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Assay Detail

CHEMBL3803233

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Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
3
Total Activities
3
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

Purine (N)-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A3 Adenosine Receptor Agonists.
Tosh DK, Ciancetta A, Warnick E, O'Connor R, Chen Z, Gizewski E, Crane S, Gao ZG, Auchampach JA, Salvemini D, Jacobson KA.
J Med Chem (2016) 59 : 3249 -3263
PubMed 26890707 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.45 9.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL431733 NAMODENOSON 3.0 1 9.34
CHEMBL3800106 1 8.31
CHEMBL3800048 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL431733 NAMODENOSON EC50 = 0.46 nM 9.34
CHEMBL3800106 EC50 = 4.86 nM 8.31
CHEMBL3800048 EC50 = 20.2 nM 7.70