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Assay Detail

CHEMBL3772951

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Functional
Agonist activity at human Adenosine A1 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysis
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
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
IC50 11 8.82 10.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770679 1 10.53
CHEMBL464859 NECA 1 9.68
CHEMBL3771184 1 9.40
CHEMBL284969 1 9.30
CHEMBL3771208 1 9.17
CHEMBL477 ADENOSINE 4.0 1 8.63
CHEMBL3770664 1 8.54
CHEMBL116903 1 8.36
CHEMBL3770310 1 8.21
CHEMBL3771290 1 7.72
CHEMBL3769641 1 7.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770679 IC50 = 0.02951 nM 10.53
CHEMBL464859 NECA IC50 = 0.2089 nM 9.68
CHEMBL3771184 IC50 = 0.3981 nM 9.40
CHEMBL284969 IC50 = 0.5012 nM 9.30
CHEMBL3771208 IC50 = 0.6761 nM 9.17
CHEMBL477 ADENOSINE IC50 = 2.344 nM 8.63
CHEMBL3770664 IC50 = 2.884 nM 8.54
CHEMBL116903 IC50 = 4.365 nM 8.36
CHEMBL3770310 IC50 = 6.166 nM 8.21
CHEMBL3771290 IC50 = 19.05 nM 7.72
CHEMBL3769641 IC50 = 37.15 nM 7.43