General Information of the Protein
Protein ID
PT01823
Protein Name
Prostaglandin F2-alpha receptor
Secondarily
Protein Name
Prostanoid FP receptor
Gene Name
PTGFR
Sequence
MSMNNSKQLVSPAAALLSNTTCQTENRLSVFFSVIFMTVGILSNSLAIAILMKAYQRFRQKSKASFLLLASGLVITDFFGHLINGAIAVFVYASDKEWIRFDQSNVLCSIFGICMVFSGLCPLLLGSVMAIERCIGVTKPIFHSTKITSKHVKMMLSGVCLFAVFIALLPILGHRDYKIQASRTWCFYNTEDIKDWEDRFYLLLFSFLGLLALGVSLLCNAITGITLLRVKFKSQQHRQGRSHHLEMVIQLLAIMCVSCICWSPFLVTMANIGINGNHSLETCETTLFALRMATWNQILDPWVYILLRKAVLKNLYKLASQCCGVHVISLHIWELSSIKNSLKVAAISESPVAEKSAST
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Lipid-like ligand receptor (family A GPCR)
>
Prostanoid receptor
Function
Receptor for prostaglandin F2-alpha (PGF2-alpha). The activity of this receptor is mediated by G proteins which activate a phosphatidylinositol-calcium second messenger system. Initiates luteolysis in the corpus luteum (By similarity). Isoforms 2 to 7 do not bind PGF2-alpha but are proposed to modulate signaling by participating in variant receptor complexes; heterodimers between isoform 1 and isoform 5 are proposed to be a receptor for prostamides including the synthetic analog bimatoprost.
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Uniprot ID
Primary ID:
P43088

Secondarily ID:
A8K9Y0
Q2KHP3
Q6RYQ6
Q9P1X4
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HGNC ID
HGNC:9600
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: CL000053 , COS-7
Compound ID Compound Name Compound Formula
CP0295469
(Z)-7-{(1R,2R,3R,5S)-2-[(E)-(R)-4-(3-Chloro-phenoxy)-3-hydroxy-but-1-enyl]-3,5-dihydroxy-cyclopentyl}-hept-5-enoic acid
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C22H29ClO6
 1
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0402541
7-{(1R,2R,3R,5S)-2-[(R)-4-(3-Chloro-phenoxy)-3-hydroxy-butyl]-3,5-dihydroxy-cyclopentyl}-heptanoic acid
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C22H33ClO6
 1
1
IC50 = 2.6 nM
   TI
   LI
   LO
   TS
CP0433187
7-[3,5-Dihydroxy-2-(3-hydroxy-4-phenylsulfanyl-butyl)-cyclopentyl]-heptanoic acid
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C22H34O5S
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0095751
(5Z,13E,15S)-9alpha,11alpha,15-trihydroxyprosta-5,13-dien-1-oic acid
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C20H34O5
 1
1
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0445340
7-{3,5-Dihydroxy-2-[3-hydroxy-4-(thiophen-2-ylsulfanyl)-butyl]-cyclopentyl}-heptanoic acid
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C20H32O5S2
 1
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
CP0438269
7-[3,5-Dihydroxy-2-(3-hydroxy-4-phenoxy-butyl)-cyclopentyl]-heptanoic acid
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C22H34O6
 1
1
IC50 = 12 nM
   TI
   LI
   LO
   TS
CP0374214
7-{2-[4-(3-Chloro-phenylsulfanyl)-3-hydroxy-butyl]-3,5-dihydroxy-cyclopentyl}-heptanoic acid
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C22H33ClO5S
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0395236
7-{2-[4-(3-Fluoro-phenylsulfanyl)-3-hydroxy-butyl]-3,5-dihydroxy-cyclopentyl}-heptanoic acid
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C22H33FO5S
 1
1
IC50 = 29 nM
   TI
   LI
   LO
   TS
CP0372737
7-[3,5-Dihydroxy-2-(3-hydroxy-4-m-tolylsulfanyl-butyl)-cyclopentyl]-heptanoic acid
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C23H36O5S
 1
1
IC50 = 63 nM
   TI
   LI
   LO
   TS
CP0377752
7-[3,5-Dihydroxy-2-(3-hydroxy-4-phenylamino-butyl)-cyclopentyl]-heptanoic acid
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C22H35NO5
 1
1
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0448266
7-{3,5-Dihydroxy-2-[3-hydroxy-4-(3-trifluoromethyl-phenylsulfanyl)-butyl]-cyclopentyl}-heptanoic acid
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C23H33F3O5S
 1
1
IC50 = 320 nM
   TI
   LI
   LO
   TS
CP0432809
7-[(1R,2R,3R,5S)-3,5-Dihydroxy-2-((S)-3-hydroxy-octyl)-cyclopentyl]-heptanoic acid
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C20H38O5
 1
1
IC50 = 350 nM
   TI
   LI
   LO
   TS
CP0402565
7-[(1R,2R,3R,5S)-3,5-Dihydroxy-2-((R)-3-hydroxy-5-phenyl-pentyl)-cyclopentyl]-heptanoic acid
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C23H36O5
 1
1
IC50 = 570 nM
   TI
   LI
   LO
   TS
CP0432810
7-{3,5-Dihydroxy-2-[3-hydroxy-4-(thiazol-2-ylsulfanyl)-butyl]-cyclopentyl}-heptanoic acid
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C19H31NO5S2
 1
1
IC50 = 1424 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0095751
(5Z,13E,15S)-9alpha,11alpha,15-trihydroxyprosta-5,13-dien-1-oic acid
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C20H34O5
 1
1 IC50 = 3 nM
CP0272414
US11149018, Example 34
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C26H27BrClN3O3
 4
1 IC50 ~ 11 nM
2 IC50 ~ 21 nM
3 IC50 ~ 22 nM
4 Ki ~ 14.8 nM
CP0041889
2-((R)-4-(4-chlorobenzyl)-5-(1-hydroxyethyl)-7-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid
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C23H24ClNO5S
 1
1 Ki > 20000 nM
CP0108218
(R)-2-(4-(4-chlorobenzyl)-5-acetyl-7-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid
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C23H22ClNO5S
 1
1 Ki > 20000 nM
Clinical Information about the Protein
Target 1 ( Prostaglandin F2-alpha receptor (PTGFR) )
Target Type Successful Target
Disease 5 Target-related Diseases  5
1 Medical abortion [ICD-11: JA00.1Z]
2 Open-angle glaucoma [ICD-11: 9C61]
3 Alzheimer disease [ICD-11: 8A20]
4 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
5 Coronary heart disease [ICD-11: BA80.Z]
Approved Drug(s) 4 Approved Drugs  4
1 Dinoprostone Approved
Medical abortion
2 Latanoprost Approved
Open-angle glaucoma
3 Travoprost Approved
Open-angle glaucoma
4 LAROPIPRANT Phase 4
Coronary heart disease
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 bimatoprost (free acid form) Clinical trial
Alzheimer disease
2 PGF2alpha Clinical trial
Solid tumour/cancer
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT04759 Prostaglandin F2-alpha receptor Mus musculus, Mouse
PT07686 Prostaglandin F2-alpha receptor Rattus norvegicus, Rat