79 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Data
Article Title
Organization
16
Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP
Novartis Institutes For Biomedical Research
22
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of sulphone-based CRTh2 antagonists.
RhôNe-Poulenc Rorer
42
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists III: the role of a hydrogen-bond acceptor in long receptor residence times.
RhôNe-Poulenc Rorer
50
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists II: lead optimization.
RhôNe-Poulenc Rorer
17
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists I.
RhôNe-Poulenc Rorer
48
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of pyrrolopiperidinone acetic acids as CRTh2 antagonists.
RhôNe-Poulenc Rorer
10
Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD(2) receptors CRTH2 and DP.
Amgen
53
Discovery of isoquinolinone indole acetic acids as antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.
Pfizer
29
Quality by design (QbD) of amide isosteres: 5,5-Disubstituted isoxazolines as potent CRTh2 antagonists with favorable pharmacokinetic and drug-like properties.
Merck Research Laboratories
35
2-(1H-Pyrazol-1-yl)acetic acids as chemoattractant receptor-homologous molecule expressed on Th2 lymphocytes (CRTh2) antagonists.
RhôNe-Poulenc Rorer
46
Isoquinoline derivatives as potent CRTH2 antagonists: design, synthesis and SAR.
Taisho Pharmaceutical
19
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
34
Evolution of novel tricyclic CRTh2 receptor antagonists from a (E)-2-cyano-3-(1H-indol-3-yl)acrylamide scaffold.
Actelion Pharmaceuticals
27
Identification of 2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid (setipiprant/ACT-129968), a potent, selective, and orally bioavailable chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) antagonist.
Actelion Pharmaceuticals
1
Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2.
University of Southern Denmark
44
Diazine indole acetic acids as potent, selective, and orally bioavailable antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.
Pfizer
33
Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis.
Oxagen
67
Novel 2-(2-(benzylthio)-1H-benzo[d]imidazol-1-yl)acetic acids: discovery and hit-to-lead evolution of a selective CRTh2 receptor antagonist chemotype.
Actelion Pharmaceuticals
17
Optimization of the Central Core of Indolinone-Acetic Acid-Based CRTH2 (DP2) Receptor Antagonists.
TBA
57
Discovery of a Novel Series of CRTH2 (DP2) Receptor Antagonists Devoid of Carboxylic Acids.
TBA
23
Isoquinoline derivatives as potent CRTH2 receptor antagonists: synthesis and SAR.
Taisho Pharmaceutical
23
Identification of prostaglandin D2 receptor antagonists based on a tetrahydropyridoindole scaffold.
Merck Frosst Canada
16
Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists.
Amgen
20
Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism.
Amgen
26
Discovery and optimization of a biphenylacetic acid series of prostaglandin D2 receptor DP2 antagonists with efficacy in a murine model of allergic rhinitis.
Amira Pharmaceuticals
48
Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981.
Astrazeneca R&D Charnwood
122
Discovery of potent, selective, and orally bioavailable alkynylphenoxyacetic acid CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases.
Merck Serono
46
Switching between agonists and antagonists at CRTh2 in a series of highly potent and selective biaryl phenoxyacetic acids.
Astrazeneca R&D Charnwood
11
Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist.
Amira Pharmaceuticals
39
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.
Merck Frosst Centre For Therapeutic Research
24
The identification of substituted benzothiophene derivatives as PGE(2) subtype 4 receptor antagonists: From acid to non-acid.
Merck Frosst Centre For Therapeutic Research
15
Azaindoles as potent CRTH2 receptor antagonists.
Merck Frosst Centre For Therapeutic Research
12
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
17
Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists.
7Tm Pharma
60
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1.
7Tm Pharma
79
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2.
7Tm Pharma
11
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
12
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
Amira Pharmaceuticals
17
7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
Novartis Institutes of Biomedical Research
35
Discovery of potent and selective DP1 receptor antagonists in the azaindole series.
Merck Frosst Centre For Therapeutic Research
22
2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
Novartis Institutes of Biomedical Research
7
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
31
Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits.
7Tm Pharma
3
Synthesis of 15R-PGD2: a potential DP2 receptor agonist.
Florida Institute of Technology
4
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
7Tm Pharma
38
Potent and Selective Human Prostaglandin F (FP) Receptor Antagonist (BAY-6672) for the Treatment of Idiopathic Pulmonary Fibrosis (IPF).
Bayer
45
Discovery of MK-8318, a Potent and Selective CRTh2 Receptor Antagonist for the Treatment of Asthma.
Merck Research Laboratory
19
The synthesis of 2,3,6-trisubstituted 1-oxo-1,2-dihydroisoquinolines as potent CRTh
Merck
24
Repurposing human PDE4 inhibitors for neglected tropical diseases. Evaluation of analogs of the human PDE4 inhibitor GSK-256066 as inhibitors of PDEB1 of Trypanosoma brucei.
Northeastern University
10
Nature of the active site of a subunit of the first component of human complement.
Michigan State University
8
S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: I. Cellular, electrophysiological, and neurochemical profile in comparison with ropinirole.
Institut De Recherches Servier
4
Proteinase-activated receptor 2 (PAR(2)): development of a ligand-binding assay correlating with activation of PAR(2) by PAR(1)- and PAR(2)-derived peptide ligands.
The University of Calgary
5
Alkyl-CoA disulfides as inhibitors and mechanistic probes for FabH enzymes.
Portland State University
58
HETEROBIFUNCTIONAL COMPOUNDS AND METHODS OF TREATING DISEASE
Halda Therapeutics OpCo