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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 1759

Nomenclature: TLR9

Family: Toll-like receptor family

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1032 3p21.2 TLR9 toll like receptor 9
Mouse 1 1032 9 F1 Tlr9 toll-like receptor 9
Rat - - 8 Tlr9 toll-like receptor 9
Previous and Unofficial Names Click here for help
CD289 | toll-like receptor 9
Database Links Click here for help
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas

Download all structure-activity data for this target as a CSV file go icon to follow link

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
agatolimod Small molecule or natural product Immunopharmacology Ligand Hs Agonist - - 5
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
hydroxychloroquine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Guide to Malaria Pharmacology Ligand Hs Antagonist 7.1 pIC50 3
pIC50 7.1 (IC50 8x10-8 M) [3]
Description: Inhibition of hTLR9 CpG2006-induced luciferase reporter gene activation.
Immunopharmacology Comments
TLR9 is an endosomal receptor detecting viral and bacterial CpG DNA and genomic DNA from some protozoan species [4]. Activated TLR9 receptors expressed by B cells and plasmacytoid dendritic cells, stimulate human B-cell proliferation, enhance antigen-specific antibody production and induce IFN-α production, IL-10 secretion and natural killer cell activity.
Immuno Process Associations
Immuno Process:  B cell (activation)
Immuno Process:  Inflammation
Immuno Process:  Immune system development
Immuno Process:  Immune regulation
Immuno Process:  Cytokine production & signalling
Immuno Process:  Chemotaxis & migration
Immuno Process:  Cellular signalling
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Asthma, susceptibility to
Disease Ontology: DOID:2841
OMIM: 600807
Disease:  Cerebral malaria
Synonyms: Malaria, susceptibility to [OMIM: 611162]
Disease Ontology: DOID:14069
OMIM: 611162
Disease:  Cervical cancer
Disease Ontology: DOID:4362
OMIM: 603956
Disease:  Endometrial cancer
Disease Ontology: DOID:1380
OMIM: 608089
Disease:  Human immunodeficiency virus type 1, susceptibility to
Synonyms: Human immunodeficiency virus infectious disease [Disease Ontology: DOID:526]
Disease Ontology: DOID:526
OMIM: 609423
Orphanet: ORPHA319269
Disease:  Lupus nephritis
Disease:  Lymphoma, non-hodgkin, familial
Description: A lymphoma that is characterized as any kind of lymphoma except Hodgkin's lymphoma. Symptoms include enlarged lymph nodes, fever, night sweats, weight loss, and lethargy.
Synonyms: Non-Hodgkin lymphoma [Disease Ontology: DOID:0060060]
Disease Ontology: DOID:0060060
OMIM: 605027
Disease:  Prostate cancer
Disease Ontology: DOID:10283
OMIM: 176807
Disease:  Systemic lupus erythematosus
Description: SLE is a complex autoimmune disease that is characterised by inflammation of various connective tissues, and symptoms include dermatitis, arthritis, inflammation of the kidneys (glomerulonephritis), vasculitis, inflammation of the tissue surrounding the heart, and seizures. It is caused by the production of autoantibodies against widely expressed nuclear, cytoplasmic, and cell surface molecules. Extracellular RNA in the circulation in combination with the presence of autoantibodies potently stimulates interferon production and immune system activation.
Disease Ontology: DOID:9074
OMIM: 152700
Orphanet: ORPHA536
General Comments
TLR9 is an intracellular detector for pathogen-derived nucleic acids, in particular CpG dinucleotides. Trafficking of endosomal TLR9 is tightly controlled to prevent inappropriate activation [2].
The potential role of TLR9 in immuno-oncology is reviewed in [1].


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1. Adams JL, Smothers J, Srinivasan R, Hoos A. (2015) Big opportunities for small molecules in immuno-oncology. Nat Rev Drug Discov, 14 (9): 603-22. [PMID:26228631]

2. Babdor J, Descamps D, Adiko AC, Tohmé M, Maschalidi S, Evnouchidou I, Vasconcellos LR, De Luca M, Mauvais FX, Garfa-Traore M et al.. (2017) IRAP+ endosomes restrict TLR9 activation and signaling. Nat Immunol, 18 (5): 509-518. [PMID:28319098]

3. Lamphier M, Zheng W, Latz E, Spyvee M, Hansen H, Rose J, Genest M, Yang H, Shaffer C, Zhao Y et al.. (2014) Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo. Mol Pharmacol, 85 (3): 429-40. [PMID:24342772]

4. Uematsu S, Akira S. (2008) Toll-Like receptors (TLRs) and their ligands. Handb Exp Pharmacol, (183): 1-20. [PMID:18071652]

5. (2006) CpG 7909: PF 3512676, PF-3512676. Drugs R D, 7 (5): 312-6. [PMID:16922592]


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