Details of the Target

General Information of Target

Target ID LDTP12487
Target Name Toll-like receptor 9 (TLR9)
Gene Name TLR9
Gene ID 54106
Synonyms
Toll-like receptor 9; CD antigen CD289
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSAANPETPNSTISREASTQSSSAAASQGWVLPEGKIVPNTVFVGGIDARMDETEIGSCF
GRYGSVKEVKIITNRTGVSKGYGFVSFVNDVDVQKIVGSQIHFHGKKLKLGPAIRKQKLC
ARHVQPRPLVVNPPPPPQFQNVWRNPNTETYLQPQITPNPVTQHVQAYSAYPHSPGQVIT
GCQLLVYNYQEYPTYPDSAFQVTTGYQLPVYNYQPFPAYPRSPFQVTAGYQLPVYNYQAF
PAYPNSPFQVATGYQFPVYNYQPFPAYPSSPFQVTAGYQLPVYNYQAFPAYPNSPFQVAT
GYQFPVYNYQAFPAYPNSPVQVTTGYQLPVYNYQAFPAYPNSPFQVATGYQFPVYNYQAF
PAYPNSPVQVTTGYQLPVYNYQAFPAYPNSPFQVATGYQFPVYNYQAFPAYPNSPVQVTT
GYQLPVYNYQAFPAYPNSAVQVTTGYQFHVYNYQMPPQCPVGEQRRNLWTEAYKWWYLVC
LIQRRD
Target Type
Clinical trial
Target Bioclass
Other
Family
Toll-like receptor family
Subcellular location
Endoplasmic reticulum membrane
Function
Key component of innate and adaptive immunity. TLRs (Toll-like receptors) control host immune response against pathogens through recognition of molecular patterns specific to microorganisms. TLR9 is a nucleotide-sensing TLR which is activated by unmethylated cytidine-phosphate-guanosine (CpG) dinucleotides. Acts via MYD88 and TRAF6, leading to NF-kappa-B activation, cytokine secretion and the inflammatory response. Controls lymphocyte response to Helicobacter infection. Upon CpG stimulation, induces B-cell proliferation, activation, survival and antibody production.
TTD ID
T11451
Uniprot ID
Q9NR96
DrugMap ID
TT2LBCR
Ensemble ID
ENST00000360658.3
HGNC ID
HGNC:15633
ChEMBL ID
CHEMBL5804

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A2780 SNV: p.Q998H .
AGS SNV: p.P100Q .
CHL1 SNV: p.H9N .
COLO792 Deletion: p.L289QfsTer24 .
COLO829 SNV: p.G514S .
HCT15 SNV: p.S569T; p.R899H .
HT SNV: p.D551G DBIA    Probe Info 
HT115 SNV: p.F56L .
Ishikawa (Heraklio) 02 ER SNV: p.P558H .
JURKAT SNV: p.R481Q .
K562 SNV: p.R311Ter .
LN229 SNV: p.M392I .
LNCaP clone FGC SNV: p.Q331H .
MCC13 SNV: p.G442E .
MELJUSO SNV: p.F517S .
MOLT4 SNV: p.R931C .
NCIH358 SNV: p.D842G .
SKMEL3 SNV: p.D842G .
SW1116 SNV: p.V591L .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IPM
 Probe Info  		N.A.  LDD0241  [1]
DBIA
 Probe Info  		C279(3.17)  LDD3408  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C255(0.90)  LDD1507  [3]
 LDCM0226  AC11 HEK-293T C255(0.99)  LDD1509  [3]
 LDCM0276  AC17 HEK-293T C255(0.79)  LDD1515  [3]
 LDCM0278  AC19 HEK-293T C255(1.04)  LDD1517  [3]
 LDCM0285  AC25 HEK-293T C255(0.81)  LDD1524  [3]
 LDCM0287  AC27 HEK-293T C255(1.10)  LDD1526  [3]
 LDCM0290  AC3 HEK-293T C255(1.03)  LDD1529  [3]
 LDCM0294  AC33 HEK-293T C255(0.92)  LDD1533  [3]
 LDCM0296  AC35 HEK-293T C255(1.08)  LDD1535  [3]
 LDCM0303  AC41 HEK-293T C255(0.79)  LDD1542  [3]
 LDCM0305  AC43 HEK-293T C255(1.12)  LDD1544  [3]
 LDCM0311  AC49 HEK-293T C255(0.84)  LDD1550  [3]
 LDCM0314  AC51 HEK-293T C255(1.02)  LDD1553  [3]
 LDCM0320  AC57 HEK-293T C255(0.93)  LDD1559  [3]
 LDCM0322  AC59 HEK-293T C255(1.06)  LDD1561  [3]
 LDCM0356  AKOS034007680 HEK-293T C255(0.93)  LDD1570  [3]
 LDCM0404  CL17 HEK-293T C255(1.00)  LDD1608  [3]
 LDCM0406  CL19 HEK-293T C255(1.15)  LDD1610  [3]
 LDCM0417  CL29 HEK-293T C255(0.80)  LDD1621  [3]
 LDCM0420  CL31 HEK-293T C255(1.01)  LDD1624  [3]
 LDCM0431  CL41 HEK-293T C255(0.88)  LDD1635  [3]
 LDCM0433  CL43 HEK-293T C255(1.07)  LDD1637  [3]
 LDCM0440  CL5 HEK-293T C255(0.93)  LDD1644  [3]
 LDCM0444  CL53 HEK-293T C255(0.91)  LDD1647  [3]
 LDCM0446  CL55 HEK-293T C255(0.98)  LDD1649  [3]
 LDCM0457  CL65 HEK-293T C255(0.94)  LDD1660  [3]
 LDCM0459  CL67 HEK-293T C255(1.08)  LDD1662  [3]
 LDCM0462  CL7 HEK-293T C255(1.04)  LDD1665  [3]
 LDCM0470  CL77 HEK-293T C255(0.91)  LDD1673  [3]
 LDCM0472  CL79 HEK-293T C255(1.05)  LDD1675  [3]
 LDCM0483  CL89 HEK-293T C255(1.11)  LDD1686  [3]
 LDCM0486  CL91 HEK-293T C255(0.98)  LDD1689  [3]
 LDCM0022  KB02 A3-KAW C279(1.76)  LDD2257  [2]
 LDCM0023  KB03 Karpas-422 C279(3.95)  LDD2830  [2]
 LDCM0024  KB05 RL C279(3.17)  LDD3408  [2]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Chloroquine Small molecular drug DB00608
Hydroxychloroquine Small molecular drug DB01611
Phase 3
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Sd-101 Oligonucleotide D08RJM
Tilsotolimod Oligonucleotide D6YD0X
Cadi-05 Vaccine D0V0JR
Imo-2125 . D0FM5M
Mgn-1703 . D0F7YW
Phase 2
Click To Hide/Show 10 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bl-7040 Small molecular drug D02GIA
Jvrs-100 Vaccine D0D4LP
Tolamba Vaccine D0GR5X
Cpg-10101 . D0C6ZS
Cyt003 . D09CEJ
Imo-2055 . D0W6HO
Imo-3100 . D08OXU
Lefitolimod . DY46GM
Mis-416 . D01UHA
Zadaxin/Lamivudine . D0C3VQ
Phase 1
Click To Hide/Show 12 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cavrotolimod Small molecular drug DBU13L
Cpg 52364 Small molecular drug D0G1TY
N-8295 Vaccine D00CQL
Ast-008 . D05ZLY
Azd1419 . D02AWQ
Cmp-001 . D7T5AN
Dv-1179 . D00CGX
Dv281 . D0X8VX
Gnkg-168 . D04CXX
Litenimod . D01SPJ
Mgn-1706 . D0U8LD
Sar-21609 . D0R8RO
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Imo-2134 . D02ZWR
Investigative
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Odn-2088 Oligonucleotide DT6N0O
Cov08-0064 Small molecular drug DX45IW
Golotimod Small molecular drug DB05475
Cpg 10101 . DB05530
Dims-9054 . D0Q2UW
Iss-1018 . DB05463
Discontinued
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ir-103 Vaccine D03GAI
Agatolimod . D0D5FQ
Ave0675 . D0B6WN
Im0-8400 . D0H4XV

References

1 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
2 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
3 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402