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Assay Detail

CHEMBL5162239

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

Binding
Agonist activity at STING in human wild-type THP1-Dual cells co-expressing ISRE reporter assessed as IRF-mediated immune response incubated for 24 hrs by QUANTI Luc based microplate reader method
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type THP1-Dual
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Stimulator of interferon genes protein (CHEMBL4523377)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of Potent Immune Modulators Targeting Stimulator of Interferon Genes Receptor.
Jeon MJ, Lee H, Lee J, Baek SY, Lee D, Jo S, Lee JY, Kang M, Jung HR, Han SB, Kim NJ, Lee S, Kim H.
J Med Chem (2022) 65 : 5407 -5432
PubMed 35315650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 5.47 9.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5201766 1 9.45
CHEMBL5174660 1 8.79
CHEMBL4793625 1 6.09
CHEMBL4440744 1 5.91
CHEMBL5169574 1 5.78
CHEMBL5187032 1 5.77
CHEMBL5194415 1 5.34
CHEMBL5176115 1 5.21
CHEMBL5205725 1 5.18
CHEMBL5205871 1 5.04
CHEMBL5197505 1 4.75
CHEMBL5199858 1 4.54
CHEMBL5173411 1 4.53
CHEMBL5185786 1 4.52
CHEMBL4465054 1 4.52
CHEMBL5192829 1 4.41
CHEMBL5200249 1 4.31
CHEMBL5196300 1 4.29
CHEMBL4522871 1 -
CHEMBL5187131 1 -
CHEMBL4438309 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5201766 EC50 = 0.3536 nM 9.45
CHEMBL5174660 EC50 = 1.624 nM 8.79
CHEMBL4793625 EC50 = 803.8 nM 6.09
CHEMBL4440744 EC50 = 1232.0 nM 5.91
CHEMBL5169574 EC50 = 1661.0 nM 5.78
CHEMBL5187032 EC50 = 1689.0 nM 5.77
CHEMBL5194415 EC50 = 4597.0 nM 5.34
CHEMBL5176115 EC50 = 6222.0 nM 5.21
CHEMBL5205725 EC50 = 6546.0 nM 5.18
CHEMBL5205871 EC50 = 9116.0 nM 5.04
CHEMBL5197505 EC50 = 17600.0 nM 4.75
CHEMBL5199858 EC50 = 28640.0 nM 4.54
CHEMBL5173411 EC50 = 29830.0 nM 4.53
CHEMBL5185786 EC50 = 30060.0 nM 4.52
CHEMBL4465054 EC50 = 30100.0 nM 4.52
CHEMBL5192829 EC50 = 39130.0 nM 4.41
CHEMBL5200249 EC50 = 48580.0 nM 4.31
CHEMBL5196300 EC50 = 51070.0 nM 4.29
CHEMBL4522871 EC50 = 102000.0 nM -
CHEMBL5187131 EC50 = 0.004028 nM -
CHEMBL4438309 EC50 < 1.0 nM -