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Assay Detail

CHEMBL5320177

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

Binding
Agonist activity at human STING in human THP1-Blue ISG cells incubated for 24 hrs in presence of PMA by luciferase reporter assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, Synthesis, and Biological Evaluation of Bipyridazine Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.
Shan B, Hou H, Zhang K, Li R, Shen C, Chen Z, Xu P, Cui R, Su Z, Zhang C, Yang R, Zhou G, Liu Y, Guo H, Chen K, Fu W, Jiang H, Zhang S, Zheng M.
J Med Chem (2023) 66 : 3327 -3347
PubMed 36808996 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 5.07 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5417158 1 6.55
CHEMBL5424638 1 6.42
CHEMBL5432208 1 5.64
CHEMBL5414312 1 5.56
CHEMBL4867353 1 5.52
CHEMBL4434776 1 5.46
CHEMBL5416014 1 5.45
CHEMBL5396779 1 5.35
CHEMBL5437805 1 5.22
CHEMBL5408678 1 4.98
CHEMBL5417810 1 4.94
CHEMBL5419901 1 4.75
CHEMBL5428811 1 4.75
CHEMBL5416022 1 4.68
CHEMBL5411646 1 4.67
CHEMBL5397751 1 4.65
CHEMBL5397964 1 4.64
CHEMBL5394539 1 4.52
CHEMBL5412983 1 4.49
CHEMBL5437286 1 4.49
CHEMBL5397564 1 4.47
CHEMBL5433989 1 4.42
CHEMBL5394751 1 -
CHEMBL5420190 1 -
CHEMBL5414917 1 -
CHEMBL5433519 1 -
CHEMBL5435779 1 -
CHEMBL5435332 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5417158 EC50 = 280.0 nM 6.55
CHEMBL5424638 EC50 = 380.0 nM 6.42
CHEMBL5432208 EC50 = 2270.0 nM 5.64
CHEMBL5414312 EC50 = 2780.0 nM 5.56
CHEMBL4867353 EC50 = 3030.0 nM 5.52
CHEMBL4434776 EC50 = 3510.0 nM 5.46
CHEMBL5416014 EC50 = 3520.0 nM 5.45
CHEMBL5396779 EC50 = 4500.0 nM 5.35
CHEMBL5437805 EC50 = 5960.0 nM 5.22
CHEMBL5408678 EC50 = 10490.0 nM 4.98
CHEMBL5417810 EC50 = 11490.0 nM 4.94
CHEMBL5419901 EC50 = 17860.0 nM 4.75
CHEMBL5428811 EC50 = 17580.0 nM 4.75
CHEMBL5416022 EC50 = 20640.0 nM 4.68
CHEMBL5411646 EC50 = 21330.0 nM 4.67
CHEMBL5397751 EC50 = 22320.0 nM 4.65
CHEMBL5397964 EC50 = 22770.0 nM 4.64
CHEMBL5394539 EC50 = 29930.0 nM 4.52
CHEMBL5412983 EC50 = 32720.0 nM 4.49
CHEMBL5437286 EC50 = 32280.0 nM 4.49
CHEMBL5397564 EC50 = 33640.0 nM 4.47
CHEMBL5433989 EC50 = 37990.0 nM 4.42
CHEMBL5394751 EC50 > 100000.0 nM -
CHEMBL5420190 EC50 = 1938000.0 nM -
CHEMBL5414917 EC50 > 100000.0 nM -
CHEMBL5433519 EC50 > 100000.0 nM -
CHEMBL5435779 EC50 > 100000.0 nM -
CHEMBL5435332 EC50 > 100000.0 nM -