PMID

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Article Title

Organization

Boronic acid-containing aminopyridine- and aminopyrimidinecarboxamide CXCR1/2 antagonists: Optimization of aqueous solubility and oral bioavailability.

Syntrix Biosystems

Boronic acid-containing CXCR1/2 antagonists: Optimization of metabolic stability, in vivo evaluation, and a proposed receptor binding model.

Syntrix Biosystems

Discovery of 2-[5-(4-Fluorophenylcarbamoyl)pyridin-2-ylsulfanylmethyl]phenylboronic Acid (SX-517): Noncompetitive Boronic Acid Antagonist of CXCR1 and CXCR2.

Syntrix Biosystems

Colloidal aggregation causes inhibition of G protein-coupled receptors.

University Of North Carolina At Chapel Hill

Chemokine receptor antagonists.

National Heart And Lung Institute

Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.

Schering-Plough Research Institute

Discovery of potent and orally bioavailable N,N'-diarylurea antagonists for the CXCR2 chemokine receptor.

Glaxosmithkline

Discovery, optimization, and pharmacological characterization of novel heteroaroylphenylureas antagonists of C-C chemokine ligand 2 function.

Telik

Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.

Genzyme

Design, synthesis, and evaluation of novel 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective CXCR2 chemokine receptor antagonists.

Wuxi Pharmatech

Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region.

Schering-Plough Research Institute

Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors.

Grupo Uriach

3,4-Diamino-1,2,5-thiadiazole as potent and selective CXCR2 antagonists.

Schering-Plough Research Institute

Fluoroalkyl alpha side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2-CXCR1 dual antagonists.

Schering-Plough Research Institute

Polyoxygenated dysidea sterols that inhibit the binding of [I125] IL-8 to the human recombinant IL-8 receptor type A.

Griffith University

Synthesis and structure-activity relationships of heteroaryl substituted-3,4-diamino-3-cyclobut-3-ene-1,2-dione CXCR2/CXCR1 receptor antagonists.

Schering-Plough Research Institute

3,4-Diamino-2,5-thiadiazole-1-oxides as potent CXCR2/CXCR1 antagonists.

Schering-Plough Research Institute

3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.

Glaxosmithkline

C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists.

Schering-Plough Research Institute

N,N'-Diarylcyanoguanidines as antagonists of the CXCR2 and CXCR1 chemokine receptors.

Glaxosmithkline

Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency.

Pharmaceutical Research Institute

Synthesis and structure-activity relationships of 3,5-diarylisoxazoles and 3,5-diaryl-1,2,4-oxadiazoles, novel classes of small molecule interleukin-8 (IL-8) receptor antagonists.

Johnson And Johnson Pharmaceutical Research And Development

Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor.

Glaxosmithkline

Design, synthesis, and evaluation of pyrrolidine based CXCR4 antagonists with in vivo anti-tumor metastatic activity.

Soochow University

Discovery of 1,5-Dihydro-4

Zhejiang University

Structural optimization of aminopyrimidine-based CXCR4 antagonists.

Soochow University

Targeting CXCR1/2: The medicinal potential as cancer immunotherapy agents, antagonists research highlights and challenges ahead.

Hangzhou Institute Of Innovative Medicine

Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.

TBA

Synthesis and structure-activity relationships of indazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists.

Glaxosmithkline

Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists.

Gsk Pharmaceuticals R & D

2',3'-Dideoxy-N6-cyclohexyladenosine: an adenosine derivative with antagonist properties at adenosine receptors.

Pharmakologisches Institut

Quantitative evaluation of each catalytic subsite of cathepsin B for inhibitory activity based on inhibitory activity-binding mode relationship of epoxysuccinyl inhibitors by X-ray crystal structure analyses of complexes.

Osaka University Of Pharmaceutical Sciences