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Assay Detail

CHEMBL894349

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Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation
2
Total Activities
2
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 Expert

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.
Colotta V, Catarzi D, Varano F, Capelli F, Lenzi O, Filacchioni G, Martini C, Trincavelli L, Ciampi O, Pugliese AM, Pedata F, Schiesaro A, Morizzo E, Moro S.
J Med Chem (2007) 50 : 4061 -4074
PubMed 17665891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.19 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL242849 1 8.42
CHEMBL230854 1 7.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL242849 EC50 = 3.8 nM 8.42
CHEMBL230854 EC50 = 11.2 nM 7.95