General Information of the Protein
Protein ID
PT01871
Protein Name
Proteinase-activated receptor 1
Secondarily
Protein Name
Coagulation factor II receptor
Thrombin receptor
Gene Name
F2R
Secondarily
Gene Name
CF2R
PAR1
TR
Sequence
MGPRRLLLVAACFSLCGPLLSARTRARRPESKATNATLDPRSFLLRNPNDKYEPFWEDEEKNESGLTEYRLVSINKSSPLQKQLPAFISEDASGYLTSSWLTLFVPSVYTGVFVVSLPLNIMAIVVFILKMKVKKPAVVYMLHLATADVLFVSVLPFKISYYFSGSDWQFGSELCRFVTAAFYCNMYASILLMTVISIDRFLAVVYPMQSLSWRTLGRASFTCLAIWALAIAGVVPLLLKEQTIQVPGLNITTCHDVLNETLLEGYYAYYFSAFSAVFFFVPLIISTVCYVSIIRCLSSSAVANRSKKSRALFLSAAVFCIFIICFGPTNVLLIAHYSFLSHTSTTEAAYFAYLLCVCVSSISCCIDPLIYYYASSECQRYVYSILCCKESSDPSSYNSSGQLMASKMDTCSSNLNNSIYKKLLT
    Show/Hide
Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Protease-activated receptor
>
Protease-activated receptor
Function
High affinity receptor for activated thrombin coupled to G proteins that stimulate phosphoinositide hydrolysis. May play a role in platelets activation and in vascular development.
    Show/Hide
Uniprot ID
Primary ID:
P25116

Secondarily ID:
Q53XV0
Q96RF7
Q9BUN4
    Show/Hide
Ensembl ID
ENSG00000181104
HGNC ID
HGNC:3537
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000023 , BTI-Tn-5B1-4
Compound ID Compound Name Compound Formula
CP0410578
US8853206, 54
   Show/Hide
C25H36N5O4+
 1
1
IC50 = 85 nM
   TI
   LI
   LO
   TS
CP0566389
US9079906, 117
   Show/Hide
C26H37N5O5
 1
1
IC50 = 98 nM
   TI
   LI
   LO
   TS
CP0536209
US9079906, 89
   Show/Hide
C25H35N5O4
 1
1
IC50 = 107 nM
   TI
   LI
   LO
   TS
CP0491576
US9079906, 239
   Show/Hide
C27H38N6O5
 1
1
IC50 = 113 nM
   TI
   LI
   LO
   TS
CP0555685
US8853206, 46
   Show/Hide
C22H30N5O3+
 1
1
IC50 = 114 nM
   TI
   LI
   LO
   TS
CP0567345
US9079906, 186
   Show/Hide
C27H40N6O4
 1
1
IC50 = 119 nM
   TI
   LI
   LO
   TS
CP0566390
US9079906, 178
   Show/Hide
C26H37N5O5
 1
1
IC50 = 126 nM
   TI
   LI
   LO
   TS
CP0480935
US8853206, 35
   Show/Hide
C26H36N5O3+
 1
1
IC50 = 132 nM
   TI
   LI
   LO
   TS
CP0480934
US8853206, 29
   Show/Hide
C26H38N5O4+
 1
1
IC50 = 136 nM
   TI
   LI
   LO
   TS
CP0507885
US9079906, 197
   Show/Hide
C27H39N5O5
 1
1
IC50 = 149 nM
   TI
   LI
   LO
   TS
CP0410577
US8853206, 27
   Show/Hide
C25H36N5O3+
 1
1
IC50 = 152 nM
   TI
   LI
   LO
   TS
CP0536211
US9079906, 221
   Show/Hide
C24H33N5O4
 1
1
IC50 = 155 nM
   TI
   LI
   LO
   TS
CP0466866
US9079906, 207
   Show/Hide
C26H36N6O5
 1
1
IC50 = 174 nM
   TI
   LI
   LO
   TS
CP0567344
US9079906, 174
   Show/Hide
C25H35N5O5
 1
1
IC50 = 183 nM
   TI
   LI
   LO
   TS
CP0542071
US9079906, 199
   Show/Hide
C27H37N5O5
 1
1
IC50 = 206 nM
   TI
   LI
   LO
   TS
CP0466602
US9079906, 215
   Show/Hide
C24H33N5O4
 1
1
IC50 = 219 nM
   TI
   LI
   LO
   TS
CP0518215
US9079906, 230
   Show/Hide
C25H35N5O3
 1
1
IC50 = 234 nM
   TI
   LI
   LO
   TS
CP0466865
US9079906, 168
   Show/Hide
C26H37N5O6
 1
1
IC50 = 257 nM
   TI
   LI
   LO
   TS
CP0556550
US9079906, 14
   Show/Hide
C27H38N6O4
 1
1
IC50 = 279 nM
   TI
   LI
   LO
   TS
CP0491575
US9079906, 163
   Show/Hide
C24H33N5O4
 1
1
IC50 = 364 nM
   TI
   LI
   LO
   TS
CP0542039
US9079906, 222
   Show/Hide
C24H32FN5O3
 1
1
IC50 = 416 nM
   TI
   LI
   LO
   TS
CP0491577
US9079906, 240
   Show/Hide
C25H35N5O5
 1
1
IC50 = 484 nM
   TI
   LI
   LO
   TS
CP0532392
US8853206, 40
   Show/Hide
C19H23ClN5O3+
 1
1
IC50 = 601 nM
   TI
   LI
   LO
   TS
CP0518212
US9079906, 50
   Show/Hide
C25H35N5O4
 1
1
IC50 = 631 nM
   TI
   LI
   LO
   TS
CP0491573
US9079906, 144
   Show/Hide
C26H36N6O4
 1
1
IC50 = 827 nM
   TI
   LI
   LO
   TS
CP0553899
US9079906, 76
   Show/Hide
C24H33N5O3
 1
1
IC50 = 951 nM
   TI
   LI
   LO
   TS
CP0515031
US9079906, 26
   Show/Hide
C26H35N5O3
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0555686
US8853206, 76
   Show/Hide
C30H43N6O4+
 1
1
IC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0466867
US9079906, 236
   Show/Hide
C25H33N5O5
 1
1
IC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0518213
US9079906, 101
   Show/Hide
C24H33N5O5
 1
1
IC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0443114
US8853206, 72
   Show/Hide
C27H39N6O4+
 1
1
IC50 = 1700 nM
   TI
   LI
   LO
   TS
CP0480936
US8853206, 60
   Show/Hide
C24H33N6O3+
 1
1
IC50 = 2100 nM
   TI
   LI
   LO
   TS
CP0550474
US9079906, 127
   Show/Hide
C25H35N5O5
 1
1
IC50 = 2500 nM
   TI
   LI
   LO
   TS
CP0563281
US8853206, 82
   Show/Hide
C25H36N5O5+
 1
1
IC50 = 8400 nM
   TI
   LI
   LO
   TS
CP0474219
US8853206, 47
   Show/Hide
C26H36N5O4+
 1
1
IC50 = 10000 nM
   TI
   LI
   LO
   TS
CP0559133
US9079906, 56
   Show/Hide
C22H27ClN6O3
 1
1
IC50 = 24000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0206175
4-Amino-N-benzyl-2-[2-{3-[1-(2,6-dichloro-benzyl)-3-pyrrolidin-1-ylmethyl-1H-indazol-6-yl]-ureido}-3-(3,4-difluoro-phenyl)-propionylamino]-butyramide
   Show/Hide
C40H42Cl2F2N8O3
 1
1 Kd = 0.15 nM
Clinical Information about the Protein
Target 1 ( Proteinase activated receptor 1 (F2R) )
Target Type Successful Target
Disease 5 Target-related Diseases  5
1 Myocardial infarction [ICD-11: BA41-BA43]
2 Acute coronary syndrome [ICD-11: BA41]
3 Artery stenosis [ICD-11: BD52]
4 Thrombosis [ICD-11: DB61-GB90]
5 Arteriosclerosis [ICD-11: BD40]
Approved Drug(s) 1 Approved Drug  1
1 Vorapaxar Approved
Myocardial infarction
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 E5555 Phase 2
Acute coronary syndrome
Discontinued Drug(s) 1 Discontinued Drug  1
1 RWJ-58259 Terminated
Artery stenosis
Investigative Drug(s) 2 Investigative Drugs  2
1 SCH-205831 Investigative
Thrombosis
2 SCH-602539 Investigative
Arteriosclerosis