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Assay Detail

CHEMBL4338398

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

Binding
Activation of recombinant human STING haplotype R71H/G230A/R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay
ChEMBL ↗
42
Total Activities
39
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

Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
Novotná B, Vaneková L, Zavřel M, Buděšínský M, Dejmek M, Smola M, Gutten O, Tehrani ZA, Pimková Polidarová M, Brázdová A, Liboska R, Štěpánek I, Vavřina Z, Jandušík T, Nencka R, Rulíšek L, Bouřa E, Brynda J, Páv O, Birkuš G.
J Med Chem (2019) 62 : 10676 -10690
PubMed 31715099 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 42 7.12 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4577528 — — 1 8.00
CHEMBL4589856 — — 1 7.70
CHEMBL4438957 — — 4 7.70
CHEMBL4465054 — — 1 7.70
CHEMBL4578839 — — 1 7.70
CHEMBL4435159 — — 1 7.70
CHEMBL4552089 — — 1 7.52
CHEMBL4465931 — — 1 7.52
CHEMBL4566174 — — 1 7.52
CHEMBL4570468 — — 1 7.52
CHEMBL4573074 — — 1 7.40
CHEMBL4459563 — — 1 7.40
CHEMBL4544112 — — 1 7.40
CHEMBL4462144 — — 1 7.40
CHEMBL4540223 — — 1 7.30
CHEMBL4476079 — — 1 7.30
CHEMBL4468010 — — 1 7.30
CHEMBL4526526 — — 1 7.22
CHEMBL4474321 — — 1 7.22
CHEMBL4466863 — — 1 7.22
CHEMBL4439796 — — 1 7.10
CHEMBL4441395 — — 1 7.10
CHEMBL4446841 — — 1 7.10
CHEMBL4444544 — — 1 7.00
CHEMBL4445083 — — 1 7.00
CHEMBL4539147 — — 1 7.00
CHEMBL4573882 — — 1 6.96
CHEMBL4449584 — — 1 6.92
CHEMBL4588248 — — 1 6.72
CHEMBL1229884 — — 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4577528 — EC50 = 10.0 nM 8.00
CHEMBL4435159 — EC50 = 20.0 nM 7.70
CHEMBL4438957 — EC50 = 20.0 nM 7.70
CHEMBL4438957 — EC50 = 20.0 nM 7.70
CHEMBL4578839 — EC50 = 20.0 nM 7.70
CHEMBL4465054 — EC50 = 20.0 nM 7.70
CHEMBL4589856 — EC50 = 20.0 nM 7.70
CHEMBL4465931 — EC50 = 30.0 nM 7.52
CHEMBL4570468 — EC50 = 30.0 nM 7.52
CHEMBL4566174 — EC50 = 30.0 nM 7.52
CHEMBL4552089 — EC50 = 30.0 nM 7.52
CHEMBL4438957 — EC50 = 30.0 nM 7.52
CHEMBL4573074 — EC50 = 40.0 nM 7.40
CHEMBL4544112 — EC50 = 40.0 nM 7.40
CHEMBL4459563 — EC50 = 40.0 nM 7.40
CHEMBL4462144 — EC50 = 40.0 nM 7.40
CHEMBL4468010 — EC50 = 50.0 nM 7.30
CHEMBL4476079 — EC50 = 50.0 nM 7.30
CHEMBL4540223 — EC50 = 50.0 nM 7.30
CHEMBL4474321 — EC50 = 60.0 nM 7.22
CHEMBL4526526 — EC50 = 60.0 nM 7.22
CHEMBL4466863 — EC50 = 60.0 nM 7.22
CHEMBL4439796 — EC50 = 80.0 nM 7.10
CHEMBL4446841 — EC50 = 80.0 nM 7.10
CHEMBL4441395 — EC50 = 80.0 nM 7.10
CHEMBL4445083 — EC50 = 100.0 nM 7.00
CHEMBL4444544 — EC50 = 100.0 nM 7.00
CHEMBL4539147 — EC50 = 100.0 nM 7.00
CHEMBL4573882 — EC50 = 110.0 nM 6.96
CHEMBL4449584 — EC50 = 120.0 nM 6.92
CHEMBL4438957 — EC50 = 130.0 nM 6.89
CHEMBL4588248 — EC50 = 190.0 nM 6.72
CHEMBL4586305 — EC50 = 200.0 nM 6.70
CHEMBL1229884 — EC50 = 200.0 nM 6.70
CHEMBL4566128 — EC50 = 210.0 nM 6.68
CHEMBL4591097 — EC50 = 250.0 nM 6.60
CHEMBL4517384 — EC50 = 300.0 nM 6.52
CHEMBL4566810 — EC50 = 310.0 nM 6.51
CHEMBL4556336 — EC50 = 400.0 nM 6.40
CHEMBL4465353 — EC50 = 480.0 nM 6.32
CHEMBL1231573 — EC50 = 900.0 nM 6.05
CHEMBL4553050 — EC50 = 1700.0 nM 5.77