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Assay Detail

CHEMBL5045529

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

Binding
Agonist activity at STING in human THP1 Dual cells assessed as IRF reporter activation incubated for 20 hrs by quanti-blue SEAP reporter gene assay
16
Total Activities
16
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

Discovery of Non-Nucleotide Small-Molecule STING Agonists <i>via</i> Chemotype Hybridization.
Cherney EC, Zhang L, Lo J, Huynh T, Wei D, Ahuja V, Quesnelle C, Schieven GL, Futran A, Locke GA, Lin Z, Monereau L, Chaudhry C, Blum J, Li S, Fereshteh M, Li-Wang B, Gangwar S, Pan C, Chong C, Zhu X, Posy SL, Sack JS, Zhang P, Ruzanov M, Harner M, Akhtar F, Schroeder GM, Vite G, Fink B.
J Med Chem (2022) 65 : 3518 -3538
PubMed 35108011 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 4.95 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4438309 1 7.46
CHEMBL5086556 1 6.28
CHEMBL5089074 1 5.85
CHEMBL5086226 1 5.77
CHEMBL5079595 1 5.43
CHEMBL5088451 1 4.89
CHEMBL4776666 1 4.43
CHEMBL5080916 1 4.32
CHEMBL5077683 1 4.24
CHEMBL5090440 1 4.23
CHEMBL4528146 1 4.11
CHEMBL5081567 1 4.11
CHEMBL5082707 1 4.10
CHEMBL5082881 1 4.02
CHEMBL5089143 1 -
CHEMBL71263 VADIMEZAN 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4438309 EC50 = 35.0 nM 7.46
CHEMBL5086556 EC50 = 530.0 nM 6.28
CHEMBL5089074 EC50 = 1400.0 nM 5.85
CHEMBL5086226 EC50 = 1700.0 nM 5.77
CHEMBL5079595 EC50 = 3700.0 nM 5.43
CHEMBL5088451 EC50 = 13000.0 nM 4.89
CHEMBL4776666 EC50 = 37000.0 nM 4.43
CHEMBL5080916 EC50 = 48000.0 nM 4.32
CHEMBL5077683 EC50 = 57000.0 nM 4.24
CHEMBL5090440 EC50 = 59000.0 nM 4.23
CHEMBL4528146 EC50 = 78000.0 nM 4.11
CHEMBL5081567 EC50 = 77000.0 nM 4.11
CHEMBL5082707 EC50 = 79000.0 nM 4.10
CHEMBL5082881 EC50 = 96000.0 nM 4.02
CHEMBL5089143 EC50 > 100000.0 nM -
CHEMBL71263 VADIMEZAN EC50 > 100000.0 nM -