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Assay Detail

CHEMBL1948461

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Functional
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as induction of cAMP production after 30 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 A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of truncated C2- or C8-substituted adenosine derivatives as dual acting A₂A and A₃ adenosine receptor ligands.
Hou X, Majik MS, Kim K, Pyee Y, Lee Y, Alexander V, Chung HJ, Lee HW, Chandra G, Lee JH, Park SG, Choi WJ, Kim HO, Phan K, Gao ZG, Jacobson KA, Choi S, Lee SK, Jeong LS.
J Med Chem (2012) 55 : 342 -356
PubMed 22142423 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.39 7.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1688379 1 7.69
CHEMBL1945563 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1688379 EC50 = 20.6 nM 7.69
CHEMBL1945563 EC50 = 80.3 nM 7.09