Target Information

Target General Infomation
Target ID
T30414
Former ID
TTDR00111
Target Name
Proteinase activated receptor 4
Gene Name
F2RL3
Synonyms
Coagulation factor II receptor-like3; PAR-4; Protease activated receptor 4; Thrombin receptor-like 3; F2RL3
Target Type
Discontinued
Function
Receptor for activated thrombin or trypsin coupled to G proteins that stimulate phosphoinositide hydrolysis. May play a role in platelets activation.
BioChemical Class
GPCR rhodopsin
Target Validation
T30414
UniProt ID
Q96RI0
Sequence
MWGRLLLWPLVLGFSLSGGTQTPSVYDESGSTGGGDDSTPSILPAPRGYPGQVCANDSDT
LELPDSSRALLLGWVPTRLVPALYGLVLVVGLPANGLALWVLATQAPRLPSTMLLMNLAA
ADLLLALALPPRIAYHLRGQRWPFGEAACRLATAALYGHMYGSVLLLAAVSLDRYLALVH
PLRARALRGRRLALGLCMAAWLMAAALALPLTLQRQTFRLARSDRVLCHDALPLDAQASH
WQPAFTCLALLGCFLPLLAMLLCYGATLHTLAASGRRYGHALRLTAVVLASAVAFFVPSN
LLLLLHYSDPSPSAWGNLYGAYVPSLALSTLNSCVDPFIYYYVSAEFRDKVRAGLFQRSP
GDTVASKASAEGGSRGMGTHSSLLQ
Drugs and Mode of Action
Drug(s) SC-47643 Drug Info Terminated Discovery agent [545332]
Inhibitor Ethyl 4-(1-benzyl-1H-indazol-3-yl)benzoate Drug Info [529139]
SC-47643 Drug Info [533764]
Pathways
KEGG Pathway Rap1 signaling pathway
Neuroactive ligand-receptor interaction
Platelet activation
Pathways in cancer
PANTHER Pathway Blood coagulation
Pathway Interaction Database PAR4-mediated thrombin signaling events
Reactome Peptide ligand-binding receptors
G alpha (q) signalling events
Thrombin signalling through proteinase activated receptors (PARs)
WikiPathways GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
Thrombin signalling through proteinase activated receptors (PARs)
GPCR ligand binding
GPCR downstream signaling
References
Ref 545332Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002874)
Ref 529139Bioorg Med Chem. 2008 Feb 1;16(3):1262-78. Epub 2007 Oct 25.Synthesis and antiplatelet activity of ethyl 4-(1-benzyl-1H-indazol-3-yl)benzoate (YD-3) derivatives.
Ref 533764J Med Chem. 1995 Jan 6;38(1):34-41.Novel thiazole-based heterocycles as selective inhibitors of fibrinogen-mediated platelet aggregation.

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