Details of the Target

General Information of Target

Target ID LDTP03867
Target Name Collagen alpha-1(XVIII) chain (COL18A1)
Gene Name COL18A1
Gene ID 80781
Synonyms
Collagen alpha-1(XVIII) chain [Cleaved into: Endostatin; Non-collagenous domain 1; NC1)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAPYPCGCHILLLLFCCLAAARANLLNLNWLWFNNEDTSHAATTIPEPQGPLPVQPTADT
TTHVTPRNGSTEPATAPGSPEPPSELLEDGQDTPTSAESPDAPEENIAGVGAEILNVAKG
IRSFVQLWNDTVPTESLARAETLVLETPVGPLALAGPSSTPQENGTTLWPSRGIPSSPGA
HTTEAGTLPAPTPSPPSLGRPWAPLTGPSVPPPSSGRASLSSLLGGAPPWGSLQDPDSQG
LSPAAAAPSQQLQRPDVRLRTPLLHPLVMGSLGKHAAPSAFSSGLPGALSQVAVTTLTRD
SGAWVSHVANSVGPGLANNSALLGADPEAPAGRCLPLPPSLPVCGHLGISRFWLPNHLHH
ESGEQVRAGARAWGGLLQTHCHPFLAWFFCLLLVPPCGSVPPPAPPPCCQFCEALQDACW
SRLGGGRLPVACASLPTQEDGYCVLIGPAAERISEEVGLLQLLGDPPPQQVTQTDDPDVG
LAYVFGPDANSGQVARYHFPSLFFRDFSLLFHIRPATEGPGVLFAITDSAQAMVLLGVKL
SGVQDGHQDISLLYTEPGAGQTHTAASFRLPAFVGQWTHLALSVAGGFVALYVDCEEFQR
MPLARSSRGLELEPGAGLFVAQAGGADPDKFQGVIAELKVRRDPQVSPMHCLDEEGDDSD
GASGDSGSGLGDARELLREETGAALKPRLPAPPPVTTPPLAGGSSTEDSRSEEVEEQTTV
ASLGAQTLPGSDSVSTWDGSVRTPGGRVKEGGLKGQKGEPGVPGPPGRAGPPGSPCLPGP
PGLPCPVSPLGPAGPALQTVPGPQGPPGPPGRDGTPGRDGEPGDPGEDGKPGDTGPQGFP
GTPGDVGPKGDKGDPGVGERGPPGPQGPPGPPGPSFRHDKLTFIDMEGSGFGGDLEALRG
PRGFPGPPGPPGVPGLPGEPGRFGVNSSDVPGPAGLPGVPGREGPPGFPGLPGPPGPPGR
EGPPGRTGQKGSLGEAGAPGHKGSKGAPGPAGARGESGLAGAPGPAGPPGPPGPPGPPGP
GLPAGFDDMEGSGGPFWSTARSADGPQGPPGLPGLKGDPGVPGLPGAKGEVGADGVPGFP
GLPGREGIAGPQGPKGDRGSRGEKGDPGKDGVGQPGLPGPPGPPGPVVYVSEQDGSVLSV
PGPEGRPGFAGFPGPAGPKGNLGSKGERGSPGPKGEKGEPGSIFSPDGGALGPAQKGAKG
EPGFRGPPGPYGRPGYKGEIGFPGRPGRPGMNGLKGEKGEPGDASLGFGMRGMPGPPGPP
GPPGPPGTPVYDSNVFAESSRPGPPGLPGNQGPPGPKGAKGEVGPPGPPGQFPFDFLQLE
AEMKGEKGDRGDAGQKGERGEPGGGGFFGSSLPGPPGPPGPPGPRGYPGIPGPKGESIRG
QPGPPGPQGPPGIGYEGRQGPPGPPGPPGPPSFPGPHRQTISVPGPPGPPGPPGPPGTMG
ASSGVRLWATRQAMLGQVHEVPEGWLIFVAEQEELYVRVQNGFRKVQLEARTPLPRGTDN
EVAALQPPVVQLHDSNPYPRREHPHPTARPWRADDILASPPRLPEPQPYPGAPHHSSYVH
LRPARPTSPPAHSHRDFQPVLHLVALNSPLSGGMRGIRGADFQCFQQARAVGLAGTFRAF
LSSRLQDLYSIVRRADRAAVPIVNLKDELLFPSWEALFSGSEGPLKPGARIFSFDGKDVL
RHPTWPQKSVWHGSDPNGRRLTESYCETWRTEAPSATGQASSLLGGRLLGQSAASCHHAY
IVLCIENSFMTASK
Target Type
Clinical trial
Target Bioclass
Other
Family
Multiplexin collagen family
Subcellular location
Secreted; Secreted, extracellular space, extracellular matrix; Secreted, extracellular space, extracellular matrix, basement membrane
Function
Probably plays a major role in determining the retinal structure as well as in the closure of the neural tube.; [Non-collagenous domain 1]: May regulate extracellular matrix-dependent motility and morphogenesis of endothelial and non-endothelial cells; the function requires homotrimerization and implicates MAPK signaling.; [Endostatin]: Potently inhibits endothelial cell proliferation and angiogenesis. May inhibit angiogenesis by binding to the heparan sulfate proteoglycans involved in growth factor signaling. Inhibits VEGFA-induced endothelial cell proliferation and migration. Seems to inhibit VEGFA-mediated signaling by blocking the interaction of VEGFA to its receptor KDR/VEGFR2. Modulates endothelial cell migration in an integrin-dependent manner implicating integrin ITGA5:ITGB1 and to a lesser extent ITGAV:ITGB3 and ITGAV:ITGB5. May negatively regulate the activity of homotrimeric non-collagenous domain 1.
TTD ID
T75788
Uniprot ID
P39060
DrugMap ID
TT63DI9
Ensemble ID
ENST00000355480.10
HGNC ID
HGNC:2195
ChEMBL ID
CHEMBL2364188

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C1706(1.61)  LDD0602  [1]
IA-alkyne
 Probe Info  		N.A.  LDD0165  [2]
YN-1
 Probe Info  		P1493(0.00); R1491(0.00)  LDD0446  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0285  AC25 HCT 116 C1706(1.61)  LDD0602  [1]
 LDCM0286  AC26 HCT 116 C1706(1.15)  LDD0603  [1]
 LDCM0287  AC27 HCT 116 C1706(1.09)  LDD0604  [1]
 LDCM0288  AC28 HCT 116 C1706(1.10)  LDD0605  [1]
 LDCM0289  AC29 HCT 116 C1706(1.02)  LDD0606  [1]
 LDCM0291  AC30 HCT 116 C1706(1.01)  LDD0608  [1]
 LDCM0292  AC31 HCT 116 C1706(1.32)  LDD0609  [1]
 LDCM0293  AC32 HCT 116 C1706(1.03)  LDD0610  [1]
 LDCM0294  AC33 HCT 116 C1706(1.03)  LDD0611  [1]
 LDCM0295  AC34 HCT 116 C1706(0.96)  LDD0612  [1]
 LDCM0349  AC83 HCT 116 C1706(0.88)  LDD0666  [1]
 LDCM0350  AC84 HCT 116 C1706(1.00)  LDD0667  [1]
 LDCM0351  AC85 HCT 116 C1706(1.00)  LDD0668  [1]
 LDCM0352  AC86 HCT 116 C1706(1.44)  LDD0669  [1]
 LDCM0353  AC87 HCT 116 C1706(0.88)  LDD0670  [1]
 LDCM0354  AC88 HCT 116 C1706(0.60)  LDD0671  [1]
 LDCM0355  AC89 HCT 116 C1706(0.60)  LDD0672  [1]
 LDCM0357  AC90 HCT 116 C1706(0.95)  LDD0674  [1]
 LDCM0358  AC91 HCT 116 C1706(0.69)  LDD0675  [1]
 LDCM0359  AC92 HCT 116 C1706(1.27)  LDD0676  [1]
 LDCM0360  AC93 HCT 116 C1706(0.88)  LDD0677  [1]
 LDCM0361  AC94 HCT 116 C1706(1.21)  LDD0678  [1]
 LDCM0362  AC95 HCT 116 C1706(1.15)  LDD0679  [1]
 LDCM0363  AC96 HCT 116 C1706(0.63)  LDD0680  [1]
 LDCM0364  AC97 HCT 116 C1706(0.85)  LDD0681  [1]
 LDCM0382  CL112 HCT 116 C1706(1.33)  LDD0699  [1]
 LDCM0383  CL113 HCT 116 C1706(0.95)  LDD0700  [1]
 LDCM0384  CL114 HCT 116 C1706(1.13)  LDD0701  [1]
 LDCM0385  CL115 HCT 116 C1706(1.34)  LDD0702  [1]
 LDCM0386  CL116 HCT 116 C1706(1.29)  LDD0703  [1]
 LDCM0403  CL16 HCT 116 C1706(0.95)  LDD0720  [1]
 LDCM0404  CL17 HCT 116 C1706(1.44)  LDD0721  [1]
 LDCM0405  CL18 HCT 116 C1706(1.21)  LDD0722  [1]
 LDCM0406  CL19 HCT 116 C1706(1.05)  LDD0723  [1]
 LDCM0408  CL20 HCT 116 C1706(0.89)  LDD0725  [1]
 LDCM0409  CL21 HCT 116 C1706(1.11)  LDD0726  [1]
 LDCM0410  CL22 HCT 116 C1706(0.72)  LDD0727  [1]
 LDCM0411  CL23 HCT 116 C1706(0.67)  LDD0728  [1]
 LDCM0412  CL24 HCT 116 C1706(0.79)  LDD0729  [1]
 LDCM0413  CL25 HCT 116 C1706(0.76)  LDD0730  [1]
 LDCM0414  CL26 HCT 116 C1706(0.61)  LDD0731  [1]
 LDCM0415  CL27 HCT 116 C1706(0.93)  LDD0732  [1]
 LDCM0416  CL28 HCT 116 C1706(0.69)  LDD0733  [1]
 LDCM0417  CL29 HCT 116 C1706(0.75)  LDD0734  [1]
 LDCM0419  CL30 HCT 116 C1706(1.06)  LDD0736  [1]
 LDCM0453  CL61 HCT 116 C1706(1.08)  LDD0770  [1]
 LDCM0454  CL62 HCT 116 C1706(1.12)  LDD0771  [1]
 LDCM0455  CL63 HCT 116 C1706(1.07)  LDD0772  [1]
 LDCM0456  CL64 HCT 116 C1706(1.25)  LDD0773  [1]
 LDCM0457  CL65 HCT 116 C1706(0.95)  LDD0774  [1]
 LDCM0458  CL66 HCT 116 C1706(1.40)  LDD0775  [1]
 LDCM0459  CL67 HCT 116 C1706(1.06)  LDD0776  [1]
 LDCM0460  CL68 HCT 116 C1706(1.04)  LDD0777  [1]
 LDCM0461  CL69 HCT 116 C1706(1.56)  LDD0778  [1]
 LDCM0463  CL70 HCT 116 C1706(1.00)  LDD0780  [1]
 LDCM0464  CL71 HCT 116 C1706(0.98)  LDD0781  [1]
 LDCM0465  CL72 HCT 116 C1706(0.99)  LDD0782  [1]
 LDCM0466  CL73 HCT 116 C1706(1.03)  LDD0783  [1]
 LDCM0467  CL74 HCT 116 C1706(1.20)  LDD0784  [1]
 LDCM0468  Fragment33 HCT 116 C1706(1.04)  LDD0785  [1]
 LDCM0022  KB02 786-O C1706(2.75)  LDD2247  [4]
 LDCM0023  KB03 A101D C1604(2.45); C1706(4.42)  LDD2667  [4]
 LDCM0024  KB05 OVCAR-3 C1604(5.76); C1706(3.98)  LDD3365  [4]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein-glutamine gamma-glutamyltransferase 2 (TGM2) Transglutaminase family P21980
Procollagen C-endopeptidase enhancer 1 (PCOLCE) . Q15113
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Nucleolin (NCL) . P19338

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
Retinostat . D0RD0Y
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Endo-cd . D0O6ZH

References

1 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.
2 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
3 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
4 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