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

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

Sumitomo Dainippon Pharma
Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility.

Dainippon Sumitomo Pharma
Discovery of Imidazoquinolines with Toll-Like Receptor 7/8 Independent Cytokine Induction.

TBA
Medicinal chemistry approaches to avoid aldehyde oxidase metabolism.

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

University of Kansas
Discovery of a highly potent series of TLR7 agonists.

Pfizer
Preliminary evaluation of a 3H imidazoquinoline library as dual TLR7/TLR8 antagonists.

University of Kansas
Toward self-adjuvanting subunit vaccines: model peptide and protein antigens incorporating covalently bound toll-like receptor-7 agonistic imidazoquinolines.

University of Kansas
Design and optimisation of orally active TLR7 agonists for the treatment of hepatitis C virus infection.

Pfizer
Syntheses of fluorescent imidazoquinoline conjugates as probes of Toll-like receptor 7.

University of Kansas
Structure-activity relationships in human toll-like receptor 7-active imidazoquinoline analogues.

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

Dainippon Sumitomo Pharma
Regioisomerism-dependent TLR7 agonism and antagonism in an imidazoquinoline.

University of Kansas
Small molecule modulators of toll-like receptors.

Schering-Plough Research Institute
Novel Phosphorylpurinone Compounds for Treating Cancer.

Smith, Gambrell & Russell
Synthesis and Optimization of 1-Substituted Imidazo[4,5-

Binghamton University School of Pharmacy and Pharmaceutical Sciences
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
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
Covalently Conjugated NOD2/TLR7 Agonists Are Potent and Versatile Immune Potentiators.

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

Smith, Gambrell & Russell
Synthesis and characterization of new potent TLR7 antagonists based on analysis of the binding mode using biomolecular simulations.

Csir-Indian Institute of Chemical Biology
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
Novel Hexahydro-1

Smith, Gambrell & Russell
Potent and Selective Inhibitors of MTH1 Probe Its Role in Cancer Cell Survival.

Astrazeneca
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
Synthesis and immunostimulatory activity of sugar-conjugated TLR7 ligands.

Kagoshima University
Further exploration of the structure-activity relationship of imidazoquinolines; identification of potent C7-substituted imidazoquinolines.

University of Kansas
A Chemical Switch for Transforming a Purine Agonist for Toll-like Receptor 7 to a Clinically Relevant Antagonist.

Csir-Indian Institute of Chemical Biology
Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[

Glaxosmithkline
Novel and Selective TLR7 Antagonists among the Imidazo[1,2-

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

University of Colorado Boulder
Selective Toll-like receptor 7 agonists with novel chromeno[3,4-d]imidazol-4(1H)-one and 2-(trifluoromethyl)quinoline/ quinazoline-4-amine scaffolds.

University of Ljubljana
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
Activity-guided development of potent and selective toll-like receptor 9 antagonists.

Csir-Indian Institute of Chemical Biology
Toll-like Receptors for the Treatment of Autoimmune, Inflammation, and Infectious Diseases.

Usona Institute
Discovery of Novel Small-Molecule Inhibitors of NF-κB Signaling with Antiinflammatory and Anticancer Properties.

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

University of Minnesota
Design and development of benzoxazole derivatives with toll-like receptor 9 antagonism.

Csir-Indian Institute of Chemical Biology
Identification and Optimization of Pyrrolo[3,2-d]pyrimidine Toll-like Receptor 7 (TLR7) Selective Agonists for the Treatment of Hepatitis B.

Janssen Pharmaceutica
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
Perspectives on SARS-CoV-2 Main Protease Inhibitors.

Michigan State University
Human plasma kallikrein inhibitors

Biocryst Pharmaceuticals
KDM5 inhibitors

Merck Sharp & Dohme
JAK kinase inhibitor compounds for treatment of respiratory disease

Theravance Biopharma R&D Ip
Compounds as neuronal histamine receptor-3 antagonists and uses thereof

Xw Laboratories
Piperidin-4-yl azetidine derivatives as JAK1 inhibitors

Incyte Holdings
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
Aza-heteroaryl compounds as PI3K-gamma inhibitors

Incyte
Fused tricyclic compounds as Raf kinase inhibitors

Beigene
Macrocycle and composition comprising thereof

Shenzhen Targetrx
6-hydroxy-5-(phenyl/heteroarylsulfonyl)pyrimidin-4(1H)-one as APJ agonists

Bristol-Myers Squibb
Imidazo[1,2-B][1,2,4]triazines as c-Met inhibitors

Incyte Incorporation
Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof

Enanta Pharmaceuticals
Pyrazolopyrimidine derivatives as BTK inhibitors for the treatment of cancer

Loxo Oncology
Potent soluble epdxide hydrolase inhibitors

Eicosis
Synthesis and biological evaluation of novel series of aminopyrimidine derivatives as urease inhibitors and antimicrobial agents.

Solapur University
Cysteine protease inhibitors and uses thereof

Columbia University
Substituted pyrrolidines as factor xia inhibitors for the treatment thromboembolic diseases

Ono Pharmaceutical
Compositions, synthesis, and methods of using phenylcycloalkylmethylamine derivatives

Reviva Pharmaceuticals
S1P receptors modulators

Akaal Pharma
Anti-viral compounds

Abbvie
Use of 1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors

Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F.
Hydroxamic acid derivative

Taisho Pharmaceutical
Tricyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors

Merck Sharp & Dohme
Heterocyclic acrylamides and their use as pharmaceuticals

Fab Pharma
TRPV3 modulators

Abbvie
Pyrazolopyrimidine compounds as kinase inhibitors

Principia Biopharma
Nitrogen-containing spirocyclic compounds and pharmaceutical uses thereof

Japan Tobacco
Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors.

Eli Lilly