PMID

Data

Article Title

Organization

Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension.

Arena Pharmaceuticals

Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP

Novartis Institutes For Biomedical Research

Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.

Askat

Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH

Jagiellonian University Medical College

Discovery of Novel Seven-Membered Prostacyclin Analogues as Potent and Selective Prostaglandin FP and EP3 Dual Agonists.

Ono Pharmaceutical

Discovery of G Protein-Biased EP2 Receptor Agonists.

Ono Pharmaceutical

Piperidine derivatives as nonprostanoid IP receptor agonists 2.

Toray Industries

Optimization of amide-based EP3 receptor antagonists.

Pfizer

Identification and biological activity of 6-alkyl-substituted 3-methyl-pyridine-2-carbonyl amino dimethyl-benzoic acid EP4 antagonists.

Eli Lilly

Piperidine derivatives as nonprostanoid IP receptor agonists.

Toray Industries

Structural optimization and structure-functional selectivity relationship studies of G protein-biased EP2 receptor agonists.

Ono Pharmaceutical

Discovery of potent aryl-substituted 3-[(3-methylpyridine-2-carbonyl) amino]-2,4-dimethyl-benzoic acid EP4 antagonists with improved pharmacokinetic profile.

Eli Lilly

Discovery of highly potent dual EP(2) and EP(3) agonists with subtype selectivity.

Ono Pharmaceutical

Discovery and characterization of a potent and selective EP4 receptor antagonist.

Eli Lilly

A selective prostaglandin E2 receptor subtype 2 (EP2) antagonist increases the macrophage-mediated clearance of amyloid-beta plaques.

Amgen

Prostanoid receptor EP2 as a therapeutic target.

Emory University

From virtual to clinical: The discovery of PGN-1531, a novel antagonist of the prostanoid EP4 receptor.

Argenta Discovery

Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases.

Novartis Institutes For Biomedical Research

1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists: Structure-activity relationships of 4- and 5-substituted benzoic acid derivatives.

Glaxosmithkline

1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists. Structure-activity relationships of 6-substituted and 5,6-disubstituted benzoic acid derivatives.

Glaxosmithkline

Fluorescent Human EP3 Receptor Antagonists.

TBA

Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists.

TBA

Discovery and optimization of CRTH2 and DP dual antagonists.

Amgen

Identification of prostaglandin D2 receptor antagonists based on a tetrahydropyridoindole scaffold.

Merck Frosst Canada

Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist.

Emd-Serono Research Institute

Structure-activity relationships and pharmacokinetic parameters of quinoline acylsulfonamides as potent and selective antagonists of the EP(4) receptor.

Merck Frosst Centre For Therapeutic Research

Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists.

Emd-Serono Research Institute

Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists.

Emd-Serono Research Institute

Comparison between two classes of selective EP(3) antagonists and their biological activities.

Merck Frosst Centre For Therapeutic Research

Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP(3) antagonists.

Merck Frosst Centre For Therapeutic Research

Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.

Fujisawa Pharmaceutical

Discovery of a potent and selective agonist of the prostaglandin EP4 receptor.

Merck Frosst Centre For Therapeutic Research

Synthesis, pharmacophore modeling and in vitro activity of 10,11-dihydrodibenzo[b,f]oxepine-4-carboxamide derivatives as novel and potent antagonists of the prostaglandin EP4 receptor.

Rottapharm Madaus

Naphthalene/quinoline amides and sulfonylureas as potent and selective antagonists of the EP4 receptor.

Merck Frosst Centre For Therapeutic Research

A novel series of potent and selective EP(4) receptor ligands: facile modulation of agonism and antagonism.

Merck Frosst Canada

The identification of substituted benzothiophene derivatives as PGE(2) subtype 4 receptor antagonists: From acid to non-acid.

Merck Frosst Centre For Therapeutic Research

Potent and highly selective DP1 antagonists with 2,3,4,9-tetrahydro-1H-carbazole as pharmacophore.

Merck Frosst Centre For Therapeutic Research

3-Urea-1-(phenylmethyl)-pyridones as novel, potent, and selective EP3 receptor antagonists.

Glaxosmithkline

Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain.

Merck Frosst Canada

Emerging targets in osteoporosis disease modification.

Amgen

1,7-Disubstituted oxyindoles are potent and selective EP(3) receptor antagonists.

Decode Chemistry

Heterocyclic 1,7-disubstituted indole sulfonamides are potent and selective human EP3 receptor antagonists.

Decode Chemistry

The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin E2 subtype 4 receptor antagonist.

Merck Frosst Centre For Therapeutic Research

Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor antagonist, as a novel antiplatelet agent that

Decode Chemistry

7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.

Novartis Institutes Of Biomedical Research

Discovery of novel aminothiadiazole amides as selective EP(3) receptor antagonists.

Glaxosmithkline

Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP(1) receptor antagonist for the treatment of inflammatory pain.

Glaxosmithkline

Discovery of potent and selective DP1 receptor antagonists in the azaindole series.

Merck Frosst Centre For Therapeutic Research

3-Acrylamide-4-aryloxyindoles: synthesis, biological evaluation and metabolic stability of potent and selective EP3 receptor antagonists.

Decode Chemistry

Peri-substituted hexahydro-indolones as novel, potent and selective human EP3 receptor antagonists.

Decode Chemistry

Highly functionalized 7-azaindoles as selective PPAR gamma modulators.

Merck Research Laboratories

Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).

Merck Frosst Canada

Identification of an indole series of prostaglandin D2 receptor antagonists.

Merck Frosst Canada

Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.

Fujisawa Pharmaceutical

Lactams as prostanoid receptor ligands. Part 4: 2-Piperidones as selective EP4 receptor agonists.

Roche Palo Alto

Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.

Fujisawa Pharmaceutical

Lactams as EP4 prostanoid receptor agonists. 3. Discovery of N-ethylbenzoic acid 2-pyrrolidinones as subtype selective agents.

Roche Palo Alto

Lactams as EP4 prostanoid receptor subtype selective agonists. Part 1: 2-Pyrrolidinones-stereochemical and lower side-chain optimization.

Roche Palo Alto

Structure-activity relationship of triaryl propionic acid analogues on the human EP3 prostanoid receptor.

Merck Frosst Centre For Therapeutic Research

Structure-activity relationship of biaryl acylsulfonamide analogues on the human EP(3) prostanoid receptor.

Merck Frosst Centre For Therapeutic Research

Synthesis and biological evaluation of prostaglandin-F alkylphosphinic acid derivatives as bone anabolic agents for the treatment of osteoporosis.

Procter & Gamble Pharmaceuticals

Structure-activity relationship on the human EP3 prostanoid receptor by use of solid-support chemistry.

Merck Frosst Canada

Design and synthesis of 13,14-dihydro prostaglandin F(1alpha) analogues as potent and selective ligands for the human FP receptor.

Procter And Gamble Pharmaceuticals

New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor.

Merck Frosst Centre For Therapeutic Research

Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.

Eli Lilly

Hit-to-lead optimization of 2-(1H-pyrazol-1-yl)-thiazole derivatives as a novel class of EP1 receptor antagonists.

Asahi Kasei Pharma

Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP

Glaxosmithkline

Synthesis and evaluation of a potent, well-balanced EP

Ono Pharmaceutical

Discovery of a novel 2-(1H-pyrazolo[3,4-b]pyridin-1-yl)thiazole derivative as an EP

Asahi Kasei Pharma

Tyrosinase inhibitory effect of benzoic acid derivatives and their structure-activity relationships.

Yonsei University

Discovery and structure-activity relationship of P1-P3 ketoamide derived macrocyclic inhibitors of hepatitis C virus NS3 protease.

Schering-Plough Research Institute

Structural requirements for factor Xa inhibition by 3-oxybenzamides with neutral P1 substituents: combining X-ray crystallography, 3D-QSAR, and tailored scoring functions.

Aventis Pharma Deutschland

Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.

Pfizer

Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 3. Structure activity relationships at C3(1,2).

Bristol-Myers Squibb

 

Ring Size effect in the PKC inhibitory activities of perhydroazepine analogs of balanol.

Sphinx Laboratories

Structure-based design of novel HIV protease inhibitors: carboxamide-containing 4-hydroxycoumarins and 4-hydroxy-2-pyrones as potent nonpeptidic inhibitors.

Upjohn