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Assay Detail

CHEMBL1107971

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Functional
Agonist activity at human adenosine A1 receptor expressed in CHO cells assessed as stimulation of ERK1/2 phosphorylation
6
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 A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Hybrid ortho/allosteric ligands for the adenosine A(1) receptor.
Narlawar R, Lane JR, Doddareddy M, Lin J, Brussee J, Ijzerman AP.
J Med Chem (2010) 53 : 3028 -3037
PubMed 20345101 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.83 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1093910 2 7.68
CHEMBL1090683 2 6.82
CHEMBL1090687 2 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1093910 EC50 = 20.89 nM 7.68
CHEMBL1093910 EC50 = 22.0 nM 7.66
CHEMBL1090683 EC50 = 151.36 nM 6.82
CHEMBL1090683 EC50 = 156.0 nM 6.81
CHEMBL1090687 EC50 = 954.99 nM 6.02
CHEMBL1090687 EC50 = 1071.0 nM 5.97