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Assay Detail

CHEMBL2403962

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

Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A3 (CHEMBL1075269)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain.
Paoletta S, Tosh DK, Finley A, Gizewski ET, Moss SM, Gao ZG, Auchampach JA, Salvemini D, Jacobson KA.
J Med Chem (2013) 56 : 5949 -5963
PubMed 23789857 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 8.70 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL431733 NAMODENOSON 3.0 1 9.82
CHEMBL2401955 1 8.59
CHEMBL2402024 1 8.48
CHEMBL2401954 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL431733 NAMODENOSON EC50 = 0.15 nM 9.82
CHEMBL2401955 EC50 = 2.6 nM 8.59
CHEMBL2402024 EC50 = 3.33 nM 8.48
CHEMBL2401954 EC50 = 13.0 nM 7.89