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Assay Detail

CHEMBL3772778

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Binding
Agonist activity at human Adenosine A2A receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Novel Adenosine Receptor Agonists That Exhibit Subtype Selectivity.
Knight A, Hemmings JL, Winfield I, Leuenberger M, Frattini E, Frenguelli BG, Dowell SJ, Lochner M, Ladds G.
J Med Chem (2016) 59 : 947 -964
PubMed 26756468 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
pEC50 7 - -
EC50 6 5.24 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464859 NECA 1 6.47
CHEMBL477 ADENOSINE 4.0 1 5.24
CHEMBL3770310 1 5.24
CHEMBL284969 1 5.00
CHEMBL3770679 1 4.80
CHEMBL331372 CGS-21680 1 4.70
CHEMBL3771290 1 -
CHEMBL3771208 1 -
CHEMBL116903 1 -
CHEMBL3770664 1 -
CHEMBL3769641 1 -
CHEMBL3771184 1 -
CHEMBL3769416 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464859 NECA EC50 = 338.84 nM 6.47
CHEMBL477 ADENOSINE EC50 = 5754.4 nM 5.24
CHEMBL3770310 EC50 = 5754.4 nM 5.24
CHEMBL284969 EC50 = 10000.0 nM 5.00
CHEMBL3770679 EC50 = 15848.93 nM 4.80
CHEMBL331372 CGS-21680 EC50 = 19952.62 nM 4.70
CHEMBL3771290 pEC50 - -
CHEMBL3771208 pEC50 - -
CHEMBL116903 pEC50 - -
CHEMBL3770664 pEC50 - -
CHEMBL3769641 pEC50 - -
CHEMBL3771184 pEC50 - -
CHEMBL3769416 pEC50 - -