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Assay Detail

CHEMBL5628191

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

Binding
Agonist activity at STING G230A/R293Q mutant (unknown origin) expressed in digitonin -permeabilized HEK293T cells preincubated for 30 mins followed by washout and measured after 5 hrs by Bright-glo luciferase assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Vinylphosphonate-based cyclic dinucleotides enhance STING-mediated cancer immunotherapy.
Dejmek M, Brazdova A, Otava T, Polidarova MP, Klíma M, Smola M, Vavrina Z, Buděšínský M, Dračínský M, Liboska R, Boura E, Birkuš G, Nencka R.
Eur J Med Chem (2023) 259 : 115685 -115685
PubMed 37567057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 6.67 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4465054 1 7.40
CHEMBL5631622 1 7.10
CHEMBL5631465 1 7.00
CHEMBL5632142 1 6.89
CHEMBL5633949 1 6.68
CHEMBL5190773 1 6.64
CHEMBL4449584 1 6.58
CHEMBL5632743 1 6.54
CHEMBL5633953 1 6.41
CHEMBL5633033 1 6.41
CHEMBL5632563 1 6.40
CHEMBL5631976 1 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4465054 EC50 = 40.0 nM 7.40
CHEMBL5631622 EC50 = 80.0 nM 7.10
CHEMBL5631465 EC50 = 100.0 nM 7.00
CHEMBL5632142 EC50 = 130.0 nM 6.89
CHEMBL5633949 EC50 = 210.0 nM 6.68
CHEMBL5190773 EC50 = 230.0 nM 6.64
CHEMBL4449584 EC50 = 260.0 nM 6.58
CHEMBL5632743 EC50 = 290.0 nM 6.54
CHEMBL5633953 EC50 = 390.0 nM 6.41
CHEMBL5633033 EC50 = 390.0 nM 6.41
CHEMBL5632563 EC50 = 400.0 nM 6.40
CHEMBL5631976 EC50 = 950.0 nM 6.02