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Assay Detail

CHEMBL2216965

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Functional
Agonist activity at human TLR7 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Toll-like receptor 7 (CHEMBL5936)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Imidazoquinolines with Toll-Like Receptor 7/8 Independent Cytokine Induction.
Shi C, Xiong Z, Chittepu P, Aldrich CC, Ohlfest JR, Ferguson DM.
ACS Med Chem Lett (2012) 3 : 501 -504
PubMed 22837811 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 5.54 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1082983 1 7.00
CHEMBL2216760 1 5.92
CHEMBL383322 RESIQUIMOD 2.0 1 5.85
CHEMBL1282 IMIQUIMOD 4.0 1 4.92
CHEMBL195276 1 4.02
CHEMBL2216759 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1082983 EC50 = 100.0 nM 7.00
CHEMBL2216760 EC50 = 1200.0 nM 5.92
CHEMBL383322 RESIQUIMOD EC50 = 1400.0 nM 5.85
CHEMBL1282 IMIQUIMOD EC50 = 12100.0 nM 4.92
CHEMBL195276 EC50 = 95000.0 nM 4.02
CHEMBL2216759 EC50 > 270000.0 nM -