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Assay Detail

CHEMBL2014404

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

Functional
Agonist activity at human recombinant adenosine receptor-1 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 45 mins prior forskolin-induction measured after 15 mins by immunoassay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element.
Tosh DK, Phan K, Deflorian F, Wei Q, Gao ZG, Jacobson KA.
ACS Med Chem Lett (2011) 2 : 626 -631
PubMed 21858244 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.69 7.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464859 NECA 1 7.99
CHEMBL2012686 1 7.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464859 NECA EC50 = 10.2 nM 7.99
CHEMBL2012686 EC50 = 40.7 nM 7.39