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Assay Detail

CHEMBL4727486

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

Binding
Antagonist activity at TLR7 in human PBMC assessed as inhibition of ssRNA40-induced IFNalpha production
15
Total Activities
15
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 7 (CHEMBL5936)
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 15 7.23 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4740968 1 8.52
CHEMBL4748638 1 8.22
CHEMBL4783510 1 7.60
CHEMBL4740820 1 7.35
CHEMBL4792072 1 7.34
CHEMBL4755173 1 7.28
CHEMBL4782200 1 7.15
CHEMBL4796453 1 7.02
CHEMBL4776103 1 6.77
CHEMBL4745239 1 6.70
CHEMBL4743698 1 6.51
CHEMBL4761527 1 6.30
CHEMBL4790219 1 -
CHEMBL4634860 1 -
CHEMBL4762866 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4740968 IC50 = 3.0 nM 8.52
CHEMBL4748638 IC50 = 6.0 nM 8.22
CHEMBL4783510 IC50 = 25.0 nM 7.60
CHEMBL4740820 IC50 = 45.0 nM 7.35
CHEMBL4792072 IC50 = 46.0 nM 7.34
CHEMBL4755173 IC50 = 53.0 nM 7.28
CHEMBL4782200 IC50 = 71.0 nM 7.15
CHEMBL4796453 IC50 = 95.0 nM 7.02
CHEMBL4776103 IC50 = 170.0 nM 6.77
CHEMBL4745239 IC50 = 200.0 nM 6.70
CHEMBL4743698 IC50 = 310.0 nM 6.51
CHEMBL4761527 IC50 = 500.0 nM 6.30
CHEMBL4790219 IC50 < 1.0 nM -
CHEMBL4634860 IC50 < 1.0 nM -
CHEMBL4762866 IC50 < 1.0 nM -