0460  CL68 HCT 116 C469(0.95)  LDD0777  [6]
 LDCM0461  CL69 HCT 116 C469(0.66)  LDD0778  [6]
 LDCM0462  CL7 HCT 116 C365(0.73); C469(0.45)  LDD0779  [6]
 LDCM0463  CL70 HCT 116 C469(0.83)  LDD0780  [6]
 LDCM0464  CL71 HCT 116 C469(0.89)  LDD0781  [6]
 LDCM0465  CL72 HCT 116 C469(1.01)  LDD0782  [6]
 LDCM0466  CL73 HCT 116 C469(0.88)  LDD0783  [6]
 LDCM0467  CL74 HCT 116 C469(0.78)  LDD0784  [6]
 LDCM0469  CL76 HCT 116 C365(1.13); C469(1.56)  LDD0786  [6]
 LDCM0470  CL77 HCT 116 C365(1.18); C469(2.90)  LDD0787  [6]
 LDCM0471  CL78 HCT 116 C365(1.12); C469(1.51)  LDD0788  [6]
 LDCM0472  CL79 HCT 116 C365(1.22); C469(1.34)  LDD0789  [6]
 LDCM0473  CL8 HCT 116 C365(1.09); C469(0.45)  LDD0790  [6]
 LDCM0474  CL80 HCT 116 C365(1.06); C469(1.06)  LDD0791  [6]
 LDCM0475  CL81 HCT 116 C365(1.18); C469(1.22)  LDD0792  [6]
 LDCM0476  CL82 HCT 116 C365(1.51); C469(1.02)  LDD0793  [6]
 LDCM0477  CL83 HCT 116 C365(1.43); C469(1.57)  LDD0794  [6]
 LDCM0478  CL84 HCT 116 C365(1.53); C469(1.05)  LDD0795  [6]
 LDCM0479  CL85 HCT 116 C365(1.11); C469(1.28)  LDD0796  [6]
 LDCM0480  CL86 HCT 116 C365(1.06); C469(0.98)  LDD0797  [6]
 LDCM0481  CL87 HCT 116 C365(1.37); C469(1.22)  LDD0798  [6]
 LDCM0482  CL88 HCT 116 C365(1.23); C469(1.11)  LDD0799  [6]
 LDCM0483  CL89 HCT 116 C365(1.50); C469(1.49)  LDD0800  [6]
 LDCM0484  CL9 HCT 116 C365(0.74); C469(0.65)  LDD0801  [6]
 LDCM0485  CL90 HCT 116 C365(1.10); C469(1.03)  LDD0802  [6]
 LDCM0486  CL91 HCT 116 C365(1.02); C469(1.15)  LDD0803  [6]
 LDCM0487  CL92 HCT 116 C365(1.20); C469(0.99)  LDD0804  [6]
 LDCM0488  CL93 HCT 116 C365(1.07); C469(1.32)  LDD0805  [6]
 LDCM0489  CL94 HCT 116 C365(1.17); C469(1.09)  LDD0806  [6]
 LDCM0490  CL95 HCT 116 C365(1.17); C469(1.06)  LDD0807  [6]
 LDCM0491  CL96 HCT 116 C365(1.04); C469(1.00)  LDD0808  [6]
 LDCM0492  CL97 HCT 116 C365(1.04); C469(1.30)  LDD0809  [6]
 LDCM0493  CL98 HCT 116 C365(1.01); C469(1.00)  LDD0810  [6]
 LDCM0494  CL99 HCT 116 C365(1.04); C469(0.99)  LDD0811  [6]
 LDCM0495  E2913 HEK-293T C365(1.11); C469(0.90)  LDD1698  [12]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C184(2.35); C365(1.19)  LDD1702  [5]
 LDCM0625  F8 Ramos C365(2.19)  LDD2187  [13]
 LDCM0576  Fragment14 Ramos C365(2.20)  LDD2193  [13]
 LDCM0582  Fragment23 Ramos C365(0.48)  LDD2196  [13]
 LDCM0468  Fragment33 HCT 116 C469(0.68)  LDD0785  [6]
 LDCM0427  Fragment51 HCT 116 C365(1.08); C469(1.07)  LDD0744  [6]
 LDCM0022  KB02 HCT 116 C469(1.25)  LDD0080  [6]
 LDCM0023  KB03 HCT 116 C469(1.05)  LDD0081  [6]
 LDCM0024  KB05 HCT 116 C469(1.37)  LDD0082  [6]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C365(0.55)  LDD2089  [5]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C469(1.09)  LDD2107  [5]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C365(0.87)  LDD2111  [5]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C184(0.78)  LDD2115  [5]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C469(1.10)  LDD2127  [5]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C469(1.60)  LDD2136  [5]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C469(1.09)  LDD2137  [5]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C365(1.00)  LDD2140  [5]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C184(0.22)  LDD2145  [5]
 LDCM0021  THZ1 HCT 116 C469(1.26); C365(0.90)  LDD2173  [6]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Integrin beta-1 (ITGB1) Integrin beta chain family P05556
Disks large homolog 1 (DLG1) MAGUK family Q12959
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Mitotic spindle assembly checkpoint protein MAD2A (MAD2L1) MAD2 family Q13257

The Drug(s) Related To This Target

Phase 2
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Aderbasib Small molecular drug D02CZF
Apratastat Small molecular drug D0HG5M
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gw-3333 Small molecular drug D03ESO
Investigative
Click To Hide/Show 21 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(2r)-n-hydroxy-2-[(3s)-3-methyl-3-{4-[(2-methylquinolin-4-yl)Methoxy]Phenyl}-2-oxopyrrolidin-1-yl]Propanamide Small molecular drug DB07145
2-(4-bromophenylsulfonamido)-n-hydroxyacetamide Small molecular drug D0NV9C
2-(Biphenyl-4-ylsulfonamido)-n-hydroxyacetamide Small molecular drug D09ZOA
Ch4474 Small molecular drug D0DD7N
Ik-862 Small molecular drug D0W2UK
Im-491 Small molecular drug D04WWO
N-hydroxy-2-(4-methoxyphenylsulfonamido)Acetamide Small molecular drug D0XK7G
N-hydroxy-3-(2-oxo-2h-chromen-3-yl)Propanamide Small molecular drug D00RNA
N-hydroxy-3-(6-methoxy-2-oxo-2h-chromen-3-yl) Small molecular drug D08ICI
Pkf-241-466 Small molecular drug D02UYR
Pkf-242-484 Small molecular drug D0H2PA
Sl422 Small molecular drug D07GEL
Sr-973 Small molecular drug D03AMR
(1s3r6s)-4-oxo-6-{4-[(2-phenylquinolin-4-yl)Methoxy]Phenyl}-5-azaspiro[2.4]Heptane-1-carboxylic Acid . DB07189
(3s)-1-{[4-(But-2-yn-1-yloxy)Phenyl]Sulfonyl}Pyrrolidine-3-thiol . DB06943
(3s)-4-{[4-(But-2-ynyloxy)Phenyl]Sulfonyl}-n-hydroxy-22-dimethylthiomorpholine-3-carboxamide . DB07964
3-{[4-(But-2-yn-1-yloxy)Phenyl]Sulfonyl}Propane-1-thiol . DB07079
4-({4-[(4-aminobut-2-ynyl)Oxy]Phenyl}Sulfonyl)-n-hydroxy-22-dimethylthiomorpholine-3-carboxamide . DB07121
Batimistat . D08VFY
Methyl (1r2s)-2-(Hydroxycarbamoyl)-1-{4-[(2-methylquinolin-4-yl)Methoxy]Benzyl}Cyclopropanecarboxylate . DB07147
N-{[4-(But-2-yn-1-yloxy)Phenyl]Sulfonyl}-5-methyl-d-tryptophan . DB07233
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dpc-333 Small molecular drug D01DVX

References

1 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580
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 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.
4 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.
5 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
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 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
8 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
9 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
10 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
11 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
12 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
13 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