Details of the Target

General Information of Target

Target ID LDTP00220
Target Name Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A)
Gene Name TNFRSF10A
Gene ID 8797
Synonyms
APO2; DR4; TRAILR1; Tumor necrosis factor receptor superfamily member 10A; Death receptor 4; TNF-related apoptosis-inducing ligand receptor 1; TRAIL receptor 1; TRAIL-R1; CD antigen CD261
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAPPPARVHLGAFLAVTPNPGSAASGTEAAAATPSKVWGSSAGRIEPRGGGRGALPTSMG
QHGPSARARAGRAPGPRPAREASPRLRVHKTFKFVVVGVLLQVVPSSAATIKLHDQSIGT
QQWEHSPLGELCPPGSHRSEHPGACNRCTEGVGYTNASNNLFACLPCTACKSDEEERSPC
TTTRNTACQCKPGTFRNDNSAEMCRKCSRGCPRGMVKVKDCTPWSDIECVHKESGNGHNI
WVILVVTLVVPLLLVAVLIVCCCIGSGCGGDPKCMDRVCFWRLGLLRGPGAEDNAHNEIL
SNADSLSTFVSEQQMESQEPADLTGVTVQSPGEAQCLLGPAEAEGSQRRRLLVPANGADP
TETLMLFFDKFANIVPFDSWDQLMRQLDLTKNEIDVVRAGTAGPGDALYAMLMKWVNKTG
RNASIHTLLDALERMEERHAREKIQDLLVDSGKFIYLEDGTGSAVSLE
Target Type
Clinical trial
Target Bioclass
Cytokine and receptor
Subcellular location
Cell membrane
Function
Receptor for the cytotoxic ligand TNFSF10/TRAIL. The adapter molecule FADD recruits caspase-8 to the activated receptor. The resulting death-inducing signaling complex (DISC) performs caspase-8 proteolytic activation which initiates the subsequent cascade of caspases (aspartate-specific cysteine proteases) mediating apoptosis. Promotes the activation of NF-kappa-B.
TTD ID
T77645
Uniprot ID
O00220
DrugMap ID
TT5WLRX
Ensemble ID
ENST00000221132.8
HGNC ID
HGNC:11904
ChEMBL ID
CHEMBL3551

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 7 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  		K443(8.50)  LDD0277  [2]
OPA-S-S-alkyne
 Probe Info  		K191(6.60)  LDD3494  [3]
BTD
 Probe Info  		C190(1.60)  LDD1700  [4]
DBIA
 Probe Info  		C221(0.97); C229(0.97)  LDD0580  [5]
5E-2FA
 Probe Info  		N.A.  LDD2235  [6]
IA-alkyne
 Probe Info  		C180(0.00); C204(0.00); C188(0.00); C145(0.00)  LDD0162  [7]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0263  AC143 HCT 116 C221(0.97); C229(0.97)  LDD0580  [5]
 LDCM0264  AC144 HCT 116 C221(0.82); C229(0.82)  LDD0581  [5]
 LDCM0265  AC145 HCT 116 C221(0.77); C229(0.77)  LDD0582  [5]
 LDCM0266  AC146 HCT 116 C221(0.97); C229(0.97)  LDD0583  [5]
 LDCM0267  AC147 HCT 116 C221(0.93); C229(0.93)  LDD0584  [5]
 LDCM0268  AC148 HCT 116 C221(0.87); C229(0.87)  LDD0585  [5]
 LDCM0269  AC149 HCT 116 C221(0.93); C229(0.93)  LDD0586  [5]
 LDCM0271  AC150 HCT 116 C221(0.98); C229(0.98)  LDD0588  [5]
 LDCM0272  AC151 HCT 116 C221(1.38); C229(1.38)  LDD0589  [5]
 LDCM0273  AC152 HCT 116 C221(0.99); C229(0.99)  LDD0590  [5]
 LDCM0274  AC153 HCT 116 C221(0.94); C229(0.94)  LDD0591  [5]
 LDCM0621  AC154 HCT 116 C221(0.83); C229(0.83)  LDD2158  [5]
 LDCM0622  AC155 HCT 116 C221(0.72); C229(0.72)  LDD2159  [5]
 LDCM0623  AC156 HCT 116 C221(0.93); C229(0.93)  LDD2160  [5]
 LDCM0624  AC157 HCT 116 C221(0.88); C229(0.88)  LDD2161  [5]
 LDCM0276  AC17 HCT 116 C221(0.98); C229(0.98)  LDD0593  [5]
 LDCM0277  AC18 HCT 116 C221(1.07); C229(1.07)  LDD0594  [5]
 LDCM0278  AC19 HCT 116 C221(0.93); C229(0.93)  LDD0595  [5]
 LDCM0280  AC20 HCT 116 C221(0.84); C229(0.84)  LDD0597  [5]
 LDCM0281  AC21 HCT 116 C221(0.88); C229(0.88)  LDD0598  [5]
 LDCM0282  AC22 HCT 116 C221(0.96); C229(0.96)  LDD0599  [5]
 LDCM0283  AC23 HCT 116 C221(0.69); C229(0.69)  LDD0600  [5]
 LDCM0284  AC24 HCT 116 C221(0.77); C229(0.77)  LDD0601  [5]
 LDCM0320  AC57 HCT 116 C221(1.00); C229(1.00)  LDD0637  [5]
 LDCM0321  AC58 HCT 116 C221(0.85); C229(0.85)  LDD0638  [5]
 LDCM0322  AC59 HCT 116 C221(0.74); C229(0.74)  LDD0639  [5]
 LDCM0324  AC60 HCT 116 C221(0.77); C229(0.77)  LDD0641  [5]
 LDCM0325  AC61 HCT 116 C221(0.88); C229(0.88)  LDD0642  [5]
 LDCM0326  AC62 HCT 116 C221(0.77); C229(0.77)  LDD0643  [5]
 LDCM0327  AC63 HCT 116 C221(0.86); C229(0.86)  LDD0644  [5]
 LDCM0328  AC64 HCT 116 C221(0.65); C229(0.65)  LDD0645  [5]
 LDCM0329  AC65 HCT 116 C221(1.26); C229(1.26)  LDD0646  [5]
 LDCM0330  AC66 HCT 116 C221(1.37); C229(1.37)  LDD0647  [5]
 LDCM0331  AC67 HCT 116 C221(1.00); C229(1.00)  LDD0648  [5]
 LDCM0332  AC68 HCT 116 C229(0.99); C221(1.06)  LDD0649  [5]
 LDCM0333  AC69 HCT 116 C229(0.92); C221(0.93)  LDD0650  [5]
 LDCM0335  AC70 HCT 116 C221(1.02); C229(1.05)  LDD0652  [5]
 LDCM0336  AC71 HCT 116 C229(0.98); C221(1.04)  LDD0653  [5]
 LDCM0337  AC72 HCT 116 C229(0.89); C221(0.98)  LDD0654  [5]
 LDCM0338  AC73 HCT 116 C229(0.86); C221(0.89)  LDD0655  [5]
 LDCM0339  AC74 HCT 116 C229(0.84); C221(0.86)  LDD0656  [5]
 LDCM0340  AC75 HCT 116 C229(0.73); C221(0.80)  LDD0657  [5]
 LDCM0341  AC76 HCT 116 C229(0.98); C221(1.06)  LDD0658  [5]
 LDCM0342  AC77 HCT 116 C229(0.96); C221(0.98)  LDD0659  [5]
 LDCM0343  AC78 HCT 116 C229(0.97); C221(1.05)  LDD0660  [5]
 LDCM0344  AC79 HCT 116 C229(0.90); C221(0.96)  LDD0661  [5]
 LDCM0346  AC80 HCT 116 C229(1.03); C221(1.08)  LDD0663  [5]
 LDCM0347  AC81 HCT 116 C229(0.93); C221(1.00)  LDD0664  [5]
 LDCM0348  AC82 HCT 116 C229(0.47); C221(0.52)  LDD0665  [5]
 LDCM0349  AC83 HCT 116 C221(0.73); C229(0.73)  LDD0666  [5]
 LDCM0350  AC84 HCT 116 C221(0.83); C229(0.83)  LDD0667  [5]
 LDCM0351  AC85 HCT 116 C221(0.81); C229(0.81)  LDD0668  [5]
 LDCM0352  AC86 HCT 116 C221(0.75); C229(0.75)  LDD0669  [5]
 LDCM0353  AC87 HCT 116 C221(0.74); C229(0.74)  LDD0670  [5]
 LDCM0354  AC88 HCT 116 C221(1.19); C229(1.19)  LDD0671  [5]
 LDCM0355  AC89 HCT 116 C221(1.15); C229(1.15)  LDD0672  [5]
 LDCM0357  AC90 HCT 116 C221(0.92); C229(0.92)  LDD0674  [5]
 LDCM0358  AC91 HCT 116 C221(0.93); C229(0.93)  LDD0675  [5]
 LDCM0359  AC92 HCT 116 C221(1.01); C229(1.01)  LDD0676  [5]
 LDCM0360  AC93 HCT 116 C221(0.77); C229(0.77)  LDD0677  [5]
 LDCM0361  AC94 HCT 116 C221(0.92); C229(0.92)  LDD0678  [5]
 LDCM0362  AC95 HCT 116 C221(0.94); C229(0.94)  LDD0679  [5]
 LDCM0363  AC96 HCT 116 C221(1.22); C229(1.22)  LDD0680  [5]
 LDCM0364  AC97 HCT 116 C221(0.87); C229(0.87)  LDD0681  [5]
 LDCM0520  AKOS000195272 MDA-MB-231 C190(1.61)  LDD2113  [4]
 LDCM0156  Aniline NCI-H1299 12.03  LDD0403  [1]
 LDCM0020  ARS-1620 HCC44 C204(0.99)  LDD2171  [5]
 LDCM0367  CL1 HCT 116 C221(0.96); C229(0.96)  LDD0684  [5]
 LDCM0368  CL10 HCT 116 C221(1.00); C229(1.00)  LDD0685  [5]
 LDCM0374  CL105 HCT 116 C221(1.06); C229(1.06)  LDD0691  [5]
 LDCM0375  CL106 HCT 116 C221(0.80); C229(0.80)  LDD0692  [5]
 LDCM0376  CL107 HCT 116 C221(0.98); C229(0.98)  LDD0693  [5]
 LDCM0377  CL108 HCT 116 C221(0.87); C229(0.87)  LDD0694  [5]
 LDCM0378  CL109 HCT 116 C221(1.10); C229(1.10)  LDD0695  [5]
 LDCM0379  CL11 HCT 116 C221(1.12); C229(1.12)  LDD0696  [5]
 LDCM0380  CL110 HCT 116 C221(1.08); C229(1.08)  LDD0697  [5]
 LDCM0381  CL111 HCT 116 C221(1.01); C229(1.01)  LDD0698  [5]
 LDCM0390  CL12 HCT 116 C221(1.15); C229(1.15)  LDD0707  [5]
 LDCM0396  CL125 HCT 116 C221(0.81); C229(0.81)  LDD0713  [5]
 LDCM0397  CL126 HCT 116 C221(1.13); C229(1.13)  LDD0714  [5]
 LDCM0398  CL127 HCT 116 C221(1.09); C229(1.09)  LDD0715  [5]
 LDCM0399  CL128 HCT 116 C221(1.03); C229(1.03)  LDD0716  [5]
 LDCM0400  CL13 HCT 116 C221(1.02); C229(1.02)  LDD0717  [5]
 LDCM0401  CL14 HCT 116 C221(1.00); C229(1.00)  LDD0718  [5]
 LDCM0402  CL15 HCT 116 C221(1.03); C229(1.03)  LDD0719  [5]
 LDCM0403  CL16 HCT 116 C221(1.33); C229(1.33)  LDD0720  [5]
 LDCM0404  CL17 HCT 116 C221(1.20); C229(1.20)  LDD0721  [5]
 LDCM0405  CL18 HCT 116 C221(1.16); C229(1.16)  LDD0722  [5]
 LDCM0406  CL19 HCT 116 C221(1.22); C229(1.22)  LDD0723  [5]
 LDCM0407  CL2 HCT 116 C221(1.04); C229(1.04)  LDD0724  [5]
 LDCM0408  CL20 HCT 116 C221(1.12); C229(1.12)  LDD0725  [5]
 LDCM0409  CL21 HCT 116 C221(1.18); C229(1.18)  LDD0726  [5]
 LDCM0410  CL22 HCT 116 C221(1.05); C229(1.05)  LDD0727  [5]
 LDCM0411  CL23 HCT 116 C221(1.10); C229(1.10)  LDD0728  [5]
 LDCM0412  CL24 HCT 116 C221(1.15); C229(1.15)  LDD0729  [5]
 LDCM0413  CL25 HCT 116 C221(1.24); C229(1.24)  LDD0730  [5]
 LDCM0414  CL26 HCT 116 C221(1.23); C229(1.23)  LDD0731  [5]
 LDCM0415  CL27 HCT 116 C221(1.26); C229(1.26)  LDD0732  [5]
 LDCM0416  CL28 HCT 116 C221(1.32); C229(1.32)  LDD0733  [5]
 LDCM0417  CL29 HCT 116 C221(1.31); C229(1.31)  LDD0734  [5]
 LDCM0418  CL3 HCT 116 C221(1.03); C229(1.03)  LDD0735  [5]
 LDCM0419  CL30 HCT 116 C221(1.12); C229(1.12)  LDD0736  [5]
 LDCM0420  CL31 HCT 116 C221(1.63); C229(1.63)  LDD0737  [5]
 LDCM0421  CL32 HCT 116 C221(1.62); C229(1.62)  LDD0738  [5]
 LDCM0422  CL33 HCT 116 C221(1.34); C229(1.34)  LDD0739  [5]
 LDCM0423  CL34 HCT 116 C221(1.72); C229(1.72)  LDD0740  [5]
 LDCM0424  CL35 HCT 116 C221(1.52); C229(1.52)  LDD0741  [5]
 LDCM0425  CL36 HCT 116 C221(1.46); C229(1.46)  LDD0742  [5]
 LDCM0426  CL37 HCT 116 C221(1.70); C229(1.70)  LDD0743  [5]
 LDCM0428  CL39 HCT 116 C221(1.36); C229(1.36)  LDD0745  [5]
 LDCM0429  CL4 HCT 116 C221(1.02); C229(1.02)  LDD0746  [5]
 LDCM0430  CL40 HCT 116 C221(1.40); C229(1.40)  LDD0747  [5]
 LDCM0431  CL41 HCT 116 C221(1.45); C229(1.45)  LDD0748  [5]
 LDCM0432  CL42 HCT 116 C221(1.06); C229(1.06)  LDD0749  [5]
 LDCM0433  CL43 HCT 116 C221(1.35); C229(1.35)  LDD0750  [5]
 LDCM0434  CL44 HCT 116 C221(1.18); C229(1.18)  LDD0751  [5]
 LDCM0435  CL45 HCT 116 C221(1.39); C229(1.39)  LDD0752  [5]
 LDCM0440  CL5 HCT 116 C221(0.90); C229(0.90)  LDD0757  [5]
 LDCM0451  CL6 HCT 116 C221(0.90); C229(0.90)  LDD0768  [5]
 LDCM0462  CL7 HCT 116 C221(1.18); C229(1.18)  LDD0779  [5]
 LDCM0473  CL8 HCT 116 C221(1.15); C229(1.15)  LDD0790  [5]
 LDCM0484  CL9 HCT 116 C221(0.90); C229(0.90)  LDD0801  [5]
 LDCM0427  Fragment51 HCT 116 C221(1.29); C229(1.29)  LDD0744  [5]
 LDCM0022  KB02 CAL-51 C145(1.99)  LDD2288  [8]
 LDCM0023  KB03 CAL-51 C145(1.81)  LDD2705  [8]
 LDCM0024  KB05 NCI-H1650 C145(2.07)  LDD3345  [8]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C190(0.90)  LDD2107  [4]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C190(0.99)  LDD2111  [4]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C190(0.57)  LDD2115  [4]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C190(0.60)  LDD2119  [4]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C190(1.05)  LDD2123  [4]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C190(0.48)  LDD2127  [4]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C190(1.05); C188(0.96)  LDD2133  [4]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C190(1.01)  LDD2134  [4]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C190(1.71)  LDD2136  [4]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C190(0.83)  LDD2137  [4]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C190(1.60)  LDD1700  [4]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C190(0.89)  LDD2144  [4]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C190(0.94)  LDD2146  [4]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C190(0.56)  LDD2148  [4]
 LDCM0021  THZ1 HCT 116 C204(0.99)  LDD2173  [5]

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
Caspase-8 (CASP8) Peptidase C14A family Q14790
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Tumor necrosis factor ligand superfamily member 10 (TNFSF10) Tumor necrosis factor family P50591
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Arf-GAP with Rho-GAP domain, ANK repeat and PH domain-containing protein 1 (ARAP1) . Q96P48
Galectin-3-binding protein (LGALS3BP) . Q08380

The Drug(s) Related To This Target

Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Mapatumumab Monoclonal antibody D0KG5D
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dr-5/Dr-4 Cross Reactive Mabs Antibody D0X3PN
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Rhapo2l/Trail . D08JRT

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 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
4 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
5 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
6 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
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 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