Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T18876 | Target Info | |||
| Target Name | Prostaglandin E2 receptor EP4 (PTGER4) | ||||
| Synonyms |
Prostanoid EP4 receptor; Prostaglandin E2 receptor EP4 subtype; PTGER2; PGE2 receptor EP4 subtype; PGE receptor EP4 subtype
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| Target Type | Clinical trial Target | ||||
| Gene Name | PTGER4 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 17 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
AH6809
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Investigative | Compound Info | ||
| Synonyms |
AH 6809; AH-6809
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| Activity |
Ki ~ 100000 nM
|
[1] | |||
| Compound Name |
(E)-3-[2-(4-Methylsulfanyl-benzyl)-phenyl]-acrylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL165010; SCHEMBL7929810; SCHEMBL7929816; (E)-3-[2-[(4-methylsulfanylphenyl)methyl]phenyl]prop-2-enoic Acid; BDBM50097794; 2-[4-(Methylthio)benzyl]benzeneacrylic acid
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| Activity |
Ki ~ 50000 nM
|
[2] | |||
| 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
|
[3] | |||
| Compound Name |
4-(2-(2-(4-Hydroxy-4-(1-propylcyclobutyl)butyl)-5-oxopyrazolidin-1-yl)ethyl)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL250153; BDBM50224579
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| Activity |
Ki ~ 50000 nM
|
[4] | |||
| 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
|
[5] | |||
| Compound Name |
Schembl20719106
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1770317; BDBM50384443; 5-(6-naphthalen-2-yl-2-oxo-1H-pyridin-3-yl)-5-propan-2-yl-1,3-oxazolidine-2,4-dione
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| Activity |
IC50 ~ 50118.72 nM
|
[6] | |||
| Compound Name |
4''-(6-Oxo-11,12-dihydro-6H-dibenzo[b,f]azocin-5-ylmethyl)-biphenyl-2-sulfonic acid phenylacetyl-amide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL328067; BDBM50081452
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| Activity |
Ki ~ 100000 nM
|
[7] | |||
| Compound Name |
N-(2-Thienylsulfonyl)-3'-(methylsulfonyl)biphenyl-2-propionamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL86820; BDBM50117682; Thiophene-2-sulfonic acid [3-(3''-methanesulfonyl-biphenyl-2-yl)-propionyl]-amide
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| Activity |
Ki ~ 100000 nM
|
[8] | |||
| 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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| Activity |
Ki ~ 100000 nM
|
[7] | |||
| Compound Name |
7-[(S)-2-((E)-(S)-3-Hydroxy-oct-1-enyl)-5-oxo-pyrrolidin-1-yl]-heptanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL295623; BDBM50142496
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| Activity |
EC50 ~ 100000 nM
|
[9] | |||
| Compound Name |
1-[2-[4-[(6-Oxo-11,12-dihydrobenzo[c][1]benzazocin-5-yl)methyl]phenyl]phenyl]sulfonyl-3-(2-thiophen-2-ylethyl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL328697; BDBM50081435
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| Activity |
Ki ~ 100000 nM
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[7] | |||
| Compound Name |
1-Butyl-3-[2-[4-[(6-oxo-11,12-dihydrobenzo[c][1]benzazocin-5-yl)methyl]phenyl]phenyl]sulfonylurea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL91270; BDBM50081446; 1-[4'-(6-Oxo-5,6,11,12-tetrahydrodibenzo[b,f]azocine-5-ylmethyl)-2-biphenylylsulfonyl]-3-butylurea
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| Activity |
Ki ~ 100000 nM
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[7] | |||
| 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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| Activity |
Ki ~ 100000 nM
|
[7] | |||
| Compound Name |
1-Benzyl-3-[2-[4-[(6-oxo-11,12-dihydrobenzo[c][1]benzazocin-5-yl)methyl]phenyl]phenyl]sulfonylurea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL90226; BDBM50081442; 1-[4'-(6-Oxo-5,6,11,12-tetrahydrodibenzo[b,f]azocine-5-ylmethyl)-2-biphenylylsulfonyl]-3-benzylurea
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| Activity |
Ki ~ 100000 nM
|
[7] | |||
| 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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| Activity |
Ki ~ 100000 nM
|
[7] | |||
| 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 ~ 100000 nM
|
[7] | |||
| Compound Name |
7-[(2S)-2-[(E,3R)-3-Hydroxyoct-1-enyl]-5-oxopyrrolidin-1-yl]heptanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
11-Deoxy-8-azaprostaglandin E(1); CHEMBL45372; BDBM50142497; 1-Pyrrolidineheptanoic acid, 2-(3-hydroxy-1-octenyl)-5-oxo-, (R*,S*-(E))-(+-)-; 7-[(S)-2-((E)-(R)-3-Hydroxy-oct-1-enyl)-5-oxo-pyrrolidin-1-yl]-heptanoic acid
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| Activity |
EC50 = 200000 nM
|
[9] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Prostanoid receptor EP2 as a therapeutic target. J Med Chem. 2014 Jun 12;57(11):4454-65. | ||||
| REF 2 | Structure-activity relationship on the human EP3 prostanoid receptor by use of solid-support chemistry. Bioorg Med Chem Lett. 2001 Mar 12;11(5):747-9. | ||||
| REF 3 | Piperidine derivatives as nonprostanoid IP receptor agonists. Bioorg Med Chem Lett. 2016 May 1;26(9):2360-4. | ||||
| REF 4 | Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists. Bioorg Med Chem Lett. 2007 Dec 1;17(23):6572-5. | ||||
| REF 5 | Piperidine derivatives as nonprostanoid IP receptor agonists 2. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2886-2889. | ||||
| REF 6 | Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists. ACS Med Chem Lett. 2010 May 14;1(7):316-20. | ||||
| REF 7 | 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 8 | Structure-activity relationship of biaryl acylsulfonamide analogues on the human EP(3) prostanoid receptor. Bioorg Med Chem Lett. 2002 Sep 16;12(18):2583-6. | ||||
| REF 9 | 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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