Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTD0652)

• DTT Name: Proteinase activated receptor 4 (F2RL3)
• Synonyms: Thrombin receptor-like 3; Protease activated receptor 4; F2RL3; Coagulation factor II receptor-like3
• Gene Name: F2RL3
• DTT Type: Literature-reported target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: PAR4_HUMAN
• TTD ID: T30414
• Sequence:
  MWGRLLLWPLVLGFSLSGGTQTPSVYDESGSTGGGDDSTPSILPAPRGYPGQVCANDSDT
  LELPDSSRALLLGWVPTRLVPALYGLVLVVGLPANGLALWVLATQAPRLPSTMLLMNLAA
  ADLLLALALPPRIAYHLRGQRWPFGEAACRLATAALYGHMYGSVLLLAAVSLDRYLALVH
  PLRARALRGRRLALGLCMAAWLMAAALALPLTLQRQTFRLARSDRVLCHDALPLDAQASH
  WQPAFTCLALLGCFLPLLAMLLCYGATLHTLAASGRRYGHALRLTAVVLASAVAFFVPSN
  LLLLLHYSDPSPSAWGNLYGAYVPSLALSTLNSCVDPFIYYYVSAEFRDKVRAGLFQRSP
  GDTVASKASAEGGSRGMGTHSSLLQ
• Function: Receptor for activated thrombin or trypsin coupled to G proteins that stimulate phosphoinositide hydrolysis. May play a role in platelets activation.
• KEGG Pathway:
  Rap1 signaling pathway (hsa04015)
  Neuroactive ligand-receptor interaction (hsa04080)
  Platelet activation (hsa04611)
  Pathways in cancer (hsa05200)
• Reactome Pathway:
  G alpha (q) signalling events (R-HSA-416476)
  Thrombin signalling through proteinase activated receptors (PARs) (R-HSA-456926)
  Peptide ligand-binding receptors (R-HSA-375276)

Molecular Interaction Atlas (MIA) of This DTT

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SC-47643	DMIE039	N. A.	N. A.	Terminated	[1]

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ethyl 4-(1-benzyl-1H-indazol-3-yl)benzoate	DM5GLP7	Discovery agent	N.A.	Investigative	[2]

References

• [1] Novel thiazole-based heterocycles as selective inhibitors of fibrinogen-mediated platelet aggregation. J Med Chem. 1995 Jan 6;38(1):34-41.
• [2] Synthesis and antiplatelet activity of ethyl 4-(1-benzyl-1H-indazol-3-yl)benzoate (YD-3) derivatives. Bioorg Med Chem. 2008 Feb 1;16(3):1262-78.