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Assay Detail

CHEMBL3413623

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Functional
Agonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
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

In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists.
Tosh DK, Finley A, Paoletta S, Moss SM, Gao ZG, Gizewski ET, Auchampach JA, Salvemini D, Jacobson KA.
J Med Chem (2014) 57 : 9901 -9914
PubMed 25422861 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 9.44 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3407783 1 9.60
CHEMBL3407774 1 9.49
CHEMBL3407784 1 9.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3407783 EC50 = 0.25 nM 9.60
CHEMBL3407774 EC50 = 0.32 nM 9.49
CHEMBL3407784 EC50 = 0.6 nM 9.22