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Assay Detail

CHEMBL5107337

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

Functional
Induction of TNFalpha secretion in human PBMC incubated for 16 hrs
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PBMC
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
Vavřina Z, Perlíková P, Milisavljević N, Chevrier F, Smola M, Smith J, Dejmek M, Havlíček V, Buděšínský M, Liboska R, Vaneková L, Brynda J, Boura E, Řezáčová P, Hocek M, Birkuš G.
J Med Chem (2022) 65 : 14082 -14103
PubMed 36201304 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 4.59 5.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5175129 1 5.84
CHEMBL5208206 1 5.58
CHEMBL5179761 1 5.17
CHEMBL5187347 1 4.87
CHEMBL4449584 1 4.73
CHEMBL5208313 1 4.61
CHEMBL4465054 1 4.44
CHEMBL5185176 1 4.42
CHEMBL5172826 1 4.36
CHEMBL4435159 1 4.35
CHEMBL5181208 1 4.30
CHEMBL5204143 1 4.28
CHEMBL5189981 1 4.27
CHEMBL5180332 1 4.18
CHEMBL5176230 1 4.00
CHEMBL5191052 1 4.00
CHEMBL5200248 1 -
CHEMBL5198498 1 -
CHEMBL5184506 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5175129 EC50 = 1430.0 nM 5.84
CHEMBL5208206 EC50 = 2660.0 nM 5.58
CHEMBL5179761 EC50 = 6720.0 nM 5.17
CHEMBL5187347 EC50 = 13640.0 nM 4.87
CHEMBL4449584 EC50 = 18720.0 nM 4.73
CHEMBL5208313 EC50 = 24560.0 nM 4.61
CHEMBL4465054 EC50 = 36030.0 nM 4.44
CHEMBL5185176 EC50 = 37590.0 nM 4.42
CHEMBL5172826 EC50 = 43380.0 nM 4.36
CHEMBL4435159 EC50 = 44540.0 nM 4.35
CHEMBL5181208 EC50 = 50600.0 nM 4.30
CHEMBL5204143 EC50 = 52450.0 nM 4.28
CHEMBL5189981 EC50 = 53860.0 nM 4.27
CHEMBL5180332 EC50 = 65770.0 nM 4.18
CHEMBL5176230 EC50 = 99700.0 nM 4.00
CHEMBL5191052 EC50 = 98800.0 nM 4.00
CHEMBL5200248 EC50 > 200000.0 nM -
CHEMBL5198498 EC50 > 200000.0 nM -
CHEMBL5184506 EC50 > 200000.0 nM -