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Assay Detail

CHEMBL3887166

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

Binding
Reporter Assay: For TLR8 and TLR7 activity testing, HEK-Blue human TLR8 or TLR7 cells, respectively, (Invivogen, San Diego, Calif., USA) transfected with a SEAP reporter (secreted embryonic alkaline phosphatase) construct were used, in which the reporter expression is regulated by the NF-κB promoter upon stimulation for 24 hr. The reporter activity was determined using Quanti Blue kit (Invivogen, San Diego, Calif., USA) at a wavelength of 640 nm.
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

4-amino-imidazoquinoline compounds
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 6.86 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3924480 1 7.57
CHEMBL3921751 1 7.30
CHEMBL3967031 1 7.26
CHEMBL3904306 1 7.22
CHEMBL3960305 1 6.89
CHEMBL3984333 1 6.87
CHEMBL3975333 1 6.86
CHEMBL3959973 1 6.82
CHEMBL3944005 1 6.71
CHEMBL3942013 1 6.65
CHEMBL383322 RESIQUIMOD 2.0 1 6.12
CHEMBL3964358 1 6.05
CHEMBL3915625 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3924480 EC50 = 27.0 nM 7.57
CHEMBL3921751 EC50 = 50.0 nM 7.30
CHEMBL3967031 EC50 = 55.0 nM 7.26
CHEMBL3904306 EC50 = 60.0 nM 7.22
CHEMBL3960305 EC50 = 130.0 nM 6.89
CHEMBL3984333 EC50 = 134.0 nM 6.87
CHEMBL3975333 EC50 = 139.0 nM 6.86
CHEMBL3959973 EC50 = 152.0 nM 6.82
CHEMBL3944005 EC50 = 195.0 nM 6.71
CHEMBL3942013 EC50 = 223.0 nM 6.65
CHEMBL383322 RESIQUIMOD EC50 = 760.0 nM 6.12
CHEMBL3964358 EC50 = 900.0 nM 6.05
CHEMBL3915625 EC50 > 100000.0 nM -