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Assay Detail

CHEMBL5354768

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

Binding
Agonist activity at STING in PMA-treated human THP-1 reporter cells incubated for 30 mins in presence of digitonin by QUANTI-Luc assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type THP-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

S-acylthioalkyl ester (SATE)-based prodrugs of deoxyribose cyclic dinucleotides (dCDNs) as the STING agonist for antitumor immunotherapy.
Xie Z, Lu L, Wang Z, Luo Q, Yang Y, Fang T, Chen Z, Ma D, Quan J, Xi Z.
Eur J Med Chem (2022) 243 : 114796 -114796
PubMed 36198216 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.14 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5397460 1 8.21
CHEMBL5427569 1 7.94
CHEMBL4465054 1 7.55
CHEMBL5190773 1 6.88
CHEMBL5413946 1 6.50
CHEMBL5416367 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5397460 EC50 = 6.2 nM 8.21
CHEMBL5427569 EC50 = 11.4 nM 7.94
CHEMBL4465054 EC50 = 28.3 nM 7.55
CHEMBL5190773 EC50 = 131.4 nM 6.88
CHEMBL5413946 EC50 = 316.6 nM 6.50
CHEMBL5416367 EC50 = 1796.0 nM 5.75