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Assay Detail

CHEMBL2072287

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Functional
Agonist activity at human A2A adenosine receptor expressed in CHO cells assessed as stimulation of forskolin-induced cAMP accumulation after 30 mins
3
Total Activities
3
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

Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening.
Tosh DK, Phan K, Gao ZG, Gakh AA, Xu F, Deflorian F, Abagyan R, Stevens RC, Jacobson KA, Katritch V.
J Med Chem (2012) 55 : 4297 -4308
PubMed 22486652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.29 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261482 1 7.64
CHEMBL2070507 1 7.57
CHEMBL2070508 1 6.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261482 EC50 = 22.9 nM 7.64
CHEMBL2070507 EC50 = 26.8 nM 7.57
CHEMBL2070508 EC50 = 225.0 nM 6.65