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Assay Detail

CHEMBL5045537

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

Binding
Displacement of fluorescein-labelled probe from human cytoplasmic domain of STING G230A/R293Q double mutant (155 to 341 residues) by time-resolved FRET-based competition binding assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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
IC50 23 5.64 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4438309 1 8.41
CHEMBL4776666 1 8.14
CHEMBL5080916 1 6.33
CHEMBL5081567 1 6.24
CHEMBL4528146 1 5.89
CHEMBL5082881 1 5.77
CHEMBL5082361 1 5.31
CHEMBL5082707 1 5.30
CHEMBL5090440 1 5.28
CHEMBL5077683 1 4.96
CHEMBL5089143 1 4.85
CHEMBL5091795 1 4.64
CHEMBL5088178 1 4.62
CHEMBL5092039 1 4.47
CHEMBL5078116 1 4.39
CHEMBL71263 VADIMEZAN 3.0 1 -
CHEMBL5079595 1 -
CHEMBL5086226 1 -
CHEMBL5086556 1 -
CHEMBL5076859 1 -
CHEMBL5082150 1 -
CHEMBL5089074 1 -
CHEMBL5088451 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4438309 IC50 = 3.9 nM 8.41
CHEMBL4776666 IC50 = 7.2 nM 8.14
CHEMBL5080916 IC50 = 470.0 nM 6.33
CHEMBL5081567 IC50 = 580.0 nM 6.24
CHEMBL4528146 IC50 = 1300.0 nM 5.89
CHEMBL5082881 IC50 = 1700.0 nM 5.77
CHEMBL5082361 IC50 = 4900.0 nM 5.31
CHEMBL5082707 IC50 = 5000.0 nM 5.30
CHEMBL5090440 IC50 = 5200.0 nM 5.28
CHEMBL5077683 IC50 = 11000.0 nM 4.96
CHEMBL5089143 IC50 = 14000.0 nM 4.85
CHEMBL5091795 IC50 = 23000.0 nM 4.64
CHEMBL5088178 IC50 = 24000.0 nM 4.62
CHEMBL5092039 IC50 = 34000.0 nM 4.47
CHEMBL5078116 IC50 = 41000.0 nM 4.39
CHEMBL71263 VADIMEZAN IC50 > 100000.0 nM -
CHEMBL5079595 IC50 > 100000.0 nM -
CHEMBL5086226 IC50 > 100000.0 nM -
CHEMBL5086556 IC50 > 100000.0 nM -
CHEMBL5076859 IC50 > 100000.0 nM -
CHEMBL5082150 IC50 > 100000.0 nM -
CHEMBL5089074 IC50 > 100000.0 nM -
CHEMBL5088451 IC50 > 100000.0 nM -