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Assay Detail

CHEMBL5036839

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

Binding
Activation of human STING REF mutant expressed in digitonin treated HEK293T cells co-expressing IRF3-activated ISRE assessed as IRF3 reporter activation by luciferase reporter gene assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 11 6.23 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4577528 1 7.16
CHEMBL5076132 1 6.89
CHEMBL5071466 1 6.85
CHEMBL5093813 1 6.75
CHEMBL4435159 1 6.68
CHEMBL5090007 1 6.44
CHEMBL5078036 1 6.04
CHEMBL4449584 1 5.37
CHEMBL1231573 1 5.08
CHEMBL5082153 1 5.06
CHEMBL1229884 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4577528 EC50 = 70.0 nM 7.16
CHEMBL5076132 EC50 = 130.0 nM 6.89
CHEMBL5071466 EC50 = 140.0 nM 6.85
CHEMBL5093813 EC50 = 180.0 nM 6.75
CHEMBL4435159 EC50 = 210.0 nM 6.68
CHEMBL5090007 EC50 = 360.0 nM 6.44
CHEMBL5078036 EC50 = 920.0 nM 6.04
CHEMBL4449584 EC50 = 4260.0 nM 5.37
CHEMBL1231573 EC50 = 8410.0 nM 5.08
CHEMBL5082153 EC50 = 8700.0 nM 5.06
CHEMBL1229884 EC50 > 45000.0 nM -