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Assay Detail

CHEMBL5036846

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

Binding
Activation of wild-type human STING expressed in digitonin treated human THP1-Dual cells co-expressing IRF3-activated ISRE assessed as IRF3 reporter activation measured after 30 mins by luciferase reporter gene assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type H69AR
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and Biological Evaluation of Phosphoester and Phosphorothioate Prodrugs of STING Agonist 3',3'-c-Di(2'F,2'dAMP).
Pimková Polidarová M, Břehová P, Kaiser MM, Smola M, Dračínský M, Smith J, Marek A, Dejmek M, Šála M, Gutten O, Rulíšek L, Novotná B, Brázdová A, Janeba Z, Nencka R, Boura E, Páv O, Birkuš G.
J Med Chem (2021) 64 : 7596 -7616
PubMed 34019405 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 5.99 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5079224 1 7.52
CHEMBL5074770 1 7.22
CHEMBL5076372 1 7.10
CHEMBL5073386 1 6.96
CHEMBL5075359 1 6.96
CHEMBL5078789 1 6.75
CHEMBL5089205 1 6.48
CHEMBL5080355 1 6.46
CHEMBL5079226 1 6.42
CHEMBL5093084 1 6.30
CHEMBL5089851 1 6.01
CHEMBL5093147 1 6.01
CHEMBL5080867 1 5.77
CHEMBL5083793 1 5.76
CHEMBL5090007 1 5.52
CHEMBL5076132 1 5.45
CHEMBL5082153 1 4.92
CHEMBL4577528 1 4.75
CHEMBL5093813 1 4.72
CHEMBL4435159 1 4.55
CHEMBL4449584 1 4.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5079224 EC50 = 30.0 nM 7.52
CHEMBL5074770 EC50 = 60.0 nM 7.22
CHEMBL5076372 EC50 = 80.0 nM 7.10
CHEMBL5073386 EC50 = 110.0 nM 6.96
CHEMBL5075359 EC50 = 110.0 nM 6.96
CHEMBL5078789 EC50 = 180.0 nM 6.75
CHEMBL5089205 EC50 = 330.0 nM 6.48
CHEMBL5080355 EC50 = 350.0 nM 6.46
CHEMBL5079226 EC50 = 380.0 nM 6.42
CHEMBL5093084 EC50 = 500.0 nM 6.30
CHEMBL5089851 EC50 = 970.0 nM 6.01
CHEMBL5093147 EC50 = 970.0 nM 6.01
CHEMBL5080867 EC50 = 1710.0 nM 5.77
CHEMBL5083793 EC50 = 1740.0 nM 5.76
CHEMBL5090007 EC50 = 3030.0 nM 5.52
CHEMBL5076132 EC50 = 3560.0 nM 5.45
CHEMBL5082153 EC50 = 12120.0 nM 4.92
CHEMBL4577528 EC50 = 17620.0 nM 4.75
CHEMBL5093813 EC50 = 19060.0 nM 4.72
CHEMBL4435159 EC50 = 28470.0 nM 4.55
CHEMBL4449584 EC50 = 58460.0 nM 4.23