Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T85467 | Target Info | |||
| Target Name | Prostaglandin E2 receptor EP3 (PTGER3) | ||||
| Synonyms |
Prostanoid EP3 receptor; Prostaglandin E2 receptor EP3 subtype; PGE2-R; PGE2 receptor EP3 subtype; PGE receptor, EP3 subtype; PGE receptor EP3 subtype
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| Target Type | Clinical trial Target | ||||
| Gene Name | PTGER3 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 22 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-[1-[2-(N-Benzoyl-4-methylanilino)ethyl]piperidin-4-yl]oxyacetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3793911; BDBM50163296
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| Compound Name |
2-[1-[2-[N-(1,3-Benzodioxole-5-carbonyl)-4-methylanilino]ethyl]piperidin-4-yl]oxyacetic acid;hydrate;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3798917; BDBM50167257
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| Activity |
Ki ~ 50000 nM
|
[2] | |||
| Compound Name |
1-[2-[4-[(6-Oxo-11,12-dihydrobenzo[c][1]benzazocin-5-yl)methyl]phenyl]phenyl]sulfonyl-3-(2-phenylethyl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL90269; BDBM50081450
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| Activity |
Ki = 51200 nM
|
[3] | |||
| Compound Name |
4-[2-[(2S)-2-[(3R)-3-[3-(4-Chloro-2-methylphenyl)phenyl]-3-hydroxypropyl]-5-oxopyrrolidin-1-yl]ethyl]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL222677; SCHEMBL5733077; BDBM50156551
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| Activity |
Ki = 54000 nM
|
[4] | |||
| Compound Name |
7-[(R)-2-((E)-(S)-4-Cyclobutyl-3-hydroxy-but-1-enyl)-5-oxo-pyrrolidin-1-yl]-heptanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL416262; BDBM50142474
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| Activity |
Ki = 56000 nM
|
[5] | |||
| Compound Name |
4-(2-((S)-2-((S)-5-Cyclobutyl-3-hydroxypentyl)-5-oxopyrrolidin-1-yl)ethyl)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL223744; BDBM50156546
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| Activity |
Ki = 77000 nM
|
[4] | |||
| Compound Name |
4-(2-((R)-2-((S,E)-5-Cyclobutyl-3-hydroxypent-1-enyl)-5-oxopyrrolidin-1-yl)ethyl)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL222782; BDBM50156553
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| Activity |
Ki = 79000 nM
|
[4] | |||
| Compound Name |
4-(2-((S)-2-((S)-3-Hydroxyoctyl)-5-oxopyrrolidin-1-yl)ethyl)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL376347; BDBM50156549
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| Activity |
Ki = 90300 nM
|
[4] | |||
| Compound Name |
7-[(2R)-2-[(E)-3-[3-(4-Chlorophenyl)phenyl]-3-hydroxyprop-1-enyl]-5-oxopyrrolidin-1-yl]heptanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL46671; SCHEMBL5733981; BDBM50142487
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| Activity |
Ki ~ 100000 nM
|
[5] | |||
| Compound Name |
7-[(R)-2-((E)-3-Biphenyl-3-yl-3-hydroxy-propenyl)-5-oxo-pyrrolidin-1-yl]-heptanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL47018; SCHEMBL5734652; BDBM50142478; 7-[(2R)-2-[(E)-3-hydroxy-3-(3-phenylphenyl)prop-1-enyl]-5-oxopyrrolidin-1-yl]heptanoic acid
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| Activity |
Ki ~ 100000 nM
|
[5] | |||
| Compound Name |
5-(2-((R)-2-((S,E)-3-Hydroxyoct-1-enyl)-5-oxopyrrolidin-1-yl)ethyl)thiophene-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL224970; BDBM50156548
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| Activity |
Ki ~ 100000 nM
|
[4] | |||
| Compound Name |
7-[(2R)-2-[(E)-3-[3-(3-Chlorophenyl)phenyl]-3-hydroxyprop-1-enyl]-5-oxopyrrolidin-1-yl]heptanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL47138; SCHEMBL5733047; BDBM50142475
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| Activity |
Ki ~ 100000 nM
|
[5] | |||
| Compound Name |
7-[(2R)-2-[(E)-3-Hydroxy-3-[3-(4-hydroxy-2-methylphenyl)phenyl]prop-1-enyl]-5-oxopyrrolidin-1-yl]heptanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL444574; SCHEMBL5732866; BDBM50142492
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| Activity |
Ki ~ 100000 nM
|
[5] | |||
| Compound Name |
4-(2-((R)-2-((S,E)-3-Hydroxy-4-(3-(methoxymethyl)phenyl)but-1-enyl)-5-oxopyrrolidin-1-yl)ethyl)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL222834; BDBM50156552
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| Activity |
Ki ~ 100000 nM
|
[4] | |||
| Compound Name |
1-[2-[4-[(6-Oxo-11,12-dihydrobenzo[c][1]benzazocin-5-yl)methyl]phenyl]phenyl]sulfonyl-3-(3-phenylpropyl)urea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL90935; BDBM50081443
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|
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| Activity |
Ki ~ 100000 nM
|
[3] | |||
| Compound Name |
7-[(R)-2-((E)-3-Hydroxy-4-phenyl-but-1-enyl)-5-oxo-pyrrolidin-1-yl]-heptanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL14359; SCHEMBL10029805; BDBM50125417; 7-[(2R)-2beta-(3-Hydroxy-4-phenyl-1-butenyl)-5-oxopyrrolizino]heptanoic acid
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| Activity |
Ki = 100000 nM
|
[5] | |||
| Compound Name |
7-{(R)-2-[(E)-3-Hydroxy-3-(3-phenoxy-phenyl)-propenyl]-5-oxo-pyrrolidin-1-yl}-heptanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL288978; SCHEMBL5733153; BDBM50142486; 7-[(2R)-2-[(E)-3-hydroxy-3-(3-phenoxyphenyl)prop-1-enyl]-5-oxopyrrolidin-1-yl]heptanoic acid
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| Activity |
Ki ~ 100000 nM
|
[5] | |||
| Compound Name |
7-[(2R)-2-[(E)-3-[3-(2-Chlorophenyl)phenyl]-3-hydroxyprop-1-enyl]-5-oxopyrrolidin-1-yl]heptanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL297578; SCHEMBL5735035; BDBM50142493
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|
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| Activity |
Ki ~ 100000 nM
|
[5] | |||
| Compound Name |
7-[(2S)-2-[(3R)-3-Hydroxy-3-[3-(4-hydroxy-2-methylphenyl)phenyl]propyl]-5-oxopyrrolidin-1-yl]heptanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL296715; SCHEMBL5732901; BDBM50142484
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| Activity |
Ki ~ 100000 nM
|
[5] | |||
| Compound Name |
1-Benzyl-1-[2-[4-[(6-oxo-11,12-dihydrobenzo[c][1]benzazocin-5-yl)methyl]phenyl]phenyl]sulfonyl-3-(2-phenylethyl)urea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL91301; BDBM50081449
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|
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| Activity |
Ki ~ 100000 nM
|
[3] | |||
| Compound Name |
1-Methyl-1-[2-[4-[(6-oxo-11,12-dihydrobenzo[c][1]benzazocin-5-yl)methyl]phenyl]phenyl]sulfonyl-3-(2-phenylethyl)urea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL327596; BDBM50081437
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|
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| Activity |
Ki ~ 100000 nM
|
[3] | |||
| Compound Name |
7-{(R)-2-[(E)-3-Hydroxy-3-(3-trifluoromethyl-phenyl)-propenyl]-5-oxo-pyrrolidin-1-yl}-heptanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL417171; SCHEMBL5733260; BDBM50142479
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|
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| Activity |
Ki = 131000 nM
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Piperidine derivatives as nonprostanoid IP receptor agonists. Bioorg Med Chem Lett. 2016 May 1;26(9):2360-4. | ||||
| REF 2 | Piperidine derivatives as nonprostanoid IP receptor agonists 2. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2886-2889. | ||||
| REF 3 | New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor. Bioorg Med Chem Lett. 1999 Sep 20;9(18):2699-704. | ||||
| REF 4 | Lactams as EP4 prostanoid receptor agonists. 3. Discovery of N-ethylbenzoic acid 2-pyrrolidinones as subtype selective agents. J Med Chem. 2004 Dec 2;47(25):6124-7. | ||||
| REF 5 | Lactams as EP4 prostanoid receptor subtype selective agonists. Part 1: 2-Pyrrolidinones-stereochemical and lower side-chain optimization. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1655-9. | ||||
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