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Assay Detail

CHEMBL3772777

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Binding
Agonist activity at human Adenosine A1 receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphai1 after 16 hrs by beta galactosidase reporter gene assay
14
Total Activities
14
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 A1 (CHEMBL226)
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
EC50 12 5.62 6.70
pEC50 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284969 1 6.70
CHEMBL3770310 1 6.50
CHEMBL116903 1 6.20
CHEMBL464859 NECA 1 6.00
CHEMBL3770679 1 6.00
CHEMBL3771208 1 5.80
CHEMBL477 ADENOSINE 4.0 1 5.60
CHEMBL3770664 1 5.40
CHEMBL3771290 1 4.80
CHEMBL3771184 1 4.80
CHEMBL3769641 1 4.00
CHEMBL331372 CGS-21680 1 -
CHEMBL3769438 1 -
CHEMBL3769408 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284969 EC50 = 199.53 nM 6.70
CHEMBL3770310 EC50 = 316.23 nM 6.50
CHEMBL116903 EC50 = 630.96 nM 6.20
CHEMBL464859 NECA EC50 = 1000.0 nM 6.00
CHEMBL3770679 EC50 = 1000.0 nM 6.00
CHEMBL3771208 EC50 = 1584.89 nM 5.80
CHEMBL477 ADENOSINE EC50 = 2511.89 nM 5.60
CHEMBL3770664 EC50 = 3981.07 nM 5.40
CHEMBL3771290 EC50 = 15848.93 nM 4.80
CHEMBL3771184 EC50 = 15848.93 nM 4.80
CHEMBL3769641 EC50 = 100000.0 nM 4.00
CHEMBL331372 CGS-21680 EC50 = 630957.34 nM -
CHEMBL3769438 pEC50 - -
CHEMBL3769408 pEC50 - -