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Assay Detail

CHEMBL976208

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

Functional
Antagonist activity at adenosine A2A receptor in Wistar-Kyoto rat aorta assessed as inhibition of phenylephrine-induced contraction treated 30 mins before phenylephrine challenge measured after 60 mins
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Aorta
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A2a (CHEMBL302)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1,3-dialkyl-8-N-substituted benzyloxycarbonylamino-9-deazaxanthines as potent adenosine receptor ligands: Design, synthesis, structure-affinity and structure-selectivity relationships.
Fernández F, Caamaño O, Isabel Nieto M, López C, García-Mera X, Stefanachi A, Nicolotti O, Isabel Loza M, Brea J, Esteve C, Segarra V, Vidal B, Carotti A.
Bioorg Med Chem (2009) 17 : 3618 -3629
PubMed 19398343 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 7.55 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL513681 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL513681 Kd = 28.18 nM 7.55