General Information of the Protein
Protein ID
PT01205
Protein Name
Prostaglandin E2 receptor EP1 subtype
Secondarily
Protein Name
Prostanoid EP1 receptor
Gene Name
PTGER1
Sequence
MSPCGPLNLSLAGEATTCAAPWVPNTSAVPPSGASPALPIFSMTLGAVSNLLALALLAQAAGRLRRRRSAATFLLFVASLLATDLAGHVIPGALVLRLYTAGRAPAGGACHFLGGCMVFFGLCPLLLGCGMAVERCVGVTRPLLHAARVSVARARLALAAVAAVALAVALLPLARVGRYELQYPGTWCFIGLGPPGGWRQALLAGLFASLGLVALLAALVCNTLSGLALLRARWRRRSRRPPPASGPDSRRRWGAHGPRSASASSASSIASASTFFGGSRSSGSARRARAHDVEMVGQLVGIMVVSCICWSPMLVLVALAVGGWSSTSLQRPLFLAVRLASWNQILDPWVYILLRQAVLRQLLRLLPPRAGAKGGPAGLGLTPSAWEASSLRSSRHSGLSHF
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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 E2 (PGE2). The activity of this receptor is mediated by G(q) proteins which activate a phosphatidylinositol-calcium second messenger system. May play a role as an important modulator of renal function. Implicated the smooth muscle contractile response to PGE2 in various tissues.
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Uniprot ID
Primary ID:
P34995

Secondarily ID:
Q5U5U4
Q86UH3
Q86VB5
Q8NHB2
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HGNC ID
HGNC:9593
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
CP0395236
7-{2-[4-(3-Fluoro-phenylsulfanyl)-3-hydroxy-butyl]-3,5-dihydroxy-cyclopentyl}-heptanoic acid
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C22H33FO5S
 1
1
IC50 = 364 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 = 380 nM
   TI
   LI
   LO
   TS
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 = 496 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 = 713 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 = 912 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 = 1100 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 = 1360 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 = 2700 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 = 4600 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 = 5000 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 = 5600 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 > 10000 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 > 10000 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 > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0055947
(15S)-prostaglandin E2
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C20H32O5
 3
1 IC50 = 1.1 nM
2 Ki = 9.1 nM
3 Ki = 18 nM
CP0167117
6-(2-(2-(2,4-difluorobenzyloxy)-5-chlorophenyl)cyclopent-1-enyl)picolinic acid
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C24H18ClF2NO3
 1
1 IC50 = 2.512 nM
CP0192211
3-[2-[5-chloro-2-(2-methylpropoxy)phenyl]-5-methylpyrrol-1-yl]benzoic acid
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C22H22ClNO3
 1
1 IC50 = 5.012 nM
CP0109669
3-(2-(2-(benzyloxy)-5-chlorophenyl)cyclopent-1-enyl)benzoic acid
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C25H21ClO3
 2
1 IC50 = 5.012 nM
2 IC50 = 12.59 nM
CP0109651
1-(2-(benzyloxy)-5-bromobenzyl)-5-methyl-1H-pyrazole-3-carboxylic acid
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C19H17BrN2O3
 1
1 IC50 = 6.31 nM
CP0766472
sodium 2-(2-(benzyloxy)-5-chlorobenzyl)thiazole-4-carboxylate
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C18H13ClNNaO3S
 1
1 IC50 = 6.31 nM
CP0109778
3-(2-(2-(benzyloxy)-5-chlorophenyl)-5-methyl-1H-pyrrol-1-yl)benzoic acid
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C25H20ClNO3
 1
1 IC50 = 7.943 nM
CP0645981
sodium 2-(5-chloro-2-isobutoxybenzyl)thiazole-4-carboxylate
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C15H15ClNNaO3S
 1
1 IC50 = 7.943 nM
CP0784948
sodium 1-(2-(benzyloxy)-5-chlorobenzyl)-5-methyl-1H-pyrazole-3-carboxylate
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C19H16ClN2NaO3
 1
1 IC50 = 10 nM
CP0370068
5-(2-(2-(benzyloxy)-5-(trifluoromethyl)phenyl)cyclopent-1-enyl)nicotinic acid
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C25H20F3NO3
 1
1 IC50 = 10 nM
CP0648581
sodium 6-(5'-chloro-2'-isobutoxybiphenyl-2-yl)picolinate
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C22H19ClNNaO3
 3
1 IC50 = 15.85 nM
2 IC50 = 16 nM
3 Ki = 2.512 nM
CP0659705
sodium 2-(2-(benzyloxy)-5-chlorophenylamino)thiazole-4-carboxylate
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C17H12ClN2NaO3S
 1
1 IC50 = 25.12 nM
CP0109664
2''-benzyloxy-5''-chloro-[1,1';2',1'']terphenyl-3-carboxylic acid
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C26H19ClO3
 1
1 IC50 = 50.12 nM
CP0095751
(5Z,13E,15S)-9alpha,11alpha,15-trihydroxyprosta-5,13-dien-1-oic acid
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C20H34O5
 1
1 IC50 = 220 nM
CP0070143
2-(2-benzoyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl)acetic acid
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C20H18N2O3
 1
1 IC50 > 10000 nM
CP0663915
4-((S)-1-((R)-1-(2-phenoxyethyl)piperidine-2-carboxamido)ethyl)benzoic acid hydrochloride
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C23H29ClN2O4
 2
1 IC50 > 25000 nM
2 Ki > 17500 nM
CP0099081
3-(3-(2-(benzyloxy)-5-chlorophenyl)thiophen-2-yl)benzoic acid
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C24H17ClO3S
 2
1 Ki = 4 nM
2 Ki = 70 nM
CP0179414
3-(2-((E)-3-(4-(benzyloxy)-3-methoxyphenyl)prop-1-enyl)phenyl)-N-(thiophen-2-ylsulfonyl)acrylamide
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C30H27NO5S2
 1
1 Ki = 1500 nM
CP0160939
(E)-3-[2-(3,4-dichlorophenyl)phenyl]-N-thiophen-2-ylsulfonylprop-2-enamide
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C19H13Cl2NO3S2
 1
1 Ki = 8200 nM
CP0277044
(E)-3-{2-[(E)-3-(2-Benzyloxy-3-methyl-phenyl)-allyl]-phenyl}-acrylic acid
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C26H24O3
 1
1 Ki = 12000 nM
CP0084755
7-{(R)-2-[(E)-3-Hydroxy-3-(1-phenyl-cyclopropyl)-propenyl]-5-oxo-pyrrolidin-1-yl}-heptanoic acid
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C23H31NO4
 1
1 Ki = 28000 nM
CP0045193
US8933098, 1
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C21H25N3O4
 1
1 Ki > 17500 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
CP0058712
N-[5-(2,6-dichlorophenyl)-1,3,4-thiadiazol-2-yl]-4-ethyl-2,3-dihydro-1,4-benzoxazine-6-carboxamide
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C19H16Cl2N4O2S
 1
1 Ki > 25118.86 nM
Clinical Information about the Protein
Target 1 ( Prostaglandin E2 receptor EP1 (PTGER1) )
Target Type Clinical trial Target
Disease 2 Target-related Diseases  2
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
2 Pollakiuria [ICD-11: MF50.1]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 PGF2alpha Clinical trial
Solid tumour/cancer
Discontinued Drug(s) 1 Discontinued Drug  1
1 ONO-8130 Terminated
Pollakiuria