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Assay Detail

CHEMBL1012745

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

Binding
Displacement of [3H]DPCPX from adenosine A1 receptor in Wistar rat brain membrane
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
Ki 1 6.23 6.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL474016 1 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL474016 Ki = 587.0 nM 6.23