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Assay Detail

CHEMBL4727489

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Antagonist activity at TLR9 in human PBMC assessed as inhibition of ODN2216-induced IFNalpha production
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PBMC
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Toll-like receptor 9 (CHEMBL5804)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway.
Alper PB,Deane J,Betschart C,Buffet D,Collignon Zipfel G,Gordon P,Hampton J,Hawtin S,Ibanez M,Jiang T,Junt T,Knoepfel T,Liu B,Maginnis J,McKeever U,Michellys PY,Mutnick D,Nayak B,Niwa S,Richmond W,Rush JS,Syka P,Zhang Y,Zhu X
Bioorg Med Chem Lett (2020) 30 : 127366 -127366
PubMed 32738975 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.58 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4634860 1 6.00
CHEMBL4796453 1 5.92
CHEMBL4783510 1 5.85
CHEMBL4782200 1 5.66
CHEMBL4755173 1 5.64
CHEMBL4748638 1 5.57
CHEMBL4790219 1 5.48
CHEMBL4776103 1 5.47
CHEMBL4792072 1 5.47
CHEMBL4740820 1 5.43
CHEMBL4745239 1 5.28
CHEMBL4761527 1 5.19
CHEMBL4740968 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4634860 IC50 = 1000.0 nM 6.00
CHEMBL4796453 IC50 = 1200.0 nM 5.92
CHEMBL4783510 IC50 = 1400.0 nM 5.85
CHEMBL4782200 IC50 = 2200.0 nM 5.66
CHEMBL4755173 IC50 = 2300.0 nM 5.64
CHEMBL4748638 IC50 = 2700.0 nM 5.57
CHEMBL4790219 IC50 = 3300.0 nM 5.48
CHEMBL4776103 IC50 = 3400.0 nM 5.47
CHEMBL4792072 IC50 = 3400.0 nM 5.47
CHEMBL4740820 IC50 = 3700.0 nM 5.43
CHEMBL4745239 IC50 = 5300.0 nM 5.28
CHEMBL4761527 IC50 = 6500.0 nM 5.19
CHEMBL4740968 IC50 > 5000.0 nM -