PMID
Data
Article Title
Organization
Identification of High-Potency Human TLR8 and Dual TLR7/TLR8 Agonists in Pyrimidine-2,4-diamines.

University of Minnesota
Incorporation of Phosphonate into Benzonaphthyridine Toll-like Receptor 7 Agonists for Adsorption to Aluminum Hydroxide.

Genomics Institute of Novartis Research Foundation
Structure-Based Design of Human TLR8-Specific Agonists with Augmented Potency and Adjuvanticity.

University of Kansas
Structural requirements for TLR7-selective signaling by 9-(4-piperidinylalkyl)-8-oxoadenine derivatives.

Glaxosmithkline
Human Toll-like receptor 8-selective agonistic activities in 1-alkyl-1H-benzimidazol-2-amines.

University of Kansas
Dihydropyrrolo[2,3-d]pyrimidines: Selective Toll-Like Receptor 9 Antagonists from Scaffold Morphing Efforts.

Sumitomo Dainippon Pharma
Identification and optimization of pteridinone Toll-like receptor 7 (TLR7) agonists for the oral treatment of viral hepatitis.

Gilead Sciences
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.

University of Kansas
Discovery of Imidazoquinolines with Toll-Like Receptor 7/8 Independent Cytokine Induction.

TBA
Structure-activity relationships in human Toll-like receptor 8-active 2,3-diamino-furo[2,3-c]pyridines.

University of Kansas
Toll-like receptor (TLR)-7 and -8 modulatory activities of dimeric imidazoquinolines.

University of Kansas
Synthesis and biological evaluation of 8-oxoadenine derivatives as toll-like receptor 7 agonists introducing the antedrug concept.

Dainippon Sumitomo Pharma
Discovery of the TLR7/8 Antagonist MHV370 for Treatment of Systemic Autoimmune Diseases.

Novartis Institutes for Biomedical Research
Identification and Optimization of Small Molecule Pyrazolopyrimidine TLR7 Agonists for Applications in Immuno-oncology.

Bristol Myers Squibb
Discovery of Novel TLR7 Agonists as Systemic Agent for Combination With aPD1 for Use in Immuno-oncology.

Bristol-Myers Squibb Research & Development
Small-Molecule Modulators Targeting Toll-like Receptors for Potential Anticancer Therapeutics.

West China Hospital
Generation and structure-activity relationships of novel imidazo-thienopyridine based TLR7 agonists: application as payloads for immunostimulatory antibody drug-conjugates.

Zymeworks
Recent advances in small molecule based cancer immunotherapy.

Southern Medical University
Novel Thienopyrrole Compounds for Treating Autoimmune Diseases and Inflammatory Conditions.

Smith, Gambrell & Russell
Structural evolution of toll-like receptor 7/8 agonists from imidazoquinolines to imidazoles.

Panjab University
If small molecules immunotherapy comes, can the prime be far behind?

Zhejiang University
Agonist and antagonist ligands of toll-like receptors 7 and 8: Ingenious tools for therapeutic purposes.

University of Montpellier
Structural Evolution and Translational Potential for Agonists and Antagonists of Endosomal Toll-like Receptors.

Csir-Indian Institute of Chemical Biology
Toll-like receptor 7 and 8 imidazoquinoline-based agonist/antagonist pairs.

University of Minnesota
Identification of 2-Pyridinylindole-Based Dual Antagonists of Toll-like Receptors 7 and 8 (TLR7/8).

Biocon Bristol Myers Squibb Research Center (Bbrc)
Development, Optimization, and In Vivo Validation of New Imidazopyridine Chemotypes as Dual TLR7/TLR9 Antagonists through Activity-Directed Sequential Incorporation of Relevant Structural Subunits.

Csir-Indian Institute of Chemical Biology
Small molecule approaches to treat autoimmune and inflammatory diseases (Part II): Nucleic acid sensing antagonists and inhibitors.

Roche Innovation Center Shanghai
Structure-Based Optimization of a Fragment-like TLR8 Binding Screening Hit to an

Novartis Institutes For Biomedical Research
Spiro(isobenzofuranazetidine) Compounds for Treating Autoimmune Diseases.

Smith, Gambrell & Russell
Systematic Optimization of Potent and Orally Bioavailable Purine Scaffold as a Dual Inhibitor of Toll-Like Receptors 7 and 9.

Csir-Indian Institute of Chemical Biology
Structure-Based Design of Highly Potent Toll-like Receptor 7/8 Dual Agonists for Cancer Immunotherapy.

Beijing Advanced Innovation Center For Human Brain Protection
Novel Triazatricycle Compounds for Treating Autoimmune Diseases.

Smith, Gambrell & Russell
Further hit optimization of 6-(trifluoromethyl)pyrimidin-2-amine based TLR8 modulators: Synthesis, biological evaluation and structure-activity relationships.

University of Ljubljana
Novel Carbazoles for Treating Inflammatory and Autoimmune Diseases.

Smith, Gambrell & Russell
Identification of a Human Toll-Like Receptor (TLR) 8-Specific Agonist and a Functional Pan-TLR Inhibitor in 2-Aminoimidazoles.

University of Kansas
Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway.

Genomics Institute of The Novartis Research Foundation
Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B.

Gilead Sciences
Modulation of the Innate Immune Response by Targeting Toll-like Receptors: A Perspective on Their Agonists and Antagonists.

University of Siena
Novel Hexahydro-1

Smith, Gambrell & Russell
Optimization of 8-oxoadenines with toll-like-receptor 7 and 8 activity.

University of Montana
Discovery of Potent and Orally Bioavailable Small Molecule Antagonists of Toll-like Receptors 7/8/9 (TLR7/8/9).

Princ
Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay.

Genomics Institute of The Novartis Research Foundation
Further exploration of the structure-activity relationship of imidazoquinolines; identification of potent C7-substituted imidazoquinolines.

University of Kansas
Human Toll-like Receptor (TLR) 8-Specific Agonistic Activity in Substituted Pyrimidine-2,4-diamines.

University of Minnesota
Rationally Designed Small-Molecule Inhibitors Targeting an Unconventional Pocket on the TLR8 Protein-Protein Interface.

The University of Tokyo
Discovery of Novel Small Molecule Dual Inhibitors Targeting Toll-Like Receptors

University of Colorado Boulder
Identification and characterization of a novel chemotype for human TLR8 inhibitors.

Freie Universit£T Berlin
Structure-activity relationship analysis of imidazoquinolines with Toll-like receptors 7 and 8 selectivity and enhanced cytokine induction.

University of Minnesota
NLRP3 Modulators for the Treatment of Autoinflammatory Disorders.

Usona Institute
Design and Synthesis of N1-Modified Imidazoquinoline Agonists for Selective Activation of Toll-like Receptors 7 and 8.

University of Minnesota
Discovery of Small Molecules as Multi-Toll-like Receptor Agonists with Proinflammatory and Anticancer Activities.

University of Colorado Boulder
3-ARYLOXYL-3-FIVE-MEMBERED HETEROARYL PROPYLAMINE COMPOUND AND USE THEREOF

Shanghai Leado Pharmatech Co.
NAMPT MODULATORS

Cytokinetics, Incorporated
FABI INHIBITORS FOR GRAM-NEGATIVE PATHOGENS

University of Illinois
HETEROCYCLIC G-PROTEIN-COUPLED RECEPTOR 52 (GPR52) AGONISTS

University Of Texas
Bicyclic compounds and their uses

Novartis
3-(1H-IMIDAZOL-2-YL)-2,3,8,8A-TETRAHYDROINDOLIZIN-5(1H)-ONE DERIVATIVES USEFUL AS FACTOR XIA INHIBITORS

Janssen Pharmaceutica
NOVEL TRICYCLIC AROMATIC HETEROCYCLIC COMPOUND AND PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION AND USE THEREOF

Shanghai Longwood Biopharmaceuticals
Compounds for the treatment of BRAF-associated diseases and disorders

Array Biopharma
Formulations of Tie-2 activators and methods of use thereof

Eyepoint Pharmaceuticals
Combination of isoindolinone derivatives with SGI-110

Astex Therapeutics
EPAC antagonists

University Of Texas
Inhibitors of RAF kinases

Kinnate Biopharma
Human plasma kallikrein inhibitors

Biocryst Pharmaceuticals
Compounds as neuronal histamine receptor-3 antagonists and uses thereof

Xw Laboratories
Substituted pyrazolo/imidazolo bicyclic compounds as PDE2 inhibitors

Merck Sharp & Dohme
Chemokine CXCR1 and CXCR2 receptor antagonist compounds, and use thereof in the treatment of chemokine-mediated pathologies

Galderma Research & Development
Fused tricyclic compounds as Raf kinase inhibitors

Beigene
Macrocycle and composition comprising thereof

Shenzhen Targetrx
Imidazo[1,2-B][1,2,4]triazines as c-Met inhibitors

Incyte Incorporation
Potent soluble epdxide hydrolase inhibitors

Eicosis
Substituted pyrrolidines as factor xia inhibitors for the treatment thromboembolic diseases

Ono Pharmaceutical
S1P receptors modulators

Akaal Pharma
Anti-viral compounds

Abbvie
Tricyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors

Merck Sharp & Dohme
Pyrazolopyrimidine compounds as kinase inhibitors

Principia Biopharma
Nitrogen-containing spirocyclic compounds and pharmaceutical uses thereof

Japan Tobacco