Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T38529 | Target Info | |||
| Target Name | Prostaglandin E2 receptor EP2 (PTGER2) | ||||
| Synonyms |
Prostanoid EP2 receptor; Prostaglandin E2 receptor EP2 subtype; PGE2 receptor EP2 subtype; PGE receptor, EP2 subtype; PGE receptor EP2 subtype; EP2 receptor
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| Target Type | Successful Target | ||||
| Gene Name | PTGER2 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 34 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
L-798,106
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Investigative | Compound Info | ||
| Synonyms |
L798106; L-798106
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| 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
|
[2] | |||
| Compound Name |
Methyl 7-[(1R,2S)-2-[3-(1-hydroxyhexyl)phenyl]-5-oxocyclopentyl]heptanoate
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2014025; CHEMBL3911438
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| Activity |
Ki = 50000 nM
|
[3] | |||
| 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
|
[4] | |||
| Compound Name |
Methyl 7-[(1R,2R,5S)-2-chloro-5-[4-(1-hydroxyhexyl)phenyl]cyclopentyl]heptanoate
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2007935; CHEMBL3898887
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| Activity |
Ki = 50000 nM
|
[3] | |||
| Compound Name |
7-[(1R,2R,5S)-2-Chloro-5-[4-(1-hydroxyhexyl)phenyl]cyclopentyl]heptan-1-ol
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2012791; CHEMBL3961847
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| Activity |
Ki = 50000 nM
|
[3] | |||
| Compound Name |
Methyl 7-[(1R,2R,5S)-2-fluoro-5-[4-(1-hydroxyhexyl)phenyl]cyclopentyl]heptanoate
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2009620; CHEMBL3957958
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| Activity |
Ki = 50000 nM
|
[3] | |||
| Compound Name |
Methyl 7-[(5S)-5-[4-(1-hydroxyhexyl)phenyl]cyclopenten-1-yl]heptanoate
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2009541; CHEMBL3947785
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| Activity |
Ki = 50000 nM
|
[3] | |||
| Compound Name |
7-[(1R,2S)-2-[3-(1-Hydroxyhexyl)phenyl]-5-oxocyclopentyl]heptanoic acid
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2010315; CHEMBL3914108
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| Activity |
EC50 = 50000 nM
|
[3] | |||
| 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
|
[5] | |||
| Compound Name |
7-{(R)-2-[(E)-3-Hydroxy-3-(5-trifluoromethyl-furan-2-yl)-propenyl]-5-oxo-pyrrolidin-1-yl}-heptanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL45418; SCHEMBL5733643; BDBM50142490
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| Activity |
Ki = 58000 nM
|
[6] | |||
| 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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| Activity |
Ki = 68000 nM
|
[6] | |||
| Compound Name |
(E)-3-[2-[3-[(E)-2-(7-Chloroquinolin-2-yl)ethenyl]phenyl]phenyl]-N-thiophen-2-ylsulfonylprop-2-enamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL314616; SCHEMBL7248587; BDBM50117683
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| Activity |
Ki = 70000 nM
|
[7] | |||
| Compound Name |
7-[(R)-2-((E)-(S)-4-Cyclohexyl-3-hydroxy-but-1-enyl)-5-oxo-pyrrolidin-1-yl]-heptanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL42129; BDBM50142477
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| Activity |
Ki = 71000 nM
|
[6] | |||
| Compound Name |
5-[3-[(5R)-3,3-Difluoro-5-[(E,3R,4S)-3-hydroxy-4-methyl-9-phenylnon-1-enyl]-2-oxopyrrolidin-1-yl]propyl]thiophene-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3893847; SCHEMBL15586955; BDBM190297; US9180116, 39D
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| Activity |
EC50 = 79000 nM
|
[8] | |||
| 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 = 85000 nM
|
[6] | |||
| Compound Name |
4''-(Benzyloxy)-1,1':3',1''-terbenzene-2-propionic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL127204; BDBM50134510; 3-(4''''-Benzyloxy-[1,1'';3'',1'''']terphenyl-2-yl)-propionic acid
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| Activity |
Ki ~ 97000 nM
|
[9] | |||
| Compound Name |
N-[4'-(6-Oxo-5,6,11,12-tetrahydrodibenzo[b,f]azocine-5-ylmethyl)-2-biphenylylsulfonyl]benzenepropanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL90227; BDBM50081436
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| Activity |
Ki ~ 100000 nM
|
[10] | |||
| 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
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[7] | |||
| 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
|
[6] | |||
| 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
|
[10] | |||
| 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 ~ 100000 nM
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[6] | |||
| Compound Name |
1-Tert-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 |
CHEMBL88154; BDBM50081456
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| Activity |
Ki ~ 100000 nM
|
[10] | |||
| 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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|
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| Activity |
Ki ~ 100000 nM
|
[10] | |||
| Compound Name |
3-(2-((6-(Benzyloxy)naphthalen-2-yl)methyl)phenyl)-N-(5-bromo-2-methoxyphenylsulfonyl)acrylamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL217941; BDBM50193935
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|
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| Activity |
Ki ~ 100000 nM
|
[1] | |||
| Compound Name |
7-[(2R)-2-[(E)-3-[3-(4-Chloro-2-methylphenyl)phenyl]-3-hydroxyprop-1-enyl]-5-oxopyrrolidin-1-yl]heptanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL298026; SCHEMBL5733175; BDBM50142476
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| Activity |
Ki ~ 100000 nM
|
[6] | |||
| 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
|
[10] | |||
| Compound Name |
alpha-Methyl-N-[4'-(6-oxo-5,6,11,12-tetrahydrodibenzo[b,f]azocine-5-ylmethyl)-2-biphenylylsulfonyl]benzeneacetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL90491; BDBM50081453
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| Activity |
Ki ~ 100000 nM
|
[10] | |||
| 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
|
[10] | |||
| 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
|
[10] | |||
| 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
|
[10] | |||
| 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
|
[10] | |||
| Compound Name |
alpha,alpha-Dimethyl-N-[4'-(6-oxo-5,6,11,12-tetrahydrodibenzo[b,f]azocine-5-ylmethyl)-2-biphenylylsulfonyl]benzenepropanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL315391; BDBM50081445
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| Activity |
Ki ~ 100000 nM
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[10] | |||
| Compound Name |
7-{(R)-2-[(E)-3-Hydroxy-3-(1-phenyl-cyclopropyl)-propenyl]-5-oxo-pyrrolidin-1-yl}-heptanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL280223; SCHEMBL6710516; SCHEMBL6710521; BDBM50125409; 7-[(2R)-2-[(E)-3-hydroxy-3-(1-phenylcyclopropyl)prop-1-enyl]-5-oxopyrrolidin-1-yl]heptanoic acid; 7-[(2R)-2beta-[3-Hydroxy-3-(1-phenylcyclopropyl)-1-propenyl]-5-oxopyrrolizino]heptanoic acid; 7-{(2R)-2-[(1E)-3-hydroxy-3-(1-phenylcyclopropyl)prop-1-enyl]-5-oxopyrrolidin-1-yl}heptanoic acid
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| Activity |
Ki = 164000 nM
|
[6] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Comparison between two classes of selective EP(3) antagonists and their biological activities. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5639-42. | ||||
| REF 2 | Piperidine derivatives as nonprostanoid IP receptor agonists. Bioorg Med Chem Lett. 2016 May 1;26(9):2360-4. | ||||
| REF 3 | US patent application no. 7799821B2, Therapeutic compounds | ||||
| REF 4 | Piperidine derivatives as nonprostanoid IP receptor agonists 2. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2886-2889. | ||||
| REF 5 | 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 6 | 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. | ||||
| REF 7 | 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 8 | US patent application no. 9180116B2, Difluorolactam compounds as EP4 receptor-selective agonists for use in the treatment of EP4-mediated diseases and conditions | ||||
| REF 9 | Structure-activity relationship of triaryl propionic acid analogues on the human EP3 prostanoid receptor. Bioorg Med Chem Lett. 2003 Nov 3;13(21):3813-6. | ||||
| REF 10 | 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. | ||||
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