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Assay Detail

CHEMBL1012744

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated cAMP accumulation
1
Total Activities
1
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 A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrido[2,3-e]-1,2,4-triazolo[4,3-a]pyrazin-1-one as a new scaffold to develop potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.
Colotta V, Lenzi O, Catarzi D, Varano F, Filacchioni G, Martini C, Trincavelli L, Ciampi O, Pugliese AM, Traini C, Pedata F, Morizzo E, Moro S.
J Med Chem (2009) 52 : 2407 -2419
PubMed 19301821 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 7.44 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL474016 1 7.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL474016 EC50 = 36.3 nM 7.44